ABSTRACT
As an important pectin enzyme, pectin methylesterase (PME) can hydrolyze methyl esters, release methanol and reduce esterification. It is essential in regulating pollen tube development, root extension, and fruit ripening. Pectin methylesterase inhibitors (PMEI) can specifically bind PME and inhibit its activity, which jointly determines the esterification degree of pectin. PMEI has important application prospects in plant pest control, fruits and vegetable processing fields. In this paper, the gene families, crystal structures, molecular recognition, and applications in plants and industry are reviewed for the PME and PMEI systems. Finally, the semi-rational design of PMEI is discussed and discussed prospected.
Subject(s)
Carboxylic Ester Hydrolases , Pectins , Carboxylic Ester Hydrolases/genetics , Carboxylic Ester Hydrolases/metabolism , Pectins/chemistry , Pectins/metabolism , Plants/metabolism , Enzyme Inhibitors/chemistryABSTRACT
BACKGROUND: Radix Salviae Miltiorrhizae (RSM), a well-known traditional Chinese medicine, has been shown to inhibit tumorigenesis in various human cancers. However, the anticancer effects of RSM on human hepatocellular carcinoma (HCC) and the underlying mechanisms of action remain to be fully elucidated. METHODS: In this study, we aimed to elucidate the underlying molecular mechanisms of RSM in the treatment of HCC using a network pharmacology approach. In vivo and in vitro experiments were also performed to validate the therapeutic effects of RSM on HCC. RESULTS: In total, 62 active compounds from RSM and 72 HCC-related targets were identified through network pharmacological analysis. RSM was found to play a critical role in HCC via multiple targets and pathways, especially the EGFR and PI3K/AKT signaling pathways. In addition, RSM was found to suppress HCC cell proliferation, and impair cancer cell migration and invasion in vitro. Flow cytometry analysis revealed that RSM induced cell cycle G2/M arrest and apoptosis, and western blot analysis showed that RSM up-regulated the expression of BAX and down-regulated the expression of Bcl-2 in MHCC97-H and HepG2 cells. Furthermore, RSM administration down-regulated the expression of EGFR, PI3K, and p-AKT proteins, whereas the total AKT level was not altered. Finally, the results of our in vivo experiments confirmed the therapeutic effects of RSM on HCC in nude mice. CONCLUSIONS: We provide an integrative network pharmacology approach, in combination with in vitro and in vivo experiments, to illustrate the underlying therapeutic mechanisms of RSM action on HCC.
ABSTRACT
This study is to establish an HPLC fingerprint by HPLC-DAD method and simultaneous quantitative analysis of 17 components of 18 batches of Citrus aurantium and 10 batches of C. sinensis. The separation was performed on an Agilent Poroshell 120 SB-C₁₈ (4.6 mm×100 mm,2.7 μm) column with the gradient elution of methanol-0.1% formic acid water, the flow was 0.6 mL•min⁻¹. The detection wavelength was set at 318 nm. The column temperature was maintained at 30 ℃. The data calculation was performed with similarity evaluation system for chromatographic fingerprint of traditional Chinese medicine (Version 2004A) together with SIMCA-P 13.0 software to clarify the differential marker between these two different species of Aurantii Fructus Immaturus. This method has good precision stability and repeatability that could provide basis for quality control and evaluation of Aurantii Fructus Immaturus.
ABSTRACT
OBJECTIVE: To investigate the effects of Yinchen Shufu Decoction on hepatocyte apoptosis and the expression of its apoptosis-regulating gene Bcl-2 and Bax in Yin-jaundice rats. METHODS: Forty-eight rats were divided randomly into 4 groups: the normal control group, Yin-jaundice model group, Yang-jaundice model group, Yinchen Shufu Decoction treatment group. The TUNEL assay and the immunohistochemistry assay were used to detect the apoptosis of hepatocytes and the expression of Bcl-2 and Bax in hepatocytes respectively. RESULTS: The rate of apoptosis cells in Yin-jaundice model group was higher significantly than that in Yang-jaundice model group and normal control group (P<0.01), the expression of Bcl-2 in Yinchen Shufu Decoction treatment group was higher significantly than that in Yin-jaundice model group (P<0.01 or P<0.05), and the expression of Bax in it was lower significantly than that in Ying-jaundice model group (P<0.01 or P<0.05). CONCLUSION: Yinchen Shufu Decoction can prevent hepatocyte apoptosis perhaps by up-regulating the expression of Bcl-2 and down-regulating the expression of Bax. It is one of the mechanisms of its treatment on Yin-jaundice.