Optimization and development of antidiabetic phytosomes by the Box-Behnken design.

Researchers have extensively reviewed on herbs and natural products for their marked clinical efficacy in some recent years, however, maximum of the newly discovered bioactive constituents offer poor bioavailability due to their large size molecules or to their poor miscibility with oils and lipids, thereby limiting their ability to pass across the lipid-rich outer membranes of the enterocytes of the small intestine. Phytosomes are more bioavailable as compared to herbal extracts owing to their enhanced capacity to cross the bio-membranes and thus reaching the systemic circulation. This study was aimed to investigate the development and optimization of antidiabetic phytosomes using a three-factor, three-level the Box-Behnken design (17 batches). The fruits of Citrullus colocynthis (L.) Momordica balsamina and Momordica dioica were extracted using Soxhlet's apparatus. The phytochemical fingerprint profile of the combined methanolic extracts was done by using high-performance thin layer chromatography (HPTLC). The polynomial quadratic equation analysis was designed to study the response (entrapment efficiency (EE), % yield) of independent significant factors at different levels. Phytosomes were characterized in terms of drug content, particle size, EE, zeta potential and in vitro dissolution. TEM analysis revealed good stability and a spherical, self-closed structure of phytosomes in complex formulations. Average particle size was found to 450 nm. Total flavonoid content was found to be 10.0 ± 0.002 µg/g. Optimized formulation was selected and was prepared using A (1:3), B (60 °C) and C (2.5 h) to give maximum yield and entrapment efficiencies (72% and 92.1 ± 5.1%). Phytosomes were found to have antidiabetic activity comparable to metformin in low dose. HPTLC showed the presence of the phyto-constituent quercetin.

Mushrooms as therapeutic agents

Mushrooms have been known for their nutritional and culinary values and used as medicines and tonics by humans for ages. In modern terms, they can be considered as functional foods which can provide health benefits beyond the traditional nutrients. There are monographs that cover the medicinal and healing properties of some individual traditional mushrooms. There has been a recent upsurge of interest in mushrooms not only as a health food which is rich in protein but also as a source of biologically active compounds of medicinal value which include complementary medicine/dietary supplements for anticancer, antiviral, hepatoprotective, immunopotentiating and hypocholesterolemic agents. However the mechanisms of the various health benefits of mushrooms to humans still require intensive investigation, especially given the emergence of new evidence of their health benefits. In the present paper the medicinal potential of mushrooms is being discussed.

In-vitro cytotoxic activity of ß-Sitosterol triacontenate isolated from Capparis decidua (Forsk.) Edgew.

OBJECTIVE: To study the isolation and characterization of the constituent responsible for the cytotoxic activity of the ethanolic extract of stem of Capparis decidua (C. decidua). METHODS: The preliminary cytotoxic effect of isolated compound (ß-Sitosterol triacontenate) was investigated by MTT assay on A549 solid tumor cells. RESULTS: IC(50) value of the ß-Sitosterol triacontenate was found to be 1 µM. The cytotoxic activity increased in a dose dependent manner in case of ß-Sitosterol triacontenate. CONCLUSIONS: The data therefore provide direct evidence for the role of ß-Sitosterol triacontenate as a potent antimetastatic agent, which can markedly inhibit the metastatic and invasive capacity of malignant cells.

In vitro anticancer activity of stachydrine isolated from Capparis decidua on prostate cancer cell lines.

In this article we report our work on the isolation, characterisation and evaluation of in vitro anticancer activity of stachydrine on solid tumour cells. The in vitro activity was assessed by MTT assay and propidium iodide (PI) staining. Further, an attempt was also made to check the effect of stachydrine on the invasion and metastasis of cancer cells by inhibiting the expression of chemokine receptors (CXCR3 and CXCR4). The influence of stachydrine on the gene expression of CXCR3 and CXCR4 at mRNA and protein levels was examined. Studies revealed a dose dependent decrease in expression of mRNA, and protein levels were observed in stachydrine-treated human prostate cancer cells (PC-3 and LNcaP) as detected by reverse transcriptase-polymerase chain reaction (RT-PCR). The data therefore provides direct evidence for the role of stachydrine as a potent anti-metastatic agent, which can markedly inhibit the malignancy and invasive capacity of malignant cancer cells.

Mechanism of action of flavonoids as anti-inflammatory agents: a review.

Flavonoids are polyphenolic compounds that occur ubiquitously in plants having a variety of biological effects both in vitro and in vivo. They have been found to have antimicrobial, antiviral, anti-ulcerogenic, cytotoxic, anti-neoplastic, mutagenic, antioxidant, antihepatotoxic, antihypertensive, hypolipidemic, antiplatelet and anti-inflammatory activities. Flavonoids also have biochemical effects, which inhibit a number of enzymes such as aldose reductase, xanthine oxidase, phosphodiesterase, Ca(+2)-ATPase, lipoxygenase, cycloxygenase, etc. They also have a regulatory role on different hormones like estrogens, androgens and thyroid hormone. They have been found to have anti-inflammatory activity in both proliferative and exudative phases of inflammation. Several mechanisms of action have been proposed to explain anti-inflammatory action of flavonoids. The aim of the present review is to give an overview of the mechanism of action of potential anti-inflammatory flavonoids.