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Correlation between enzymes inhibitory effects and antioxidant activities of standardized fractions of methanolic extract obtained from Ficus deltoidea leaves

AFRICAN JOURNAL OF BIOTECHNOLOGY (Impact Factor: 0.57). 12/2011; 10(67):15184-15194. DOI: 10.5897/AJB11.1365

ABSTRACT

Recently, there has been increasing interest in Ficus deltoidea (Moracea) due to its chemical composition and the potential health benefits. The leaves of the plant have been suggested to have potential antidiabetic effects. Inhibition of carbohydrate-hydrolysing enzymes, such as -glucosidase and -amylase is one of the therapeutic approaches to control postprandial hyperglycemia. In this study, enzymes inhibitory effect and antioxidant properties of different fractions of methanolic extract obtained from F. deltoidea leaves was evaluated. Further, the possible relationship between pharmacological properties and phytochemical content of fractions was investigated. The n-butanol fraction showed significant -glucosidase and -amylase inhibitory effects (IC 50 values 15.1 and 39.42 µg/ml, respectively) along with the remarkable antioxidant activity when compared to the other fractions. High performance liquid chromatography (HPLC) chemical profiling of the n-butanol fraction revealed that the contents of isovitexin (24.63 mg/g) and vitexin (8.3 mg/g) were found to be significantly higher than the other fractions. These results indicate that F. deltoidea could be the potential source of promising anti-diabetic drug.

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    • "with the UPR for removing unfolded proteins to favor survival of stressed cells [15] [16]. Apigenin-8-C-D glucopyranoside (vitexin), is a natural flavonoid compound, and has been reported to exhibit a wide range of pharmacological effects [17] [18] [19] [20] [21]. The seed coat extract of mungbean contains vitexin and isovitexin as major antioxidant components, which can prevent heat stress-induced oxidative injury in rats [22]. "
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    ABSTRACT: Aims: Cells possess multiple methods for counteracting the deleterious consequences of stress induced by physical and chemical stimuli. Heat stress causes variations in the cellular environment, leading to cellular morbidity or mortality. Natural compounds that contain phenolic antioxidants, offer various therapeutic and biological activities. Vitexin, a natural flavonoid, has been reported to treat various pathologies due to its multifaceted effects. Herein, we investigated the therapeutic efficacy of vitexin and its underlying mechanism against heat stress in human lung epithelial cells. Main methods: Effect of vitexin on the expression of molecular chaperones, antioxidant enzymes, mitogen activated protein kinases (MAPKs), endoplasmic reticulum (ER)-stress and autophagy were measured by immunoblotting. qRT-PCR and EMSA was performed for Hsp90 expression and HSF-1 binding affinity. Cell viability was assessed by MTT and LDH assay. Detection of autophagy was confirmed by acridine orange staining. Role of Hsp90 inhibition on signaling pathways was elucidated by using specific chemical inhibitor, radicicol. Key findings: Whereas hyperthermia reduced cell viability, result of MTT and LDH assay showed that vitexin pre-treatment enhanced cell viability after heat stress. EMSA analysis shows DNA binding affinity of HSF-1 during heat stress. Vitexin upregulated Hsp90 expression, subsequently activating ER-stress induced autophagy. Modulation of MAPKs expression and fluorescence image analysis showed vacuole accumulation, indicating autophagic flux in cells. Hsp90 inhibition reversed the effect of vitexin and activates the apoptosis pathway. Significance: Our data suggest that vitexin can protect against hyperthermic cellular injury by induction of Hsp90 expression, antioxidant activity and MAPKs via ER stress-induced autophagy.
    No preview · Article · Oct 2015 · Life sciences
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    • "Mas Cotek (family of Moraceae) is a plant that is traditionally used for postdelivery treatment, uterus contraction, treating gout, hypertension, diabetes, cholesterol and sugar reduction as well as for improving blood circulation [19]. This herb also possesses medicinal values involving the antioxidative activity and anti-hyperglycemic affect [20]. Halia Bara is a traditional health-promoting herb widely used for the treatment of indigestion, sore throats, rheumatism, and hypertension [21]. "
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    ABSTRACT: In the local Malaysian context, herbal plants such as Eurycoma longifolia (Tongkat Ali), Orthosiphon stamineus (MisaiKucing), Ficus deltoidea (Mas Cotek), Zingiber officinale (Halia Bara) and Barringtonia racemosa (Putat) are known and widely used for its therapeutic properties. The first part of this study aims to screen for the anti-protozoal activity of these herbal plant extracts against Blastocystis sp. isolate subtype (ST) 3. Herbal extract with the highest efficacy was further fractionized into water and ethyl acetate fractions and tested against ST1, ST3 and ST5 Blastocystis sp. isolates. These isolates were also exposed to allopathic drugs, Metronidazole (MTZ), Tinidazole, Trimethoprim-sulfamethoxazole(TMP-SMX), Ketoconazole and Nitazoxanide for comparison purpose. Blastocystis sp. isolates from human-derived stool samples were exposed to herbal extracts and allopathic drugs at a concentration of 0.1 mg/ml and 1.0 mg/ml and were incubated at 37 °C. Growth profile studies were carried out. After 72 h of treatment, the viability of Blastocystis sp. as a result of the effects of the drugs and herbal extracts were assessed. Based on the screening process, amongst all the extracts, Tongkat Ali exhibited the highest anti-protozoal activity at 1.0 mg/ml. Between the water and ethyl acetate fractions of Tongkat Ali, the ethyl acetate fraction exhibited a slightly higher percentage of anti-protozoal activity at 1.0 mg/ml across subtypes, ST1 (94.9 %), ST3 (95.1 %) and ST5 (94.3 %). When tested with allopathic drugs, at the same concentration, MTZ exhibited the highest anti-protozoal activity across subtypes, ST1 (95.8 %), ST3 (93.4 %) and ST5 (90.8 %). This study is the first to describe the anti-protozoal properties of Tongkat Ali against Blastocystis sp. isolates. Ethyl acetate fraction of Tongkat Ali demonstrated the highest anti-protozoal activity against Blastocystis sp. isolates and showed a sizeable reduction in the cell count which was comparable with MTZ. Tongkat Ali also demonstrated a more uniformed sensitivity across subtypes in comparison to the allopathic drugs.
    Full-text · Article · Jun 2015 · Parasites & Vectors
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    • "(Moraceae) is a native wild evergreen shrub in Malaysia and widely distributed in Southeast Asian countries. It is locally known as Emas Cotek and Mas Cotek [10]. Decoction of F. deltoidea leaves was extensively utilized in folk medicine to decrease symptom of diabetes, hyperlipidemia and hypertension [11]. "
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    ABSTRACT: Background Recently, there has been increasing interest in Ficus deltoidea Jack. (Moraceae) due to its chemical composition and the potential health benefits. The present study was undertaken to investigate the effect of extracts of F. deltoidea leaves on diabetes. Methods The petroleum ether, chloroform and methanol extracts of F. deltoidea were prepared and subjected to standardization using preliminary phytochemical and HPLC analysis. Dose selection was made on the basis of acute oral toxicity study (50–5000 mg/kg b. w.) as per OECD guidelines. Diabetes mellitus was induced with streptozotocin and rats found diabetic were orally administered with the extract (250, 500 and 1000 mg/kg) for 14 days. Levels of blood glucose and insulin were measured in control as well as diabetic rats on 0, 7 and 14th day. In addition, glucose metabolism regulating gene expression was assessed using RT-PCR. Results HPLC analysis revealed that the methanol extract is enriched with C-glycosylflavones particularly, vitexin and isovitexin. In oral glucose tolerance test, oral administration of the methanol extract increased the glucose tolerance. The methanol extract showed significant (P < 0.01) antidiabetic activity. The extract treatment caused significant reduction (p < 0.01) in elevated fasting blood glucose level in streptozotocin-induced diabetic rats. The streptozotocin-related weight loss in rats was noticeably reversed by the extract treatment. Finally, RT-PCR analysis revealed a novel mechanisms for the anti-diabetic action of methanol extract of F. deltoidea. The extract exerted its effect via an increase of insulin secretion which impeded the hepatic glucose production, via down-regulation of phosphoenolpyruvate carboxykinase and glucose-6-phosphatase genes expression on one hand, and up-regulation of hepatic GK and PPARγ genes expression on the other hand. The extract caused an increased expression of GLUT-4 gene expression in skeletal muscles which leads to normalize the hyperglycemia. The extract also nullified the toxic effects of streptozitocin by blocking its entry into the islet β-cells through reducing the expression of GLUT-2 gene. Conclusion It can be concluded that, F. deltoidea could potentially inhibits the streptozitocin-induced hyperglycemia in rats. Further the herb can be utilized as useful remedy for alleviation of diabetes complications.
    Full-text · Article · Jul 2014 · BMC Complementary and Alternative Medicine
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