Synthesis of 1-(4-methylbenzyl)-2-methyl-octahydro-isoquinoline hydrochloride / 中国药科大学学报

@#1-(4-Methylbenzyl)-2-methyl-octahydro-isoquinoline hydrochloride(1)is the key intermediate to prepare a new type of antitussives agent phosphate dimemorfan. 4-methyl-phenylacetic acid as a raw materials, was chlorinated with thionyl chloride to obtain 4-methyl-phenylacetyl chloride, followed by reaction with 2-cyclohexenyl amine, then cyclization, reduction, methylation and salt formation by HCl were taken out to give the desired product 1. The total yield is 54%, and the purity is greater than 98%. This synthetic process is characterized with available raw materials, simple in operation with high yield and purity, and suitable for large-scale production.

Expectorant and Antitussive Effect of Hedera helix and Rhizoma coptidis Extracts Mixture

PURPOSE: This study aims to investigate the additive effect of the Hedera helix (HH) and Rhizoma coptidis (RC) extracts mixture on antitussive and expectorant activities in animals. MATERIALS AND METHODS: The expectorant assay was performed with phenol red secretion in mice trachea. Mice or guinea pigs were randomly divided into groups of 8 each, including negative and positive control groups. After gastric administration of the test extracts in mice, 2.5% phenol red solution (0.2 mL) was intraperitoneally injected. Trachea was dissected and optical density of tracheal secretion was measured. After gastric administration of the test extracts in guinea pigs, the antitussive activities were assessed using a citric acid-induced cough measurement. RESULTS: The extracts of HH and RC significantly increased tracheal secretion and inhibited cough. The mixture of HH and RC extracts in a 1:1 concentration at a dose of 200 mg/kg showed a more potent effect on phenol red secretion (25.25+/-3.14) and cough inhibition (61.25+/-5.36) than the individual use of each extracts [phenol red secretion; HH 13.39+/-4.22 (p=0.000), RC 20.78+/-2.50 (p=0.010), cough inhibition; HH 9.89+/-4.14 (p=0.010), RC 30.25+/-7.69 (p=0.000)]. A 3:1 ratio mixture of HH to RC demonstrated an optimal expectorant effect (p<0.001), and this mixture showed expectorant and antitussive effects in a dose-dependent manner. CONCLUSION: This study provides evidence for antitussive and expectorant effect of a 3:1 mixture of HH and RC, which may be a useful therapeutic option for respiratory diseases.

A case of pneumonia; cough and accompanying body pain by the cough were effectively treated with acupuncture / 全日本鍼灸学会雑誌

Pneumonia is one of major causes of cough, which sometimes resists medication and remarkably deteriorates QOL of the patient. We report a case of pneumonia in a person suffering from severe cough and pain in the general body accompanied by cough for which conventional medication did not work but was improved by acupuncture treatment. <BR>A 47-year-old woman was diagnosed by her physician with pneumonia on August 2, 200X. Although antibiotics were administered, her symptoms were not improved. She visited Meiji University of Integrative Medicine Hospital and was hospitalized on the same day. Despite strict medication with antibiotics, antitussive agent and expectorant during hospitalization, her severe cough and body pain remained unchanged. <BR>Acupuncture treatment was then started on August 7. The basic meridian points used were LU1 (Zhongfu), LU5 (Chize), BL13(Feishu), LU7 (Leique), LI4 (Hegu), GB20 (Fengchi), GB14 (Danzhui), ST12 (Quepen), ST11 (Qishe), and CV22 (Tiantu). The acupuncture needles were retained for ten minutes at these points in each session. After ten acupuncture treatments for over seven days, the VAS for body pain accompanied by cough showed a remarkable improvement. Also, significant relief in cough was observed every time immediately after treatment. <BR>We suggested that acupuncture treatment might be useful for cough and/or pain in the body accompanied by cough in a patient with pneumonia.