Background and purpose: Polycaprolactone nanocapsules incorporated with triazole derivatives in t... more Background and purpose: Polycaprolactone nanocapsules incorporated with triazole derivatives in the presence and absence of selenium nanoparticles were prepared and evaluated as antiproliferative and anticancer agents. Polycaprolactone nanoparticles were prepared using the emulsion technique. Experimental approach: The prepared capsules were characterized using FT-IR, TEM and DLS measurements. The synthesized triazolopyrimidine derivative in the presence and absence of selenium nanoparticles encapsulated in polycaprolactone was tested for its in vitro antiproliferative efficiency towards human breast cancer cell line (MCF7) and murine fibroblast normal cell line (BALB/3T3) in comparison to doxorubicin as a standard anticancer drug. Key results: The results indicated that encapsulated polycaprolactone with selenium nanoparticles (SeNPs) and triazole-SeNPs were the most potent samples against the tested breast cancer cell line (MCF7). On the other hand, all compounds showed weak ...
The relationships between maternal nutritional status and volume and composition of mother’s milk... more The relationships between maternal nutritional status and volume and composition of mother’s milk and its reflection on the infant were studied in fifty seven mothers, attending in child Welfare Clinic IN Ain Shams University Hospital and El Sahel Teaching Hospital. Two sets of analysis were performed. The first one was to assess the production of milk of moderately nourished mothers. The second one was undertaken to determine whether changes in nutritional status within individual woman affected their milk production. Mother and infant anthropometric measures were recorded monthly through the first 4 months of location. The amount of milk, fat, lactose and protein concentrations were measured by test weighing method, Gerber method, gravimetric method and micro-Kjeldahl method respectively. The metabolic energy concentration of milk specimen was calculated. The present study showed that milk production increased gradually through the time of the study. Milk, fat and protein concentr...
Detoxification is one of the main vital tasks performed by the liver. The purpose of this study w... more Detoxification is one of the main vital tasks performed by the liver. The purpose of this study was to investigate whether mustard in its normal or nanoparticles could confer a protective/therapeutic effect against TAA-induced acute liver failure in experimental animal models. Mustard ethanolic extract was analyzed by HPLC/MS. To induce liver failure, male rats were injected with 350 mg/kg bw TAA IP, then treated orally with a dose of 100 mg/kg for 15 d of mustard extract and its nanoform before and following induction. The levels of serum liver functions, total cholesterol (TCHo), total glyceride (TG), total bilirubin (TBIL), hepatic malonaldhyde (MDA) and nitric oxide (NO),glutathione (GSH), sodium oxide dismutase (SOD), as well as tumor necrosis factor (TNF-α,) and interleukin 6 (IL-6), were estimated. DNA genotoxicity and hepatic pathology, and immunohistologic (IHC) changes were assayed. The antioxidant content of Phenolic acids, flavonoids in mustard ethanolic extract substant...
The reactions are reported of 4-(furan-3-ylcarbonyl)-1,5-diphenylpyrrolidine-2,3-dione with six c... more The reactions are reported of 4-(furan-3-ylcarbonyl)-1,5-diphenylpyrrolidine-2,3-dione with six classes of organophosphorus reagents: carboalkoxymethylene triphenylphosphoranes, triphenyl (phenylimino)-λ 5-phosphane, trialkylphosphonoacetates, trialkylphosphites, tris (dialkylamino)phosphines, and Lawesson's reagent. Several of the products showed antitumour activity.
Condensation of 1-acetyl-1,2,3,4-tetrahydro-9H-carbazole (2) with some amino compounds furnished ... more Condensation of 1-acetyl-1,2,3,4-tetrahydro-9H-carbazole (2) with some amino compounds furnished the corresponding imino derivatives 3a-e. Compound 3a reacted with chloroacetic acid and underwent cyclization to give the thiazolidine derivative 5. Also, treatment of 3c with thionyl chloride caused cyclization to yield the [1,2,6]thiadiazino derivative 6, which gave the corresponding N-formyl derivative 7 upon heating with ethyl formate. In addition, interaction of 3d with ethyl cyanoacetate yielded the monoamide of malonic acid derivative 8. Acylation of carbazole 1 with succinoyl chloride or phenylacetyl choride produced the corresponding azepine (11) and 1,9-diphenyl acetyl derivatives (14), respectively. Compounds 11, 14 were further reacted to give the carbazole derivatives 12, 13 and 15a,b. The cytotoxic activity for some of the prepared compounds against breast cancer B 20 is discussed.
A series of sulfapyridine-polyhydroxyalkylidene (or arylidene)-imino derivatives (Schiff's bases)... more A series of sulfapyridine-polyhydroxyalkylidene (or arylidene)-imino derivatives (Schiff's bases) 2a-c and 4a-e were prepared by condensation of 4-amino-N-pyridin-2-ylbenzenesulfonamide (1) with different monosaccharides or with aromatic aldehydes. Treatment of 2a-c with thioglycolic acid led to the formation of the C-nucleosides (3a-c), while treatment of 4a-e with thioglycolic and/or thiosalicylic acids afforded the corresponding 2-arylthiazolidin-4-one or 2-arylbenzothiazin-4-one derivatives 5a-e and/or 6a-e, respectively. Some representative examples of the newly prepared compounds showed considerable cytotoxic effect against breast carcinoma cell line MCF7 and cervix carcinoma cell line HELA in comparison with 5-flurouracil and doxorubicin. AutoDock molecular docking into PTK has been done for lead optimization of the compounds in study as potential PTK inhibitors.
Drugs with antioxidant mechanisms are being widely proposed as starting point for the development... more Drugs with antioxidant mechanisms are being widely proposed as starting point for the development of new therapeutic interventions in several pathological disorders associated with oxidative damage, caused by reactive oxygen species (ROS), including hydrogen peroxide, superoxide anion and hydroxyl radical, under conditions of 'oxidative stress.' 1,2) This term refers to an imbalance between ROS production and detoxification, in favour of the former, and it is characterized by excessive production of ROS and/or reduction in the responsible for their metabolism antioxidant defences. 3,4) The quinoline ring system is often found in natural alkaloids and in many synthetic derivatives exhibiting antibacterial, immunomodulatory, anti-inflammatory and antioxidant properties. 5-11) Among these compounds, the novel quinolinone derivative TA 270 (4-hydroxy-1-methyl-3-octyloxy-7sinapinoylamino-2(1H)-quinolinone, Fig. 1), was initially designed as ROS scavenger and further pharmacological results suggest its therapeutic use in bronchial asthma. 12) Also, the antiulcer drug rebamipide, (2-(4-chlorobenzoylamino)-3-[2-(1H)-quinolinon-4-yl]propionic acid, Fig. 1) developed in Japan, inhibits lipid peroxidation and has a suppressive effect on oxygen derived free radical production in gastric mucosa. Rebamipide has been selected from a series of over 500 synthesized quinolinone derivatives tested for gastroprotective action and was found to possess anti-inflammatory properties, by stimulating endogenous prostaglandin and mucus glycoprotein synthesis and inhibiting inflammatory cytokines and chemokines. 13,14) It has been shown by the EPR (electron paramagnetic resonance) spin trapping method that rebamipide scavenges hydroxyl radicals and inhibits superoxide production. 15) Structure-activity studies revealed that the 3,4-double bond and the 2-oxo functionality of the quinolinone moiety are important determinants of the hydroxyl radical scavenging properties of this class of compounds and a
The current study aimed to evaluate the GC/MS profiling of Chiliadenus montanus leaves extract wh... more The current study aimed to evaluate the GC/MS profiling of Chiliadenus montanus leaves extract which consists of 48 compounds, nine of them are major and represented 52.55 % from the total peak areas. The ameliorative effect towards the CCl4-induced hepatotoxicity in male Wistar rats through measuring certain biochemical parameters content in the liver were analyzed. CCl4 diluted 1:9 (v/v) in olive oil was injected intraperitoneally followed by oral administration of methanolic plant extract (200 mg/kg body weight). The CCl4-treated rats showed a significant decline in the studied hematological parameters, the serum levels of high-density lipoprotein (HDL), albumin (A) as well as the hepatic levels of glutathione (GSH) and activities of catalase (CAT), superoxide dismutase (SOD) , glutathione reductase (GR), elevation in the levels of total lipids (TL), triglycerides (TG), total cholesterol (TC), low-density lipoproteins (LDL), globulin (G), total bilirubin (TBil) , alanine and aspa...
6-Amino-2-thiouracil (1) was condensed with benzenesulfonyl chloride and p-toluenesulfonyl chlori... more 6-Amino-2-thiouracil (1) was condensed with benzenesulfonyl chloride and p-toluenesulfonyl chloride in presence of pyridine as an acid binder to give sulfonamides 2a, b, which could be methylated in basic medium to give methylmercapto derivatives 3a, b, which in turn reacted with bromine in glacial acetic acid to yield 5-bromo derivatives 4a, b. On the other hand, compounds 2a, b were cyclocondensed with monochloroacetyl chloride, p-tolualdehyde in glacial acetic acid/ pyridine, and ethyl bromoacetate to give the corresponding thiazolopyrimidines 5a, b, 6a, b, and 7a, b, respectively; also compounds 2a, b were hydrazinolyzed to compounds 8a, b, which could be cyclized to triazolopyrimidines 9a, b in presence of formic acid. They could also be condensed with p-anisaldehyde to give hydrazones 10a, b. In another pathway, compounds 2a, b were reacted with monochloroacetic acid in basic medium to give acetic acid derivatives 11a, b. It can be deduced from the preliminary screening results that the cell lines most sensitive to the antiproliferative activity of tested compounds are human liver HEPG2 and colon cancer HT-29. All selected compounds exhibited moderate to strong growth inhibition activity against the HEPG2 cell line with 50 % inhibitory concentration (IC 50) ranging between 1 and 10 lg/ml. The most active compounds, which revealed antiproliferative activity also against human colon HT-29 and breast MCF-7 cell lines, were 3a, 3b, 4a, and 10a.
Background and purpose: Polycaprolactone nanocapsules incorporated with triazole derivatives in t... more Background and purpose: Polycaprolactone nanocapsules incorporated with triazole derivatives in the presence and absence of selenium nanoparticles were prepared and evaluated as antiproliferative and anticancer agents. Polycaprolactone nanoparticles were prepared using the emulsion technique. Experimental approach: The prepared capsules were characterized using FT-IR, TEM and DLS measurements. The synthesized triazolopyrimidine derivative in the presence and absence of selenium nanoparticles encapsulated in polycaprolactone was tested for its in vitro antiproliferative efficiency towards human breast cancer cell line (MCF7) and murine fibroblast normal cell line (BALB/3T3) in comparison to doxorubicin as a standard anticancer drug. Key results: The results indicated that encapsulated polycaprolactone with selenium nanoparticles (SeNPs) and triazole-SeNPs were the most potent samples against the tested breast cancer cell line (MCF7). On the other hand, all compounds showed weak ...
The relationships between maternal nutritional status and volume and composition of mother’s milk... more The relationships between maternal nutritional status and volume and composition of mother’s milk and its reflection on the infant were studied in fifty seven mothers, attending in child Welfare Clinic IN Ain Shams University Hospital and El Sahel Teaching Hospital. Two sets of analysis were performed. The first one was to assess the production of milk of moderately nourished mothers. The second one was undertaken to determine whether changes in nutritional status within individual woman affected their milk production. Mother and infant anthropometric measures were recorded monthly through the first 4 months of location. The amount of milk, fat, lactose and protein concentrations were measured by test weighing method, Gerber method, gravimetric method and micro-Kjeldahl method respectively. The metabolic energy concentration of milk specimen was calculated. The present study showed that milk production increased gradually through the time of the study. Milk, fat and protein concentr...
Detoxification is one of the main vital tasks performed by the liver. The purpose of this study w... more Detoxification is one of the main vital tasks performed by the liver. The purpose of this study was to investigate whether mustard in its normal or nanoparticles could confer a protective/therapeutic effect against TAA-induced acute liver failure in experimental animal models. Mustard ethanolic extract was analyzed by HPLC/MS. To induce liver failure, male rats were injected with 350 mg/kg bw TAA IP, then treated orally with a dose of 100 mg/kg for 15 d of mustard extract and its nanoform before and following induction. The levels of serum liver functions, total cholesterol (TCHo), total glyceride (TG), total bilirubin (TBIL), hepatic malonaldhyde (MDA) and nitric oxide (NO),glutathione (GSH), sodium oxide dismutase (SOD), as well as tumor necrosis factor (TNF-α,) and interleukin 6 (IL-6), were estimated. DNA genotoxicity and hepatic pathology, and immunohistologic (IHC) changes were assayed. The antioxidant content of Phenolic acids, flavonoids in mustard ethanolic extract substant...
The reactions are reported of 4-(furan-3-ylcarbonyl)-1,5-diphenylpyrrolidine-2,3-dione with six c... more The reactions are reported of 4-(furan-3-ylcarbonyl)-1,5-diphenylpyrrolidine-2,3-dione with six classes of organophosphorus reagents: carboalkoxymethylene triphenylphosphoranes, triphenyl (phenylimino)-λ 5-phosphane, trialkylphosphonoacetates, trialkylphosphites, tris (dialkylamino)phosphines, and Lawesson's reagent. Several of the products showed antitumour activity.
Condensation of 1-acetyl-1,2,3,4-tetrahydro-9H-carbazole (2) with some amino compounds furnished ... more Condensation of 1-acetyl-1,2,3,4-tetrahydro-9H-carbazole (2) with some amino compounds furnished the corresponding imino derivatives 3a-e. Compound 3a reacted with chloroacetic acid and underwent cyclization to give the thiazolidine derivative 5. Also, treatment of 3c with thionyl chloride caused cyclization to yield the [1,2,6]thiadiazino derivative 6, which gave the corresponding N-formyl derivative 7 upon heating with ethyl formate. In addition, interaction of 3d with ethyl cyanoacetate yielded the monoamide of malonic acid derivative 8. Acylation of carbazole 1 with succinoyl chloride or phenylacetyl choride produced the corresponding azepine (11) and 1,9-diphenyl acetyl derivatives (14), respectively. Compounds 11, 14 were further reacted to give the carbazole derivatives 12, 13 and 15a,b. The cytotoxic activity for some of the prepared compounds against breast cancer B 20 is discussed.
A series of sulfapyridine-polyhydroxyalkylidene (or arylidene)-imino derivatives (Schiff's bases)... more A series of sulfapyridine-polyhydroxyalkylidene (or arylidene)-imino derivatives (Schiff's bases) 2a-c and 4a-e were prepared by condensation of 4-amino-N-pyridin-2-ylbenzenesulfonamide (1) with different monosaccharides or with aromatic aldehydes. Treatment of 2a-c with thioglycolic acid led to the formation of the C-nucleosides (3a-c), while treatment of 4a-e with thioglycolic and/or thiosalicylic acids afforded the corresponding 2-arylthiazolidin-4-one or 2-arylbenzothiazin-4-one derivatives 5a-e and/or 6a-e, respectively. Some representative examples of the newly prepared compounds showed considerable cytotoxic effect against breast carcinoma cell line MCF7 and cervix carcinoma cell line HELA in comparison with 5-flurouracil and doxorubicin. AutoDock molecular docking into PTK has been done for lead optimization of the compounds in study as potential PTK inhibitors.
Drugs with antioxidant mechanisms are being widely proposed as starting point for the development... more Drugs with antioxidant mechanisms are being widely proposed as starting point for the development of new therapeutic interventions in several pathological disorders associated with oxidative damage, caused by reactive oxygen species (ROS), including hydrogen peroxide, superoxide anion and hydroxyl radical, under conditions of 'oxidative stress.' 1,2) This term refers to an imbalance between ROS production and detoxification, in favour of the former, and it is characterized by excessive production of ROS and/or reduction in the responsible for their metabolism antioxidant defences. 3,4) The quinoline ring system is often found in natural alkaloids and in many synthetic derivatives exhibiting antibacterial, immunomodulatory, anti-inflammatory and antioxidant properties. 5-11) Among these compounds, the novel quinolinone derivative TA 270 (4-hydroxy-1-methyl-3-octyloxy-7sinapinoylamino-2(1H)-quinolinone, Fig. 1), was initially designed as ROS scavenger and further pharmacological results suggest its therapeutic use in bronchial asthma. 12) Also, the antiulcer drug rebamipide, (2-(4-chlorobenzoylamino)-3-[2-(1H)-quinolinon-4-yl]propionic acid, Fig. 1) developed in Japan, inhibits lipid peroxidation and has a suppressive effect on oxygen derived free radical production in gastric mucosa. Rebamipide has been selected from a series of over 500 synthesized quinolinone derivatives tested for gastroprotective action and was found to possess anti-inflammatory properties, by stimulating endogenous prostaglandin and mucus glycoprotein synthesis and inhibiting inflammatory cytokines and chemokines. 13,14) It has been shown by the EPR (electron paramagnetic resonance) spin trapping method that rebamipide scavenges hydroxyl radicals and inhibits superoxide production. 15) Structure-activity studies revealed that the 3,4-double bond and the 2-oxo functionality of the quinolinone moiety are important determinants of the hydroxyl radical scavenging properties of this class of compounds and a
The current study aimed to evaluate the GC/MS profiling of Chiliadenus montanus leaves extract wh... more The current study aimed to evaluate the GC/MS profiling of Chiliadenus montanus leaves extract which consists of 48 compounds, nine of them are major and represented 52.55 % from the total peak areas. The ameliorative effect towards the CCl4-induced hepatotoxicity in male Wistar rats through measuring certain biochemical parameters content in the liver were analyzed. CCl4 diluted 1:9 (v/v) in olive oil was injected intraperitoneally followed by oral administration of methanolic plant extract (200 mg/kg body weight). The CCl4-treated rats showed a significant decline in the studied hematological parameters, the serum levels of high-density lipoprotein (HDL), albumin (A) as well as the hepatic levels of glutathione (GSH) and activities of catalase (CAT), superoxide dismutase (SOD) , glutathione reductase (GR), elevation in the levels of total lipids (TL), triglycerides (TG), total cholesterol (TC), low-density lipoproteins (LDL), globulin (G), total bilirubin (TBil) , alanine and aspa...
6-Amino-2-thiouracil (1) was condensed with benzenesulfonyl chloride and p-toluenesulfonyl chlori... more 6-Amino-2-thiouracil (1) was condensed with benzenesulfonyl chloride and p-toluenesulfonyl chloride in presence of pyridine as an acid binder to give sulfonamides 2a, b, which could be methylated in basic medium to give methylmercapto derivatives 3a, b, which in turn reacted with bromine in glacial acetic acid to yield 5-bromo derivatives 4a, b. On the other hand, compounds 2a, b were cyclocondensed with monochloroacetyl chloride, p-tolualdehyde in glacial acetic acid/ pyridine, and ethyl bromoacetate to give the corresponding thiazolopyrimidines 5a, b, 6a, b, and 7a, b, respectively; also compounds 2a, b were hydrazinolyzed to compounds 8a, b, which could be cyclized to triazolopyrimidines 9a, b in presence of formic acid. They could also be condensed with p-anisaldehyde to give hydrazones 10a, b. In another pathway, compounds 2a, b were reacted with monochloroacetic acid in basic medium to give acetic acid derivatives 11a, b. It can be deduced from the preliminary screening results that the cell lines most sensitive to the antiproliferative activity of tested compounds are human liver HEPG2 and colon cancer HT-29. All selected compounds exhibited moderate to strong growth inhibition activity against the HEPG2 cell line with 50 % inhibitory concentration (IC 50) ranging between 1 and 10 lg/ml. The most active compounds, which revealed antiproliferative activity also against human colon HT-29 and breast MCF-7 cell lines, were 3a, 3b, 4a, and 10a.
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Papers by Mohsen Soliman