Table of Content

15 December 1992, Volume 1 Issue 2

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Full Papers

Application of 2D-NMR Techniques in the Structure Determination of Hypodematine

Ya-Min Chen, Ying-Hua Lu, Yan-Jun Chen, Cun-Sheng Ma, De-Quan Yu

1992, 1(2):  1-6. 

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A novel alkaloid, named hypodematine, was isolated from the whole plant of a fern.Htpodematium sinemse lwatsuki.Its structure has been elucidated to have a novel skeleton of benzo-azacyclooctatetraene with a phenyl substituent by means of ¹H-¹H COSY. ¹H-¹³C COSY.and long-range ¹H-¹³C COSY spectroscopy.

Studies on the Chemical Constituents of Melia azedarach

Ren-Sheng Xu, Wen-Han Lin^*, Jiu Han, Wen-Lu Wang, Shan-Huan Zhao^**

1992, 1(2):  7-11. 

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A new compound named melianoninol I, along with five known cornpounds melianol II, melianone III, meliandiol IV, vanillin V and vanillic acid VI was isolated from the fruits of Melia azedarach L.. Their structures were elucidated by IR, MS, ¹H NMR, ¹³C NMR, and other spectral evidence. Compounds II, III, IV possess different insecticidal effects. and I exhibits a certain antifeeding property against the cabbage worm. Pieris rapae L..

16-Hydroxytriptolide: An Active Compound from Tripterygium wilfordii

Peng-Cheng Ma, Xie-Yu Lu, Jing-Jing Yang, Qi-Tai Zheng

1992, 1(2):  12-18. 

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From the dried roots and leaves of Tripterygium wilfordii 1.2, a new diterpenoid triepoxide, 16-hydroxytriptolide was isolated, and its structure and stereochemistry elucidated as 16-S-hydroxy-triptolide on the basis of spectral data IR, MS, UV, ¹H NMR, ¹³C NMR, ²D NMR, Selective Long-range DEPT and x-ray crystallographic analysis. This compound showed definite antiinflammatory action, strong immunosuppressive and antifertile activities. In addition, a known compound, triptolide was also isolated and all the spectral signals of ¹H NMR and ¹³C NMR were assigned.

Study of the Relationship Between the Chemical Structure and the Anticonvulsant Activity of the 3-Pyrazolidinones

Zhe-Shan Quan, Xiao-Ping Lei, Ren-Li Li

1992, 1(2):  19-26. 

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The Hansch approach was used in the quantitative structure anticonvulsant activity studies of the previously synthesized 1-substituted-and 1.5-disubstituted-3-pyrazo-lidinones. Correlation analysis predicted that 1.5-disubstituted-3-pyrazoljdinones in which 1- substituent is n-propyl but not benzyl, with the total hydrophobic constant of 1-and 5-substituents (∑л) equals to 4.5 (optimum value) will have the most potent activity. On the basis of this analysis eleven 5-substituted and I-n-butyl-5-substituted-3-pyrazolidinones were synthesized. Pharmacological tests indicated that the prediction of the Hansch analysis of the 3-pyrazolidinones is correct. The Hansch analysis, by including these 11 compounds, gives an almost identical correlation with that previously obtained.

Studies on the Synthesis, Anticonvulsant Activity, and the Structure-Activity Relationships of Phenyl Pyridazinones and their GABA Derivatives

Ping Xu, Shu-Yu Wang, Wei-Qin Liu

1992, 1(2):  27-34. 

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In searching for effective anticonvulsant agents, fourteen 6-aryl-4.5-dihydro-3(2H) pyridazinones. Fifteen 6-aryl-3(2H) pyridazinones, and seventeen 3-GABA derivatives of 6-aryIpyridazines have been synthesized, and evaluated in mice for the ability to antagonize maximal electroshock seizure (MES). The ED50 values showed that 6-(2',4'-dichlorophenyt)-3(2H) pyridazinone was the most potent anticonvulsant among these corn- pounds (ED50 = 10.15 mg/kg). The structure-activity relationships of the aryl pyridazinones were studied. The result showed that: (1)the higher the value of the hydrophobic parameter л of the substituent on the phenyl ring. The more potent the anticonvulsant activity of the cornpound. And (2) only the compounds with an electron withdrawing substituent on the phenyl ring exhibited appreciable anticonvulsant activity.

Structure-activity Relationships of Vasorelaxing Effect of Polyarginine Oligopeptides

Ming-Di Gu, Shi-Qi Peng^*, Xue-Qing Guo, Xiu-Rong Jiang, Meng-Shen Cai, Shu-Yun Dong, Li Zhang, Yue Zhang, Chao-Shu Tang

1992, 1(2):  35-41. 

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Based on the EDRF(endothelium derived relaxing factor)-like effects for polyarginine Arg-Arg-OH was selected as the lead compound and its derivatives Arg-Arg-OCH3. Arg Arg-Arg-OH, HO-ArgCOCH2CH2COArg-OH, HO-ArgCOCH2COArg-OH, were synthesized. These substances showed on bioassay various degrees of vasorelaxant activities. With protection for the C-terminal of Arg-Arg-OH with a methyl ester. The vasorelaxing activitv was decreased. In contrast.when the N-terminal of Arg-OH was protected with malonic acid or butane diacid. The biological activites were lower than those of Arg-Arg-OH due to the lowered metabolic rate. With protection of N-terminal of Arg-Arg-OH with L-Arg residue.Arg-Arg-Arg-OH was obtained, which showed a vasorelaxing activity better than that of Arg-Arg-OH. The bioactivities observed on the Wister's rats for the former com- pound become the experimental basis for prodrug design of EDRF.

A Preliminary Study of Rotundine-Polyion Complex Release System

Shi-Shen Xie, Xiang-Jun Liu, Yu-Xin Zhang, Jin-Lin Zhang, De-Yun Zhang, Yan-Lin Wang, Dun Li, Dan Ni

1992, 1(2):  42-48. 

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A rotundine-polyion complex (PIC) release system was prepared first by granulation of rotundine containing chitosan acetate solution and then by complexing with carboxymethyl glucomannan (CMGM) solution on the granular surface. The granules have an average diameter of 1.38~1.53 mm and the drug content reaches 62.89%. The external release tests showed T50 to be 45 min and the total release time 4 h in an artificial gastric juice, while no more than 60% of the drug was released in the same period of time in an artificial intestinal fluid. The various factors affecting the external release were examined.

Effects of Tremella Polysaccharide on Immune Function of Physically-Stressed Mice

Jin-Ying Cui, Zhi-Bin Lin

1992, 1(2):  49-53. 

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An immunosuppressive animal model induced by physical stress that forced mice to swim in cold water (14±1 ºC) and the restorative effect of Tremella polysac charide (TP) on the suppressed immune function by stress were studied in mice. It was found that the spleen plaque forming cell (PFC) response to sheep red blood cells, delayed cutaneous hypersensitivity (DCH) induced by dinitrochlorobenzene and the lymphocyte proliferation stimulated by concanavalin A (Con A) were significantly decreased in stressed mice. In addition. The maximal decrease of PFC was reached in 9-12 days after stress. A-drenolectomy could not affect the decrease of PFC in stressed mice. TP(200, 400 mg/kg) ig for 8-14 days significantly restored the PFC.DCH and lymphocyte proliferation to nor- mal level in stressed mice.

Effects of MK-801 and Schizandrol A on DA/DOPAC Measured by Voltammetry in Ischemic Rat Striatum

Jian-Jun Zhang, Xin-Yi Niu

1992, 1(2):  54-58. 

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The time course of changes in the levels of extracellular DA/DOPAC in rat striatum during brain ischemia and reperfusion was measured by the method of in vivo differential normal pulse voltammetry (DNPV). Acute cerebral ischemia of rats was produced by four-vessel occlusion. The effects of (+)-MK-801 and schizandrol A on the change of DA/DOPAC were investigated. The results showed that the DA/DOPAC peak in- creased markedly during 6 min of ischemia and, after reperfusion, the peak height decreased gradually. Both (+)-MK-801 and schizandrol A significantly inhibited the DA release after ischemia in the striatum.

SOD-like Activities of Fifteen Constituents from Rhubarb

Lu-Wen Shi, Chun-Su Lu, Jun-Hua Zheng, Zhi-Cen Lou

1992, 1(2):  59-64. 

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It is important to search for the ingredients with SOD-like activity present in Chinese traditional drugs. Four classes of constituents including fifteen compounds isolated from Chinese rhubarb were studied for their SOD-like activity by determining the percentage of scavenging effect of the superoxide radical anion (O2^-·), (S%), The results showed that the SOD-like activities of four tanninoid compounds were stronger among which (-)-epi- catechin has the strongest SOD-like activity at lower concentrations: the activity of five stilbene compounds is weaker:while chrysophanol-8-glucoside and desoxyrhaponticin have no SOD-like activity and, on the contrary.may promote the production of O2^-·.

Classification of Chinese Traditional Drug-"Beimu" (Bulbus Fritillariae) by Pyrolysis High Resolution Gas Chromatography-Pattern Recognition

Xing-Chun Fang, Ping Li, Lin Tian, Deng-Kui An^*

1992, 1(2):  65-72. 

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The combination of pyrolysis high resolution gas chromatography and pat- tern recognition techniques is a powerful tool for the classification of traditional Chinese drug. A study has been completed on 55 Beimu samples of five different geographic origins: Eastern China. Central China. South-western China, North-western China and North-eastern China. Principal component analysis and SIMCA are applied to effectively classifying the samples according to the origin of the plants. The chemical information contained in the high resolution gas chromatographic data is sufficient to characterize the geographic origin of samples.

GC Determination of Active Cannabinoids in Cannabis of Chinese Origin and Survey of Their Contents

Ji-Hong Zhu, Yong-Qing Li, Xing-Hua Bao

1992, 1(2):  73-80. 

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A method of GC determination using tetracosane as the internal standard for active cannabinoids cannabidiol. ∆⁹-tetrahydrocannabinol and cannabinol of cannabis is described. The method is simple and accurate and has been applied to investigate the contents of active cannabinoids in cannabis of Chinese origin. Information was obtained from provinces and autonomous region of China. Three pure cannabinoids used as the reference substances were extracted and isolated successfully from cannabis.

Communications

Constituents of Chinese Drug Fangfeng, the Root of Saposhnikovia divaaricata

De-An Guo, Zhi-An Liu^*, Zhi-Cen Lou

1992, 1(2):  81-83. 

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Potencies of Four Stereoisomers of Ansiodamine On Muscarinic Receport

Xin-Yi Niu, Zhi-Hong Ren, Lan Xie

1992, 1(2):  84-86. 

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