RESUMEN
Plants are fantastic sources for present day life saving drugs. Monocrotaline a natural ligand exhibits dose-dependent cytotoxicity with potent antineoplastic activity. This study was intended to disclose the therapeutic potential of monocrotaline against hepatocellular carcinoma. The in silico predictions have highlighted the antineoplastic potential, druglikeness and biodegradability of monocrotaline. The in silico docking study has provided an insight and evidence for the antineoplastic activity of monocrotaline against p53, HGF and TREM1 proteins which play a threatening role in causing hepatocellular carcinoma. The mode of action of monocrotaline was determined experimentally by in vitro techniques such as XTT assay, NRU assay and whole cell brine shrimp assay have further supported our in silico studies. The in vitro cytotoxicity of monocrotaline was proved at IC50 24.966 µg/mL and genotoxicity at 2 X IC50 against HepG2 cells. Further, the credible druglike properties with non-mutagenicity, non-toxic on mammalian fibroblast and the potential antineoplastic activity through in vitro experimental validations established monocrotaline as a novel scaffold for liver cancer with superior efficacy and lesser side effects.
Asunto(s)
Antineoplásicos/farmacología , Carcinoma Hepatocelular/patología , Proliferación Celular/efectos de los fármacos , Neoplasias Hepáticas/patología , Monocrotalina/farmacología , Animales , Células 3T3 BALB , Simulación por Computador , Células Hep G2 , Factor de Crecimiento de Hepatocito/metabolismo , Humanos , Glicoproteínas de Membrana/metabolismo , Ratones , Simulación del Acoplamiento Molecular , Receptores Inmunológicos/metabolismo , Receptor Activador Expresado en Células Mieloides 1 , Proteína p53 Supresora de Tumor/metabolismoRESUMEN
OBJECTIVE@#To compare the efficacy for phytochemical, antibacterial and antioxidant activities of petroleum ether, chloroform, ethanol, and aqueous extracts of in vitro propagated plants and field grown plants of Crotalaria sps., for against five human pathogens.@*METHODS@#The preliminary phytochemistry, antimicrobial and antioxidant activities were evaluated using disc diffusion and DPPH radical scavenging methods.@*RESULTS@#The ethanolic extract of in vitro raised Crotalaria retusa (C. retusa) was effective on tested microorganisms and optimal ZOI values of 38 mm was obtained against Pseudomonas aeruginosa (P. aeruginosa). The optimal concentration (IC50) required for 50% inhibition of the DPPH radical scavenging was 57.6 μ g/mL obtained for ethanolic extract of in vitro propagated C. retusa. The in vitro propagated C. retusa has significant pharmacological activities while the Crotalaria prostrate (C. prostrate) and Crotalaria medicaginea (C. medicaginea) has low pharmacological activites. It was cleared that ethanolic extract of in vitro regenerated plants was most effective.@*CONCLUSIONS@#These findings indicate compounds isolated from ethanolic extracts of Crotalaria sps., possesses pharmacological properties and potential to develop natural compounds based pharmaceutical products. The IC(50) values for ethanolic extracts of Crotalaria sps. was evaluated through the Linear regression analysis (R(2) ≤ 1).
Asunto(s)
Humanos , Alcanos , Antibacterianos , Farmacología , Antioxidantes , Farmacología , Fraccionamiento Químico , Cloroformo , Crotalaria , Química , Etanol , Depuradores de Radicales Libres , Farmacología , Modelos Lineales , Fitoterapia , Extractos Vegetales , Química , Farmacología , Plantas Medicinales , Química , Solventes , Especificidad de la EspecieRESUMEN
Objective To compare the efficacy for phytochemical, antibacterial and antioxidant activities of petroleum ether, chloroform, ethanol, and aqueous extracts of in vitro propagated plants and field grown plants of Crotalaria sps., for against five human pathogens. Methods The preliminary phytochemistry, antimicrobial and antioxidant activities were evaluated using disc diffusion and DPPH radical scavenging methods. Results The ethanolic extract of in vitro raised Crotalaria retusa (C. retusa) was effective on tested microorganisms and optimal ZOI values of 38 mm was obtained against Pseudomonas aeruginosa (P. aeruginosa). The optimal concentration (IC50) required for 50% inhibition of the DPPH radical scavenging was 57.6 μ g/mL obtained for ethanolic extract of in vitro propagated C. retusa. The in vitro propagated C. retusa has significant pharmacological activities while the Crotalaria prostrate (C. prostrate) and Crotalaria medicaginea (C. medicaginea) has low pharmacological activites. It was cleared that ethanolic extract of in vitro regenerated plants was most effective. Conclusions These findings indicate compounds isolated from ethanolic extracts of Crotalaria sps., possesses pharmacological properties and potential to develop natural compounds based pharmaceutical products. The IC