Pharmacognosy

Endophytic Aspergillus species represent an inexhaustible source for many medicinally important secondary metabolites. The current study isolated the endophytic Aspergillus niger (OL519514) fungus from Opuntia ficus-indica fruit peels. The antibacterial activities were reported for both Aspergillus species and Opuntia ficus-indica fruit peel extract. Extraction of the endophytic fungal metabolites using ethyl acetate and fractionation was performed, yielding dihydroauroglaucin (C1), isotetrahydroauroglaucin (C2), and cristatumin B (C3). Resistant bacterial strains were used to investigate the efficiency of the total fungal ethyl acetate extract (FEA) and the isolated compounds. FEA showed promising wide spectrum activity. (C3) showed excellent activity against selected Gram-negative resistant bacteria; However, (C2) exhibited tremendous activity against the tested Gram-positive resistant strains; conversely, (C1) possessed the lowest antibacterial activity compared to the two other ...

Purpose: the non-edible fruit parts of Casimiroa edulis Llave et were evaluated for their active constituents and their potential as antioxidants, anti-inflammatory and antitumor activity. Methods: Fruits peel (FP) and seeds kernel (SK) of Casimiroa edulis Llave et Lex. were extracted successively with hexane and then methanol. Fatty acids were prepared from hexane extracts and identified by GC. Total flavonoid, phenolic acids and tannins contents in methanol extracts were determined by UV spectrophotometer and identified by HPLC. Antioxidant, in-vitro anti-inflammatory activity and antitumor effect against Caco-2 cell line were determined. Results: GC analysis of hexane extracts showed that oleic acid (47.00%) was the major unsaturated fatty acids in both extracts while lignoceric acid (15.49%) is the most abundant saturated fatty acid in (FP). Total phenolic, flavonoid and tannin contents in (FP) & (SK) methanol extracts were; 37.5±1.5, 10.79±0.66 and 22.28±0.23 for (FP); 53.5±1.5...

The aim of the present study is to investigate the effect of different altitude on the chemical composition and antimicrobial activity of the essential oil prepared from wild Libyan growing Thymus capitatus L. aerial parts collected from Al-Jabal Akhdar. Two different altitudes were chosen represented by Abu-Draa (650 m above the see level) and Sidi Al-Hamey (850 m above the see level). This study concerned with both qualitative and quantitative variations. The percentage yield for T. capitatus essential oils yield were 1.5% and 1.04% for both Abu-Draa and Sidi Al-Hamry respectively. GC/MS analysis for each essential oil revealed the identification of 14 volatile components corresponding to 91.99% from Abu-Draa and 23 compounds corresponding to 96.54% from Sidi Al-Hamrey. Carvcrol was the major volatile component present in both essential oils of Abu-Draa and Sidi Al-Hamrey regions (58.56% and 24.28% respectively). The second major volatile compound present in the essential oil prepared from Abu-Draa is b-caryophyllene (7.41%) followed by its oxide (6.26%); on the other hand Gamma-terpinene is the second major volatile compound present in Sidi Alhamry prepared oil (16.18%) followed by caryophyllene oxide (10.43%). Both phenolic and phenolic ethers are dominated in both examined oils (62.51, 33.74% respectively) resulting in a great antimicrobial activity for both of them which is more prominent in that oil prepared from the low altitude Abu-draa.

Araucaria is a small genus of evergreen coniferous trees, widely used for ornamental and timber purposes. Araucaria species are rich in essential oils. In this study, the essential oils obtained from the foliage of Araucaria heterophylla (Salisb.) and Araucaria bidwillii Hook were analyzed using GC and GC/MS. Cytotoxicity of both essential oils was assessed on three human cancer cell lines using MTT assay. Twenty nine compounds were annotated in A. heterophylla essential oil, whereas forty three were identified in A. bidwillii accounting for 95.16% and 81.06% of the total volatile oil composition, respectively. Pinene (70.85%), D-limonene (4.26%) and germacrene D (2.99%) represented the major compounds in A. heterophylla. Beyerene (35.65%), transnerolidol (13.66% 6.09%) dominated in A. bidwillii. Both oils showed potent cytotoxicity against all tested cancer cell lines (Hep-G2, MCF-7 and Caco-2) exhibiting IC50 values of 0.70, 3.20 and 1.10 g/ ml for A. heterophylla; and 1.67, 1.10 and 1.32 g/ml for A. bidwillii, respectively. Caspase-3 activation indicated that the cytotoxicity of A. bidwillii essential oil is mediated via caspase-dependent apoptosis. These findings suggest that the essential oils of A. heterophylla and A. bidwilli offer promising anticancer drug candidates pertaining to the synergistic effects of their individual components.

Objectives Combined chemotherapy and radiotherapy usually associated with various comorbidities especially on rapidly proliferating cells as testis. This study aimed to characterize main constituents of Ocimum basilicum L. (OB) aqueous extract and examine its protective effect on doxorubicin/irradiation (DOXO/IR)-induced testicular injury in rats. Methods Spectrophotometric analysis showed considerable amount of polyphenolic (146.31 µg/mg) and flavonoid contents (28.63 µg/mg); UPLC-ESI-MS/MS analysis revealed that the major flavonoid was apigenin-O-glucoside (7.53%) followed by luteolin (5.94%), while rosmarinic acid was the major polyphenolic (15.76%) followed by caftaric acid (9.39%); rutin and querctin were also present and were quantified using high-performance liquid chromatography. Administration of OB extract (200 mg/kg per day; p.o.) to DOXO/IR rats resulted in marked improvement of associated testicular damage. Key findings Ocimum basilicum L. significantly decreased testic...

Euryops pectinatus is a South African ornamental plant belonging to family Asteraceae. The present work evaluates the cytotoxic activity and phytochemical profile of the flower extract. Metabolite profiling was performed using HPLC-PDA-ESI-MS/MS. Total phenolics and flavonoids content were assessed. Cytotoxicity was evaluated against 6 different cancer cell lines using MTT assay. The possible underlying mechanism was proposed. We analyzed whether the extract could overcome the resistance of multidrug-resistant cancer cells for doxorubicin. The effect of combination of E. pectinatus with doxorubicin was also studied. Additionally, the potential inhibitory activity of the identified phytochemicals to PB1 protein was analyzed using in silico molecular docking. Twenty-five compounds were tentatively identified. Total phenolic and flavonoid contents represented 49.41 ± 0.66 and 23.37 ± 0.23 µg/mg dried flower extract, respectively. The extract showed selective cytotoxicity against Caco2 ...

Active components from natural sources are the current focus in most pharmacological research to provide new therapeutic agents for clinical use. Essential oils from the Pinus species have been traditionally used in medicine. This study aimed to investigate the chemical profile of two Pinus species, Pinus halepensis L. and Pinus pinea Mill, from different altitudes in Libya and study the effect of environmental conditions on the biological activities of essential oils. A clevenger apparatus was used to prepare the essential oils by hydrodistillation. Analyses were done using GC/MS. Anthelmintic and antimicrobial activities were tested against the earthworm Allolobophora caliginosa, gram-positive bacteria, gram-negative bacteria, and fungi. Different chemical profiles were observed among all tested essential oils, and terpenes were the most dominant class. All studied essential oils from the Pinus species exhibited a remarkable anthelmintic activity compared to the standard piperazin...

Gazania longiscapa DC and Gazania rigens L. are species of cultivated ornamental plant that grow in Egypt. Genus Gazania has a role in folk medicine to prevent toothache; this study presents a comparative investigation of genetic and botanical features of root, rhizome, leaves and flowers of the two Gazania species and comparing their biological activity as analgesic and anti inflammatory as related to their folk medicinal use.

Eradication of Helicobacter pylori is a challenge due to rising antibiotic resistance and GIT-related disorders. Cuminum cyminum, Pimpinella anisum, and Carum carvi are fruits belonging to the Apiaceae family. Their essential oils were extracted, analyzed using GC-MS, tested for anti-H. pylori activity by a micro-well dilution technique, identified for potential anti-H. pylori inhibitors by an in-silico study, and investigated for anti-inflammatory activity using a COX-2 inhibition assay. Results showed that the main components of C. cyminum, P. anisum, and C. carvi were cumaldehyde (41.26%), anethole (92.41%), and carvone (51.38%), respectively. Essential oil of C. cyminum exhibited the greatest anti-H. pylori activity (3.9 µg/mL) followed by P. anisum (15.63 µg/mL), while C. carvi showed the lowest activity (62.5 µg/mL). The in-silico study showed that cumaldehyde in C. cyminum has the best fitting energy to inhibit H. pylori.C. cyminum essential oil showed the maximum ability to ...

Due to its rising antibiotic resistance and associated inflammations, Helicobacter pylori poses a challenge in modern medicine. Salvia officinalis, a member of the Lamiaceae family, is a promising medicinal herb. In this regard, a phytochemical screening followed by GC-MS and LC-MS was done to evaluate the chemical profile of the total ethanolic extract (TES) and the essential oil, respectively. The anti-H. pylori and the anti-inflammatory activities were evaluated by a micro-well dilution technique and COX-2 inhibition assay. Potential anti-H. pylori inhibitors were determined by an in silico study. The results revealed that the main metabolites were flavonoids, sterols, volatile oil, saponins, and carbohydrates. The LC-MS negative ionization mode demonstrated 12 compounds, while GC-MS showed 21 compounds. Carnosic acid (37.66%), epirosmanol (20.65%), carnosol1 (3.3%), and 12-O-methyl carnosol (6.15%) were predominated, while eucalyptol (50.04%) and camphor (17.75%) were dominant i...

Pimenta racemosa is a commonly known spice used in traditional medicine to treat several ailments. In this study, comprehensive phytochemical profiling of the essential oils and methanol extracts of P. racemosa leaves and stems was performed, alongside assessing their potential Helicobacter pylori inhibitory activity in vitro and in silico. The essential oils were chemically profiled via GC-MS. Moreover, the methanol extracts were profiled using HPLC-PDA-ESI-MS/MS. The antibacterial activity of the essential oils and methanol extracts against H. pylori was determined by adopting the micro-well dilution method. GC-MS analysis unveiled the presence of 21 constituents, where eugenol represented the major component (57.84%) and (59.76%) in both leaves and stems of essential oils, respectively. A total of 61 compounds were annotated in both leaves and stems of P. racemosa methanolic extracts displaying richness in phenolic compounds identified as (epi)catechin and (epi)gallocatechin mono...

One of the most widely distributed soft coral species, found especially in shallow waters of the Indo-Pacific region, Red Sea, Mediterranean Sea, and also the Arctic, is genus Sacrophyton. The total number of species belonging to it was estimated to be 40. Sarcophyton species are considered to be a reservoir of bioactive natural metabolites. Secondary metabolites isolated from members belonging to this genus show great chemical diversity. They are rich in terpenoids, in particular, cembranoids diterpenes, tetratepenoids, triterpenoids, and ceramide, in addition to steroids, sesquiterpenes, and fatty acids. They showed a broad range of potent biological activities, such as antitumor, neuroprotective, antimicrobial, antiviral, antidiabetic, antifouling, and anti-inflammatory activity. This review presents all isolated secondary metabolites from species of genera Sacrophyton, as well as their reported biological activities covering a period of about two decades (1998–2019). It deals with 481 metabolites, including 323 diterpenes, 39 biscembranoids, 11 sesquiterpenes, 53 polyoxygenated sterols, and 55 miscellaneous and their pharmacological activities.

Culex pipiens mosquitoes are vectors to many viruses and can transmit diseases such as filariasis and avian malaria. The present study evaluated the larvicidal activity of marine-derived endophytic fungi Aspergillus nomius and Aspergillus flavus from the soft coral Sarcophyton ehrenbergi along with two known cyclodepsipeptide compounds, scopularide A (1) and B (2), isolated from A. flavus extract, against third-instar larvae of C. pipiens, using distilled water as a negative control and toosenedanin as a positive control. The structures of the isolated compounds were confirmed by various spectroscopic analyses. The lethal concentrations (LC50 and LC90) were calculated by probit analysis. Scopularide A was the most potent after 96 h treatment, with LC50 and LC90 values of 58.96 and 994.31 ppm, respectively, and with 82.66% mortality at a concentration of 300 ppm. To unravel the biochemical mechanism of the tested extracts and compounds, their effects against protease, chitinase, phen...

Rhizomes of ginger are commonly used as a spice and for home remedies in either fresh or dry form. This study aimed to assess the effect of sun drying on the volatile constituents, total phenolic and flavonoid content, and the antiviral activity of ginger against low-pathogenic human coronavirus. The antiviral effect of the major volatile compounds was predicted through molecular docking. GC/MS was employed for profiling the volatile constituents of both fresh and dry ginger oils. Moreover, chemometric analysis was applied to discriminate between fresh and dry ginger and to investigate the correlation between their volatile constituents and the antiviral activity using principal component analysis (PCA) and partial least-squares regression (PLS-R). GC/MS analysis revealed that the major effects of the drying process were an increase in α-curcumene and β-sesquiphellandrene. Moreover, total phenolic and flavonoid contents of dried ginger decreased considerably. A PCA score plot reveal...

Background Endophytic Aspergillus species produce countless valuable bioactive secondary metabolites. In the current study, Aspergillus flavus an endophyte from the soft coral Sarcophyton ehrenbergi was chemically explored and the extracted phytoconstituents were subsequently evaluated for antimicrobial activity. This is accomplished by employing nuclear magnetic resonance (NMR) spectroscopy and computational techniques. Additionally, An in vitro anticancer analysis of A. flavus total extract against breast cancer cells (MCF-7) was investigated. Result Six compounds were separated from the crude alcohol extract of the endophytic Aspergillus flavus out of which anhydro-mevalonolactone was reported for the first time. The anti-fungal and anti-Helicobacter pylori properties of two distinct compounds (Scopularides A and B) were assessed. Additionally, computational research was done to identify the binding mechanisms for all compounds. Both the compounds were found to be active against ...

LC-ESI-MS/MS was used for a comprehensive characterization of ethanol extract from the leaves of three Pistacia species. After optimization of the method and the use of the negative ionization mode, a total of 42 different compounds were identified, of which 22 were tentatively characterized in P. chinensis Bunge, 33 in P. khinjuk stocks and 25 in P. lentiscus L. leaves. Flavonoids, phenolic acids, and their derivatives were the most abundant identified compounds. LC-MS/MS revealed identification of 15, 18 and 6 not previously detected compounds in P. chinensis Bunge, P. khinjuk Stocks, and P. lentiscus L. respectively. The three extracts were also tested for their cytotoxic activities against human PC3 prostate cancer, A549 lung cancer, MCF7 breast cancer and HepG2 liver cancer. Generally, all the extracts have a moderate cytotoxic activity against lung, breast and prostate cancer, with different IC 50. However, only P. lentiscus L. showed moderate activity against liver cancer.

Background As an external organ, the skin protects the whole body against hazardous external influences. Ultraviolet (UV) radiation is one of these influences which in high amount can cause DNA damage, and even skin cancer. Hence, it is important to promote skin protection with commercially available remedies, and with a healthy diet. Certain vegetables when applied topically or consumed orally may help minimize the effect of UV radiation. The study's goal is to isolate lycopene from tomatoes and evaluate its influence on cell cycle and viability in melanoma cell lines. The cell cycle was examined using flow cytometry, and apoptotic cells were identified using annexin/propidium iodide (PI) markers. Moreover, a molecular modeling and molecular dynamics (MD) simulation were performed to evaluate the stability and dynamics behavior of the compound. The obtained results revealed that lycopene caused apoptosis and stopped the cell cycle in human skin carcinoma MDA-MB-435 cells with an IC 50 value of 12.14 ± 3.37 uM. It demonstrated a noteworthy ability to inhibit cell growth and improve apoptosis. The effect was dose dependent leading to suppression of cell cycle progression in the G2/M phase. In silico molecular docking investigation confirmed these findings, where the tested compound showed hydrophobic binding with key amino acids. ADME/TOPKAT study along with the Swiss ADME online tool revealed that lycopene exhibits good drug-like properties. According to our results, lycopene may be effective in treating human skin carcinoma.