Ishihara H, Ozaki H, Sato K, Hori M, Karaki H, Watabe S, Kato Y, Fusetani N, Hashimoto K, Uemura D
Department of Veterinary Pharmacology, Faculty of Agriculture, University of Tokyo, Japan.
J Pharmacol Exp Ther. 1989 Jul;250(1):388-96.
Calyculin-A (CL-A), a novel marine toxin isolated from Discodermia calyx, caused contraction in the smooth muscle of guinea pig taenia ceci and rat aorta in the presence or absence (with 1 mM ethylene glycol bis(beta-aminoethyl ether)-N,N'-tetraacetic acid) of external Ca++ at concentrations ranging from 1 X 10(-8) to 1 X 10(-6) M. In the presence of external Ca++, the contraction induced by CL-A was accompanied by an increase in the cytosolic free Ca++ concentration [( Ca++]cyt) as measured by the fluorescence indicator fura-2. Verapamil (3 X 10(-6) M) inhibited the increase in [Ca++]cyt, but not tension development caused by CL-A. In the absence of external Ca++, CL-A still caused contraction without changing [Ca++]cyt. Thus, from studies with intact smooth muscle it was demonstrated that, in the absence of external Ca++, CL-A can induce a contraction that was not accompanied by an increase in [Ca++]cyt. In permeabilized taenia, CL-A caused contraction in the absence of Ca++ (with 2 mM ethylene glycol bis(beta-aminoethyl ether)N,N'-tetraacetic acid) at concentrations similar to those required to contract intact tissue. This contraction was inhibited by the nonselective kinase inhibitors such as amiloride (1 X 10(-3) M) and K-252a (2 X 10(-5) M). Low concentrations of Ca++ (approximately 1 X 10(-6) M) augmented the CL-A-induced contraction in the permeabilized taenia. In native actomyosin prepared from chicken gizzard CL-A induced phosphorylation of the 20 kDa myosin light chain (MLC) in the absence of Ca++.(ABSTRACT TRUNCATED AT 250 WORDS)
花萼海绵诱癌毒素A(CL-A)是一种从花萼盘海绵中分离出的新型海洋毒素,在有或无(加入1 mM乙二醇双(β-氨基乙醚)-N,N'-四乙酸)细胞外钙离子的情况下,浓度范围为1×10⁻⁸至1×10⁻⁶ M时,均可引起豚鼠盲肠带和大鼠主动脉平滑肌收缩。在有细胞外钙离子存在时,CL-A诱导的收缩伴随着胞质游离钙离子浓度[Ca²⁺]cyt的增加,这是通过荧光指示剂fura-2测量的。维拉帕米(3×10⁻⁶ M)抑制了[Ca²⁺]cyt的增加,但不抑制CL-A引起的张力发展。在无细胞外钙离子时,CL-A仍可引起收缩,且不改变[Ca²⁺]cyt。因此,通过对完整平滑肌的研究表明,在无细胞外钙离子时,CL-A可诱导不伴有[Ca²⁺]cyt增加的收缩。在通透的盲肠带中,CL-A在无钙离子(加入2 mM乙二醇双(β-氨基乙醚)N,N'-四乙酸)时,以与收缩完整组织所需浓度相似的浓度引起收缩。这种收缩被非选择性激酶抑制剂如阿米洛利(1×10⁻³ M)和K-252a(2×10⁻⁵ M)抑制。低浓度的钙离子(约1×10⁻⁶ M)增强了通透盲肠带中CL-A诱导的收缩。在从鸡砂囊制备的天然肌动球蛋白中,CL-A在无钙离子时诱导20 kDa肌球蛋白轻链(MLC)磷酸化。(摘要截断于250字)