Desdiani, Desdiani and Rengganis, Iris and Djauzi, Samsuridjal and Setiyono, Agus and Sadikin, Mohamad and Jusman, Sri Widia A and Siregar, Nuryati Chairani and Suradi, Suradi and Eyanoer, Putri C and Fadilah, Fadilah (2020) In vitro Assay and Study Interaction of Uncaria gambir (Hunter) Roxb. as Anti-fibrotic Activity Against A549 Cell Line. Pharmacognosy Journal, 12 (6). pp. 1231-1240. ISSN 0975-3575

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Abstract

Aim: The aim of this study is to finding inhibitor potential from several compounds in gambir plant by using in vitro MTT assay and study interaction with molecular docking. The interaction of amino acids on the binding site with substances in the gambir plant was analyzed to determine its potential as a herbal-based therapy candidate for pulmonary fibrosis. Material and Methods: Protein target using TGFβ1 and NF-κB and compounds from gambir plant ((+)-Catechin. Epigallocatechin gallate, (+)-Epicatechin, Gambiriin A1, Gambiriin A2, Gambiriin B1, Gambiriin B2, Gambiriin C, Procyanidin B1, Procyanidin B3). Result: The results from docking analysis observed that compounds from gambir fruit contain anti-fibrotic activity which act by inhibiting DNA transcription of NF-κB and TGF-β1receptors. The compound Procyanidin B3, an essential amino acid, contains a hydrogen bond with the greatest NF-κB inhibitory activity on Gly214 and Lys337. Compounds from Uncaria gambir (Hunter) Roxb. can be an inhibitor to TGFβ1, all the compounds are on the active site of TGFβ1, and use native ligand which is an inhibitor of TGFβ1 (Naphtyridine). The positive compound catechin has the highest inhibitory activity. Gambiriin B1 and Gambiriin A2 are the most identical compounds with similar affinity binding value. Uncaria gambir (Hunter) Roxb. is already a proven antifibrotic which is further confirmed by (IC50: 19,255 ± 1.08 μg/ml, p < 0.05) in A549 cell line. Conclusion: The results demonstrated that Gambiriin have cytotoxic effects and was found potentially as anti-fibrotic by MTT assay and in silico evaluation.

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