1.Study on the idiosyncrasy oforganic chemistry textbook for traditional Chinese medicine organic chemistry
Chinese Journal of Medical Education Research 2005;0(06):-
The Organic Chemistry textbook for traditional Chinese medicine should be connected with this speciality and possese its own characteristic. First,the content in textbook should be chosen according to this specility,so that some outlying teaching content irrelevant to the speciality can be deleted but some correlated content be added to the textbook. Secondly,a lot of examples from traditional Chinese medicine should be inserted in the textbook,especially at "Classification and nomenclature","Important compounds"and"Exercise".
2.Identify Polysaccharide in Holothuria atra Jeager by Spectroscopy
Xican LI ; Shaohui DU ; Ling HUANG ; Dongfeng CHEN
China Pharmacy 2005;0(13):-
OBJECTIVE:To establish the method to identify the polysaccharide element in Holothuria atra Jeager by spectroscopy.METHODS:The purity of polysaccharide in Holothuria atra Jeager was determined by electrophoretic method;the infrared absorption spectrum,ultraviolet absorption spectrum,carbon spectra and hydrogen spectra of NMR were identified in structure by infrared spectrophotometry,ultraviolet spectrophotometry and NMR spectrometry respectively.RESULTS:The gel band after electrophoresis took blue color and the results of spectrum determination accountable for each other.CONCLUSION:Uniformly constituent of polysaccharose was found in the Holothuria atra Jeager,which was an acidic polysaccharose with vitriolic esterfunction,without glucopeptide;?-configuration,?-glucopyranose was found and the intramolecular hydrogen bond was formed by hydroxide radical.
3.Improvement in Soxhlet Extraction with Ore and Shell Hard Chinese Materia Medica
Xican LI ; Kunwang HUANG ; Bingyi LAI ; Wenming LAI
China Pharmacy 2007;0(30):-
OBJECTIVE:To discuss the improvement in Soxhlet extraction with ore and shell hard Chinese meteria madica taking Plastrum Testudinis as example.METHODS:On the basis of normal Soxhlet extracter,larger Soxhlet extracter on Plastrum Testudinis was experimented using saturated salt-water-bath,quadruplicity cover circle and timer.Large Soxhlet extracter was compared with normal Soxhlet extracter and stirring-reflux method by HPLC analysis,yield and clearance rate of DPPH.RESULTS:There were no significant difference between normal and larger Soxhlet extracters,but the stirring-reflux method was inferior to these two methods.CONCLUSION:The improved larger Soxhlet extraction is a thorough,high-efficient,convenient,economical and healthy extracting method for ore and shell hard Chinese materia medica.
4.Feature Extraction and Image Recognition of Achyranthes bidentata and Cyathula officinalis
Nai WANG ; Wenbiao LU ; Xiuhua LING ; Lijin LIANG ; Xican LI ; Rui LI
China Pharmacy 2017;28(12):1670-1673
OBJECTIVE:To extract the feature of Achyranthes bidentata and Cyathula officinalis,and to establish image recog-nition method. METHODS:The microscopic image stitching of A. bidentata and C. officinalis was implemented by MATLAB. The color,invariant moment,stripes and the features of vascular bundle in cross section were extracted. The data was organized into da-ta matrix,and then data matrix was standardized by Zscore function;principal components were analyzed through Princomp func-tion. BP nerve network recognition mode was adopted. RESULTS:The microstructures in the micro images of the samples were kept integrated. The measured data of 27 characteristics were acquired in each group of sample. Through principal component analy-sis,the parameters of 11 main components were selected to establish BP never network. The average recognition rate of BP nerve network was 100% between 2 medicinal material relatives (n=50). CONCLUSIONS:The method can be used for micro-image auto Stitching of Chinese medicinal materials and image recognition of A. bidentata and C. officinalis.
5.Free Radical Scavenging Action of Volatile Oil from Piper longum L.and Its Relationship with Molecular Structure
Xican LI ; Xiaojun ZHAO ; Xueming XIE ; Yuansheng ZHONG ; Chunhua HUANG ; Dongfeng CHEN
Traditional Chinese Drug Research & Clinical Pharmacology 1993;0(03):-
Objective To observe the free radical scavenging action of volatile oil from Piper longum L.growing in Hainan Province and to explore the relationship of the action with molecular structure.Methods 1,1-Diphenyl-2-picrylhydrazyl radical(DPPH) method was used to determine the scavenging action.The components of volatile oil were analyzed by GC-MS,and their molecular structures were identified by databank.Results(1)The volatile oil from Piper longum L.had scavenging actions on free radicals in a concentration-dependent manner.(2)Forty one compounds were found in volatile oil from Piper longum L.growing in Hainan Province,in which the amount of carbon-carbon double bond(C=C) was in predomination.Conclusion Carbon-carbon double bond(C=C)is the essential functional group for free radical scavenging action of volatile oil from Piper longum L.
6.Discovery and identification of EIF2AK2 as a direct key target of berberine for anti-inflammatory effects.
Wei WEI ; Qingxuan ZENG ; Yan WANG ; Xixi GUO ; Tianyun FAN ; Yinghong LI ; Hongbin DENG ; Liping ZHAO ; Xintong ZHANG ; Yonghua LIU ; Yulong SHI ; Jingyang ZHU ; Xican MA ; Yanxiang WANG ; Jiandong JIANG ; Danqing SONG
Acta Pharmaceutica Sinica B 2023;13(5):2138-2151
Using chemoproteomic techniques, we first identified EIF2AK2, eEF1A1, PRDX3 and VPS4B as direct targets of berberine (BBR) for its synergistically anti-inflammatory effects. Of them, BBR has the strongest affinity with EIF2AK2 via two ionic bonds, and regulates several key inflammatory pathways through EIF2AK2, indicating the dominant role of EIF2AK2. Also, BBR could subtly inhibit the dimerization of EIF2AK2, rather than its enzyme activity, to selectively modulate its downstream pathways including JNK, NF-κB, AKT and NLRP3, with an advantage of good safety profile. In EIF2AK2 gene knockdown mice, the inhibitory IL-1β, IL-6, IL-18 and TNF-α secretion of BBR was obviously attenuated, confirming an EIF2AK2-dependent anti-inflammatory efficacy. The results highlight the BBR's network mechanism on anti-inflammatory effects in which EIF2AK2 is a key target, and inhibition of EIF2AK2 dimerization has a potential to be a therapeutic strategy against inflammation-related disorders.
7.Evolution and development of potent monobactam sulfonate candidate IMBZ18g as a dual inhibitor against MDR Gram-negative bacteria producing ESBLs.
Zhiwen LI ; Zhihao GUO ; Xi LU ; Xican MA ; Xiukun WANG ; Rui ZHANG ; Xinxin HU ; Yanxiang WANG ; Jing PANG ; Tianyun FAN ; Yonghua LIU ; Sheng TANG ; Haigen FU ; Jingpu ZHANG ; Yinghong LI ; Xuefu YOU ; Danqing SONG
Acta Pharmaceutica Sinica B 2023;13(7):3067-3079
A series of new monobactam sulfonates is continuously synthesized and evaluated for their antimicrobial efficacies against Gram-negative bacteria. Compound 33a (IMBZ18G) is highly effective in vitro and in vivo against clinically intractable multi-drug-resistant (MDR) Gram-negative strains, with a highly druglike nature. The checkerboard assay reveals its significant synergistic effect with β-lactamase inhibitor avibactam, and the MIC values against MDR enterobacteria were reduced up to 4-512 folds. X-ray co-crystal and chemoproteomic assays indicate that the anti-MDR bacteria effect of 33a results from the dual inhibition of the common PBP3 and some class A and C β-lactamases. Accordingly, preclinical studies of 33a alone and 33a‒avibactam combination as potential innovative candidates are actively going on, in the treatment of β-lactamase-producing MDR Gram-negative bacterial infections.