Inhibition of Helicobacter pylori and Its Associate Urease by Labdane Diterpenoids Isolated from Andrographis paniculata.

The present study was carried out to evaluate anti-Helicobacter pylori and its associated urease activity of labdane diterpenoids isolated from Andrographis paniculata. A molecular docking analysis was performed by using ArgusLab 4.0.1 software. The results obtained indicate that compound A possesses strong inhibition to H. pylori, 28 ± 2.98 (minimum inhibitory concentration, 9 µg/mL), and its urease, 85.54 ± 2.62% (IC50 , 20.2 µg/mL). Compounds B, C, and D also showed moderate inhibition to H. pylori and its urease. The obtained results were in agreement with the molecular docking analysis of compounds. The phytochemicals under investigation were found to be promising antibacterial agents. Moreover, the isolated compounds can be considered as a resource for searching novel anti-H. pylori agents possessing urease inhibition.

Evaluation of anti-inflammatory activity of selected medicinal plants used in Indian traditional medication system in vitro as well as in vivo.

The present study was carried out to evaluate in vivo and in vitro anti-inflammatory potential of selected medicinal plants used in Indian traditional medication. The sequentially extracted plant samples as, Cissus quadrangularis, Plumbago zeylanica, Terminalia bellarica and Terminalia chebula in water, ethanol and hexane were evaluated in-vitro for COX-1 and 2 inhibitory and antioxidant activities. The in vivo anti-inflammatory activity of selected samples showing promising COX-2 inhibition was assessed using carrageenan and Phorbol Myristate Acetate (PMA) induced mice edema animal model. The results obtained reveals that most of the plants were found to inhibit COX-2 activity as compared to COX-1. It was observed that the extracts of T. bellarica (73.34 %) and T. chebula (74.81 %) showed significant COX-2 selective inhibition as compared to other samples. The ethanol extract of the selected plants demonstrated effective DPPH, OH and superoxide radical scavenging activity. In vivo anti-inflammatory study shows that, T. bellarica and T. chebulla had a significant impact on inhibition of edema formation. The cytotoxicity evaluation study of ethanolic fraction of selected medicinal plants indicates that the selected samples have no effect on cell viability. HPTLC fingerprint of flavonoids of the selected samples was also prepared as a measure of quality control. The results obtained may be useful in strengthening the standardization of the selected botanicals. Moreover the selected plants can be considered as a resource for searching novel anti-inflammatory agents possessing COX-2 inhibition.

Synthesis and biological evaluation of asymmetric indole curcumin analogs as potential anti-inflammatory and antioxidant agents.

Abstract A series of asymmetric indole curcumin analogs were synthesized and evaluated as possible inhibiters of pro-inflammatory enzymes such as COX-2, pro-inflammatory cytokines as TNF-α and IL-6, trypsin and ß-glucuronidase. They were also tested for antioxidant activities. The results showed that compounds 5e and 5h were found to be the most potent inhibitors of COX-2 (83.33%, 82.50%) and ß-glucuronidase (67.80%, 64.12%). All the synthesized compounds exhibited promising activity against IL-6 in a range of 71-100% at 10 µM concentration. Compounds 5f, 5h, 5e, 5c and 5d showed significant inhibition against TNF-α (28-51%) and IL-6 (87-98%) with low toxicity (45-51%) against CCK-8 cells. With few exceptions, all other compounds were found to be good to excellent inhibitors of IL-6 and moderate inhibitors of TNF-α; however, the toxicity profiles of these compounds need to be ameliorated in further optimization studies. Amongst the tested compounds, 5c, 5b, 5j and 5g were found to possess excellent reducing activity and 5b, 5c and 5h were moderate DPPH (1,1-diphenyl-2-picryl hydrazine) radical scavengers.