Role of Goldenberry (Fruits with Husk) Extract in Ameliorating the Architecture and Osmotic Fragility of Red Blood Cells in Obese Rats.

Goldenberry (GB) is a promising fruit that can be a constituent in many possible nourishments. No notifications were obtained regarding the impact of exposure to goldenberry extract in the viewpoint of blood rheological properties as well as erythrocyte osmotic fragility of red blood cells (RBCs) in obese rats. A substantial reduction in plasma triglyceride, total cholesterol, and LDL, with a considerable increment in HDL levels relative to the obese group (p ≤ 0.05), was observed in rats receiving low and high doses of GB, accompanied by restoration of SOD activity and GSH levels. Rheological parameters of rats' blood have been studied over a wide range of shear rates (225-1875 s-1). A significant decrease in blood viscosity in rats who received low and high doses of GB extract was compatible with every shear rate compared to the control group. The shear stress values of the obese rats reduced appreciably (p ≤ 0.05) in all values of shear rate (from 75 to 500 s-1) proportional to the control group, while in the groups that received low and high doses of GB extract, shear stress was restored to the control values. Finally, administration of GB extract significantly decreased yield stress and indices of whole blood aggregation, with an extremely substantial increment in flow rate, in rats given low or high doses of GB compared to obese ones. The result also showed a decrease in both the average raised osmotic fragility and the hemolysis rate in rats after supplementation with low and high doses of GB extract.

Evaluation of the cytotoxic, anticancer, and genotoxic activities of Acacia nilotica flowers and their effects on N-methyl-N-nitrosourea-induced genotoxicity in mice.

PURPOSE: In this study, two main research objectives were examined: (1) the cytotoxic and anticancer activities of the aqueous methanol extract from Acacia nilotica flowers on three human cancer cells, namely lung A549, breast MCF-7, and leukemia THP-1 cells, and (2) the genotoxic effects of A. nilotica extract and its influence on DNA damage induced by N-methyl-N-nitrosourea (MNU) in mice. METHODS: Mice were orally treated with A. nilotica extract (200, 500, and 800 mg/kg for 4 days) with or without MNU (80 mg/kg intraperitoneally for 24 h). RESULTS: In vitro experiments showed that A549 cells were the most sensitive to A. nilotica extract among the tested cell lines. A. nilotica extract inhibited A549 cell proliferation by blocking the cell cycle at the G2/M phase and accumulating apoptotic cells in the sub-G0/G1 phase in A549 cells. In vivo experiments showed that MNU induced positive and negative genotoxicity in bone marrow cells and spermatocytes, respectively. Negative genotoxicity was observed in A. nilotica extract-treated groups only. However, A. nilotica extract (800 mg/kg) remarkably increased comet tail formation in bone marrow cells. Unexpectedly, the absence of antigenotoxicity was observed in three cotreated groups with A. nilotica extract and MNU compared with the MNU-treated group. Astonishingly, cotreatment with MNU and A. nilotica extract at a dose above 200 mg/kg remarkably increased micronucleus and comet tail formation in bone marrow cells compared with the MNU-treated group. CONCLUSIONS: A. nilotica extract possessed anticancer activity with relative genotoxic effects at high doses.

Anti-Obesity Evaluation of Averrhoa carambola L. Leaves and Assessment of Its Polyphenols as Potential α-Glucosidase Inhibitors.

Averrhoa carambola L. is reported for its anti-obese and anti-diabetic activities. The present study aimed to investigate its aqueous methanol leaf extract (CLL) in vivo anti-obese activity along with the isolation and identification of bioactive compounds and their in vitro α-glucosidase inhibition assessment. CLL improved all obesity complications and exhibited significant activity in an obese rat model. Fourteen compounds, including four flavone glycosides (1-4) and ten dihydrochalcone glycosides (5-12), were isolated and identified using spectroscopic techniques. New compounds identified in planta included (1) apigenin 6-C-(2-deoxy-ß-D-galactopyranoside)-7-O-ß-D-quinovopyranoside, (8) phloretin 3'-C-(2-O-(E)-cinnamoyl-3-O-ß-D-fucopyranosyl-4-O-acetyl)-ß-D-fucopyranosyl-6'-O-ß-D fucopyranosyl-(1/2)-α-L arabinofuranoside, (11a) phloretin3'-C-(2-O-(E)-p-coumaroyl-3-O-ß-D-fucosyl-4-O-acetyl)-ß-D-fucosyl-6'-O-(2-O-ß-D-fucosyl)-α-L-arabinofuranoside, (11b) phloretin3'-C-(2-O-(Z)-p-coumaroyl-3-O-ß-D-fucosyl-4-O-acetyl)-ß-D-fucosyl-6'-O-(2-O-ß-D-fucosyl)-α-L-arabinofuranoside. Carambolaside M (5), carambolaside Ia (6), carambolaside J (7), carambolaside I (9), carambolaside P (10a), carambolaside O (10b), and carambolaside Q (12), which are reported for the first time from A. carambola L. leaves, whereas luteolin 6-C-α-L-rhamnopyranosyl-(1-2)-ß-D-fucopyranoside (2), apigenin 6-C-ß-D-galactopyranoside (3), and apigenin 6-C-α-L-rhamnopyranosyl-(1-2)-ß-L-fucopyranoside (4) are isolated for the first time from Family. Oxalidaceae. In vitro α-glucosidase inhibitory activity revealed the potential efficacy of flavone glycosides, viz., 1, 2, 3, and 4 as antidiabetic agents. In contrast, dihydrochalcone glycosides (5-11) showed weak activity, except for compound 12, which showed relatively strong activity.

Novel Neuroprotective Potential of Bunchosia armeniaca (Cav.) DC against Lipopolysaccharide Induced Alzheimer's Disease in Mice.

Bunchosia armeniaca (Cav.) DC (Malpighiaceae) is one of the well-known traditionally used remedies worldwide. This study aims to explore the leaves' metabolome via Quadrupole-Time-of-Flight-Liquid-Chromatography-Mass Spectrometry and to investigate the neuroprotective effect of leaves using lipopolysaccharide (LPS) induced Alzheimer's disease model. Mice were administered LPS (0.25 mg/kg/day; intraperitoneal) as well as methanolic extract (BME), dichloromethane (BDMF), and butanol (BBF) fractions (each 200 mg/kg/day; oral) for one week. BME and BBF improved behavioral activity on the Y maze test, decreased brain content of inflammatory markers such as nuclear factor kappa B and interleukin 1 beta, and prevented the elevation of cytochrome P450 2E1, and glial fibrillary acidic protein compared to the LPS-administered group. Histopathological examination of several brain parts confirmed the neuroprotective effect of the tested extracts. In addition, BBF exhibited higher activity in all tested in vitro antioxidant and acetylcholinesterase inhibition assays. Metabolic profiling offered tentative identification of 88 metabolites, including mainly flavonoids, phenolic acids, and coumarins. Several detected metabolites, such as quercetin, apigenin, baicalin, vitexin, and resveratrol, had previously known neuroprotective effects. The current study highlighted the possible novel potential of B. armeniaca in preventing memory impairment, possibly through its antioxidant effect and inhibition of acetylcholinesterase, inflammatory and oxidative stress mediators.

Polyphenol Content, Antioxidant, Cytotoxic, and Genotoxic Activities of Bombax ceiba Flowers in Liver Cancer Cells Huh7.

OBJECTIVE: Bombax ceiba (red Silk cotton tree) has great ethnopharmacological significance due to its widespread use to treat various diseases such as dysentery, inflammation, and tuberculosis. Despite decades of research, the studies on the in vitro anticancer/genotoxic activity of B. ceiba flower remains restricted. Thus, the present research explored the effect of ethanol extract from B. ceiba flowers on three human cancer cells, including lung A549 and liver HepG2 and Huh7 cell lines. METHODS: Cytotoxic and genotoxic activity of B. ceiba extract was examined by MTT and comet assay, respectively. Further, B. ceiba extract was analysed to determine total polyphenol content and DPPH antiradical scavenging activity. RESULTS: ethanol extract from B. ceiba flowers had a high polyphenols content with very potent antioxidant activity. Further, B. ceiba extract displayed moderate cytotoxicity against Huh7 cells and no cytotoxicity against HepG2 and A549 cells. The comet assay findings showed that Huh7 cells treated with four concentrations of B. ceiba extract (» IC50, ½ IC50, IC50, and double IC50) increased the comet tail formation within 48 h in a concentration-dependent manner. CONCLUSION: ethanol extract from B. ceiba flowers exhibited its cytotoxicity through induction of DNA fragmentation in Huh7 cells.

A new cycloartane triterpene and other phytoconstituents from the aerial parts of Euphorbia dendroides.

New cycloartane-type triterpene 23 R/S-3ß-hydroxycycloart-24-ene-23-methyl ether 1a,b (as an C-23 epimeric mixture), along with ten known compounds, including 1 steroid, 3 fatty acids and 6 triterpenoids were isolated from the aerial parts of Euphorbia dendroides L. (Euphorbiaceae). The known compounds (2-11) were identified using 1 D & 2 D-NMR spectra and by comparison with data reported in the literature as well as using GC-MS for the isolated fatty acids. The new compound 1 (a,b) was elucidated by comprehensive 1 D & 2 D NMR experiments as well as LR & HR-FAB-MS. In addition, the isolated cycloartane-type triterpenoids have been tested for in vitro cytotoxicity against different cell lines. The new compound 1 (a,b) exhibited good to weak selective cytotoxic activities against HepG2, Huh-7, KLM-1, 1321N1 and HeLa cell lines with IC50 values of 20.67 ± 0.72, 16.24 ± 0.53, 22.59 ± 0.94, 25.99 ± 0.31 and 40.50 ± 3.14 µM, respectively.

Nephroprotective, cytotoxic and antioxidant activities of Euphorbia paralias.

OBJECTIVE: To investigate the effect of the ethyl acetate fraction of the aerial parts of E. paralias L. F. Euphorbiaceae on nephroprotective, cytotoxic, and antioxidant. METHODS: different spectroscopic and spectrophotometric methods were applied to identify phytoconstituents. The nephroprotective potential of E. paralias ethyl acetate fraction (Ep EtOAc) was evaluated in male rats with thioacetamide-induced kidney injury, as wll as cytotoxic activity was evaluated using a viability assay, and the antioxidant activity was evaluated using the DPPH method. Results: quantitative estimation of total phenolics and flavonoids of E. paralias was performed using unique spectrophotometric methods. The polyphenolic compounds gallic acid (1), ellagic acid (2), kaempferol-3-O-(6″-O-galloyl-ß-D-glucopyranoside) (3), quercetin-3-O-ß-D-glucopyranoside (4) and quercetin-3-O-ß-D-arabinoside (5) were isolated from the ethyl acetate fraction of the aerial parts of E. paralias. The thioacetamide administration resulted in marked nephrotoxicity, but pretreatment with Ep EtOAc significantly attenuated the nephrotoxicity through alteration of kidney biomarkers, thereby improving the redox status of the tissue and restoring serum biochemical parameters nearly to normal levels. This study revealed a significant cytotoxic and strong antioxidant effect. Conclusion: we conclude that the Ep EtOAc may be used in the future as nephroprotective, cytotoxic, and antioxidant agent derived from a natural source.

New antimicrobial metabolites from the medicinal herb Artemisia herba-Alba.

Artemisia herba-alba is widely used in traditional medicines for the treatment of several diseases. From the aerial parts organic extract of A. herba-alba, two new compounds, 1,3,8-trihydroxyeudesm-4-en-7α,11ßH-12,6α-olide (1) and 5-ß-​D-​glucopyranosyloxy​-​7-methoxy-​6H-​benzopyran-​2-​one (2), respectively, together with five known metabolites: 3α,8ß-dihydroxygermacr-4(15),9(10)-dien-7ß,11αH,12,6α-olide (3), 1ß,8α-dihydroxy-11α,13-dihydrobalchanin (4), 11-epiartapshin (5), tomenin (6) and benzoic acid, p-​(ß-​D-​glucopyranosyloxy)​-​methyl ester (7), were isolated and identified. The chemical structures were proven depending upon spectroscopic analysis, including 1 D/2D NMR as and ESI-MS. Compound 1 inhibited Gram-positive bacteria Bacillus subtilis and Staphylococcus aureus. Compounds 2 and 3 exhibited antibacterial activity against both gram-positive and gram-negative bacteria.

Metabolite profiles of Pulicaria crispa and P. incisa in relation to their in-vitro/ in-vivo antioxidant activity and hepatoprotective effect: A comparative mass spectrometry-based metabolomics.

Plants of the genus Pulicaria (family: Asteraceae) are widely used in central Asia and the Middle East for treatment of different human diseases. Ultra performance liquid chromatography coupled to high resolution mass spectrometry (UPLC/MS) was utilized to establish the metabolic profiles of two Pulicaria species: P. crispa and P. incisa. 122 metabolites were identified including flavonoids (37), phenolic acids (22), sesquiterpenes (17), diterpenes (7), and fatty acids (27), with enrichment in methoxylated flavonoids (20), caffeoylquinic acid conjugates (14) xanthane sesquiterpenes (9) and hydroxylated fatty acids (20) in both Pulicaria species. The metabolite profile of P. incisa was characterized by the presence of tri- and tetra-methoxylated flavonoids while xanthane sesquiterpenes were the main chemical markers of P. crispa. Additionally, a novel sesquiterpene acid (dihydropulicaric acid) was annotated in both species based on its MS fragments. Antioxidant activity for P. crispa and P. incisa methanol extracts was assessed in vitro based on DPPH and ABTS assays and further in vivo using chlorpromazine intoxicated rat model. Results revealed that P. incisa extract was more effective in inhibiting both DPPH and ABTS free radicals (IC50 0.36 and 0.52 mg/mL, respectively) than P. crispa (IC50 0.51 and 0.73 mg/mL). In the animal model, antioxidant activity of P. incisa (20 mg/kg/day) was also slightly higher causing a 55 % reduction in MDA levels and 65 % increase in GSH activity compared to untreated animals. Furthermore, both extracts showed a hepatoprotective effect as revealed by improvement in levels of serum biomarkers of liver functions: total bilirubin, alanine transaminase (ALT) and aspartate transaminase (AST) comparable to silymarin at 25 mg/kg/day. These findings were also supported by the preserved integrity of the hepatic tissues of animals receiving either extracts at a dose of 20 mg/kg b.wt. The present study reveals for the potential antioxidant and hepatoprotective effects for Pulicaria in relation to its bioactive metabolites.

Nutrient and Sensory Metabolites Profiling of Averrhoa Carambola L. (Starfruit) in the Context of Its Origin and Ripening Stage by GC/MS and Chemometric Analysis.

Averrhoa carambola L. is a tropical tree with edible fruit that grows at different climatic conditions. Despite its nutritive value and reported health benefits, it is a controversial fruit owing to its rich oxalate content. The present study aimed at investigating aroma and nutrient primary metabolites distribution in A. carambola fruits grown in Indonesia, Malaysia (its endemic origin) versus Egypt, and at different ripening stages. Two techniques were employed to assess volatile and non-volatile metabolites including headspace solid-phase micro-extraction (HS-SPME) joined with gas chromatography coupled with mass-spectrometry (GC-MS) and GC-MS post silylation, respectively. Twenty-four volatiles were detected, with esters amounting for the major class of volatiles in Egyptian fruit at ca. 66%, with methyl caproate as the major component, distinguishing it from other origins. In contrast, aldehydes predominated tropically grown fruits with the ether myristicin found exclusively in these. Primary metabolites profiling led to the identification of 117 metabolites viz. sugars, polyols and organic acids. Fructose (38-48%) and glucose (21-25%) predominated sugar compositions in ripe fruits, whereas sorbitol was the major sugar alcohol (2.4-10.5%) in ripe fruits as well. Oxalic acid, an anti-nutrient with potential health risks, was the major organic acid detected in all the studied fruits (1.7-2.7%), except the Malaysian one (0.07%). It increases upon fruit ripening, including considerable amounts of volatile oxalate esters detected via SPME, and which must not be omitted in total oxalate determinations for safety assessments.

A new flavonol glycoside and other flavonoids from the aerial parts of Taverniera aegyptiaca.

Isolation of flavonoids from the aerial parts of Taverniera aegyptiaca Bioss. (Fabaceae) led to identification of one new flavonol glycoside, isorhamnetin-3-O-α-l-rhamnopyranosyl-(1→2)-α-l-arabinopyranoside (1), along with eleven compounds, which previously have not been isolated from this plant quercetin-3-O-α-l-rhamnopyranosyl-(1→2)-[α-l-rhamnopyranosyl-(1→6)-ß-d-galactopyranoside] (2), isorhamnetin-3-O-α-l-arabinopyranoside (3), quercetin-3-O-α-l-rhamnopyranosyl-(1→6)-ß-d-glucopyranoside (4), isorhamnetin-3-O-α-l-rhamnopyranosyl-(1→6)-ß-d-glucopyranoside (7), isorhamnetin 3-O-α-l-rhamnopyranosyl-(1→2)-[α-l-rhamnopyranosyl-(1→6)-ß-d-galactopyranoside] (8), isorhamnetin 3-O-α-l-rhamnopyranosyl-(1→2)-[α-l-rhamnopyranosyl-(1→6)-ß-d-glucopyranoside] (9), kaempferol 3-O-α-l-rhamnopyranosyl-(1→2)-[α-l-rhamnopyranosyl-(1→6)-ß-d-galactopyranoside] (10), isorhamnetin (11), 4,4'-dihydroxy-2'-methoxychalcone (12), formononetin (13) and calycosin (15)] and some compounds already known from this plant [quercetin-3-O-robinobioside (5), isorhamnetin-3-O-robinobioside (6), afrormosin (14) and odoratin (16)].

Ellagic Acid Holds Promise Against Hepatocellular Carcinoma in an Experimental Model: Mechanisms of Action

This research work was initiated to explore the efficacy of ellagic acid in mitigation of hepatocarcinogenesis in rats. Rats were distributed into 4 groups; negative control, hepatocellular carcinoma (HCC), doxorubicin and ellagic acid. Serum alpha-fetoprotein (AFP), glypican-3 (GPC-3), signal transducer and activator of transcription 3 (STAT3) and suppressors of cytokine signaling 3 (SOCS3) levels were assayed by ELISA. Immunohistochemical examination of hepatic VEGF expression was also conducted, along with histological procedures for examination of liver tissue sections. Significant elevation in serum AFP, GPC-3 and STAT3 levels with a significant drop in SOCS3 were observed in the HCC group. In contrast, the treated groups showed significant decline in serum AFP, GPC-3 and STAT3 levels and significant increase in SOCS3. Additionally, the HCC group declared mild positive immunoreaction for VEGF in hepatocytes while treatment with doxorubicin or ellagic acid was associated with a negative immunoreaction for VEGF. These results were supported by histological examination of liver tissue. The obtained findings suggested that ellagic acid may have beneficial chemopreventive role against hepatocarcinogenesis through its apoptotic, antiangiogenic and antiproliferative activities.

Phenolic metabolites, biological activities, and isolated compounds of Terminalia muelleri extract.

CONTEXT: Terminalia muelleri Benth. (Combretaceae), is rich with phenolics that have antioxidant and cytotoxic activities. No screening studies were published before on T. muelleri. OBJECTIVE: The study focused on isolation and identification of secondary metabolites from aqueous methanol leaf extract of T. muelleri and evaluation of its biological activities. MATERIALS AND METHODS: The n-butanol extract was chromatographed on polyamide 6, and eluted with H2O/MeOH mixtures of decreasing polarity, then separated by different chromatographic tools that yielded 10 phenolic compounds. The antioxidant activity of the extract was evaluated by investigating its total phenolic and flavonoid content and DPPH scavenging effectiveness. The extract and the two acylated flavones were evaluated for their anticancer activity towards MCF-7 and PC3 cancer cell lines. Molecular docking study of the acylated flavones was performed against topoisomerase enzyme. RESULTS AND DISCUSSION: Two acylated flavonoids, apigenin-8-C-(2″-O-galloyl) glucoside 1 and luteolin-8-C-(2″-O-galloyl) glucoside 2, were isolated and identified for the second time in nature, with eight tannins (3-10), from the leaves of T. muelleri. The extract and compound 10 showed the most significant antioxidant activity (IC50 = 3.55 and 6.34 µg/mL), respectively. The total extract and compound 2 demonstrated cytotoxic effect against MCF-7 with IC50 = 29.7 and 45.2 µg/mL respectively, while compound 1 showed cytotoxic effect against PC3 (IC50 = 40.8 µg/mL). The docking study of compounds 1 and 2 confirmed unique binding mode in the active site of human DNA topoisomerase enzyme. CONCLUSIONS: Terminalia muelleri is a promising medicinal plant as it possesses high antioxidant activity and moderate cytotoxic activity against MCF-7.

Metformin, an Anthropogenic Contaminant of Seidlitzia rosmarinus Collected in a Desert Region near the Gulf of Aqaba, Sinai Peninsula.

A phytochemical investigation of Seidlitzia rosmarinus collected along the shoreline of the Gulf of Aqaba in the remote southern desert region of the Sinai peninsula has revealed the presence of the registered drug metformin (4). However, analysis of the 14C content revealed the drug to be an anthropogenic contaminant. Consequently, natural product researchers should be aware that compounds isolated from plants might originate from environmental contamination rather than biosynthesis. The new natural product N-(4-hydroxyphenylethyl)-α-chloroferuloylamide was isolated as a mixture of the E and Z isomers along with a number of other well-established secondary metabolites.

Gallic acid against hepatocellular carcinoma: An integrated scheme of the potential mechanisms of action from in vivo study.

The global burden of hepatocellular carcinoma is increasing; actually, it is estimated as 750,000 new cases annually. This study was initiated to emphasize the possibility that gallic acid could alleviate hepatocarcinogenesis in vivo. In this study, 40 rats were enrolled and distributed as follows; group 1 was set as negative control, while all of groups 2, 3, and 4 were orally received N-nitrosodiethylamine for hepatocellular carcinoma induction. Group 2 was left untreated, whereas groups 3 and 4 were orally treated with gallic acid and doxorubicin, respectively. The current data indicated that gallic acid administration in hepatocellular carcinoma bearing rats yielded significant decline in serum levels of alpha-fetoprotein, glypican-3, and signal transducer and activator of transcription 3 along with significant enhancement in serum suppressors of cytokine signaling 3 level. Also, gallic acid-treated group displayed significant downregulation in the gene expression levels of hepatic gamma glutamyl transferase and heat shock protein gp96. Intriguingly, treatment with gallic acid remarkably ameliorated the destabilization of liver tissue architecture caused by N-nitrosodiethylamine intoxication as evidenced by histopathological investigation. In conclusion, this study demonstrates that the hepatocarcinogenic effect of N-nitrosodiethylamine can be abrogated by gallic acid supplementation owing to its affinity to regulate signal transducer and activator of transcription 3 signaling pathway through its outstanding bioactivities including antioxidant, anti-inflammatory, apoptotic, and antitumor effects.

Bougainvillea spectabilis flowers extract protects against the rotenone-induced toxicity.

OBJECTIVE: To investigate the effect of two extracts of Bougainvillea spectabilis (B. spectabilis) flowers with yellow and pink/purple on brain oxidative stress and neuronal damage caused in rats by systemic rotenone injection. METHODS: Rotenone 1.5 mg/kg was given three times per week alone or in combination with B. spectabilis flowers extracts (25 mg or 50 mg) via the subcutaneous route for 2 weeks. Brain concentrations of the lipid peroxidation marker malondialdehyde (MDA), reduced glutathione, nitric oxide (nitrite), the pro-inflammatory cytokine interleukin-1beta (Il-1ß) as well as butyrylcholinesterase, and paraoxonase-1 (PON-1) activities, were determined. Histopathology and caspase-3 immunohistochemistry were also performed. RESULTS: Rotenone resulted in significant increases of brain MDA (the product of lipid peroxidation), and nitric oxide content along with decreased brain reduced glutathione. There were also marked and significant inhibition of brain PON-1 and BChE activities and increased Il-1ß in brain of rotenone-treated rats. B. spectabilis flowers extract itself resulted in brain oxidative stress increasing both lipid peroxidation and nitrite content whilst inhibiting PON-1 activity. The yellow flowers extract inhibited BChE activity and increased brain Il-1ß. When given to rotenone-treated rats, B. spectabilis extracts, however, decreased lipid peroxidation while their low administered doses increased brain GSH. Brain nitrite decreased by the pink extract but showed further increase by the yellow extract. Either extract, however, caused further inhibition of PON-1 activity while the yellow extract resulted in further inhibition of BChE activity. Histopathological studies indicated that both extracts protected against brain, liver and kidney damage caused by the toxicant. CONCLUSIONS: These data indicate that B. spectabilis flowers extracts exert protective effect against the toxic effects of rotenone on brain, liver and kidney. B. spectabilis flowers extracts decreased brain lipid peroxidation and prevented neuronal death due to rotenone and might thus prove the value in treatment of Parkinson's disease.

Biochemical and molecular evidences for the antitumor potential of Ginkgo biloba leaves extract in rodents.

Hepatocellular carcinoma (HCC) is one of the deadliest primary cancers, with a 5-year survival rate of 10% or less. This study was undertaken to elucidate the underlying biochemical and molecular mechanisms in favor of N-nitrosodiethylamine-induced hepatocellular carcinoma. Furthermore, the aim of this work was extended to explore the efficacy of Ginkgo biloba leaves extract in deterioration of HCC in rats. In the current study, HCC group experienced significant downregulation of ING-3 gene expression and upregulation of Foxp-1 gene expression in liver. Treatment of HCC groups with Ginkgo biloba leaves extract resulted in upregulation of ING-3 and downregulation of Foxp-1 gene expression in liver. In addition, there was significant increase in serum alpha-fetoprotein (AFP), carcinoembryonic antigen (CEA) and glypican-3 (GPC-3) levels in HCC group versus the negative control group. In contrast, the groups with HCC subjected to either high or low dose of Ginkgo biloba leaves extract elicited significant reduction (P<0.05) of AFP, CEA and GPC-3 in serum compared to the untreated HCC rats. Besides, histological examination of liver tissue sections of rats in HCC group revealed typical anaplasia. Interestingly, treatment with Ginkgo biloba leaves extract elicited marked improvement in the histological feature of liver tissue in HCC groups. In conclusion, this research indicated that the carcinogenic potency of N-nitrosodiethylamine targeted multiple systems on the cellular and molecular levels. In addition, the results of the current study shed light on the promising anticancer activity of Ginkgo biloba leaves extract in treatment of hepatocellular carcinoma induced chemically in the experimental model through its apoptotic and antiproliferative properties.

Quercetin Confers Tumoricidal Activity Through Multipathway Mechanisms in A N-Methylnitrosourea Rat Model of Colon Cancer

Objective: This research was conducted to explore mechanisms behind the potency of quercetin in inhibiting colon cancer induced in an experimental model. Materials and Methods: Forty adult male rats of Wistar strain were distributed into 4 groups; a negative control group, a colon cancer bearing group, a quercetin-treated group and a 5-fluorouracil (5-FU)-treated group. Serum TAG72 and GAL3 levels were quantified by ELISA. Colonic Wnt5a and Axin-1 gene expression was estimated by PCR. In addition, colonic tissues were subjected to immunohistochemical examination of Bax expression and histological investigation of histopathological alterations. Results: Quercetin elicited significant reduction in serum TAG72 and GAL3 levels, in addition to significant suppression of colonic Wnt5a gene expression and amplification of colonic Axin-1 gene expression. Also, it caused moderate positive reaction for Bax in mucosal epithelium. Conclusion: The present research provides experimental evidence about the activity of quercetin in the colon cancer of rats. Inhibitory effects on cancer development might be ascribable to regulatory action on Wnt signaling and induction of apoptosis.

Cornigerin, a new sesqui-lignan from the hepatoprotective fractions of Cynara cornigera L.

The ethanol extract of Cynara cornigera L. was fractionated and the fractions were subjected to hepatoprotective assays using Wistar albino rats at a dose of 500 and 250mg/kg. The liver injury was induced in rats using carbon tetrachloride. Biochemical parameters such as aspartate aminotransferase (AST), alanine aminotransferase (ALT), alkaline phosphatase (ALP) and total bilirubin were estimated as reflections of the liver condition, with silymarin as a positive control. Phytochemical investigation and chromatographic separation of the hepatoprotective fractions led to the isolation of a new sesqui-lignan namely cornigerin (1), along with eight known compounds: apigenin (2), luteolin (3), ß-sitosterol glycoside (4), apigenin 7-O-ß-D-glucopyranoside (5), luteolin-7-O-ß-D-glucopyranoside (6), apigenin-7-O-rutinoside (7), cynarin 1,5-di-O-caffeoylquinic acid (8), and apigenin-7-O-ß-D-glucuronide (9). This is the first report for the isolation of 8 and 9 from this plant.

Antihepatotoxic Effect and Metabolite Profiling of Panicum turgidum Extract via UPLC-qTOF-MS.

BACKGROUND: Panicum turgidum, desert grass, has not reported any detailed phytochemical or biological study as yet. OBJECTIVE: To establish P. turgidum secondary metabolite profile and to assess its antihepatotoxic effect. MATERIALS AND METHODS: Ultra-performance liquid chromatography (UPLC) coupled to quadrupole high-resolution time of flight mass spectrometry (qTOF-MS) was used for large-scale secondary metabolites profiling in P. turgidum extract, alongside assessing median lethal dose (LD50) and hepatoprotective effect against carbon tetrachloride (CCl4) intoxication. RESULTS: A total of 39 metabolites were identified with flavonoids as the major class present as O/C-glycosides of luteolin, apigenin, isorhamnetin and naringenin, most of which are first time to be reported in Panicum sp. Antihepatotoxic effect of P. turgidum crude extract was revealed via improving several biochemical marker levels and mitigation against oxidative stress in the serum and liver tissues, compared with CCl4 intoxicated group and further confirmed by histopathological examination. CONCLUSION: This study reveals that P. turgidum, enriched in C-flavonoids, presents a novel source of safe antihepatotoxic agents and further demonstrates the efficacy of UPLC-MS metabolomics in the field of natural products drug discovery. SUMMARY: UPLC coupled to qTOF-MS was used for large scale secondary metabolites profiling in P. turgidum.A total of 39 metabolites were identified with flavonoids amounting as the major metabolite class.Anti-hepatotoxic effect of P. turgidum extract was revealed via several biochemical markers and histopathological examination.This study reveals that P. turgidum, enriched in C-flavonoids, present a novel source of antihepatotoxic agents. Abbreviations used: UPLC: Ultra-performance liquid chromatography (UPLC), LD50: median lethal dose, MDA: malondialdehyde, GSH: glutathione reductase, CAT: catalase, SOD: superoxide dismutase, ALT: alanine aminotransferase, AST: aspartate aminotransferase, ALP: alkaline phosphatase, TG: triglycerides.