TY - JOUR
T1 - In vitro assay and study interaction of Uncaria gambir (Hunter) Roxb. as anti-fibrotic activity against A549 cell line
AU - Desdiani, Desdiani
AU - Rengganis, Iris
AU - Djauzi, Samsuridjal
AU - Setiyono, Agus
AU - Sadikin, Mohamad
AU - Jusman, Sri Widia A.
AU - Siregar, Nuryati Chairani
AU - Suradi,
AU - Eyanoer, Putri C.
AU - Fadilah, Fadilah
N1 - Publisher Copyright:
© 2020 Phcogj.Com.
PY - 2020/12
Y1 - 2020/12
N2 - 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.
AB - 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.
KW - Gambiriin compounds
KW - Inhibitor of p50 NF-κB
KW - Molecular docking
KW - Pulmonary fibrosis
KW - TGF-β1 receptors
UR - http://www.scopus.com/inward/record.url?scp=85092320142&partnerID=8YFLogxK
U2 - 10.5530/PJ.2020.12.172
DO - 10.5530/PJ.2020.12.172
M3 - Article
AN - SCOPUS:85092320142
SN - 0975-3575
VL - 12
SP - 1232
EP - 1240
JO - Pharmacognosy Journal
JF - Pharmacognosy Journal
IS - 6
ER -