Background Changes in blood lipid level (dyslipidemia) play a central role in the onset and pathogenesis of macrovascular complications of diabetes mellitus. Traditional herbal healers commonly use anti-diabetic polyherbal formulations to provide a multi-therapeutic approach for the treatment of diabetes mellitus and its associated complications. The effect of the aqueous leaf extracts of Leptadenia hastata (pers) Decne, Momordica balsamina Linn and their combination on lipid profile of streptozotocin (STZ)-induced diabetic rats was therefore evaluated in the present study. Results We evaluated the serum lipid profile and blood glucose level of STZ-induced diabetic rats (60 mg/kg body weight) treated with the aqueous leaf extracts of L. hastata (400 mg/kg) and M. balsamina (200 mg/kg) alone and in combination (400 + 200 mg/kg) after a period of 4 weeks. A significantly decreased (p < 0.05) level of total cholesterol (TC), triglyceride (TG), very low-density lipoprotein (VLDL) and low-density lipoprotein (LDL) cholesterol levels and increased (p < 0.05) level of high-density lipoprotein (HDL) cholesterol was observed in all the treated groups when compared to the untreated diabetic rats. Furthermore, the combination treatment was potentially a more effective blood lipid-lowering (p < 0.05) agent when compared to the single treatments. Conclusion Results from this study demonstrated the blood lipid-lowering potential of the aqueous leaf extracts of L. hastata, M. balsamina, and their combination. However, the polyherbal combination could be more potent in controlling diabetes mellitus, associated dyslipidemia, and its complications.
The in silico simulations and predictions approach in evaluation of pharmacokinetic properties of new chemical entities (NCEs) is fast becoming an acceptable trend in natural products research and drug discovery. This paper focuses on the properties of trolline with respect to its anti-inflammatory and MCF-7 breast cancer cell line growth inhibition effects and an attempt to predict physico-chemical druglike properties in silico. The compound was isolated for the first time from aerial parts of Mirabilis jalapa and the structure was elucidated by 1D and 2D NMR, FTIR and mass spectroscopic analyses. The compound was screened for anti-inflammatory and anti-MCF-7 cell lines proliferation using chemoluminiscence oxidative burst and MTT assays respectively. Predictions on physico-chemical properties central to oral route drug administration were done using commercial software Admet predictor. Results show anti-inflammatory effects at IC 50 concentration of 53.8 µg/ml and 48% mortality of breast cancer cell lines at 50 µM concentration. Predictions suggest moderate solubility of 1.72 to 2.92 mg/ml across pH range of 1.6 to 6.8 in simulated solvent systems and effective jejunal permeability of 5.61 x 10 -4 cm/s. The compound was also predicted to be 60% unbound to plasma proteins and an LD 50 of 950 mg/kg in rats. The compound, trolline had clinically important bioactive effects, probably possess promising drug-like properties suitable for further high throughput screening.
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