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In Vitro Antiplasmodial and Cytotoxic Activities of Compounds from the Roots of Eriosema montanum Baker f. (Fabaceae).

ABSTRACT: Malaria remains one of the leading causes of death in sub-Saharan Africa, ranked in the top three infectious diseases in the world. Plants of the Eriosema genus have been reported to be used for the treatment of this disease, but scientific evidence is still missing for some of them. In the present study, the in vitro antiplasmodial activity of the crude extract and compounds from Eriosema montanum Baker f. roots were tested against the 3D7 strain of Plasmodium falciparum and revealed using the SYBR Green, a DNA intercalating compound. The cytotoxicity effect of the compounds on a human cancer cell line (THP-1) was assessed to determine their selectivity index. It was found that the crude extract of the plant displayed a significant antiplasmodial activity with an IC50 (µg/mL) = 17.68 ± 4.030 and a cytotoxic activity with a CC50 (µg/mL) = 101.5 ± 12.6, corresponding to a selective antiplasmodial activity of 5.7. Bioactivity-guided isolation of the major compounds of the roots' crude extract afforded seven compounds, including genistein, genistin and eucomic acid. Under our experimental conditions, using Artemisinin as a positive control, eucomic acid showed the best inhibitory activity against the P. falciparum 3D7, a well-known chloroquine-sensitive strain. The present results provide a referential basis to support the traditional use of Eriosema species in the treatment of malaria.

SUBMITTER: Tomani JCD

PROVIDER: S-EPMC8125995 | biostudies-literature | 2021 May

REPOSITORIES: biostudies-literature

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In Vitro Antiplasmodial and Cytotoxic Activities of Compounds from the Roots of Eriosema montanum Baker f. (Fabaceae).

Tomani Jean Claude Didelot JCD Bonnet Olivier O Nyirimigabo Alain A Deschamps William W Tchinda Alembert Tiabou AT Jansen Olivia O Ledoux Allison A Mukazayire Marie Jeanne MJ Vanhamme Luc L Frédérich Michel M Muganga Raymond R Souopgui Jacob J

Molecules (Basel, Switzerland) 20210510 9

Malaria remains one of the leading causes of death in sub-Saharan Africa, ranked in the top three infectious diseases in the world. Plants of the Eriosema genus have been reported to be used for the treatment of this disease, but scientific evidence is still missing for some of them. In the present study, the in vitro antiplasmodial activity of the crude extract and compounds from Eriosema montanum Baker f. roots were tested against the 3D7 strain of Plasmodium falciparum an ...[more]

PMID: 34068519

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Project description:Ethnopharmacological relevanceTurraea robusta and Turraea nilotica are African medicinal plants used for the treatment of a wide variety of diseases, including malaria. The genus Turraea is rich in limonoids and other triterpenoids known to possess various biological activities.Materials and methodsFrom the stem bark of T. robusta six compounds, and from various parts of T. nilotica eleven compounds were isolated by the use of a combination of chromatographic techniques. The structures of the isolated compounds were elucidated using NMR and MS, whilst the relative configuration of one of the isolated compounds, toonapubesin F, was established by X-ray crystallography. The antiplasmodial activities of the crude extracts and the isolated constituents against the D6 and W2 strains of Plasmodium falciparum were determined using the semiautomated micro dilution technique that measures the ability of the extracts to inhibit the incorporation of (G-(3)H, where G is guanine) hypoxanthine into the malaria parasite. The cytotoxicity of the crude extracts and their isolated constituents was evaluated against the mammalian cell lines African monkey kidney (vero), mouse breast cancer (4T1) and human larynx carcinoma (HEp2).ResultsThe extracts showed good to moderate antiplasmodial activities, where the extract of the stem bark of T. robusta was also cytotoxic against the 4T1 and the HEp2 cells (IC50<10 μg/ml). The compounds isolated from these extracts were characterized as limonoids, protolimonoids and phytosterol glucosides. These compounds showed good to moderate activities with the most active one being azadironolide, IC50 2.4 ± 0.03 μM and 1.1 ± 0.01 μM against the D6 and W2 strains of Plasmodium falciparum, respectively; all other compounds possessed IC50 14.4-40.5 μM. None of the compounds showed significant cytotoxicity against vero cells, yet four of them were toxic against the 4T1 and HEp2 cancer cell lines with piscidinol A having IC50 8.0 ± 0.03 and 8.4 ± 0.01 μM against the 4T1 and HEp2 cells, respectively. Diacetylation of piscidinol A resulted in reduced cytotoxicity.ConclusionFrom the medicinal plants T. robusta and T. nilotica, twelve compounds were isolated and characterized; two of the isolated compounds, namely 11-epi-toonacilin and azadironolide showed good antiplasmodial activity with the highest selectivity indices.

Project description:Medicinal plants with documented traditional uses remain an important source for the treatment of a wide range of ailments. Evidence shows that majority of the Ethiopian population are still dependent on traditional medicine. Aloe pulcherrima Gilbert & Sebsebe is one of the endemic Aloe species traditionally used for the treatment of malaria and wound healing in central, Southern and Northern part of Ethiopia. The aim of the current study was, therefore, to isolate active compounds from roots of A. pulcherrima and evaluate for their antibacterial and antiplasmodial activities using standard test strains. Bioassay-guided sequential extraction and column chrom-atographic separation were employed for the isolation of bioactive pure compounds. The structures of the compounds were determined by 1D and 2D NMR spectro-scopic techniques. Disk diffusion method was employed to evaluate the antibacterial activities of the isolated compounds against four bacterial strains specifically (Staphylococcus aureus ATCC 25923, Bacillus subtilis ATCC 6633, Escherichia coli ATCC 35218, Pseudomonas aeruginosa ATCC 27853). The malaria SYBR Green I-based in vitro assay technique was used for in vitro antiplasmodial activity evaluation of the compounds against chloroquine resistant (D6) and -sensitive (W2) strains of P. falciparum. Three compounds, chrysophanol, aloesaponarin I and aloesaponarin II were isolated from the acetone extracts of roots of A. pulcherrima. Evaluation of antibacterial activities revealed that aloesaponarin I and aloesaponarin II had significant activities against all the bacterial strains with inhibition zone diameters ranging from 18-27 mm as compared to the reference drug (gentamicin), which displayed inhibition zone diameter ranging between 20 mm (B. subtilis) and 25 mm (P. aeruginosa). The isolated compounds showed moderate in vitro antiplasmodial activity against both chloroquine resistant (W2) -sensitive (D6) strains. Isolation of chrysophanol, aloesaponarin I and aloesaponarin II from roots of A. pulcherrima is the first report of its kind. The finding could be used for further comprehensive evaluation of the isolated compounds for their antibacterial and antimalarial activities besides consideration of the same for potent drug development.

Project description:BackgroundThe root of Baliospermum montanum has been used as an ingredient of traditional Thai medicines for the treatments of several diseases including itching eczema, muscle and joint inflammation, and cancer. Few studies have been done on phytochemical components of this root. In this study, we isolated major compounds of the crude ethanolic extract of B. montanum root and developed and validated a high performance liquid chromatographic (HPLC) method for the determination of its major components. We then investigated anti-allergic, anti-inflammatory and cytotoxic activities of the extract.MethodsThe aims of this study were to investigate in vitro activities including inhibitory effect of β-hexosaminidase released from RBL-2H3 cells, inhibition of nitric oxide (NO) production from RAW 264.7 cells and cytotoxic activity against cancerous liver cell lines (HepG2 and KKU M156) by using sulforhodamine B (SRB) assay. Isolation of major components was conducted by using column chromatographic method. Isolated major compounds were analyzed by using high performance liquid chromatography (HPLC).ResultsThe crude extract exhibited the highest cytotoxic activity, with IC50 less than 1 μg/mL, while its anti-allergy and anti-inflammation were also potent with IC50 less than 6 μg/mL. Three propiophenones isolated from B. montanum root exhibited moderate cytotoxic activities (IC50 > 20 μg/mL). Two of the propiophenones found were major components that can be detected by HPLC. The developed and validated HPLC method showed good accuracy, precision, and linearity.ConclusionThe results of this study suggested that ethanolic extract of of B.montanum root can be a potential source of anti-allergy, anti-inflammation, and anti-cancer compounds. The isolated compounds can serve as markers when B. montanum is used in herbal remedies but not as overall responsive markers. The HPLC method developed may be useful for quality control in the production of the extract and for further formulation developments. However, investigation of several associated biological activities is necessary before the development can proceed further. Minor active compounds should be isolated and a more sensitive analytical method should be developed to detail the key responsive components of the ethanolic extract of B. montanum root.

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 Antiplasmodial and Cytotoxic Activities of Compounds from the Roots of Eriosema montanum Baker f. (Fabaceae).

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In Vitro Antiplasmodial and Cytotoxic Activities of Compounds from the Roots of <i>Eriosema montanum Baker f.</i> (Fabaceae).

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