30 research outputs found

    Serotonin transporter affinity of (−)-loliolide, a monoterpene lactone from Mondia whitei

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    AbstractMondia whitei (Apocynaceae) is used in traditional medicine to treat nervous disorders. Previous studies have shown in vivo antidepressant-like activity in the forced swimming test and affinity to the serotonin transporter of an ethanolic leaf extract of M. whitei. The aim of this study was to isolate the compound(s) responsible for in-vitro serotonin transporter affinity in M. whitei. Bioassay guided isolation lead to the identification of the monoterpene lactone (−)-loliolide. An ethanol extract was prepared from dry leaves. The residue was dissolved in ethyl acetate, extracted with water by liquid–liquid partitioning. This was followed by VLC fractionation. Through HPLC-UV separation the active compound was isolated and characterized by GC-MS, LC-MS and 1H-NMR. The activity of (−)-loliolide was tested in a serotonin transporter binding assay using [3H]-citalopram as ligand, giving an IC50-value of 997µM, corresponding to a Ki-value of 409µM. Loliolide is a non-nitrogenous compound and might bind to the transporter in a different way to nitrogen-containing inhibitors. The results provide a rationale for the use of M. whitei in the treatment of depression and other central nervous system diseases in traditional medicine

    In vitro cytotoxic and mutagenic evaluation of thirteen commercial herbal mixtures sold in KwaZulu-Natal, South Africa

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    AbstractCytotoxic and mutagenic effects of thirteen commercial herbal mixtures sold in KwaZulu-Natal, South Africa were evaluated using the neutral red uptake (NRU) assay and the Ames test. The herbal mixtures tested included Umzimba omubi, Umuthi wekukhwehlela ne zilonda, Mvusa ukunzi, Umpatisa inkosi, Imbiza ephuzwato, Vusa umzimba, Ingwe® muthi mixture, Ibhubezi™, Supreme one hundred™, Sejeso herbal mixture Ingwe®, Lion izifozonke Ingwe®, Stameta™ BODicare® and Ingwe® special muti. The relative cytotoxicity of the herbal mixtures was established by determining their NI50 values (50% inhibition of neutral red uptake). The test revealed that the most toxic herbal mixture was Umpatisa inkosi with an NI50 value of 0.016mg/mL and the least toxic mixture was Stameta™ BODicare® with an NI50 value of 28.00mg/mL. The herbal mixtures showed no mutagenic effects against Salmonella typhimurium tester strains TA98, TA100, TA102, TA1535 and TA1537 when the assay was done without S9 metabolic activation. However, four herbal mixtures, Umpatisa inkosi, Imbiza ephuzwato, Vusa umzimba and Stameta™ BODicare® showed mutagenic effects against TA98 but not the rest of the tester strains after using S9 metabolic activation. Umpatisa inkosi also exhibited weak mutagenic activity against TA1535 after metabolic activation. The remaining mixtures did not show mutagenic effects against all the tester strains after S9 metabolic activation. The cytotoxic and mutagenic results reported here offer a step toward determining the safety of commercial herbal mixtures in South Africa. Herbal mixtures showing higher cytotoxic and mutagenic effects need to be further investigated for their possible effects on humans

    Acetylcholinesterase inhibitory activity of plants used as memory- enhancers in traditional South African medicine

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    In traditional South African medicine there are a few plants used to improve memory and to treat Alzheimer's disease. Aqueous and ethanol extracts of five of these plants: Malva parviflora (leaves), Boophane disticha (leaves and bulbs), Albizia adianthifolia (stem bark), Albizia suluensis (root bark) and Crinum moorei (bulbs) were investigated. They were screened for acetylcholinesterase (AChE) inhibiting activity using thin- layer chromatography (TLC) and microtitre plate assays. Inhibition of AChE is an important approach in treating Alzheimer's disease. Promising results were obtained with bulbs of B. disticha and C. moorei. The aqueous and ethanol extracts of B. disticha (0.1mgml−1) yielded 38% and 27% inhibition in the microplate assay, respectively, while the ethanol extract of C. moorei had good dose-dependent inhibiting activity with 67% inhibition at the highest concentration. Aqueous and ethanol extracts of C. moorei and B. disticha showed AChE inhibiting activity in the TLC assay
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