Protein kinase B (PknB) is one of the Mycobacterium tuberculosis serine/threonine protein kinases and has an essential role in sustaining mycobacterial growth. Here, we identified and characterized a novel small molecule compound named IMB-YH-8 that inhibited PknB and served as anti-mycobacteria lead compound. IMB-YH-8 inhibited PknB auto-phosphorylation and the phosphorylation of GarA by PknB in a dose-dependent manner.
View Article and Find Full Text PDFNaunyn Schmiedebergs Arch Pharmacol
July 2017
Reactive oxygen species (ROS) is a pivotal pathogenic factor in the development of osteoporosis. Dalbergioidin (DAL) can be isolated from Uraria crinite, an edible herb used as a natural food for childhood skeletal dysplasia. Recent research has implicated DAL as having an antiosteoporosis effect, although the mechanism of this is unclear.
View Article and Find Full Text PDFNaunyn Schmiedebergs Arch Pharmacol
June 2015
Pancreatic cancer is a devastating disease with a poor prognosis. It ranks as the fourth or fifth most common cancer in men and women and has the lowest 5-year survival rate. Therefore, there is an urgent need to develop novel therapeutic agents for pancreatic cancer.
View Article and Find Full Text PDFA series of chalcones a1-20 bearing a 4-OMe groups on the A-ring were initially synthesized and their anticancer activities towards HepG2 cells evaluated. Subsequently, a series of chalcones b1-42 bearing methoxy groups at the 2' and 6'-positions of the B-ring were synthesized and their anticancer activities towards five human cancer cell lines (HepG2, HeLa, MCF-7, A549 and SW1990) and two non-tumoral human cell lines evaluated. The results showed that six compounds (b6, b8, b11, b16, b18, b22, b23 and b29) displayed promising activities, with compounds b22 and b29 in particular showing higher levels of activity than etoposide against all five cancer cell lines.
View Article and Find Full Text PDFIn this study, we investigated the neuroprotective effects of madecassoside, isolated from the Chinese medicinal herb Centella asiatica, in the rat model of early phase of parkinsonism. During intragastric administrations of madecassoside for 7 days, the rats were injected with MPTP on the 7th day. And for the following 14 days, madecassoside were also administered.
View Article and Find Full Text PDFThe apical sodium-dependent bile salt transporter (ASBT) plays a pivotal role in maintaining bile acid homeostasis. Inhibition of ASBT would reduce bile acid pool size and lower cholesterol levels. In this report, a series of novel arylsulfonylaminobenzanilides were designed and synthesized as potential inhibitors of ASBT.
View Article and Find Full Text PDFChaihu-jia-longgu-muli-tang (CLM) has been used for treating depressive disorders for thousands of years in China. In the present study, we investigated the antidepressant-like effect of the saponins extracted from CLM (SCLM) in rats subjected to unpredictable chronic mild stress (UCMS). The ameliorative effect of SCLM on symptom of depression through behavior tests including: sucrose preference test, open-field test and forced-swimming test was investigated.
View Article and Find Full Text PDFIn this study, we investigated the neuroprotective effects of asiaticoside, a triterpenoid saponin isolated from the Chinese medicinal herb Centella asiatica, in the rats model of Parkinsonism induced by 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP). Rats were first injected with MPTP. One day after surgery, asiaticoside was administered and the behavioral tests were assessed.
View Article and Find Full Text PDFSET and MYND domain-containing protein 3 (SMYD3) is a histone methyltransferase that plays an important role in transcriptional regulation in human carcinogenesis. It can specifically methylate histone H3 at lysine 4 and activate the transcription of a set of downstream genes, including several oncogenes (e.g.
View Article and Find Full Text PDFAim Of The Study: Traditional Chinese medicine Zhen-Wu-Tang (ZWT) is a well-known PentaHerbs formula from "Treatise on Febrile Disease". This study is to elucidate its neuroprotective effect and mechanism of ameliorative effect of the syndrome of Parkinson's disease (PD).
Materials And Methods: The ameliorative effect of ZWT on symptom of PD through behavior tests including: swimming test, the tail suspension test and open-field test was investigated.
Weakly agglomerated nanocrystalline scandia doped tin oxide powders with high surface area (170-220 m(2)/g) and uniform size (3-4 nm) were synthesized for the first time by a two-step hydrothermal process in the presence of urea, followed by the calcination between 500 and 1200 degrees C. The structure and texture of the binary oxide system were characterized by thermogravimetry and differential thermal analysis, Brunauer-Emmett-Teller-specific surface area analysis, transmission electron microscopy, X-ray diffraction, Raman spectroscopy, and X-ray photoelectron spectroscopy. A metastable scandium tin oxide solid solution in tetragonal structure was formed for the scandia content lower than 6 mol % as the samples were calcined at 800 degrees C, and the excess Sc atoms were dispersed at the surface of the crystallites above this limit.
View Article and Find Full Text PDF