Lambertic Acid

Network Pharmacology and Molecular Docking Reveal the Mechanism of Isodon ternifolius (D. Don) Kudo Against Liver Fibrosis.[Pubmed:37576085]

Drug Des Devel Ther. 2023 Aug 7;17:2335-2351.

AIM: Many studies have demonstrated the hepatoprotective or anti-fibrotic effects of Isodon ternifolius, but its pharmacological basis and mechanism remain unclear. In this study, we used in vitro models to validate the predicted results and revealed the potential mechanism of action and active ingredients through network pharmacology methods and molecular docking. METHODS: The chemical components of Isodon ternifolius were identified by literatures. Potential targets of Isodon ternifolius were predicted by Swiss Target Prediction. The disease targets were collected through the databases of Gene Card. Common targets of Isodon ternifolius and liver fibrosis were obtained by online tool Venny 2.1. PPI protein interaction network was obtained using String database, and target protein interaction network was drawn using Cytoscape software. Signaling pathway enrichment analysis was performed on drug-disease targets with of DAVID database. RESULTS: Twenty-one potential active ingredients and 298 potential targets were predicted by Swiss Target Prediction platform. Ninety pathways related to liver fibrosis were obtained by KEGG enrichment. The TLR4, MAPK and PI3K-Akt signaling pathways are mostly associated with liver fibrosis. Molecular docking techniques were used to validate the core target proteins TNF, Akt1, MAPK1, EGFR and TLR4 binding to the ingredients of Isodon ternifolius, which showed that a multitude of ingredients of Isodon ternifolius were able to bind to the above target proteins, especially 2alpha-hydroxy oleanolic acid and (-)-Lambertic Acid. Our experimental validation results showed that Isodon ternifolius inhibited the activation of PI3K-Akt and ERK1/2 signaling pathways. CONCLUSION: Through a network pharmacology approach and in vitro cell assay, we predicted and validated the active compounds of Isodon ternifolius and its potential targets for LF treatment. The results suggest that the mechanism of Isodon ternifolius treating LF by inhibiting angiogenesis may be related to the ERK1/2 and PI3K/Akt signaling pathways.

Antimicrobial Activities of Salacia oblonga Wall Leaf and Root Extracts Against Different Bacterial Strains and Fungal Isolates.[Pubmed:35612657]

Curr Microbiol. 2022 May 25;79(7):204.

Antibiotic resistance and the hazardous nature of synthetic drugs is threatening issue in the health sector. The alternative for this problem is to focus on plants that attribute to various compounds that exhibit therapeutic properties. Therefore, the study aims to evaluate the antimicrobial efficacy of Salacia oblonga leaf and root extracts against tested human pathogens. The S. oblonga extracts showed a significant zone of inhibition against bacteria and fungi. The leaf and root extracts of S. oblonga are prepared using low polar to high polar solvents in the Soxhlet apparatus and tested on the selected bacterial and fungal strains. Agar well diffusion and broth dilution methods evaluate antibacterial activity, antifungal activity, and Minimum Inhibitory Concentration (MIC) of extracts. Among the extracts tested, the ethyl acetate extract of root showed more antimicrobial activity against the tested bacterial and fungal strains. The most susceptible bacterial and fungal species against ethyl acetate extract are Micrococcus luteus, Mycobacterium tuberculosis, Microsporum canis, Trichophyton interdigitale, and Microsporum gypseum. The MIC for bacteria ranged from 13.0 to > 200 microg/ml, whereas for fungi, the MIC ranged from 25.9 to > 200 microg/ml. Ethyl acetate extract of root with 100 microg/ml concentration showed 29.1 mm and 28.7 mm zone of inhibition against bacterial strains M. luteus and M. tuberculosis, respectively. The ethyl acetate extract of root with a 100 microg/ml concentration showed 15.8, 15.2, and 15.6 mm zone of inhibition against fungal isolates M. canis, T. interdigitale, and M. gypseum, respectively. The activity of root and leaf extracts increased in a concentration-dependent manner, and further, the compounds isolated from the crude extracts of leaf and root showed antimicrobial activity. Structural elucidation of isolated compounds Lambertic Acid and Ferruginol was done using NMR spectroscopy. Reports indicate that Lambertic Acid was isolated previously, but the isolation of hydroxy Ferruginol from S. oblonga leaf extract was reported unprecedented.

Identification and characterization of potential antioxidant components in Isodon amethystoides (Benth.) Hara tea leaves by UPLC-LTQ-Orbitrap-MS.[Pubmed:33385513]

Food Chem Toxicol. 2021 Feb;148:111961.

Isodon amethystoides (Benth.) Hara (IA) tea is a commonly used dietetic Chinese herb and employed for the treatments of tumor and lung abscess. To assess chemical composition and antioxidant capacity of IA leaves extract, a UPLC-LTQ-Orbitrap-MS method and antioxidant tests were used, respectively. 17 compounds were identified including Vinyl caffeate (1), 3,4-dimethoxyphenyl-beta-D-glucopyranoside (2), Rutin (3), Quercetin (4), Loliolide (5), Caffeic acid (6), Rubesanolide D (7), Isorhamnetin (8), Lambertic Acid (9), 6, 7-Dehydroroyleanone (10), Dihydrorabdokunmin C (11), Nervosin (12), Quercitrin (13), Vitexin (14), beta-sitosterol (15), Wangzaozin A (16), Amethystonoic acid (17). Among these, 1-14 compounds were novel and have not been reported ever before in IA while component 10 was a novel finding within this genus. Flavonoid components showed better free radical scavenging ability and profound correlation was observed between diterpenoid compounds content and flavonoids activity. Our results provide experimental basis for extraction and separation of chemical constituents of IA which are antioxidant in nature.