1.The function and drug development progress of free fatty acid receptor 1 in chronic inflammatory diseases
Xue-feng GAO ; Cun-yu FENG ; Ya-xin FU ; Lei-lei CHEN ; Shuai-nan LIU ; Yi HUAN
Acta Pharmaceutica Sinica 2023;58(6):1505-1514
As a member of G protein coupled-receptors superfamily, free fatty acid receptor 1 (FFAR1), is also known as GPR40, has been shown to regulate numerous pathophysiological processes in a variety of tissues and organs. The activated FFAR1 has a variety of biological functions. For instance, it can not only regulate metabolism of fatty acids and glucose, but also play an important role in immune inflammatory response, it may be a potential drug target for the treatment of various chronic inflammatory diseases. In this review, we focus on the recent researches of FFAR1's action in the regulation of pathophysiological processes, its molecular mechanism and new agonists development. At the same time, this review will take the discovery of series FFAR1 agonists as examples, and display the applied prospects of FFAR1.
2.Interpretation of Intelligence Attribute of Supramolecular "Qi Chromatography" Theory of Traditional Chinese Medicine and Its Combined Application with Artificial Intelligence
Hai-ying LI ; Kai-wen DENG ; Xue PAN ; Ding-fang CHEN ; Yue-feng WU ; Min-cun WANG ; Yan-zi ZHOU ; Yan-tao YANG ; Fu-yuan HE
Chinese Journal of Experimental Traditional Medical Formulae 2022;28(5):227-233
In the era of artificial intelligence based on big data, data acquisition, storage and processing are more convenient, which provides a guarantee for accelerating the development of traditional Chinese medicine (TCM), but it has not yet achieved organic integration with TCM theory. Based on preliminary research on the supramolecular "Qi chromatography" theory of TCM, combined with the current development trend of artificial intelligence, this paper analyzed the biological intelligence attribute of the function of TCM supramolecular "imprinting template", in order to provide reference for the development of TCM drug innovation. Both the human body and Chinese materia medica are giant complex supramolecular bodies evolved from natural organisms. According to the "imprinting template", the "social molecules" are controlled step by step to form the meridians and viscera. The interaction produces the original theory of TCM, in which the self-recognition, self-assembly, self-organization and self-replication of the "imprinting template" reflect the "intelligence" function attributes:the human body uses the "imprinting template" to self-identify and sense the ingredients of TCM, and store the memory information database in the meridian and collateral organs in the form of "imprinting template", and then pass the "imprinting template". The comparison, analysis, and judgment of imprinting templates guide the self-assembly, self-organization and self-replication among "molecular society", synthesize biological machines, produce biological functions, repair or strengthen biological supramolecular bodies, and present the most basic "intelligence" attribute. This suggests that the theory of theory-method-prescription-medicine of TCM is the weak embodiment of biological "intelligence", while the human brain function is the strong embodiment of biological "intelligence". Since the intelligent function of supramolecular "imprinting template" runs through the natural world, artificial intelligence that can characterize the strong "intelligence" form of the human brain will also be integrated into all aspects of the natural world, suggesting the development direction of "intelligence" functionalization of drug innovation mode.
3.A novel robust nomogram based on peripheral monocyte counts for predicting lymph node metastasis of prostate cancer.
Jia-Wei ZHOU ; Yun-Hua MAO ; Yang LIU ; Hai-Tao LIANG ; Chandni Chandur SAMTANI ; Yue-Wu FU ; Yun-Lin YE ; Gang XIAO ; Zi-Ke QIN ; Cun-Dong LIU ; Jian-Kun YANG ; Qi-Zhao ZHOU ; Wen-Bin GUO ; Kang-Yi XUE ; Shan-Chao ZHAO ; Ming-Kun CHEN
Asian Journal of Andrology 2021;23(4):409-414
Accurate methods for identifying pelvic lymph node metastasis (LNM) of prostate cancer (PCa) prior to surgery are still lacking. We aimed to investigate the predictive value of peripheral monocyte count (PMC) for LNM of PCa in this study. Two hundred and ninety-eight patients from three centers were divided into a training set (n = 125) and a validation set (n = 173). In the training set, the independent predictors of LNM were analyzed using univariate and multivariate logistic regression analyses, and the optimal cutoff value was calculated by the receiver operating characteristic (ROC) curve. The sensitivity and specificity of the optimal cutoff were authenticated in the validation cohort. Finally, a nomogram based on the PMC was constructed for predicting LNM. Multivariate analyses of the training cohort demonstrated that clinical T stage, preoperative Gleason score, and PMC were independent risk factors for LNM. The subsequent ROC analysis showed that the optimal cutoff value of PMC for diagnosing LNM was 0.405 × 109 l
5.Quantitative Integration and Verification of Components and Target Clusters of Traditional Chinese Medicine Based on Supramolecular Qi Chromatography Theory
Hai-ying LI ; Xue PAN ; Min-cun WANG ; Yan-zi ZHOU ; Ding-fang CHEN ; Yue-feng WU ; Yi-qun ZHOU ; Fu-yuan HE
Chinese Journal of Experimental Traditional Medical Formulae 2021;27(21):207-213
The application of modern scientific theories and technologies to explore the mechanism of Chinese medicine and its compounds is one of the key issues in realizing the modernization of traditional Chinese medicine (TCM) research. Chinese medicine and its compounds produce comprehensive pharmacodynamics through multiple components acting on multiple targets, the core of clarifying the mechanism is to solve the key scientific problems of static correlation and dynamic integration verification between the components and the target network topology. At present, the effective method to clarify the mechanism of Chinese medicine and its compounds is to statically correlate the topological network of
6.Construction of Evaluating Method and Experimental Research for Targeting of Traditional Chinese Medicine Preparations Based on Supramolecular Qi Chromatography Theory
Min-cun WANG ; Chao HU ; Yu-ting HE ; Yan-zi ZHOU ; You-zhi LIU ; Qi-meng FAN ; Ding-fang CHEN ; Hai-ying LI ; Xue PAN ; Yi-qun ZHOU ; Fu-yuan HE
Chinese Journal of Experimental Traditional Medical Formulae 2021;27(20):113-120
Objective:To construct the targeting evaluation method of traditional Chinese medicine (TCM) preparations based on supramolecular Qi chromatography theory, and to study the liver targeting effect of Bupleuri Radix on Pien Tze Huang. Method:The molecular connectivity index (MCI) was used to analyze the characteristics of imprinted template and liver targeting tendency of TCM mainly attributed to liver meridian and components of Pien Tze Huang, and combined with target dynamics and total statistical moment principle, aimed at the independent action characteristics of multi-component imprinted template of TCM, a method for evaluating the targeting of TCM preparations was established. Hepatoma rats in Pien Tze Huang group, Bupleuri Radix
7.Analysis of quality difference based on Astragalus membranaceus var. mongholicus in genuine region.
Chen-Guang ZHAO ; Cun-Yu LI ; Shan YANG ; Qi-Long XU ; Yun-Feng ZHENG ; Yu-Fu WANG ; Hong-Yang LI ; Guo-Ping PENG
China Journal of Chinese Materia Medica 2020;45(13):3183-3190
This work is to establish the fingerprint of Astragalus membranaceus var. mongholicus by HPLC-ELSD method, and to analyze the simulated wildness degree of A. membranaceus var. mongholicus in the genuine region of Inner Mongolia, Ningxia and Gansu. Compared with wild A. membranaceus var. mongholicus, the quality differences of A. membranaceus var. mongholicus in the genuine region were analyzed by identification of chromatographic peaks and similarity evaluation, cluster analysis(CA), principal components analysis(PCA) and orthogonal partial least squares discriminant analysis(OPLS-DA). HPLC fingerprints of A. membranaceus var. mongholicus in different genuine regions are established. The qualitative analysis of mass spectrometry identified 18 components. The similarity evaluation shows that the similarity of 32 batches of A. membranaceus var. mongholicus samples was 0.688-0.993. Among them, the similarity of samples in Shanxi, Inner Mongolia, Ningxia is 0.688-0.993, 0.835-0.989, 0.934-0.988, respectively and the similarity of samples in Gansu is 0.729-0.876 except No. 25 sample. The results of CA show that the samples of A. membranaceus var. mongholicus can be grouped into four categories according to the production area except the No. 11 and No. 25 samples. The results of PCA indicate that 32 batches of A. membranaceus var. mongholicus samples can be clustered according to quality and origin, and the quality of A. membranaceus var. mongholicus in Inner Mongolia is the closest to the wild breed. The results of OPLS-DA indicate that there are six components that can distinguish the wild and domestic A. membranaceus var. mongholicus, which are malonylastragaloside Ⅰ, astragaloside Ⅰ, calycosin-7-O-β-D-glycoside-6″-O-malonate, calycosin-7-O-β-D-glycoside, formononetin-7-O-β-D-glycoside-6″-O-malonate, and astrapterocarpan-3-O-β-D-glycoside-6″-O-malonate. The established method can be used to analyze differences between A. membranaceus var. mongholicus origin and planting environment, and can provide references for the protection and replacement of wild A. membranaceus var. mongholicus resources, and the cultivation, processing and production of A. membranaceus var. mongholicus.
Astragalus propinquus
;
China
8.Diversity and difference of endophytes in Dendrobium huoshanense with different growth years.
Shao-Tong CHEN ; Jun DAI ; Xue-Ping JIANG ; Xiang-Wen SONG ; Cun-Wu CHEN ; Nai-Fu CHEN ; Lan-Ping GUO ; Bang-Xing HAN
China Journal of Chinese Materia Medica 2019;44(6):1145-1150
In order to explore endophytes diversity and difference in Dendrobium huoshanense,in this paper,the metagenomics method was used to analyze the endophytic bacteria and fungi community of 5 groups include 30 samples in different growth years. The results indicate that 3 540 bacterial OTUs were identified from D. huoshanense,and there are 138 OTUs in 5 groups simultaneously;2 168 fungal OTUs were identified,and 143 OTUs exist in 5 groups simultaneously. The dominate endophytic bacteria community are Sphingomonas sp.,Acinetobacter sp.,Burkholderia sp.,Methylobacterium sp.,Enterococcus sp.,Bacillus sp.,the difference endophytic bacteria community are Oceanobacillusd sp.,Actinomycetospora sp.,Paenibacillus sp.. The dominate endophytic fungi community are Zasmidium sp.,Zymoseptoria sp.,Alternaria sp.,Cladosporium sp.,Fusarium sp.,the difference endophytic fungi community are Cyphellophore sp.,Fusarium sp.. The results of clustering revealed that both the endophytic bacteria and the endophytic fungi,ⅢY2 and ⅢY3 are complete clustered,and ⅡY1 and ⅢY1 are also cluster completely. These enriched the species and resources of endophytic bacteria and fungi in D. huoshanense,and provided a theoretical reference for the reasonable harvest of D. huoshanense.
Ascomycota
;
Bacteria
;
Dendrobium
;
Endophytes
;
Fungi
;
Fusarium
;
Phylogeny
9.A real-time fluorescence quantitative PCR method for source identification of Crocus sativus and Carthamus tinctorius.
Quan-Fang ZHANG ; Yan-Yan LIU ; Qing-Qing TAN ; Xin-Xin JIANG ; Xue-Yan CHEN ; Fu-Cun GE ; Xun BU ; Yong-Qing ZHANG
China Journal of Chinese Materia Medica 2018;43(23):4575-4581
The specific PCR primer was designed base on ITS2 sequence in GenBank, and we developed a SYBRGreen real-time fluorescence quantitative PCR system for identification of Crocus sativus and Carthamus tinctorius source. Compared with Chinese herbal medicine DNA barcode technique, this method showed characteristics of shorter time, higher specificity and sensitivity. Using this method to detect 15 samples, 4 were C. sativus, 8 were C. tinctorius, and the other 3 samples were none of them. The result was in accordance with Chinese herbal medicine DNA barcode. This study lays the foundation for identification of related Chinese medical materials.
Carthamus tinctorius
;
Crocus
;
Real-Time Polymerase Chain Reaction
10.Analysis of influencing factors of secondary metabolites contents in cultivated Polygala tenuifolia.
Ya-Jie PU ; Dan-Dan WANG ; Yan YAN ; Hong-Ling TIAN ; Bing PENG ; Xue-Mei QIN ; Cun-Gen MA ; Chen-Hui DU ; Ben-Xiang HU ; Fu-Sheng ZHANG
China Journal of Chinese Materia Medica 2017;42(16):3167-3177
This work was launched to explore the effect of habitat and growth year on the secondary metabolites contents of cultivated Polygala tenuifolia. The samples of cultivated P. tenuifolia were analyzed by ultra-high performance liquid chromatography(UPLC)-quadrupole time-of-flight mass spectrometry(Q-TOF MS), and the obtained data were analyzed using multiple statistical analysis and cluster analysis. The results showed that compared with growth year, habitat is a main influencing factor which affected the secondary metabolites contents of P. tenuifolia. The contents of sucrose esters and oligosacchride multi-esters are greatly dependent on the habitat (the sample-AG with high levels of components of tenuifoliside B and tenuifoliside C, and the sample-FY with high levels of 3,6'-disinapoyl sucrose, tenuifoliose S, tenuifoliose L, and tenuifoliose V). There is no obvious effect of habitat and growth year on xanthone. The contents of triterpene saponins are greatly dependent on the growth year, and the content of parts of triterpene saponins increased as time goes on.The result indicated that the effect of habitat and growth year on different types of secondary metabolites is not completely equivalent. This study will contribute to the breeding of P. tenuifolia and amendment of current commodity criteria.

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