Anti-tumor and antioxidant activity of kaempferol-3-O-alpha-L-rhamnoside (Afzelin) isolated from Pithecellobium dulce leaves.

BACKGROUND: Pithecellobium dulce (Roxb.), an evergreen medium-sized, spiny tree which have vast nutritional values and widely used in ayurvedic medicines and home remedies. The plant has also been a rich source of biologically active compounds. The present study was designed to isolate pure compound from ethyl acetate fraction of methanol extract of leaves and to know the efficacy as antioxidant as well as its anti-tumor activity on Ehrlich ascites carcinoma cell (EAC).  METHODS: The leaves were extracted with methanol and fractionated with different solvents. The isolation of the compound was carried out by column chromatography from ethyl acetate fraction (EAF) and structure was revealed by 1H-NMR and 13C NMR. The antioxidant activity was investigated by the scavenging of 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radicals as well as the inhibition of oxidative damage of pUC19 plasmid DNA, hemolysis and lipid peroxidation induced by a water-soluble free radical initiator 2,2'-azo (2-asmidinopropane) dihydrochloride (AAPH) in human erythrocytes. In vivo anti-tumor activity of the compound was also evaluated by determining the viable tumor cell count, hematological profiles of experimental mice along with observing morphological changes of EAC cells by fluorescence microscope. RESULTS: The isolated compound kaempferol-3-O-alpha-L-rhamnoside effectively inhibited AAPH induced oxidation in DNA and human erythrocyte model and lipid per oxidation as well as a stronger DPPH radical scavenging activity. In anti-tumor assay, at a dose of 50 mg/kg body weight exhibit about 70.89 ± 6.62% EAC cell growth inhibition, whereas standard anticancer drug vincristine showed 77.84 ± 6.69% growth inhibition. CONCLUSION: The compound may have a great importance as a therapeutic agent in preventing oxidative damage of biomolecules and therapeutic use in chemotherapy.

A flavone from the ethyl acetate extract of Leea rubra leaves with DNA damage protection and antineoplastic activity.

Among the major constituents of Leea rubra (Family Vitaceae) leaves, phenolic and flavonoind compounds are most important for therapeutic purposes and the plant parts have been used in traditional medicine to treat several diseases for long. Thus, in order to scientifically confirm the traditional uses of the L. rubra leaves, the present study was designed to investigate the efficacy of the isolated flavones against AAPH induced oxidative damage to pUC19 DNA by gel electrophoresis and antineoplastic activity was evaluated on Ehrlich ascites carcinoma (EAC) bearing Swiss albino mice by evaluating percentage inhibition of cell growth, morphological changes of EAC cells and hematological parameters of the mice. The isolation was carried out by column chromatography and structure was revealed by 1H-NMR and 13C NMR. The result shows that, the isolated compound was identified as myricetin 4'-methoxy-3-O-α-l-rhamnopyranoside based on previously reported data. The isolated flavone effectively inhibited AAPH-induced oxidative damage to DNA; because it could inhibit the formation of circular and linear forms of the DNA. In anti-proliferative assay, 76% growth inhibition of EAC cells was observed as compare to the control mice (p<0.05) at a dose 100 mg/kg body weight. Thus the isolated flavone showed great importance as a possible therapeutic agent in preventing oxidative damage to DNA and the chronic diseases caused by such DNA damage, and can also become important in cancer chemotherapy.

The protective and antioxidant effects of Hygrophila schulli seeds on oxidative damage of DNA and RBC cellular membrane.

Medicinal plants are sources of antioxidant which may protect the body against oxidative stress related diseases and can be used as human food supplements. In this investigation, seeds of Hygrophila schulli (M. R. Almeida & S. M. Almeida) (Fam.-Acanthaceae), a herbaceous plant well known for its medicinal properties, has been examined for antioxidant activity of crude methanolic extract (CME) and its fraction using in vitro and in vivo assay as well as their protective activity against oxidative damage of DNA and RBC. Total phenolic and flavonoid content have also been estimated using the aluminum chloride colorimetric and Folin-Ciocalteu method. Among the different fractions of CME, Ethyl acetate fraction (EAF) had higher antioxidant activity in vitro assay and was selected for in vivo antioxidant activity in cadmium intoxicated mice. The EAF showed a significant (p < 0.05) increase in serum catalase and SOD activity compared to the control group. TBARS levels were restored to 17.42 and 19.19 nmol/mg protein, respectively, after treatment with EAF and standard ascorbic acid (AA); compared to the normal group (14.96 nmol/mg protein). Similarly, levels of albumin, bilirubin, uric acid, and alkaline phosphatase were also brought back to normal levels. EAF's protective role against oxidative damage of DNA has shown a significant reduction in destroying of nicked DNA. RBC as a target of oxidation by H2O2 and HOCl, EAF showed inhibition of oxidation in a concentration-dependent manner, compared to standard gallic acid. In this study, we confirmed that EAF could scavenge reactive oxygen species (ROS) thus preventing DNA strand scission and the extract can be used as a functional food or nutraceutical product for health benefits.

Evaluation of in vitro anti-inflammatory and antibacterial potential of Crescentia cujete leaves and stem bark.

BACKGROUND: The various parts of Cresecentia cujete have some important biological activities. In folklore medicine leaves are used to treat hematomas, tumors and hypertension. Fruit decoction is used to treat diarrhea, stomachaches, cold, bronchitis, cough, asthma, and urethritis. The present study was designed to explore the anti-inflammatory and antibacterial potential of C. cujete leaves and stem bark. Anti-inflammatory activity was evaluated by in vitro human red blood cell (HRBC) membrane stabilization method and antibacterial activity by disc diffusion method. METHODS: In vitro anti-inflammatory activity was evaluated by human red blood cell (HRBC) membrane stabilization method while in vitro antibacterial activity was evaluated using cultures of Escherichia coli and Staphylococcus aureus by disc diffusion method. Total phenolic (TPC) and total flavonoid contents (TFC) of the crude extract and fractions were also determined by Folin-Ciocalteu's phenol reagent and by aluminium chloride method, respectively. RESULTS: The crude ethanol extract (CEE) of leaves and bark (concentration of each 1.0 mg/ml) demonstrated strong membrane stabilizing activity (53.86 and 61.85% protection, respectively), whereas their chloroform fractions (CHF) revealed moderate activity (48.74 ± 0.56 and 43.55 ± 6.20 %, respectively) compared with standard aspirin (concentration 0.10 mg/ml) which showed 75.81% protection in this test. All the samples showed a dose dependent anti-inflammatory activity in HRBC membrane stabilization test. Total phenolic (TPC) and total flavonoid contents (TFC) of the crude extract and fractions were also determined. Again, in in vitro antibacterial study, the extractives exhibited potent antibacterial activity. CONCLUSION: Results from this study showed that the leaves and bark of C. cujete possessed anti-inflammatory as well as antibacterial activities indicating that the plant extract has therapeutic potential against the bacterial infection and also have effect on disease processes by causing destabilization of biological membranes.

Pesticidal and pest repellency activities of rhizomes of Drynaria quercifolia (J. Smith) against Tribolium castaneum (Herbst).

BACKGROUND: Tribolium castaneum (Herbst) is a harmful pest of stored grain and flour-based products in tropical and subtropical region. In the present study, rhizome of Drynaria quercifolia (J. Smith) was evaluated for pesticidal and pest repellency activities against T. castaneum, using surface film method and filter paper disc method, respectively. In addition, activity of the isolated compound 3,4-dihydroxybenzoic acid was evaluated against the pest. RESULTS: Chloroform soluble fraction of ethanol extract of rhizome of D. quercifolia showed significant pesticidal activity at doses 0.88 to 1.77 mg/cm(2) and significant pest repellency activity at doses 0.94 to 0.23 mg/cm(2). No pesticidal and pest repellency activity was found for petroleum ether, ethyl acetate and methanol soluble fractions of ethanol extract as well as for 3,4-dihydroxybenzoic acid. CONCLUSION: Considering our findings it can be concluded that chloroform soluble fraction of rhizome of D. quercifolia is useful in controlling T. castaneum of stored grain and flour-based products.

Antioxidant activities of ethanol extracts and fractions of Crescentia cujete leaves and stem bark and the involvement of phenolic compounds.

BACKGROUND: Antioxidant compounds like phenols and flavonoids scavenge free radicals and thus inhibit the oxidative mechanisms that lead to control degenerative and other diseases. The aim of this study was to investigate the antioxidant activity in vitro, total phenolic and flavonoid contents in ethanol extracts and fractions of Crescentia cujete leaves and stem bark. METHODS: Crescentia cujete leaves and bark crude ethanol extract (CEE) and their partitionates petroleum ether (PEF), chloroform (CHF), ethyl acetate (EAF) and aqueous (AQF) were firstly prepared. Different established testing methods, such as 1, 1-diphenyl-2-picryl hydrazyl (DPPH) radical, ferric reducing power (FRP), and total antioxidant capacity (TAC) assays were used to detect the antioxidant activity. Further, the total yield, total phenolic (TPC) and total flavonoid contents (TFC) of CEE and all the fractions were determined. Ethanol extracts of both leaves and stem bark were also subjected to preliminary phytochemical screening to detect the presence of secondary metabolites, using standard phytochemical methods (Thin layer chromatography and spray reagents). RESULTS: Phytochemical screening of crude ethanol extract of both leaves and stem bark revealed the presence of steroids, flavonoids, saponins, tannins, glycosides and terpenoids. All the fractions and CEE of leaves and bark exhibited antioxidant activities, however, EAF of leaves showing the highest antioxidant activity based on the results of DPPH, FRP and TAC assay tests. The above fraction has shown the significant DPPH scavenging activity (IC50 = 8.78 µg/ml) when compared with standard ascorbic acid (IC50 =7.68 µg/ml). The TAC and FRP activities increased with increasing crude extract/fractions content. The TPC (371.23 ± 15.77 mg GAE/g extract) and TFC (144.64 ± 5.82 mg QE/g extract) of EAF of leaves were found significantly higher as compared to other solvent fractions for both leaves and bark. TPC were highly correlated with the antioxidant activity (R2 = 0.9268 and 0.8515 in DPPH test for leaves and bark, respectively). CONCLUSION: The results of the study show that leaves of C. cujete possesses significant free radical scavenging properties compared with stem bark and a clear correlation exists between the antioxidant activity and phenolic content.

Pesticidal and pest repellency activities of rhizomes of Drynaria quercifolia (J. Smith) against Tribolium castaneum (Herbst)

BACKGROUND: Tribolium castaneum (Herbst) is a harmful pest of stored grain and flour-based products in tropical and subtropical region. In the present study, rhizome of Drynaria quercifolia (J. Smith) was evaluated for pesticidal and pest repellency activities against T. castaneum, using surface film method and filter paper disc method, respectively. In addition, activity of the isolated compound 3,4-dihydroxybenzoic acid was evaluated against the pest. RESULTS: Chloroform soluble fraction of ethanol extract of rhizome of D. quercifolia showed significant pesticidal activity at doses 0.88 to 1.77 mg/cm² and significant pest repellency activity at doses 0.94 to 0.23 mg/cm². No pesticidal and pest repellency activity was found for petroleum ether, ethyl acetate and methanol soluble fractions of ethanol extract as well as for 3,4-dihydroxybenzoic acid. CONCLUSION: Considering our findings it can be concluded that chloroform soluble fraction of rhizome of D. quercifoliais useful in controlling T. castaneum of stored grain and flour-based products.

Studies on the anti-diarrheal properties of leaf extract of Desmodium puchellum.

OBJECTIVE: To evaluate the pharmacological activity against diarrhea of methanol and petroleum ether extract of Desmodium puchellum (Family: Fabaceae) leaves. METHODS: The extract was evaluated for castor oil-induced diarrhea and enteropooling as well as intestinal motility in rats. Both of the extracts were given to the rats at 200 mg/kg orally. Loperamide was used as a standard drug for diarrhea. RESULTS: The diarrheal severity was reduced significantly (P<0.05) by methanol and petroleum ether extracts by 31.95% and 28.33%, respectively, whereas 54.75% inhibition was found for standard drug loperamide at 5 mg/kg. The two extracts also significantly (P<0.05) reduced the intestinal volume in case of castor oil induced enteropooling. CONCLUSIONS: It is concluded that both fractions contain some biologically active ingredients that are active for anti-diarrheal actions whereas methanol fraction has better potential.