Higenamine이 심근 Sarcoplasmic Reticulum의 칼슘운반에 미치는 영향에 관한 연구

• 영문명: The Effect of Higenamine on the Calcium Transport of Cardiac Sarcoplasmic Reticulum
• 발행기관: 대한약리학회
• 저자명: 김주현(Joo Hyun Kim) 이영균(Yung Kyoon Lee) 김혜원(Hae Won Kim) 김명석(Myung Suk Kim) 박찬웅(Chan Woong Park) 임정규(J
• 간행물 정보: 『대한약리학잡지』제18권 제2호, 79~88쪽, 전체 10쪽
• 주제분류: 의약학 > 기타의약학
• 파일형태: PDF
• 발행일자: 1982.12.31

영문 초록

Higenamine(dl-demethylcoclaurine, dl-1-(4-hydroxybenzyl)-6,7-dihydroxy-1,2,3,4-tetrah-ydroisoquinoline hydrochloride), which has recently been isolated from Aconite root by Drs. Kosuge and Yokota, has known to be the main cardiotonic component of the Aconite root. The present study was undertaken to investigate the effects of Higenamine on the calcium binding and release and ATPase activity of fragmented cardiac sarcoplasmic reticulum under in vitro condition. The calcium binding and release of sarcoplasmic reticulum were measured by using the double-beam spectrophotometer and the calcium sensitive dye, murexide. In the presence of 10^-4 ~ 5 X 10^-3M of Higenamine, the maximal calcium binding and the initial binding rate of porcine cardiac sarcoplasmic reticulum were inhibited dose dependently by up to 43%. However, the calcium release from cardiac sarcoplasmic reticulum, which was loaded with Ca⁺⁺(50μM), was stimulated in dose dependent manner. When incubated in the medium of 20 mM Tris-maleate(pH 7.0), 100 mM KCl, 10 mM MgCl₂, 0.05mM CaCl₂ and 0.014 ~ 1 mM Tris-ATP at 30˚C in the presence of Higenamine (10^-4 ~ 5 X 10^-3M), both Ca⁺⁺-and Mg⁺⁺-ATPase of sarcoplasmic reticulum were inhibited non-competitively by Higenamine and values of K_i were 4.896 mM and 6.875 mM respectively. It is suggested from the above findings that the cardiotonic effects of Higenamine might be partially explained by the inhibition of calcium binding and the stimulation of calcium release from the sarcoplasimic reticulum which may increase the free intracellular calcium that is available in the contraction of the cardiac muscle fiber.