ABSTRACT
Tuberculosis is a serious zoonotic disease causing approximately 10 million new cases worldwide every year.The emergence of various drug-resistant strains of Mycobacterium tuberculosis is currently an important challenge intuberculosispre-vention and control,and an urgent need exists to develop new anti-tuberculosis drugs to treat drug-resistant tuberculosis and shorten the treatment time.The discovery of drug targets is a bottleneck inthe development of new anti-tuberculosis drugs.At present,the widely reported drug targets for tuberculosis include primarily new targets related to the biosynthesis of Mycobac-terium tuberculosis components and immune metabolic pathways.In addition,host-directed therapiestargeting the host immune system have become a research hotspot in recent years.Adjuvant host-directed therapies can enhance the therapeutic effect of tuberculosis and shorten treatment times by affecting granuloma formation,autophagy,host immune metabolism and the intra-cellular killing mechanism,as well as regulating pulmonary inflammation.The discovery of these new targets provides new ide-as for the future development of safe and effective new anti-tuberculosis drugs.
ABSTRACT
Three new prenylated stilbenes, named as cajanusins A-C (1-3), and one new natural product cajanusin D (4), along with six known derivatives (5-10) were isolated from the leaves of Cajanus cajan. Their structures were fully elucidated by means of extensive spectroscopic methods and comparison with data in the reported literatures. The new compounds of 1 and 2 were evaluated for in vitro cytotoxic activities against a panel of human cancer cell lines.
ABSTRACT
Objective To investigate the effect of Wulong Xiaozheng Pill (WXP) on the migration and invasion of human gastric cancer cell-line BGC-823 and its mechanism. Methods WXP, IGF-1, and LY294002 were added on BGC-823 cells. Then the inhibitory effect of WXP was detected by MTT assay. Transwell assay was performed to determine the migration and invasion capacity of on BGC-823 cells. Expressions of VEGF, MMP-2, and MMP-9 were detected by ELISA, while the expressions of related proteins and mRNA in PI3K/NF-κB signaling pathway were detected by Western blotting and RT-PCR. Results WXP can inhibit the proliferation, adhesion, invasion, and migration of BGC-823 cells. In addition, WXP inhibited the expression of VEGF, MMP-2 and MMP-9 protein in BGC-823 cells. WXP significantly inhibited the expression of p-PI3K, p-Akt, p-IKK-a, and p-NF-κB p65Ser 276 proteins, PI3K, Akt, IKKa, and NF-κB mRNA, which showed a time-dependent and dose-dependent manner. Conclusion WXP inhibit the capacity, migration and invasion of BGC-823 cells by blocking PI3K/NF-κB signaling pathway.
ABSTRACT
Two new naphthalenone compounds were isolated from green walnut husks of Juglans mandshurica and their structures were identified as 4-butoxybutoxy-5,8-dihydroxy-3,4-dihydro-2H-naphthalen-1-one (1), 4-ethoxyethoxy-5,8-dihydroxy-3,4-dihydro-2H-naphthalen-1-one (2). Compounds 1 and 2 were named as Juglanstetralone A (1) and Juglanstetralone B (2). Compound 1 showed more significant anti-tumor activity than 2 against gastric cancer BGC-823 cells, wih the IC50 of 125.89 (g(mL(-1).