Objective: Liver cancer is one of the most common causes of cancer death, with reduced survival r... more Objective: Liver cancer is one of the most common causes of cancer death, with reduced survival rates. The development of new chemotherapeutic agents is essential to find effective cytotoxic drugs that give minimum side effects to the surrounding healthy tissues. The main objective of the present study was to evaluate the cytotoxic effects and mechanism of cell death induced by the crude and diethyl ether extract of Xylocarpus mouccensis on the human hepatocellular carcinoma cell line. Methods: The cytotoxicity activity was measured using the MTS assay. The mode of cell death determined by the apoptosis study, DNA fragmentation analysis done by using the TUNEL system. The pathway study or mechanism of apoptosis observed by study caspases 8, 9, 3/7 Glo-caspases method. Results: In this study, the methanol extracts prepared from leaf Xylocarpus mouccensis leaf produced cytotoxicity effect with IC 50 (72hr) < 30µg/ml. The IC 50 value at 72 hours exerted by diethyl ether extract of Xylocarpus moluccensis leaf was 0.22 µg/ml, which was more cytotoxic than to that of crude methanol extract. The results obtained by the colorimetric TUNEL system suggest that methanol crude extract of Xylocarpus moluccensis (leaf), diethyl ether extract of Xylocarpus moluccensis (leaf) and methanol extract of Xylocarpus granatum (bark) induced DNA fragmentation in the HepG2 cell line. Besides, the caspase-Glo assay demonstrated that diethyl ether leaf extract of Xylocarpus moluccensis triggered apoptotic cell death via activation of caspases-8, and-3/7 However, no visible activation was noticed for caspase-9. Furthermore, TLC indicates the presence of potential metabolites in an extract of Xylocarpus moluccensis. Conclusion: Thus, the present study suggests the remarkable potential of active metabolites in the extract of Xylocarpus moluccensis as a future therapeutic agent for the treatment of cancer.
Atherosclerosis is the main cause of cardiovascular diseases which in turn, lead to the highest n... more Atherosclerosis is the main cause of cardiovascular diseases which in turn, lead to the highest number of mortalities globally. This pathophysiological condition is developed due to a constant elevated level of plasma cholesterols. Statin is currently the widely used treatment in reducing the level of cholesterols, however, it may cause adverse side effects. Therefore, there is an urgent need to search for new alternative treatment. PCSK9 is an enzyme responsible in directing LDL-receptor (LDL-R)/LDL-cholesterols (LDL-C) complex to lysosomal degradation, preventing the receptor from recycling back to the surface of liver cells. Therefore, PCSK9 offers a potential target to search for small molecule inhibitors which inhibit the function of this enzyme. In this study, a marine invertebrate Acanthaster planci, was used to investigate its potential in inhibiting PCSK9 and lowering the levels of cholesterols. Cytotoxicity activity of A. planci on human liver HepG2 cells was carried out u...
Hystatin is a group of compounds resulted from the derivatization of aaptamine. A series of hysta... more Hystatin is a group of compounds resulted from the derivatization of aaptamine. A series of hystatin 2 derivatives (3, 5-15) have been synthesized and characterized using modern spectroscopic techniques, namely IR, 1 H and 13 C NMR, UV-Vis and Mass Spectrometer. The synthesized compounds were evaluated for their antibacterial activity against selected bacterial strains of both Gram positive and Gram negative groups, namely Bacillus cereus, Staphylococcus aureus, Micrococcus sp, Escherichia coli, Pseudomonas aeruginosa and Klebsiella pneumoniae using standard microbiological protocol of disc-diffusion method. The antibacterial activities of the compounds were assessed by the presence and absence of inhibition zones and minimum inhibition concentration (MIC) values. In general, most of the derivatives showed significant antibacterial activity towards Gram positive bacteria. It was observed that compound 6 exhibited bacterial inhibition activity against all tested bacteria. Nonetheless...
The study was conducted to explore the anticholinesterase inhibition property of eugenol derived ... more The study was conducted to explore the anticholinesterase inhibition property of eugenol derived molecules. Ten eugenol derivatives were synthesized and evaluated for the inhibitory activities against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) by Ellman’s method. Most of the tested derivatives showed higher inhibition on BChE than AChE, however, their overall inhibitory activity was weak. In contrast, three derivatives (compounds 3,6,9) showed higher and good AChE inhibitory activity of more than 50% inhibition at 10 μg/mL. Among them, compound 9bearing a ethyl substituent at para position of the benzoyl ring showed the most potent AChE inhibition, with IC50 of 5.64 μg/mL. Ligand-protein docking simulation was also performed for the most active derived molecules (compounds 3,6,9).
Background: Quercus infectoria galls (QI) extracts were previously reported to have cytotoxicity ... more Background: Quercus infectoria galls (QI) extracts were previously reported to have cytotoxicity effects towards human cervical cancer cells, HeLa. However, the underlying molecular mechanisms of the extracts have been poorly determined. Objective: The present study was undertaken to examine the effect of ethyl acetate extracts of QI (EAQI) on cell cytotoxicity and induction of apoptosis in HeLa cells. Materials and Method: The in vitro cytotoxicity was investigated by using the MTT [3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyl tetrazolium bromide] assay and the OD values were read at 570 nm. Meanwhile the induction of apoptosis was measured by using acridine orange and propidium iodide (AO/PI) staining, flow cytometry analysis of annexin V/PI staining and cell cycle distribution. Results: MTT assay showed that EAQI exhibited cytotoxicity effect on HeLa cells with IC 50 of 11.50 ± 0.50 µg/ml. HeLa cells underwent apoptosis in response to EAQI treatment, demonstrated by an increase in the percentage of apoptotic cell stained with AOPI from 1.00% to 10.33% compared to untreated cell population (p<0.05) at 72 hours of treatment. The evidence of early apoptosis in treated cells were also observed in annexin V/PI staining. Furthermore, an increase of cell population in sub G0/G1 phase revealed that apoptosis as the mode of cell death in HeLa cells treated with EAQI. Conclusion: These findings indicated that EAQI significantly inhibits HeLa cell growth through induction of apoptosis. Further studies are needed to confirm the mechanism of cell death by expression of apoptotic cascade in HeLa cells treated with EAQI.
In this study, Peperomia pellucida was subjected to the determination of biological activity and ... more In this study, Peperomia pellucida was subjected to the determination of biological activity and isola tion of chemical constituents. Two samples of this plant we re used, which were the air-dried and freeze-dried. The sequential maceration of the plant utilized three d ifferent solvents with increasing polarities, namel y dichloromethane, ethyl acetate and methanol. The Th in Layer Chromatography (TLC) profile showed there was no significant different in the chemical constituents in both samples. All six crude extracts displayed i n v tro antimicrobial activity on Pseudomonas aeruginosa, w ith minimum inhibition zone 9.0±1.7 mm and no activ ity on 7 other type of bacteria (Escherichia coli, Klebsiell a pneumonia, Salmonella sp., Bacillus subtilis, Mic rococcus sp., Staphylococcus aureus and Streptococcus uberis). In addition, antioxidant activity of all of the crude extracts was determined using DPPH (2,2-diphenyl-picryhdrazyl) r adical scavenging assay. Among the extracts methano ...
The inhibitory effects of nutmeg essential oil and three components of this oil at different conc... more The inhibitory effects of nutmeg essential oil and three components of this oil at different concentrations were tested by GABA-induced chloride current (I GABA) stimulation through gamma-aminobutyric acid type A (GABAA) receptors comprising of α1β2γ2s subtype using the two-microelectrode voltage clamp technique on Xenopus laevis oocytes. The essential oil of the kernels of Myristica fragrans was extracted by steam distillation and was analysed by gas chromatography-mass spectrometer (GC-MS) technique. A total of 16 compounds were isolated from the essential oil. The essential oil showed promising activity by enhanced I GABA up to 100% of stimulation when tested at 100 nL/mL. For dose dependent activity, α-terpineol and myristicin showed statistical significant potentiation of I GABA. α-Terpineol was found to induce an enhancement of I GABA modulation (EC5-10) by 229.6±23.8% and 326.3±43.8%, at 100 μM and 500 μM, respectively. Myristicin induced an enhancement up to 237.6±35.1% at 5...
Inhibition of aldose reductase (ALR2) by using small heterocyclic compounds provides a viable app... more Inhibition of aldose reductase (ALR2) by using small heterocyclic compounds provides a viable approach for the development of new antidiabetic agents.
Aims: Piper sarmentosum or locally known as Kaduk, is a tropical herb plant that was investigated... more Aims: Piper sarmentosum or locally known as Kaduk, is a tropical herb plant that was investigated for its phenolic content by previous researchers. The present study aimed at the analysis of crude methanolic extract of P. sarmentosum leaves for phenolic compounds identification and its anti-amoebic properties against pathogenic Acanthamoeba castellanii. Methodology and results: Folin-Ciocalteu assay was used to determine P. sarmentosum leaves methanolic extract (PSLME)'s total phenolic content (TPC). The extract was further characterized by using gas chromatography-mass spectrometry (GC-MS), reverse phase-high performance liquid chromatography (RP-HPLC) and liquid chromatographymass spectrometry (LC-MS) analyses to determine the chemical constituents in methanolic PSLME extract. The cytotoxicity of the extract was evaluated through the determination of inhibition concentration for half of cell population (IC50) of pathogenic A. castellanii followed by cell morphological analysis using inverted light and scanning electron microscopies. Acridine-orange/Propidium iodide (AOPI) staining was also conducted to determine the integrity of cell membrane for quantitative analysis. The results demonstrated that the TPC from PSLME was 142.72 mg [GAE]/g with a total of 33 phenolic compounds identified. The IC50 value obtained for A. castellanii was low (74.64 μg/mL) which indicates promising anti-acanthamoebic activity. Microscopy analyses showed that the plant extract caused cells encystment, in which exhibited by distinctive morphological changes on the cells shape and organelle, as well as shortening of acanthopodia. The dual staining and its quantitative analysis prove compromised membrane integrity in the treated amoeba. Conclusion, significance and impact of study: This finding provides the evidence that PSLME contains active phenolic compounds contributing to the anti-acanthamoebic activity on pathogenic Acanthamoeba species.
Asian Journal of Pharmaceutical and Clinical Research, Nov 1, 2017
Objective: This study aimed to investigate the anti-inflammatory activity of methanol extract and... more Objective: This study aimed to investigate the anti-inflammatory activity of methanol extract and fractions of bacteria associated with sponge (Haliclona amboinensis) and to evaluate their effect in reducing NO production and inhibiting cyclooxygenase-1 (COX-1), cyclooxgenase-2 (COX-2) and secretory phospholipase A2 (sPLA2) activity. Methods: All bacterial isolates were cultured and supernatants were collected for the extraction of secondary metabolites using diaion HP-20 to obtain methanol extracts. Evaluation of cytotoxicity property was carried out on macrophage cell lines (RAW264.7) by 3-(4,5-dimethylthiazol-2-yl) 2,5-diphenyl tetrazoliumbromide assay. Anti-inflammatory screening was done by inducible nitric oxide assay on RAW264.7 cell lines with lipopolysaccharide (LPS) stimulation. Dianion HP-20 was used to remove salt content. A selected methanol extract was subjected to further fractionations by C-18 reverse phase and their anti-inflammatory potential was evaluated by COX-1 and COX-2, and sPLA2 enzymatic assay. Results: Seven methanol extracts showed no cytotoxic property against RAW 264.7 cell line (inhibitory concentration 50% > 30 µg/ml) and selected for anti-inflammatory screening assay. Result showed methanol extract HM 1.2 reduced NO production >80% and it has been selected for phytochemical screening, further fractionations and assay. Phytochemical screening showed alkaloids and terpenoids present in the HM 1.2. The HM 1.2 and its fractions (F1, F2, F1C1, F1C2, F1C3, and F1C4) were proven to inhibit COX-1, COX-2, and sPLA2 activity in the range of 60.516-116.886%, 20.554-116.457%, and 70.2667-114.8148%, respectively. Conclusions: This study revealed that bacteria associated with H. amboinensis have produced anti-inflammatory activity via reducing NO production and inhibiting COX-1, COX-2, and sPLA2 activity.
International Journal of Research in Pharmaceutical Sciences, 2020
Cancer is unchecked growth of normal cells. The screening of new potential agents is vital to dev... more Cancer is unchecked growth of normal cells. The screening of new potential agents is vital to develop effective cytotoxic drugs with reduced side effects. Thecytotoxic effects, mode of cell death and screening of phytochemicals which induced cell death by the mangrove plant Xylocarpus granatum extract on the human hepatocellular carcinoma cell line was studied. The crude methanol extract of Xylocarpusgranatum(bark) partitioning produced the high yield in diethyl ether (54.08%)followed by butanol (37.12%) and aqueous (3.21%).The Xylocarpus granatum bark extract produced a cytotoxic effect with IC50 <30 µg/ml as compared to leaf and root (IC50> 100 µg/ml). The DNA fragmentation study done to determine the mode of cell death. The results attained by the colorimetric TUNEL system propose that Xylocarpus moluccensis extract induced DNA fragmentation in the HepG2 cell line. The darkly stained nuclei observed in HepG2cells treated with Xylocarpus moluccensis(diethyl ether) extract fo...
Breast cancer is amongst frequently diagnosed cancer type throughout the world. Due to reduced ef... more Breast cancer is amongst frequently diagnosed cancer type throughout the world. Due to reduced efficacy of current chemotherapeutics, several natural products have been screened for better alternatives. The cytotoxic activity of fractions prepared from leaves extract of Vitex rotundifolia (V. rotundifolia) on human breast cancer cell line, MCF-7 was studied. The fractions F1, F2, F3, and F5 of V. rotundifolia produced concentration-dependent cytotoxic effects on MCF-7 cell line. The relative potential of cytotoxicity of the fractions on MCF-7 cell line was found to be F3 > F2 > F5 > F1. The active fractions induce apoptosis in MCF-7 cell line determined by annexin V base assay. The phosphatidylserine externalization and the presence of DNA fragmentation in treated cells confirms the early and late apoptosis in treated cells. The V. rotundifolia fractions induced apoptosis by both pathways; extrinsic pathways via activation of caspase-8 and intrinsic pathways through enhanced bax/bcl-2 ratio and activation of caspase-3/7 and caspase-9 proapoptotic proteins. Furthermore, chemical profiling indicates various phenolic, flavonoids, and terpenoids compounds in the active fractions. Thus, V. rotundifolia might be a suitable candidate to investigate further and develop molecular targeted cancer therapeutics by understanding the fundamental mechanisms involved in the regulation of cell death in cancer cells.
Natural products play a crucial role in drug discovery. In the last decade, the advent of marine ... more Natural products play a crucial role in drug discovery. In the last decade, the advent of marine natural product research has produced a remarkable number of compounds, particularly those isolated from marine sponges, with a broad range of activities for the treatment of human and animal diseases. In this study, five known alkaloids namely aaptamine (1), 9-demethylaaptamine (2), 4- N-methylaaptamine (3), 9-methoxyaaptamine (4), 9-demethyloxyaaptamine (5), an uncommon amide in sponge, 4-hydroxybenzamide (6) and 3 β,5α-cholesterol (7) were isolated from the butanol extract of Aaptos aaptos (Schmidt, 1864) by bioactivity-guided isolation. Their structures were determined based on a detailed analysis of their 1D and 2D spectroscopic NMR and EIMS spectral data as well as comparison with literature data. Cytotoxic activity and anti-atherosclerotic property of the compounds were determined based on their ability to increase the transcriptional activity of SRB1 promoter and PPRE in human li...
Centella asiatica is an herbal plant that contains phytochemicals that are widely believed to hav... more Centella asiatica is an herbal plant that contains phytochemicals that are widely believed to have positive effects on cognitive function. The adolescent stage is a critical development period for the maturation of brain processes that encompass changes in physical and psychological systems. However, the effect of C. asiatica has not been extensively studied in adolescents. The aim of this study was therefore to investigate the effects of a C. asiatica extract on the enhancement of learning and memory in adolescent rats. The locomotor activity, learning, and memory were assessed by using open field test and water T-maze test. This study also examined changes in neuronal cell morphology using cresyl violet and apoptosis staining. We also performed immunohistochemical study to analyse the expression of the glutamate AMPA receptor (α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) GluA1 subunit and the GABA receptor (γ-Aminobutyric Acid) subtype GABA α1 subunit in the hippocampus o...
The Malaysian journal of medical sciences : MJMS, 2018
Bamboo shoot has been used as a treatment for epilepsy in traditional Chinese medicine for genera... more Bamboo shoot has been used as a treatment for epilepsy in traditional Chinese medicine for generations to treat neuronal disorders such as convulsive, dizziness and headaches. 4-hydroxybenzoic acid (4-hba) is a non-flavonoid phenol found abundantly in shoots (bamboo), fruits (strawberries and apples) and flowers. Kv1.4 is a rapidly inactivating -related member of the voltage-gated potassium channels with two inactivation mechanisms; the fast N-type and slow C-type. It plays vital roles in repolarisation, hyperpolarisation and signaling the restoration of resting membrane potential through the regulation of the movement of K across the cellular membrane. Chemical compounds from bamboo shoots were purified and identified as major palmitic acids mixed with other minor fatty acids, palmitic acid, 4-hydroxybenzaldehyde, lauric acid, 4-hydroxybenzoic acid and cholest-4-ene-3-one. The response of synthetic 4-hydroxybenzoic acid was tested on Kv1.4 potassium channel which was injected into ...
The α 1 β 2 γ 2 subtype of GABA A receptors is the most commonly found GABA A receptor subtype in... more The α 1 β 2 γ 2 subtype of GABA A receptors is the most commonly found GABA A receptor subtype in the mammalian cortex and hippocampus. It is expressed heterologously in the Xenopus laevis oocyte as a α 1 β 2 γ 2 S/L subtype for application as an in vitro model for the screening of compounds that modulate receptor activities. In fact, 4-hydroxybenzaldehyde (4-HB) has been identified as one of the major components in Dendrocalamus asper bamboo shoots in our previous study, and the current study showed that at 101.7 µM, 4-HB significantly reduced the GABA-induced chloride current of GABA A receptors expressed on Xenopus oocytes, indicating a possible GABAergic antagonistic effect at high concentrations.
Vibriosis is one of diseases which often results in mass mortality of Penaeus monodon larval rear... more Vibriosis is one of diseases which often results in mass mortality of Penaeus monodon larval rearing systems. It attacks shrimp of all stages in zoea, mysis and shrimp postlarva stage. This disease is caused by Vibrio spp, particularly Vibrio harveyi (a luminescent bacterium). Several kinds of antibiotics and chemical material have been used to overcome the disease but they have side effects to environment and human. The searching of bioactive compounds as an alternative treatment has been done for multi purposes. In this study diethyl eter, butanol and aqueous extract of Indonesian sponges Aaptos aaptos and Callyspongia pseudoreticulata were tested for in vitro activity against Vibrio spp. and Vibrio harveyi by using disc diffusion method. The result showed that all extracts of Aaptos aaptos gave a positive antibacterial activity towards those pathogenic bacteria. Meanwhile, only butanol extract of Callyspongia pseudoreticulata obtained to exhibit an antibacterial activity on those...
ABSTRACT Objective: The aims of this study were to identify and evaluate the chemical markers of ... more ABSTRACT Objective: The aims of this study were to identify and evaluate the chemical markers of Ficus deltoidea Jack (FD) varieties namely var. deltoidea, var. trengganuensis, var. kunstleri, var. motleyana, var. intermedia, var. borneensis, var. bilobata and var. angustifolia by high performance thin layer chromatography (HPTLC) and to discriminate between the varieties based on Fourier transform infra-red (FTIR) data. Methods: Methanol extracts of eight varieties and water extracts of five varieties were subjected to HPTLC and FTIR fingerprinting analysis. Quantification of markers (vitexin and isovitexin) was performed by HPTLC. Cluster analysis of principal component analysis (PCA) and hierarchical cluster analysis (HCA) was employed to discriminate between the varieties based on their FTIR data. Results: Two markers, vitexin and isovitexin, were found in all of the varieties, but their contents were varied in the different samples. Cluster analysis (PCA and HCA) was employed t...
Four compounds were isolated from the ethyl acetate crude extract of Xestospongia sp., namely ben... more Four compounds were isolated from the ethyl acetate crude extract of Xestospongia sp., namely benzoic acid, 2-phenylacetic acid, 2-hydroxyl-1H-inden-1-one and 6-styryl-5,6-dihydropyran-2-one. The structures of these compounds were elucidated based on spectroscopic methods including nuclear magnetic resonance (NMR-1D and 2D), UV, IR, mass spectrometry and comparison with literature data. The ethyl acetate extract showed weak antityrosinase and acethylcholinasterase activities. Benzoic acid and 2-phenylacetic acid, were found to posses weak free radical-scavenging activity.
In vitro and in vivo studies of the activity of Phaleria macrocarpa Boerl (Thymelaeaceae) leaves ... more In vitro and in vivo studies of the activity of Phaleria macrocarpa Boerl (Thymelaeaceae) leaves against the therapeutic target for hypercholesterolemia were done using the HDL receptor (SR-BI) and hypercholesterolemia-induced Sprague Dawley rats. The in vitro study showed that the active fraction (CF6) obtained from the ethyl acetate extract (EMD) and its component 2',6',4-trihydroxy-4'-methoxybenzophenone increased the SR-BI expression by 95% and 60%, respectively. The in vivo study has proven the effect of EMD at 0.5 g/kgbw dosage in reducing the total cholesterol level by 224.9% and increasing the HDL cholesterol level by 157% compared to the cholesterol group. In the toxicity study, serum glutamate oxalate transaminase (SGOT) and serum glutamate pyruvate transaminase (SGPT) activity were observed to be at normal levels. The liver histology also proved no toxicity and abnormalities in any of the treatment groups, so it can be categorized as non-toxic to the rat liver. The findings taken together show that P. macrocarpa leaves are safe and suitable as an alternative control and prevention treatment for hypercholesterolemia in Sprague Dawley rats.
Objective: Liver cancer is one of the most common causes of cancer death, with reduced survival r... more Objective: Liver cancer is one of the most common causes of cancer death, with reduced survival rates. The development of new chemotherapeutic agents is essential to find effective cytotoxic drugs that give minimum side effects to the surrounding healthy tissues. The main objective of the present study was to evaluate the cytotoxic effects and mechanism of cell death induced by the crude and diethyl ether extract of Xylocarpus mouccensis on the human hepatocellular carcinoma cell line. Methods: The cytotoxicity activity was measured using the MTS assay. The mode of cell death determined by the apoptosis study, DNA fragmentation analysis done by using the TUNEL system. The pathway study or mechanism of apoptosis observed by study caspases 8, 9, 3/7 Glo-caspases method. Results: In this study, the methanol extracts prepared from leaf Xylocarpus mouccensis leaf produced cytotoxicity effect with IC 50 (72hr) < 30µg/ml. The IC 50 value at 72 hours exerted by diethyl ether extract of Xylocarpus moluccensis leaf was 0.22 µg/ml, which was more cytotoxic than to that of crude methanol extract. The results obtained by the colorimetric TUNEL system suggest that methanol crude extract of Xylocarpus moluccensis (leaf), diethyl ether extract of Xylocarpus moluccensis (leaf) and methanol extract of Xylocarpus granatum (bark) induced DNA fragmentation in the HepG2 cell line. Besides, the caspase-Glo assay demonstrated that diethyl ether leaf extract of Xylocarpus moluccensis triggered apoptotic cell death via activation of caspases-8, and-3/7 However, no visible activation was noticed for caspase-9. Furthermore, TLC indicates the presence of potential metabolites in an extract of Xylocarpus moluccensis. Conclusion: Thus, the present study suggests the remarkable potential of active metabolites in the extract of Xylocarpus moluccensis as a future therapeutic agent for the treatment of cancer.
Atherosclerosis is the main cause of cardiovascular diseases which in turn, lead to the highest n... more Atherosclerosis is the main cause of cardiovascular diseases which in turn, lead to the highest number of mortalities globally. This pathophysiological condition is developed due to a constant elevated level of plasma cholesterols. Statin is currently the widely used treatment in reducing the level of cholesterols, however, it may cause adverse side effects. Therefore, there is an urgent need to search for new alternative treatment. PCSK9 is an enzyme responsible in directing LDL-receptor (LDL-R)/LDL-cholesterols (LDL-C) complex to lysosomal degradation, preventing the receptor from recycling back to the surface of liver cells. Therefore, PCSK9 offers a potential target to search for small molecule inhibitors which inhibit the function of this enzyme. In this study, a marine invertebrate Acanthaster planci, was used to investigate its potential in inhibiting PCSK9 and lowering the levels of cholesterols. Cytotoxicity activity of A. planci on human liver HepG2 cells was carried out u...
Hystatin is a group of compounds resulted from the derivatization of aaptamine. A series of hysta... more Hystatin is a group of compounds resulted from the derivatization of aaptamine. A series of hystatin 2 derivatives (3, 5-15) have been synthesized and characterized using modern spectroscopic techniques, namely IR, 1 H and 13 C NMR, UV-Vis and Mass Spectrometer. The synthesized compounds were evaluated for their antibacterial activity against selected bacterial strains of both Gram positive and Gram negative groups, namely Bacillus cereus, Staphylococcus aureus, Micrococcus sp, Escherichia coli, Pseudomonas aeruginosa and Klebsiella pneumoniae using standard microbiological protocol of disc-diffusion method. The antibacterial activities of the compounds were assessed by the presence and absence of inhibition zones and minimum inhibition concentration (MIC) values. In general, most of the derivatives showed significant antibacterial activity towards Gram positive bacteria. It was observed that compound 6 exhibited bacterial inhibition activity against all tested bacteria. Nonetheless...
The study was conducted to explore the anticholinesterase inhibition property of eugenol derived ... more The study was conducted to explore the anticholinesterase inhibition property of eugenol derived molecules. Ten eugenol derivatives were synthesized and evaluated for the inhibitory activities against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) by Ellman’s method. Most of the tested derivatives showed higher inhibition on BChE than AChE, however, their overall inhibitory activity was weak. In contrast, three derivatives (compounds 3,6,9) showed higher and good AChE inhibitory activity of more than 50% inhibition at 10 μg/mL. Among them, compound 9bearing a ethyl substituent at para position of the benzoyl ring showed the most potent AChE inhibition, with IC50 of 5.64 μg/mL. Ligand-protein docking simulation was also performed for the most active derived molecules (compounds 3,6,9).
Background: Quercus infectoria galls (QI) extracts were previously reported to have cytotoxicity ... more Background: Quercus infectoria galls (QI) extracts were previously reported to have cytotoxicity effects towards human cervical cancer cells, HeLa. However, the underlying molecular mechanisms of the extracts have been poorly determined. Objective: The present study was undertaken to examine the effect of ethyl acetate extracts of QI (EAQI) on cell cytotoxicity and induction of apoptosis in HeLa cells. Materials and Method: The in vitro cytotoxicity was investigated by using the MTT [3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyl tetrazolium bromide] assay and the OD values were read at 570 nm. Meanwhile the induction of apoptosis was measured by using acridine orange and propidium iodide (AO/PI) staining, flow cytometry analysis of annexin V/PI staining and cell cycle distribution. Results: MTT assay showed that EAQI exhibited cytotoxicity effect on HeLa cells with IC 50 of 11.50 ± 0.50 µg/ml. HeLa cells underwent apoptosis in response to EAQI treatment, demonstrated by an increase in the percentage of apoptotic cell stained with AOPI from 1.00% to 10.33% compared to untreated cell population (p<0.05) at 72 hours of treatment. The evidence of early apoptosis in treated cells were also observed in annexin V/PI staining. Furthermore, an increase of cell population in sub G0/G1 phase revealed that apoptosis as the mode of cell death in HeLa cells treated with EAQI. Conclusion: These findings indicated that EAQI significantly inhibits HeLa cell growth through induction of apoptosis. Further studies are needed to confirm the mechanism of cell death by expression of apoptotic cascade in HeLa cells treated with EAQI.
In this study, Peperomia pellucida was subjected to the determination of biological activity and ... more In this study, Peperomia pellucida was subjected to the determination of biological activity and isola tion of chemical constituents. Two samples of this plant we re used, which were the air-dried and freeze-dried. The sequential maceration of the plant utilized three d ifferent solvents with increasing polarities, namel y dichloromethane, ethyl acetate and methanol. The Th in Layer Chromatography (TLC) profile showed there was no significant different in the chemical constituents in both samples. All six crude extracts displayed i n v tro antimicrobial activity on Pseudomonas aeruginosa, w ith minimum inhibition zone 9.0±1.7 mm and no activ ity on 7 other type of bacteria (Escherichia coli, Klebsiell a pneumonia, Salmonella sp., Bacillus subtilis, Mic rococcus sp., Staphylococcus aureus and Streptococcus uberis). In addition, antioxidant activity of all of the crude extracts was determined using DPPH (2,2-diphenyl-picryhdrazyl) r adical scavenging assay. Among the extracts methano ...
The inhibitory effects of nutmeg essential oil and three components of this oil at different conc... more The inhibitory effects of nutmeg essential oil and three components of this oil at different concentrations were tested by GABA-induced chloride current (I GABA) stimulation through gamma-aminobutyric acid type A (GABAA) receptors comprising of α1β2γ2s subtype using the two-microelectrode voltage clamp technique on Xenopus laevis oocytes. The essential oil of the kernels of Myristica fragrans was extracted by steam distillation and was analysed by gas chromatography-mass spectrometer (GC-MS) technique. A total of 16 compounds were isolated from the essential oil. The essential oil showed promising activity by enhanced I GABA up to 100% of stimulation when tested at 100 nL/mL. For dose dependent activity, α-terpineol and myristicin showed statistical significant potentiation of I GABA. α-Terpineol was found to induce an enhancement of I GABA modulation (EC5-10) by 229.6±23.8% and 326.3±43.8%, at 100 μM and 500 μM, respectively. Myristicin induced an enhancement up to 237.6±35.1% at 5...
Inhibition of aldose reductase (ALR2) by using small heterocyclic compounds provides a viable app... more Inhibition of aldose reductase (ALR2) by using small heterocyclic compounds provides a viable approach for the development of new antidiabetic agents.
Aims: Piper sarmentosum or locally known as Kaduk, is a tropical herb plant that was investigated... more Aims: Piper sarmentosum or locally known as Kaduk, is a tropical herb plant that was investigated for its phenolic content by previous researchers. The present study aimed at the analysis of crude methanolic extract of P. sarmentosum leaves for phenolic compounds identification and its anti-amoebic properties against pathogenic Acanthamoeba castellanii. Methodology and results: Folin-Ciocalteu assay was used to determine P. sarmentosum leaves methanolic extract (PSLME)'s total phenolic content (TPC). The extract was further characterized by using gas chromatography-mass spectrometry (GC-MS), reverse phase-high performance liquid chromatography (RP-HPLC) and liquid chromatographymass spectrometry (LC-MS) analyses to determine the chemical constituents in methanolic PSLME extract. The cytotoxicity of the extract was evaluated through the determination of inhibition concentration for half of cell population (IC50) of pathogenic A. castellanii followed by cell morphological analysis using inverted light and scanning electron microscopies. Acridine-orange/Propidium iodide (AOPI) staining was also conducted to determine the integrity of cell membrane for quantitative analysis. The results demonstrated that the TPC from PSLME was 142.72 mg [GAE]/g with a total of 33 phenolic compounds identified. The IC50 value obtained for A. castellanii was low (74.64 μg/mL) which indicates promising anti-acanthamoebic activity. Microscopy analyses showed that the plant extract caused cells encystment, in which exhibited by distinctive morphological changes on the cells shape and organelle, as well as shortening of acanthopodia. The dual staining and its quantitative analysis prove compromised membrane integrity in the treated amoeba. Conclusion, significance and impact of study: This finding provides the evidence that PSLME contains active phenolic compounds contributing to the anti-acanthamoebic activity on pathogenic Acanthamoeba species.
Asian Journal of Pharmaceutical and Clinical Research, Nov 1, 2017
Objective: This study aimed to investigate the anti-inflammatory activity of methanol extract and... more Objective: This study aimed to investigate the anti-inflammatory activity of methanol extract and fractions of bacteria associated with sponge (Haliclona amboinensis) and to evaluate their effect in reducing NO production and inhibiting cyclooxygenase-1 (COX-1), cyclooxgenase-2 (COX-2) and secretory phospholipase A2 (sPLA2) activity. Methods: All bacterial isolates were cultured and supernatants were collected for the extraction of secondary metabolites using diaion HP-20 to obtain methanol extracts. Evaluation of cytotoxicity property was carried out on macrophage cell lines (RAW264.7) by 3-(4,5-dimethylthiazol-2-yl) 2,5-diphenyl tetrazoliumbromide assay. Anti-inflammatory screening was done by inducible nitric oxide assay on RAW264.7 cell lines with lipopolysaccharide (LPS) stimulation. Dianion HP-20 was used to remove salt content. A selected methanol extract was subjected to further fractionations by C-18 reverse phase and their anti-inflammatory potential was evaluated by COX-1 and COX-2, and sPLA2 enzymatic assay. Results: Seven methanol extracts showed no cytotoxic property against RAW 264.7 cell line (inhibitory concentration 50% > 30 µg/ml) and selected for anti-inflammatory screening assay. Result showed methanol extract HM 1.2 reduced NO production >80% and it has been selected for phytochemical screening, further fractionations and assay. Phytochemical screening showed alkaloids and terpenoids present in the HM 1.2. The HM 1.2 and its fractions (F1, F2, F1C1, F1C2, F1C3, and F1C4) were proven to inhibit COX-1, COX-2, and sPLA2 activity in the range of 60.516-116.886%, 20.554-116.457%, and 70.2667-114.8148%, respectively. Conclusions: This study revealed that bacteria associated with H. amboinensis have produced anti-inflammatory activity via reducing NO production and inhibiting COX-1, COX-2, and sPLA2 activity.
International Journal of Research in Pharmaceutical Sciences, 2020
Cancer is unchecked growth of normal cells. The screening of new potential agents is vital to dev... more Cancer is unchecked growth of normal cells. The screening of new potential agents is vital to develop effective cytotoxic drugs with reduced side effects. Thecytotoxic effects, mode of cell death and screening of phytochemicals which induced cell death by the mangrove plant Xylocarpus granatum extract on the human hepatocellular carcinoma cell line was studied. The crude methanol extract of Xylocarpusgranatum(bark) partitioning produced the high yield in diethyl ether (54.08%)followed by butanol (37.12%) and aqueous (3.21%).The Xylocarpus granatum bark extract produced a cytotoxic effect with IC50 <30 µg/ml as compared to leaf and root (IC50> 100 µg/ml). The DNA fragmentation study done to determine the mode of cell death. The results attained by the colorimetric TUNEL system propose that Xylocarpus moluccensis extract induced DNA fragmentation in the HepG2 cell line. The darkly stained nuclei observed in HepG2cells treated with Xylocarpus moluccensis(diethyl ether) extract fo...
Breast cancer is amongst frequently diagnosed cancer type throughout the world. Due to reduced ef... more Breast cancer is amongst frequently diagnosed cancer type throughout the world. Due to reduced efficacy of current chemotherapeutics, several natural products have been screened for better alternatives. The cytotoxic activity of fractions prepared from leaves extract of Vitex rotundifolia (V. rotundifolia) on human breast cancer cell line, MCF-7 was studied. The fractions F1, F2, F3, and F5 of V. rotundifolia produced concentration-dependent cytotoxic effects on MCF-7 cell line. The relative potential of cytotoxicity of the fractions on MCF-7 cell line was found to be F3 > F2 > F5 > F1. The active fractions induce apoptosis in MCF-7 cell line determined by annexin V base assay. The phosphatidylserine externalization and the presence of DNA fragmentation in treated cells confirms the early and late apoptosis in treated cells. The V. rotundifolia fractions induced apoptosis by both pathways; extrinsic pathways via activation of caspase-8 and intrinsic pathways through enhanced bax/bcl-2 ratio and activation of caspase-3/7 and caspase-9 proapoptotic proteins. Furthermore, chemical profiling indicates various phenolic, flavonoids, and terpenoids compounds in the active fractions. Thus, V. rotundifolia might be a suitable candidate to investigate further and develop molecular targeted cancer therapeutics by understanding the fundamental mechanisms involved in the regulation of cell death in cancer cells.
Natural products play a crucial role in drug discovery. In the last decade, the advent of marine ... more Natural products play a crucial role in drug discovery. In the last decade, the advent of marine natural product research has produced a remarkable number of compounds, particularly those isolated from marine sponges, with a broad range of activities for the treatment of human and animal diseases. In this study, five known alkaloids namely aaptamine (1), 9-demethylaaptamine (2), 4- N-methylaaptamine (3), 9-methoxyaaptamine (4), 9-demethyloxyaaptamine (5), an uncommon amide in sponge, 4-hydroxybenzamide (6) and 3 β,5α-cholesterol (7) were isolated from the butanol extract of Aaptos aaptos (Schmidt, 1864) by bioactivity-guided isolation. Their structures were determined based on a detailed analysis of their 1D and 2D spectroscopic NMR and EIMS spectral data as well as comparison with literature data. Cytotoxic activity and anti-atherosclerotic property of the compounds were determined based on their ability to increase the transcriptional activity of SRB1 promoter and PPRE in human li...
Centella asiatica is an herbal plant that contains phytochemicals that are widely believed to hav... more Centella asiatica is an herbal plant that contains phytochemicals that are widely believed to have positive effects on cognitive function. The adolescent stage is a critical development period for the maturation of brain processes that encompass changes in physical and psychological systems. However, the effect of C. asiatica has not been extensively studied in adolescents. The aim of this study was therefore to investigate the effects of a C. asiatica extract on the enhancement of learning and memory in adolescent rats. The locomotor activity, learning, and memory were assessed by using open field test and water T-maze test. This study also examined changes in neuronal cell morphology using cresyl violet and apoptosis staining. We also performed immunohistochemical study to analyse the expression of the glutamate AMPA receptor (α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) GluA1 subunit and the GABA receptor (γ-Aminobutyric Acid) subtype GABA α1 subunit in the hippocampus o...
The Malaysian journal of medical sciences : MJMS, 2018
Bamboo shoot has been used as a treatment for epilepsy in traditional Chinese medicine for genera... more Bamboo shoot has been used as a treatment for epilepsy in traditional Chinese medicine for generations to treat neuronal disorders such as convulsive, dizziness and headaches. 4-hydroxybenzoic acid (4-hba) is a non-flavonoid phenol found abundantly in shoots (bamboo), fruits (strawberries and apples) and flowers. Kv1.4 is a rapidly inactivating -related member of the voltage-gated potassium channels with two inactivation mechanisms; the fast N-type and slow C-type. It plays vital roles in repolarisation, hyperpolarisation and signaling the restoration of resting membrane potential through the regulation of the movement of K across the cellular membrane. Chemical compounds from bamboo shoots were purified and identified as major palmitic acids mixed with other minor fatty acids, palmitic acid, 4-hydroxybenzaldehyde, lauric acid, 4-hydroxybenzoic acid and cholest-4-ene-3-one. The response of synthetic 4-hydroxybenzoic acid was tested on Kv1.4 potassium channel which was injected into ...
The α 1 β 2 γ 2 subtype of GABA A receptors is the most commonly found GABA A receptor subtype in... more The α 1 β 2 γ 2 subtype of GABA A receptors is the most commonly found GABA A receptor subtype in the mammalian cortex and hippocampus. It is expressed heterologously in the Xenopus laevis oocyte as a α 1 β 2 γ 2 S/L subtype for application as an in vitro model for the screening of compounds that modulate receptor activities. In fact, 4-hydroxybenzaldehyde (4-HB) has been identified as one of the major components in Dendrocalamus asper bamboo shoots in our previous study, and the current study showed that at 101.7 µM, 4-HB significantly reduced the GABA-induced chloride current of GABA A receptors expressed on Xenopus oocytes, indicating a possible GABAergic antagonistic effect at high concentrations.
Vibriosis is one of diseases which often results in mass mortality of Penaeus monodon larval rear... more Vibriosis is one of diseases which often results in mass mortality of Penaeus monodon larval rearing systems. It attacks shrimp of all stages in zoea, mysis and shrimp postlarva stage. This disease is caused by Vibrio spp, particularly Vibrio harveyi (a luminescent bacterium). Several kinds of antibiotics and chemical material have been used to overcome the disease but they have side effects to environment and human. The searching of bioactive compounds as an alternative treatment has been done for multi purposes. In this study diethyl eter, butanol and aqueous extract of Indonesian sponges Aaptos aaptos and Callyspongia pseudoreticulata were tested for in vitro activity against Vibrio spp. and Vibrio harveyi by using disc diffusion method. The result showed that all extracts of Aaptos aaptos gave a positive antibacterial activity towards those pathogenic bacteria. Meanwhile, only butanol extract of Callyspongia pseudoreticulata obtained to exhibit an antibacterial activity on those...
ABSTRACT Objective: The aims of this study were to identify and evaluate the chemical markers of ... more ABSTRACT Objective: The aims of this study were to identify and evaluate the chemical markers of Ficus deltoidea Jack (FD) varieties namely var. deltoidea, var. trengganuensis, var. kunstleri, var. motleyana, var. intermedia, var. borneensis, var. bilobata and var. angustifolia by high performance thin layer chromatography (HPTLC) and to discriminate between the varieties based on Fourier transform infra-red (FTIR) data. Methods: Methanol extracts of eight varieties and water extracts of five varieties were subjected to HPTLC and FTIR fingerprinting analysis. Quantification of markers (vitexin and isovitexin) was performed by HPTLC. Cluster analysis of principal component analysis (PCA) and hierarchical cluster analysis (HCA) was employed to discriminate between the varieties based on their FTIR data. Results: Two markers, vitexin and isovitexin, were found in all of the varieties, but their contents were varied in the different samples. Cluster analysis (PCA and HCA) was employed t...
Four compounds were isolated from the ethyl acetate crude extract of Xestospongia sp., namely ben... more Four compounds were isolated from the ethyl acetate crude extract of Xestospongia sp., namely benzoic acid, 2-phenylacetic acid, 2-hydroxyl-1H-inden-1-one and 6-styryl-5,6-dihydropyran-2-one. The structures of these compounds were elucidated based on spectroscopic methods including nuclear magnetic resonance (NMR-1D and 2D), UV, IR, mass spectrometry and comparison with literature data. The ethyl acetate extract showed weak antityrosinase and acethylcholinasterase activities. Benzoic acid and 2-phenylacetic acid, were found to posses weak free radical-scavenging activity.
In vitro and in vivo studies of the activity of Phaleria macrocarpa Boerl (Thymelaeaceae) leaves ... more In vitro and in vivo studies of the activity of Phaleria macrocarpa Boerl (Thymelaeaceae) leaves against the therapeutic target for hypercholesterolemia were done using the HDL receptor (SR-BI) and hypercholesterolemia-induced Sprague Dawley rats. The in vitro study showed that the active fraction (CF6) obtained from the ethyl acetate extract (EMD) and its component 2',6',4-trihydroxy-4'-methoxybenzophenone increased the SR-BI expression by 95% and 60%, respectively. The in vivo study has proven the effect of EMD at 0.5 g/kgbw dosage in reducing the total cholesterol level by 224.9% and increasing the HDL cholesterol level by 157% compared to the cholesterol group. In the toxicity study, serum glutamate oxalate transaminase (SGOT) and serum glutamate pyruvate transaminase (SGPT) activity were observed to be at normal levels. The liver histology also proved no toxicity and abnormalities in any of the treatment groups, so it can be categorized as non-toxic to the rat liver. The findings taken together show that P. macrocarpa leaves are safe and suitable as an alternative control and prevention treatment for hypercholesterolemia in Sprague Dawley rats.
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