Whiting P, Sparks S, Dinan L
Department of Biological Sciences, University of Exeter, Washington Singer Laboratories, Devon, United Kingdom.
Arch Insect Biochem Physiol. 1997;35(3):279-99. doi: 10.1002/(SICI)1520-6327(199705)35:3<279::AID-ARCH3>3.0.CO;2-P.
Ecdysteroid titres have been determined in adult female house crickets (Acheta domesticus) in relation to reproductive maturation. Ecdysteroid levels in newly emerged adult females are low except in the gut and carcass, which probably reflects the remnants of the preecdysial ecdysteroid peak. Ecdysteroid levels in all compartments increase markedly once ovarian weight surpasses 10 mg. Apolar ecdysteroid conjugates (ecdysone 22-fatty acyl esters) predominate in ovarian tissue throughout ovarian maturation, but low levels of free ecdysteroid and polar conjugated ecdysteroids are also present. During this period, two peaks of ecdysteroids (mainly free and apolar conjugated ecdysteroids) are observed in the haemolymph, gut, and carcass compartments. The peaks in the haemolymph occur when the ovarian mass reaches 30 and 100 mg. The gut and carcass may be acting as sinks or sites of metabolism for the hormone released from the ovaries. The rate of ecdysone acylation by ovaries was found to be developmentally regulated, increasing from low levels in the immature ovaries of newly emerged females as the ovaries increase in size. A semiquantitative assay has been developed to identify compounds which inhibit the conversion of [3H]ecdysone into 22-fatty acyl [3H]ecdysone by ovaries in vitro. A number of ecdysteroids possessing a free hydroxyl group as C-22 as well as the side-chain stereochemistry of ecdysone effectively inhibit this conversion, probably by acting as competitive substrates. In the cases of 20-hydroxyecdysone and ponasterone A, it was clearly demonstrated that these compounds are converted to a mixture of C-22 fatty acyl esters. Several other compounds which have been suggested to affect ecdysteroid metabolism/mode of action in other systems were also tested for their effects on the acyltransferase activity of ovaries in vitro.
已测定成年雌性家蟋蟀(Acheta domesticus)体内蜕皮甾体滴度与生殖成熟的关系。新羽化的成年雌性体内蜕皮甾体水平较低,肠道和体壁除外,这可能反映了蜕皮前蜕皮甾体峰值的残留。一旦卵巢重量超过10毫克,所有组织中的蜕皮甾体水平都会显著增加。在整个卵巢成熟过程中,非极性蜕皮甾体结合物(蜕皮酮22 - 脂肪酰酯)在卵巢组织中占主导地位,但也存在低水平的游离蜕皮甾体和极性结合蜕皮甾体。在此期间,在血淋巴、肠道和体壁组织中观察到两个蜕皮甾体峰值(主要是游离和非极性结合蜕皮甾体)。当卵巢质量达到30毫克和100毫克时,血淋巴中出现峰值。肠道和体壁可能是卵巢释放激素的储存库或代谢场所。发现卵巢的蜕皮酮酰化速率受发育调控,随着卵巢大小增加,从新羽化雌性未成熟卵巢中的低水平开始上升。已开发出一种半定量测定法,用于鉴定在体外抑制卵巢将[3H]蜕皮酮转化为22 - 脂肪酰[3H]蜕皮酮的化合物。许多在C - 22位具有游离羟基以及具有蜕皮酮侧链立体化学结构的蜕皮甾体有效地抑制了这种转化,可能是作为竞争性底物起作用。在20 - 羟基蜕皮酮和波那甾酮A的情况下,清楚地表明这些化合物转化为C - 22脂肪酰酯的混合物。还测试了其他几种在其他系统中被认为会影响蜕皮甾体代谢/作用方式的化合物对卵巢体外酰基转移酶活性的影响。