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In vitro anti-HIV and cytotoxic effects of pure compounds isolated from Croton macrostachyus Hochst. Ex Delile.

ABSTRACT: Croton macrostachyus is an important plant in traditional African medicine, widely utilized to treat a variety of diseases. In Kenya, HIV-infected patients use leaf and root decoctions of the plant as a cure for cough, back pain, bleeding, skin diseases, warts, pneumonia, and wounds. This study aimed to evaluate the anti-HIV activities and cytotoxic effects of extracts and chemical constituents isolated from C. macrostachyus. In our previous study we demonstrated that the hexane, CH₂Cl₂, ethyl acetate and methanol soluble fractions of a 1:1 v/v/ CH₂Cl₂/MeOH crude extracts of the leaves and stem bark of C. macrostachyus exhibited potent anti-HIV activities against HIV-1 with IC₅₀ values ranging from 0.02-8.1 μg/mL and cytotoxicity effects against MT-4 cells ranging from IC₅₀ = 0.58-174 μg/mL. Hence, hexane soluble extract of 1:1 v/v/ CH₂Cl₂/MeOH crude extract of the leaves of C. macrostachyus, that was more potent against HIV-1 at IC₅₀ = 0.02 μg/mL was subjected to column chromatography leading to the isolation of 2-methoxy benzyl benzoate (1), lupenone (2), lupeol acetate (3), betulin (4), lupeol (5), sitosterol (6) and stigmasterol (7). Lupenone (2), lupeol acetate (3) and betulin (4) exhibited anti-HIV-1 inhibition at IC₅₀ = 4.7 nM, 4.3 and 4.5 μg/mL respectively. The results obtained from this study support the potential of C. macrostachyus, as a source of anti-HIV constituents.

SUBMITTER: Terefe EM

PROVIDER: S-EPMC9202147 | biostudies-literature | 2022 Jun

REPOSITORIES: biostudies-literature

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In vitro anti-HIV and cytotoxic effects of pure compounds isolated from Croton macrostachyus Hochst. Ex Delile.

Terefe Ermias Mergia EM Okalebo Faith A FA Derese Solomon S Langat Moses K MK Mas-Claret Eduard E Aljarba Nada H NH Alkahtani Saad S Batiha Gaber El-Saber GE Ghosh Arabinda A El-Masry Eman A EA Muriuki Joseph J

BMC complementary medicine and therapies 20220615 1

Croton macrostachyus is an important plant in traditional African medicine, widely utilized to treat a variety of diseases. In Kenya, HIV-infected patients use leaf and root decoctions of the plant as a cure for cough, back pain, bleeding, skin diseases, warts, pneumonia, and wounds. This study aimed to evaluate the anti-HIV activities and cytotoxic effects of extracts and chemical constituents isolated from C. macrostachyus. In our previous study we demonstrated that the hexane, CH<sub>2</sub>C ...[more]

PMID: 35705943

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Project description:Utilization of agricultural waste such as nonedible seed oil for the synthesis of biodiesel via catalytic transesterification is one of the effective ways for the partial replacement of petroleum-based fuels in the area of renewable energy development and is beneficial to CO, CO2, and unburned hydrocarbon (HC) emission reduction to the environment. In this regard, the current study investigates the synthesis of fatty acid methyl esters (FAMEs) from Croton macrostachyus kernel oil by considering parameter interaction and optimization to maximize the yield of fatty acid methyl esters (FAMEs). The response surface methodology-central composite design (RSM-CCD) was applied to optimize the C. macrostachyus fatty acid methyl ester (CMKO-FAME) synthesis process by varying the process parameters such as reaction time (1-2 h), molar ratio (6:1-12:1), and catalyst loading (1-2 wt %). The optimum conditions for the transesterification of C. macrostachyus kernel oil (CMKO) were found to be a methanol to oil ratio of 11.98:1, catalyst loading of 1.03 wt %, and reaction time of 2 h, resulting in the conversion of 95.03 wt % C. macrostachyus kernel oil into its mono FAMEs. The fuel properties of CMKO and its FAMEs were determined based on ASTM D6751 and EN 14214 standards. Further, the CMKO and its FAMEs were characterized using Fourier transform infrared (FT-IR), gas chromatography-mass spectrometry (GC-MS), and nuclear magnetic resonance spectroscopy (NMR). The fatty acid composition of CMKO was myristic acid (1.36%), palmitic acid (11.35%), stearic acid (5.11%), oleic acid (18.64%), gadoleic acid (0.34%), linoleic acid (49.084%), and linolenic acid (14.1%). The purity of the produced methyl esters was determined by 1H NMR and found to be 95.52%, which was quite in good agreement with the experimentally observed yield of 95.39 wt %. The produced CMKO-FAME was blended with diesel fuel at various ratios (B5, B10, B15, and B20) to evaluate the engine performance and emission characteristics in a diesel engine. The engine brake thermal efficiency is lower, the brake-specific fuel consumption (BSFC) using CMKO-FAME blends is higher, and the temperature of exhaust gas emitted after combustion also increased as compared to diesel fuel. Similarly, using produced FAME blends, the emission emitted such as HC, NOx, and CO is reduced. However, the engine fueled with the produced FAME blends increased the level of CO2 into the atmosphere when compared to diesel fuel. The performance and emission characteristics of diesel engine result show that the blend of CMKO-FAME and diesel can be used as a fuel in a diesel engine without any modification of the engine.

Project description:BackgroundAngelica shikokiana is a Japanese medicinal herb that is included among food and drug preparations protecting against cancer; however, there is no previous report about the cytotoxicity of A. shikokiana or its bioactive compounds.ObjectiveThis study was designed to investigate the cytotoxic activities of A. shikokiana methanol extract (AME) and its isolated compounds and to identify the molecular mechanisms of the cytotoxicity.Materials and methodsCytotoxicity and selectivity was investigated by measuring the IC50 values on five cancer cell lines; human hepatocellular carcinoma, rhabdomyosarcoma (RD), colorectal carcinoma, human epithelioma and human breast adenocarcinoma and one normal cell line; human lung fibroblasts. The effects on tubulin polymerization and histone deacetylase 8 (HDAC8), were examined to determine the mechanism of cytotoxicity. Docking study was designed to examine the binding affinity to the target molecules.ResultsMethanol extract and some of its isolated coumarins and flavonoids showed potent, selective cytotoxicity against cancer cell lines. AME and all isolated compounds inhibited tubulin polymerization. Angelicin and kaempferol-3-O-rutinoside were the most active compounds. Phenolic compounds and furanocoumarins showed binding affinity to colchicine binding site rather than the vinblastine binding site of tubulin microtubules. On the other side, quercetin, kaempferol, luteolin, chlorogenic acid, and methyl chlorogenate exhibited the strongest activity against HDAC8 and the highest affinity to trichostatin A binding site.ConclusionThese findings provide the first scientific evidence of the cytotoxicity of AME through inhibition of tubulin polymerization and HDAC8 activity through its coumarin and flavonoid content.SummaryThe present study provides for the first time a clue for the cytotoxic activities of the AME. Our results indicate that the cytotoxic activities are partially related to the ability of AME to inhibit tubulin polymerization and HDAC8 activity. Isolated compounds; Angelicin and kaempferol-3-O-rutinoside showed the strongest inhibition of tubulin polymerization through binding to colchicine binding domain of tubulin microtubules. Phenolic compounds; quercetin, luteolin, kaempferol, chlorogenic acid and methyl chlorogenate exhibited a strong inhibition of HDAC8 through binding to TSA binding site. This, however, further detailed pharmacological and in vivo studies should be the next step in evaluating the cytotoxic activities of AME and its active compounds that are currently ongoing. Abbreviations used: AME: Methanol extract of the aerial part of A. shikokiana, HDACs: Histone deacetylases,HDAC8: Histone deacetylase 8.

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In vitro anti-HIV and cytotoxic effects of pure compounds isolated from Croton macrostachyus Hochst. Ex Delile.

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In vitro anti-HIV and cytotoxic effects of pure compounds isolated from Croton macrostachyus Hochst. Ex Delile.

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