长臀鮠脑垂体和血清中促性腺激素的生殖周期变化

Changes in the pituitary and serum gonadotropin levels of Cranoglanis bouderius were studied at different stages of ovarian development.Based on African catfish gonadotropin(cfGTH) and its anti-serum(Racf),heterologous radio-immunoassay(RIA) for the gonadotropin(GTH) of Cranoglanis bouderius was developed.The pituitary GTH contents at the late development stage were significantly higher than that at the mature,ovulation or regressed stages,while serum GTH levels at maturation and ovulation were significantly higher than that at late development and regressed stages,Injection of gonadotropin-releasing hormone analogue(GnRH-A) stimulated GTH secretion.Domperidone (DOM) had no effect on the basal serum GTH level.Injection of GnRH-A and DOM significantly enhanced the GTH levels stimulated by GnRH-A alone.These results indicate that GTH release in Cranoglanis bouderius is under the dual regulation of gonadotropin releasing hormone(GnRH) and dopamine(DA) from the hypothalamus,but DA can only inhibit GTH release induced by GnRH and not basal GTH release[Acta Zoologica Sinica 49(3):399-403.2003].     

促性腺激素释放激素类似物对长臀(鱼危)脑垂体促性腺激素分泌的影响

采用离体灌流孵育技术和促性腺激素的放射免疫测定方法,对长臀(鱼危)(Cranoglanis bouderius)脑垂体碎片促性腺激素的分泌进行了研究.结果表明:持续的促性腺激素释放激素类似物(GnRH-A)能显著刺激退化期的长臀(鱼危)离体脑垂体碎片促性腺激素(GTH)的分泌,并且长臀(鱼危)脑垂体碎片对持续的GnRH-A刺激未表现出脱敏性,该结果与胡子鲇和鲇鱼相似,而与金鱼和鲤科鱼类不同;重复脉冲GnRH-A刺激对长臀(鱼危)脑垂体碎片GTH分泌具有促进作用,而且存在剂量依存关系,与鲇鱼和鲤科鱼类相类似.上述结果表明在长臀(鱼危)的人工繁殖中可以用持续高浓度GnRH-A刺激对长臀(鱼危)进行催熟和催产.     

长臀(鱼危)生长激素的生殖周期变化

国内外学者对硬骨鱼类的GH的季节变动及神经内分泌调控有一定的研究,其中在鲤科和鲑鳟鱼类研究的较为深入,近来一些学者对鲇形目的胡子鲇科、(鱼危)科[1]和鲇科[2]做了一定的研究,研究结果表明,GH分泌和神经内分泌调节机理与鲤科鱼类在某些方面存在一定差异.     

促性腺激素释放激素类似物对长臀wei脑垂体促性腺激素分泌的影响

采用离体灌流孵育技术和促性腺激素的放射免疫测定方法,对长臀wei(Cranoglanis bouderius)脑垂体碎片促性腺激素的分泌进行了研究。结果表明：持续的促性腺激素释放激素类似物(GnRH-A)能显著刺激退化期的长臀wei离体脑垂体碎片促性腺激素(GTH)的分泌,并且长臀wei脑垂体碎片对持续的GnRH-A刺激未表现出脱敏性,该结果与胡子鲇和鲇鱼相似,而与金鱼和鲤科鱼类不同;重复脉冲GnRH-A刺激对长臀wei脑垂体碎片GTH分泌具有促进作用,而且存在剂量依存关系,与鲇鱼和鲤科鱼类相类似。上述结果表明在长臀wei的人工繁殖中可以用持续高浓度GnRH-A刺激对长臀wei进行催熟和催产。     

长臀鮠生长激素的生殖周期变化

国内外学者对硬骨鱼类的GH的季节变动及神经内分泌调控有一定的研究,其中在鲤科和鲑鳟鱼类研究的较为深入,近来一些学者对鲇形目的胡子鲇科、科和鲇科做了一定的研究,研究结果表明,GH分泌和神经内分泌调节机理与鲤科鱼类在某些方面存在一定差异。如鲤科鱼类中,GnRH起着GH释放因子的作用,但非洲鲇鱼和鲇鱼中却未证实GnRH刺激GH释放,并且鲇鱼中GH分泌的季节变化与生殖之间有密切联系。       

鲤鱼脑垂体促性腺激素含量年周期变化的研究

本文报道了用蟾蜍离体卵巢跌卵的方法来研究鲤鱼脑垂体里的促性腺激素含量的年周期变化情况,以解决我国鲩、青、鲢、鳙人工繁殖工作中应用鲤鱼脑垂体作为催产剂的质量问题。实验是在1962—1963年进行的。实验结果表明：鲤鱼脑垂体对蟾蜍离体卵巢有明显的跌卵效果;鲤鱼脑垂体里的促性腺激素是常年存在的,但随季节的不同而含量亦有所不同。全年中以2—3月份的脑垂体里促性腺激素的含量最高,10月份为最低,其他月份则是逐渐递升与递减的关系,因而呈现出一明显的年周期变化规律,这对指导收集鲤鱼脑垂体的最适季节具有一定的实用意义。对鱼类脑垂体的生理探讨方面也提供了一些新的资料。     

促性腺激素释放激素类似物对长臀鮠脑垂体促性腺激素分泌的影响

采用离体灌流孵育技术和促性腺激素的放射免疫测定方法,对长臀鮠(Cranoglanis bouderius)脑垂体碎片促性腺激素的分泌进行了研究。结果表明：持续的促性腺激素释放激素类似物(GnRH-A)能显著刺激退化期的长臀鮠离体脑垂体碎片促性腺激素(GTH)的分泌,并且长臀鮠脑垂体碎片对持续的GnRH-A刺激未表现出脱敏性,该结果与胡子鲇和鲇鱼相似,而与金鱼和鲤科鱼类不同;重复脉冲GnRH-A刺激对长臀鮠脑垂体碎片GTH分泌具有促进作用,而且存在剂量依存关系,与鲇鱼和鲤科鱼类相类似。上述结果表明在长臀鮠的人工繁殖中可以用持续高浓度GnRH-A刺激对长臀鮠进行催熟和催产。     

鲑鱼促性腺激素释放激素（sGnRH）调节鲤鱼脑垂体生长激素分泌的离体研究

ｓＧｎＲＨ同时刺激离体灌流孵育的鲤鱼脑垂体ＧｔＨ和ＧＨ分泌,ＧｔＨ和ＧＨ对ｓＧｎＲＨ脉冲式刺激的分泌反应的时间进程和剂量依存关系相似。生长抑素显著抑制基础的ｓＧｎＲＨ刺激的ＧＨ分泌,但对ＧｔＨ分泌没有影响。阿扑吗啡以剂量依存方式显著抑制基础的ｓＧｎＲＨ促进的ＧｔＨ分泌,并显著刺激ＧＨ分泌,但对ｓＧｎＲＨ促进的ＧＨ分泌无影响。     

多马胺能药物对鲇鱼促性腺激素（GtH）分泌活动的影响

以珠江流域鲇鱼（silurus asotus)为实验材料,研究了多巴胺（DA）能药物（DA及其D－2型受体拮抗物 ,DOM）对鲇鱼促性腺激素（GtH)释放的影响,结果表明,在性腺发育的各个时期,单独注射DOM（5ug/g)均不能显著提高鲇鱼血液基础GtH水平,当DOM与LHRH－A联合注射时能显著增强LHRH－A刺激GtH释放的作用;DA只能抑制GnRH诱导的GtH释放,对基础GtH释放无抑制作用,这种生殖内分泌调节方式与鲇形目的革胡子鲇（Clarias gariepinus)和大鳍Hu（Mystus macropterus)相似,而与鲤形目的鲁科（Cyrpindiae)鱼类不同。     

人卵泡促性腺激素释放肽（hF－GRP）的STM研究

人卵泡促性腺激素释放肽（ｈＦ－ＧＲＰ）为一只含１４个氨基酸的多肽类激素,我们已经用２Ｄ－ＮＭＲ技术测定了它的溶液构象,本文又用ＳＴＭ技术观察了ｈＦ－ＧＲＰ单层铺展时的分子图象,测得其分子大小约为２．４ｎｍ,并用２Ｄ－ＮＭＲ结果较好地解释了所得的图象。     

Design and synthesis of a gonadotropin-releasing hormone (GnRH) analogue, [Tyr(OMe)5,d-Glu6,Aze9]GnRH: Receptor binding, gonadotropin release and ovulation studies

Summary Gonadotropin-releasing hormone (GnRH) stimulates the release and synthesis of gonadotropin hormones (GtH) and is the key regulator of reproduction. The present study was carried out to design a potent GnRH analogue containing Tyr(OMe) at position 5 and ad-amino acid at position 6. This was based on a previous study in which [Tyr(OMe)⁵]GnRH was shown to have reduced potency compared to GnRH. A novel GnRH peptide containing Tyr(OMe)⁵ andd-Glu⁶ in combination with other substitutions at positions 9 and 10 was synthesized in the present study and tested for binding to the rat pituitary as well as potency in terms of gonadotropin (GtH) release in the goldfish pituitary and ovulation in sea bass. The results demonstrate that the replacement of the glycine residue at position 6 with ad-Glu in combination with the substitution of proline at position 9 with azetidine (Aze) increased the binding and biological activity of [Tyr(OMe)⁵]GnRH. The observed increased potency is likely to be related to the improved resistance to degradation. The present findings may lead to the development of a more potent GnRH agonist for inducing ovulation in fish.     

不同水温下氟甲砜霉素在斑点叉尾鮰体内的药代动力学研究

研究不同水温(18℃和28℃)条件下,单剂量(10mg/kgb·w)强饲氟甲砜霉素,在斑点叉尾鮰(Ictaluruspunc-tatus)体内药代动力学特征.采用高效液相色谱紫外检测法可以同时检测血浆中氟甲砜霉素及其代谢物氟甲砜霉素的浓度.用3p97药代动力学软件处理药时数据.结果表明:在不同水温条件下氟甲砜霉素在斑点叉尾鮰体内的药时数据均符合一室开放式模型.药时规律符合理论方程C血浆=71921(e-0.036t-e-0.18t)和C血浆=91061(e-0.081t-e-0.301t).18℃和28℃的条件下,主要药代动力学参数:吸收半衰期T1/2ka分别为31845h和21301h,消除半衰期T1/2ke分别为191118h和81519h,达峰时间Tpeak分别为111136h和51953h,最大血药浓度Cmax分别为41074μg/mL和41226μg/mL,曲线下面积AUC分别为1741547(μg/mL)/h和811279(μg/mL)/h,平均驻留时间MRT分别为271581h和121290h,相对表观分布容积V/F(c)分别为11580L/kg和115121L/kg.采用氟甲砜霉素防治斑点叉尾鮰细菌性疾病,建议在18℃左右口服10mg/kg体重剂量的氟甲砜霉素,2d给药1次;在28℃左右口服10mg/kg体重剂量的氟甲砜霉素,1d给药1次.试验过程中在斑点叉尾鮰血浆样品中未检测到氟甲砜霉素的主要代谢物氟甲砜霉素胺.       

Effects of mammalian gonadotropin-releasing hormone analogue, pimozide, and the combination on plasma gonadotropin levels in different seasons and induction of ovulation in female catfish

In the catfish Heteropneustes fossilis , 0.5μg g-¹ B.W. mGnRH-A alone or the low dose of 0.05 μg g^-1 B.W. in combination with pimozide [a dopamine (DA)-receptor antagonist, 5 or l0μg g^-1 B.W.], caused a preovulatory surge in plasma gonadotropin (GTH) and induced a high rate of ovulation. The ovulatory response of the catfish to the low dose of mGnRH-A when given alone was not effective in the early (July) but was effective in the late spawning season (August). Plasma GTH response to these treatments showed seasonal variations. Pimozide administration potentiated the response to mGnRH-A in a season-dependent manner, being effective only in the prespawning and spawning phases. Pimozide treatment alone did not affect plasma GTH. These observations suggest that the release of GTH from the pituitary is subject to seasonal differences in the sensitivity of the GnRH system and the degree of its modulation by dopamine.     

The effects of aromatizable androgens,non-aromatizable androgens,and estrogens on gonadotropin release in castrated African catfish,Clarias gariepinus (Burchell)

Summary To study the feedback mechanism of gonadal hormones on GTH secretion in male African catfish, the effects of castration and steroid replacement on GTH release, pituitary GTH content, and ultrastructural appearance of gonadotropes were investigated.Castration resulted in an increase in plasma GTH levels, a decrease in pituitary GTH content, and a degranulation of many gonadotropes. The aromatizable androgens testosterone and androstenedione were able to abolish the castration-induced increase in plasma GTH. This was accompanied with a restoration of pituitary GTH content and a regranulation of gonadotropes. The non-aromatizable androgens 5-dihydrotestosterone and 11-hydroxyandros tenedione did not have these effects. Replacement with estrone or estradiol resulted in an increase in pituitary GTH, however, without abolishing the elevated plasma GTH levels; ultrastructurally, many gonadotropes showed a welldeveloped granular endoplasmic reticulum together with a regranulation.The results of the present study indicate the significance of androgen aromatization in the feedback mechanism of gonadal steroids on the brain-pituitary axis.     

Synthesis and in vitro evaluation of small-molecule [18F] labeled gonadotropin-releasing hormone (GnRH) receptor antagonists as potential PET imaging agents for GnRH receptor expression

Two novel small molecule gonadotropin-releasing hormone (GnRH) receptor antagonists (12 and 13) of the furamide-class were synthesized and evaluated in vitro for their receptor binding affinities for the rat GnRH receptor. Radiolabeling with no carrier added fluorine-18 of the appropriate precursors was investigated in a one-step reaction. Log P (Octanol/PBS pH 7.4) and serum stability of the compounds were investigated. The antagonists showed low nM affinity for the rat GnRH receptor. ¹⁸F-radiolabled compounds were obtained in high radiochemical purity (>95%) and specific activity (>75 GBq/μmol). These findings suggest this class of compounds holds promise as potential probes for PET targeting of GnRH-receptor expression.     

Changes in the non-structural carbohydrate content of cotton (Gossypium spp.) fibres at different stages of development

The neutral sugars (glucose, fructose, and sucrose) and the sugar phosphates (glucose 6-phosphate, glucose 1-phosphate and fructose 6-phosphate) soluble in hot aqueous 80% methanol from the fibres of cotton — Gossypium arboreum L., G. barbadense L., and G. hirsutum L. — were determined at various stages of fibre development. In addition, the (13)--D-glucan content was measured and in the case of G. arboreum the rate of (13)--D-glucan and cellulose synthesis was determined with [¹⁴C]sucrose as the precursor. For each of the species a similar chronology was obtained for the changes in content of the various non-structural carbohydrates. At the early stages of secondary wall formation, glucose and fructose exhibited a maximum which was closely followed by a maximum in the (13)--D-glucan content and in the sugar phosphates. On the other hand, the sucrose content increased regularly until fibre maturity. The rates of synthesis of (13)--D-glucan and of cellulose were highest following the maximum in the (13)--D-glucan content, when the latter was being depleted.Abbreviations DMSO dimethyl-sulphoxide - DPA days post anthesis - UDP-glucose uridinediphosphoglucose