Plants of the genus Desmodium (Fabaceae), such as Desmodium styracifolium (Osbeck) Merr. and Desmodium gyrans (L. f.) DC., have a long history of medical use in Traditional Chinese Medicine to treat various ailments including rheumatism, pyrexia, dysentery, wounds, cough, malaria, hepatitis, hemoptysis, etc. In the theory of Traditional Chinese Medicine, most species have the effect of relieving internal heat or fever, neutralizing toxins, inhibiting pain, invigorating blood circulation, suppressing cough and alleviating dyspnea.
"entified as important ingredients ( Chidambaram et al . , 2013 ) . Since Desmodium species are known to include huge numbers of flavonoids and alkaloids , terpenoids , steroids , phenols , phenylpropanoids , glycosides , and a number of volatile oils , some of these could be expected to be active components exerting ethnopharmacological efficacy ( Ma et al . , 2011 ) . In spite of the ethnopharmacological value of this plant , the present knowledge of its biological properties is still marginal , except for its antiox - idant properties ( Chidambaram et al . , 2013 ) . Therefore , an inves - tigation of the anti - inflammatory activities of Codariocalyx motorius was preferentially performed . In a"
[Show abstract][Hide abstract] ABSTRACT: Ethnopharmacological relevance:
Codariocalyx motorius (Houtt.) H. Ohashi (Fabaceae) is one of several ethnopharmacologically valuable South Asian species prescribed as an herbal medicine for various inflammatory diseases. Due to the lack of systematic studies on this plant, we aimed to explore the inhibitory activity of Codariocalyx motorius toward inflammatory responses using its ethanolic extract (Cm-EE).
Materials and methods:
Lipopolysaccharide (LPS)-treated macrophages and a HCl/EtOH-induced gastritis model were used for evaluation of the anti-inflammatory activity of Cm-EE. HPLC and spectroscopic analysis were employed to identify potential active components. Mechanistic approaches to determine target enzymes included kinase assays, reporter gene assays, and overexpression of target enzymes.
Cm-EE strongly suppressed nitric oxide (NO) and prostaglandin E2 (PGE2) release. Cm-EE-mediated inhibition was observed at the transcriptional level in the form of suppression of NF-κB (p65) translocation and activation. This extract also lowered the levels of phosphorylation of Src and Syk, their kinase activity, and their formation of signalling complexes by binding to the downstream enzyme p85/PI3K. In accord with these findings, the phosphorylation of p85 induced by overexpression of Src or Syk was also diminished by Cm-EE. Orally administered Cm-EE clearly inhibited gastritic ulcer formation and the phosphorylation of IκBα and Src in HCl/EtOH-treated stomachs of mice. By phytochemical analysis, luteolin and its glycoside, apigenin-7-O-glucuronide, and scutellarein-6-O-glucuronide were identified as major components of Cm-EE. Among these, it was found that luteolin was able to strongly suppress NO and PGE2 production under the same conditions.
Syk/Src-targeted inhibition of NF-κB by Cm-EE could be a major anti-inflammatory mechanism contributing to its ethno pharmacological role as an anti-inflammatory herbal medicine.
Journal of Ethnopharmacology 05/2014; 155(1). DOI:10.1016/j.jep.2014.05.013 · 3.00 Impact Factor
[Show abstract][Hide abstract] ABSTRACT: In spite of availability of moderately protective vaccine and antibiotics, new antibacterial agents are urgently needed to decrease the global incidence of Klebsiella pneumonia infections. MurF ligase, a key enzyme, which participates in the bacterial cell wall assembly, is indispensable to existence of K. pneumonia. MurF ligase lack mammalian vis-à-vis and have high specificity, uniqueness, and occurrence only in eubacteria, epitomizing them as promising therapeutic targets for intervention. In this study, we present a unified approach involving homology modeling and molecular docking studies on MurF ligase enzyme. As part of this study, a homology model of K. pneumonia (MurF ligase) enzyme was predicted for the first time in order to carry out structurebased drug design. The accuracy of the model was further validated using different computational approaches. The comparative molecular docking study on this enzyme was undertaken using different phyto-ligands from Desmodium sp. and a known antibiotic Ciprofloxacin. The docking analysis indicated the importance of hotspots (HIS 281 and ASN 282) within the MurF binding pocket. The Lipinski's rule of five was analyzed for all ligands considered for this study by calculating the ADME/Tox, drug likeliness using Qikprop simulation. Only ten ligands were found to comply with the Lipinski rule of five. Based on the molecular docking results and Lipinki values 6-Methyltetrapterol A was confirmed as a promising lead compound. The present study should therefore play a guiding role in the experimental design and development of 6-Methyltetrapterol A as a bactericidal agent.
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