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Identification of Novel BCL- 2-Specific Inhibitors from Murva - A Promising Ayurvedic Anticancer Agent (In Vitro & In Vivo Studies)
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| Author:
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RAJU ASIRVATHAM, APARNA ANN MATHEW, PRIYA PN, MARTIN C, DINU GEORGE, DAISY PA
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| Abstract:
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This study focused on identification of antiproliferative mechanism of Murva by in silico methods and compared
the in vivo anticancer activity of methanol extracts of Marsdenia tenacissima (MEMT) and Sansevieria roxburghiana
(MESR), are known to be Murva. PASS online study was carried out with Dresgenin from M.tenacissima and
Lupeol from S.roxburghiana to know the possible biological activities and were taken as ligands for the target
BCL-2 protein. Tryphan blue dye exclusion assay was done with different concentration of MEMT and MESR.
In in vivo, 90 mice were organized in to 9 groups with ten mice in each. All animals except group I,
intraperitoneal inoculated with DLA cell lines. Group I-normal control received distilled water, Group II
cancer control received distilled water, Group III -received 20mg/kg of standard 5- Fluorouracil, i.p, Group IV -
100mg/kg of Venetoclax, p.o, Group V &VI treated with 100 and 200mg/kg of MEMT, Group VII &VIII treated
with 50 and 100mg/kg of MESR and IX received combination of MEMT & MESR for 14 days. On 15th day
haematological and tissue antioxidant level were measured. Insilico study results revealed that ligand has
antineoplastic and Caspase 3 stimulant activity, binding scores of -9.1 and -9.2 (Kcal/mol) with BCL-2. In vitro
cytotoxicity result showed MEMT (56%), MESR (68%) and the combination (92%) of cell death. In in vivo study,
most significant (p<0.001) effect with combination on altered haematological and antioxidant level. The
pharmacological effect was due the binding of Dresgenin and Lupeol binds with BCL- 2 protein.
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| Keyword:
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Murva, Marsdenia tenacissima, Sansevieria roxburghiana, insilico studies, anticancer, molecular docking, DLA, Tryphan blue
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| EOI:
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| DOI:
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https://doi.org/10.31838/ijpr/2021.13.02.228
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| Download:
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