ABSTRACT
The prevalence of obesity is alarmingly increasing in the last few decades and leading to many serious public health concerns worldwide. The dysregulated lipid homeostasis due to various genetic, environmental and lifestyle factors is considered one of the critical putative pathways mediating obesity. Nonetheless, the scientific advancements unleashing the molecular dynamics of lipid metabolism have provided deeper insights on the emerging roles of lipid hydrolysing enzymes, including pancreatic lipase. It is hypothesized that inhibiting pancreatic lipase would prevent the breakdown of triglyceride and delays the absorption of fatty acids into the systemic circulation and adipocytes. Whilst, orlistat is the only conventional pancreatic lipase enzyme inhibitor available in clinics, identifying the safe clinical alternatives from plants to inhibit pancreatic lipase has been considered a significant advancement. Consequently, plants which have shown significant potential to combat obesity are now revisited for its abilities to inhibit pancreatic lipase. In this regard, our review surveyed the potential of medicinal plants and its phytoconstituents to inhibit pancreatic lipase and to elicit anti-obesity effects. Thus, the review collate and critically appraise the potential of medicinal plants and phyto-molecules inhibiting pancreatic lipase enzyme and consequently modulating triglyceride absorption in gut, and discuss its implications in the development of novel therapeutic strategies to combat obesity.
Subject(s)
Anti-Obesity Agents/therapeutic use , Enzyme Inhibitors/therapeutic use , Lipase/antagonists & inhibitors , Obesity/drug therapy , Phytotherapy , Humans , Pancreas/enzymologyABSTRACT
CONTEXT: Cocculus hirsutus (L.) Diels (Menispermaceae) is used in Indian folk system of alternative medicine for rheumatism, eczema, diabetics, inflammation, and neuralgia. OBJECTIVE: To evaluate antitumor activities of C. hirsutus in vitro and in vivo. MATERIALS AND METHODS: C. hirsutus was successively extracted using hexane, petroleum ether, chloroform, ethyl acetate, methanol, and water. In vitro cytotoxicity was assessed by the MTT assay. Phytochemical analyses were conducted with methanol extract of C. hirsutus (MECH) and in vivo antitumor activity was carried out with MECH using Dalton's lymphoma ascites (DLA) mouse model. Antioxidant properties were assessed by estimating superoxide dismutase (SOD), catalase (CAT), and lipid peroxidation. RESULTS AND DISCUSSION: Phytochemical studies indicated a high content of total alkaloid (165.6 mg/100 g), total phenolic (43.5 GAE mg/g), and total flavanoid (4.97 RE mg/g) in MECH. Anti-proliferative activity against the breast cancer cell line MCF-7 showed IC50 values of 221.5 ± 16.68, 255 ± 17.88, 213 ± 8.4, 147 ± 7.9, and 229 ± 8.02 µg/ml with hexane, petroleum ether, chloroform, ethyl acetate, methanol, and aqueous extracts, respectively. A significant (p < 0.01) decrease in packed cell volume, viable cell count, and increased lifespan (58 and 77%) was observed. Hematological and serum biochemical profiles were restored to normal levels in MECH-treated mice. MECH-treated group significantly (p < 0.001) decreased SOD, lipid peroxidation, and CAT towards normal. CONCLUSION: C. hirsutus exhibited significant in vitro and in vivo antitumor activities that are reasonably attributed to endogenous antioxidant mechanisms.
Subject(s)
Antineoplastic Agents, Phytogenic/pharmacology , Cocculus/chemistry , Lymphoma/pathology , Plant Extracts/pharmacology , Alkaloids/analysis , Animals , Antineoplastic Agents, Phytogenic/chemistry , Antineoplastic Agents, Phytogenic/toxicity , Antioxidants/pharmacology , Catalase/metabolism , Cell Count , Cell Death/drug effects , Cell Line, Tumor , Cell Survival/drug effects , Drug Screening Assays, Antitumor , Female , Flavonoids/analysis , Humans , Lipid Peroxidation/drug effects , Lymphoma/drug therapy , Male , Mice , Phenols/analysis , Plant Extracts/chemistry , Plant Extracts/toxicity , Solvents/chemistry , Superoxide Dismutase/metabolismABSTRACT
BACKGROUND: Nigella sativa Linn (Ranunculaceae) is popularly known as black cumin with a wide spectrum of pharmacological activities including anti-inflammatory, antibacterial, antifungal and antihelmenthic. The seeds are externally applied for eruptions of skin. The seeds are used traditionally for psoriasis tropicus with general pain and eruption of patches. OBJECTIVE: The ethanolic extract of Nigella sativa seeds were evaluated for antipsoriatic activity. MATERIALS AND METHODS: The screening of antipsoriatic activity of 95% of ethanolic extract of Nigella sativa seeds by using mouse tail model for psoriasis and in vitro antipsoriatic activity was carried out by SRB Assay using HaCaT human keratinocyte cell lines. RESULTS: The ethanolic extract of Nigella sativa seeds extract produced a significant epidermal differentiation, from its degree of orthokeratosis (71.36±2.64) when compared to the negative control (17.30±4.09%). This was equivalent to the effect of the standard positive control, tazarotene (0.1%) gel, which showed a (90.03±2.00%) degree of orthokeratosis. The 95% ethanolic extract of Nigella sativa shown IC50 239 µg/ml, with good antiproliferant activity compared to Asiaticoside as positive control which showed potent activity with IC50 value of 20.13 µg/ml. CONCLUSION: The ethanolic extract of Nigella sativa seeds also showed increase in relative epidermal thickness when compared to control group by confirming its traditional use in psoriasis treatment.
