ANTIPLASMODIAL ACTIVITIES OF THE STEM BARK EXTRACT OF ARTOCARPUS ALTILIS FORSBERG

Background: The potential of Artocarpus altilis stem bark as a safe antimalarial agent, and the identification of its antimalarial constituents was explored.  Materials and Methods:The air-dried stem bark was extracted with 70% ethanol, filtered and concentrated in vacuo to obtain the extract (EE). The extract was successively partitioned to give n-hexane (AAH),dichloromethane (AAD), ethyl acetate (AAE)n-butanol (AAB)and aqueous (AAQ)fractions respectively after determining the acute toxicity using Lorke’s method. These were each evaluated for chemosuppressive antimalarial activities (0-200mg/kg) against chloroquine-sensitive Plasmodium berghei-berghei-infected albino mice. Normal saline and chloroquine, 10 mg/kg were negative and positive control respectively.The survival times and percentage survivors of the mice in both experiments were determined after observation for twenty-eight days post-drug administration. The five (5) column chromatographic (CC) fractions, AAH1, AAH2, AAH3, AAH4andAAH5 obtained from the most active AAH, were also evaluated for antimalarial activities (0-50mg/kg). Further column purification and repeated PTLC of AAH5 yielded three bands, which were finally subjected to GC-MS analysis. Results:EE gave ED50 and LD50 values of 227.17and >5000 mg/kg while its partitioned fractions gave ED50 values as follows: AAH, 79.14; AAD, 215.59;AAE, 160.46,AAB,81.42; and AAQ, 90.85 mg/kg respectively. The primary CC fractions also gave ED50 values as follows:AAH1 21.95;AAH2, 26.96;AAH3,21.30; AAH4, 20.92 andAAH5, 20.75 mg/kg respectively to identify AAH5 as the putative fraction. GC-MS analysis revealed eleven major compounds (1–11) in the three PTLC bands as the antiplasmodial constituents of the plant. Conclusion:The stem bark of A. altilis is a potential agent in malaria control which is safe for oral use

In vitro induction of rat liver mitochondrial membrane permeability transition pore opening by solvent extracts of Momordica charantia leaves

Alteration of mitochondrial functions such as permeability transition (PT), a process associated with the uncoupling of oxidative phosphorylation, has been found to play a vital role in the apoptotic process induced by certain anti-cancer agents. When triggered, PT facilitates the release of mitochondrial apoptogenic proteins which in turn activate the caspase cascade of apoptosis. Thus, this study investigated the in vitro effects of varying concentrations (0.2, 0.4, 0.6, 0.8 and 1.0 mg/ml) of different leaf extracts [Crude Water-Soluble Extract (CWSE), Decoction (DE) and Methanol Extract (ME)] of Momordica charantia (M. charantia), a purported anti-cancer plant of the family Cucurbitaceae on normal rat liver mitochondria. Opening of mitochondrial membrane permeability transition pore (MMPTP) was spectrophotometrically assayed under succinate-energized condition. Results obtained showed concentration-dependent and significant (P<0.05) increases in the extents to which MMPTP opening was induced by the three extract types when compared with the control group. Inductions caused by CWSE and DE increased with increasing concentrations while those caused by ME decreased with increasing concentrations, giving the maximum induction at 1.0 mg/ml (8.1-fold increase) of CWSE and the least induction at 1.0 mg/ml (4.3-fold increase) of ME, respectively. Spermine, a reference inhibitor of MMPTP opening, reversed all observed openings. These results indicate that the tested leaf extracts of M. charantia are potent (CWSE being the most potent) MMPTP opening inducers and the pathway by which M. charantia causes apoptosis in cancer cells is probably mitochondrial-mediated (intrinsic)

In vitro induction of rat liver mitochondrial membrane permeability transition pore opening by solvent extracts of Momordica charantia leaves

Alteration of mitochondrial functions such as permeability transition (PT), a process associated with the uncoupling of oxidative phosphorylation, has been found to play a vital role in the apoptotic process induced by certain anti-cancer agents. When triggered, PT facilitates the release of mitochondrial apoptogenic proteins which in turn activate the caspase cascade of apoptosis. Thus, this study investigated the in vitro effects of varying concentrations (0.2, 0.4, 0.6, 0.8 and 1.0 mg/ml) of different leaf extracts [Crude Water-Soluble Extract (CWSE), Decoction (DE) and Methanol Extract (ME)] of Momordica charantia (M. charantia), a purported anti-cancer plant of the family Cucurbitaceae on normal rat liver mitochondria. Opening of mitochondrial membrane permeability transition pore (MMPTP) was spectrophotometrically assayed under succinate-energized condition. Results obtained showed concentration-dependent and significant (P<0.05) increases in the extents to which MMPTP opening was induced by the three extract types when compared with the control group. Inductions caused by CWSE and DE increased with increasing concentrations while those caused by ME decreased with increasing concentrations, giving the maximum induction at 1.0 mg/ml (8.1-fold increase) of CWSE and the least induction at 1.0 mg/ml (4.3-fold increase) of ME, respectively. Spermine, a reference inhibitor of MMPTP opening, reversed all observed openings. These results indicate that the tested leaf extracts of M. charantia are potent (CWSE being the most potent) MMPTP opening inducers and the pathway by which M. charantia causes apoptosis in cancer cells is probably mitochondrial-mediated (intrinsic)

Evaluation of the Antihyperglycaemic Activities, Safety and Phytochemical Profile of Celtis zenkeri Engl

Objective: The study evaluated the hyperglycaemia-lowering effects, safety, and phytochemical profile of Celtis zenkeri leaf extract in order to justify its antidiabetic folkloric usage.&nbsp;Methods: &nbsp;Modified OECD test guidelines were used to assess its acute and sub-acute toxicity while its effect on blood parameters such as blood glucose, and haematological and biochemical levels were evaluated using appropriate assays. Both in vitro and in vivo antihyperglycaemic assays were used for the antidiabetic studies while histology of the pancreas, liver, and kidney of the rats was examined after treatment with the extract at 250, 500, and 1000 mg/kg for 21 days. &nbsp;GC-MS analysis was used to determine the chemical constituents of the extract.&nbsp;Results: The results obtained showed that the leaf extract of C. zenkeri was not toxic in rats at 5000 mg/kg. It elicited a significant decrease in the blood glucose levels of the animals but did not affect the haematological and biochemical components of normal rats. It significantly inhibited &alpha;-amylase and &alpha;-glucosidase actions and gave comparable activity to glibenclamide (5 mg/kg) at all time points at 200 and 400 mg/kg. The extract comparably reduced blood glucose levels with glibenclamide at 100 and 200 mg/kg on days 10 and 14 in drug-induced diabetic rats and maintained the histoarchitecture of the liver, kidney, and pancreas at 250 and 500 mg/kg.Conclusion: The study justified the ethnomedicinal use of C. zenkeri in diabetes management