Aldose reductase inhibitor form Cassia glauca: A comparative study of cytotoxic activity with Ag nanoparticles (NPs) and molecular docking evaluation.

UPLC-MS/MS profiling of Cassia glauca leaves extract revealed the identification of 10 flavonoids. Kaempferol 3-O-ß-D-rutinoside was isolated and studied for its cytotoxic activity. It showed high cytotoxic effects against MCF-7 (IC50 of 4.6±0.038 µg/ml) and HepG-2 (IC50 of 8.2±0.024 µg/ml) cancer cell lines, compared to the leaves extracts, their Ag nanoparticles, and doxorubicin. Moreover, Kaempferol 3-O-ß-D-rutinoside exerted a synergistic cytotoxic effect with doxorubicin on MCF-7 cell lines. It was discovered as kinases and aldose reductase inhibitor while rationalizing its cytotoxic activity through molecular docking study. Thus, it is expected that the cardiotoxic effects of doxorubicin can be also decreased by using Kaempferol 3-O-ß-D-rutinoside due to its aldose reductase inhibitory effect. These findings suggested that Kaempferol 3-O-ß-D-rutinoside could be used in combination with chemotherapeutic drugs to increase the sensitivity to their cytotoxic activity and protect against their side effects.

Chemical Composition and Biological Activities of the Essential Oil from Leaves and Flowers of Pulicaria incisa sub. candolleana (Family Asteraceae).

The composition of the essential oil isolated from leaves and flowers of Pulicaria incisa sub. candolleana E. Gamal-Eldin, growing in Egypt, was analysed by GC and GC-MS. Forty-nine and 68 compounds were identified from the oils of the leaves and flowers accounting for 86.69 and 84.29%, respectively of the total detected constituents. Both leaves and flowers oils were characterized by the high content of carvotanacetone with 66.01, 50.87 and chrysanthenone 13.26, 24.3%, respectively. The cytotoxic activity of both essential oils was evaluated against hepatocellular carcinoma cell line HEPG-2, using MTT assay and vinblastine as a reference drug. Leaf oil showed higher activity with IC50 11.4 µg/ml compared with 37.4 µg/ml for flower oil. The antimicrobial activity of both oils was evaluated using agar well diffusion method towards two representatives for each of Gram positive and Gram negative bacteria as well as four representatives for fungi. The minimum inhibitory concentration of both essential oils against bacterial and fungal strains was obtained in the range of 0.49 - 15.63 µg/ml.

Glucosinolates profile, volatile constituents, antimicrobial, and cytotoxic activities of Lobularia libyca.

CONTEXT: Brassicaceae plants are associated with protection against cancers due to their glucosinolate contents. OBJECTIVES: We investigate fresh leaves, roots and ripe seeds of Lobularia libyca (Viv.) C.F.W. Meissn. (Brassicaceae) to identify their glucosinolate constituents, antimicrobial and cytotoxic activities Materials and methods: The glucosinolates were identified using GC-MS analysis of their hydrolysis products and LC-MS analysis in the case of seeds. Disc diffusion (1 mg/disc) and minimum inhibitory concentration (0-160 µg/mL) methods were used to evaluate the antimicrobial activity of seed hydrolysate. In vitro cytotoxicity against colorectal HCT-116, hepatic HUH-7, breast MCF-7 and lung A-549 cells was evaluated for seed hydrolysate (0.01-100 µg/mL) using the sulforhodamine B assay and doxorubicin as a standard Results: Three glucosinolates were identified for the first time in this plant and genus Lobularia. Glucoiberverin was the major compound accumulated in the seeds and leaves, while glucoiberin and glucoerucin were detected only in the seeds. No glucosinolates were detected in roots under the same experimental conditions. Other volatile constituents, e.g., terpenes and fatty acids were only identified in the seeds. The seed hydrolysate showed significant antimicrobial activities against Candida albicans and Pseudomonas aeruoginosa (MIC = 64 and 82 µg/mL, respectively). The seed hydrolysate exhibited a marked selective cytotoxicity in vitro against colorectal, hepatic and breast cancer cell lines. The IC50 values were 0.31, 2.25 and 37 µg/mL, respectively. DISCUSSION AND CONCLUSION: The results indicated the antimicrobial activity of L. libyca and the selective effect of the seed hydrolysate as a cytotoxic drug that is potentially more active than doxorubicin against HCT-116.

Cytotoxic ellagitannins from Reaumuria vermiculata.

Three ellagitannins and one disulfated flavonol were isolated from the aerial parts of Reaumuria vermiculata L. Besides that, 16 known compounds were characterized as well. The structures of all compounds were elucidated on the basis of spectroscopic data including 1D and 2D NMR and ESI HR-FTMS. The in vivo antioxidant activity using the oxygen radical absorbance capacity (ORAC) method, of the extract, its column fractions and two of the isolated ellagitannins was accomplished. In addition, a possible cytotoxicity of the extract and two of the new ellagitannins on HaCaT human keratinocytes and the activity of both compounds against the prostate cancer cell line (PC-3) were also assessed, whereby a potent cytotoxicity with IC50 less than 1 µg/ml was determined for both compounds. Besides, the extract exhibited a potential cytotoxic effect against four different solid tumor cell lines, namely liver (Huh-7), colorectal (HCT-116), breast (MCF-7) and prostate (PC-3). The IC50s were found to be substantially low (ranged from 1.3±0.15 to 2.4±0.22 µg/ml) with relatively low resistance possibility reaching to 0% in the case of Huh-7 cell.

Anti-inflammatory activity of Pistacia khinjuk in different experimental models: isolation and characterization of its flavonoids and galloylated sugars.

The present study aimed at isolating and elucidating the structure of the main components of Pistacia khinjuk L. and exploring its potential anti-inflammatory effect in different experimental models. The extract was evaluated for anti-inflammatory activity by measuring paw volume in three experimental models. Then, prostaglandin E2 (PGE2) level, ear edema, tissue myeloperoxidase (MPO) activity, histopathology, nitric oxide (NO) level, and tumor necrosis factor-α (TNF-α) level were assessed. Seven phenolic compounds, mainly flavonoids and galloylated compounds, were isolated from the aqueous methanol extract: gallic acid (1), methyl gallate (2), quercetin-3-O-ß-D-4C1-galactopyranoside (hyperin) (3), myricetin-3-O-α-L-¹C4-rhamnopyranoside (myricitrin) (4), 1,6-digalloyl-ß-D-glucose (5), 1,4-digalloyl-ß-D-glucopyranoside (6), and 2,3-di-O-galloyl-(α/ß)-4C1-glucopyranose (nilocitin) (7). The anti-inflammatory activity was evidenced by decreased carrageenan-induced rat paw edema and PGE2 elevation. In the croton oil-induced ear edema model, MPO activity was significantly inhibited, and inflammatory histopathological changes were ameliorated. In the rat air pouch model, NO generation and TNF-α release were significantly inhibited. The isolation and nuclear magnetic resonance spectral data of compound 6 from the genus Pistacia are revealed for the first time. Also, P. khinjuk L. aqueous methanol extract possesses anti-inflammatory activity in several experimental models.

Antioxidant and hepatoprotective activities of Egyptian moraceous plants against carbon tetrachloride-induced oxidative stress and liver damage in rats.

CONTEXT: In the absence of reliable liver-protective drugs in modern medicine, a large number of medicinal preparations are recommended for treatment of liver disorders. OBJECTIVE: The antioxidant, hepatoprotective and kidney protective activities of methanol extracts of Ficus carica Linn. (Moraceae) leaves and fruits and Morus alba Linn. root barks (Moraceae) are evaluated here. MATERIALS AND METHODS: Liver and kidney damage were induced in rats by carbon tetrachloride in a subcutaneous dose of 1 mL (40% v/v in corn oil)/kg. The extract was given intraperitoneally at doses of 50 mg/kg (F. carica leaf and M. alba root bark) and 150 mg/kg (F. carica fruit). The activity of the extracts was comparable to that of silymarin, a known hepatoprotective agent. Antioxidant activity was evaluated by measuring blood glutathione (GSH) content, superoxide dismutase (SOD), catalase (CAT) activities, and malondialdehyde equivalent (MDA). Hepatoprotective activity was evaluated by measuring serum levels of aspartate aminotransferase (AST), alanine aminotransferase (ALT), alkaline phosphatase (ALP), total bilirubin, and total protein. These biochemical observations were supported by histopathological examination of liver sections. Kidney function was evaluated by measuring plasma urea and creatinine. RESULTS: Methanol extracts of Ficus carica and Morus alba showed potent antioxidant and hepatoprotective activities; in-depth chromatographic investigation of the most active extract (Ficus carica leaf extract) resulted in identification of umbelliferone, caffeic acid, quercetin-3-O-ß-d-glucopyranoside, quercetin-3-O-α-l-rhamnopyranoside, and kaempferol-3-O-α-l-rhamnopyranoside. DISCUSSION AND CONCLUSION: These findings demonstrate that the phenolic constituents of Ficus carica leaf and Morus alba root bark are responsible at least in part for the observed protective effects.

A trimethoxyellagic acid glucuronide from Conocarpus erectus leaves: isolation, characterization and assay of antioxidant capacity.

The new trimethoxy-ellagic glycoside, 3,3',4'-tri-O-methylellagic acid 4-O-beta-glucupyranuronide and twelve known phenolics were isolated from the leaves of Conocarpus erectus L. (Combretaceae). Structures of all compounds were determined on the basis of spectroscopic methods and chemical degradation. The new compound, together with four of the isolated known constituents and the plant extract itself, showed potent inhibitory effect against reactive oxygen species attack on salicylic acid in a dose-dependent manner adopting xanthine/hypoxanthine oxidase assay.

Rubus sanctus protects against carbon tetrachloride-induced toxicity in rat isolated hepatocytes: isolation and characterization of its galloylated flavonoids.

OBJECTIVES: Rubus sanctus Schreb., known from the Bible as 'holy thorn bush', grows wild in Egypt. Rubus sanctus aqueous alcoholic extract (RE) contains a complicated phenolic mixture (ellagitanins, flavonoids and caffeic acid derivatives). In this study, the phytochemical investigation of the plant was re-evaluated. Herein, we report on the isolation and identification of three galloylated flavonoids, namely kaempferol-3-O-(6''-O-galloyl)-(4)C(1)-beta-d-galactopyranoside, quercetin-3-O-(6''-O-galloyl)-(4)C(1)-beta-d-galactopyranoside and myricetin-3-O-(6''-O-galloyl)-(4)C(1)-beta-d-galactopyranoside for the first time from the Rubus genus. We further aimed at evaluating the potential protective effects of RE against carbon tetrachloride (CCl(4))-induced toxicity in isolated rat hepatocytes. METHODS: Based on an initial concentration-response experiment, a concentration of 100 mug/ml was selected to investigate the hepatoprotective activity of RE. KEY FINDINGS: Pretreatment with RE afforded protection as indicated by counteracting CCl(4)-induced cell death, and reduced glutathione depletion. In addition, RE ameliorated CCl(4)-induced enzyme leakage by 40% for lactate dehydrogenase, 30% for alanine aminotransferase and 20% for aspartate aminotransferase as compared with CCl(4)-treated cells. Moreover, RE counteracted CCl(4)-induced lipid peroxidation and inhibited spontaneous lipid peroxidation in the control group. CONCLUSIONS: In conclusion, RE protects against CCl(4)-induced toxicity in isolated rat hepatocytes.

Caffeoyl sugar esters and an ellagitannin from Rubus sanctus.

The new natural caffeoyl esters, 3,6-di-O-caffeoyl-(alpha/beta)-glucose and 1-O-caffeoyl-beta-xylose, together with the hitherto unknown natural tannin, 2,3-O-hexahydroxydiphenoyl-4,6-O-sanguisorboyl-(alpha/beta)-glucose, have been isolated from the aqueous alcohol aerial part extract of Rubus sanctus. Establishment of all structures was based on the chemical and spectral evidence, including ESI-MS and 2D NMR.

Unique phenolic carboxylic acids from Sanguisorba minor.

The unique phenolic carboxylic acids, 4,8-dimethoxy-7-hydroxy-2-oxo-2H-1-benzopyran-5,6-dicarboxylic acid and 2-(4-carboxy-3-methoxystyryl)-2-methoxysuccinic acid were isolated and identified from the whole Sanguisorba minor plant. The known phenolics, gallic acid; ellagic acid; quercetin-3-O-(6"-galloylglucose); beta-glucogallin; 2,3-hexahydroxydiphenoyl-(alpha/beta)-glucose; 1-galloyl-2,3-hexahydroxydiphenoyl-alpha-glucose together with its beta-isomer were also characterized. Structures were established by conventional methods of analysis and confirmed by NMR and ESI-MS spectral analysis.