Glutamate-activated chloride channels: Unique fipronil targets present in insects but not in mammals

Selectivity to insects over mammals is one of the important characteristics for a chemical to become a useful insecticide. Fipronil was found to block cockroach GABA receptors more potently than rat GABA_A receptors. Furthermore, glutamate-activated chloride channels (GluCls), which are present in cockroaches but not in mammals, were very sensitive to the blocking action of fipronil. The IC₅₀s of fipronil block were 30 nM in cockroach GABA receptors and 1600 nM in rat GABA_A receptors. Moreover, GluCls of cockroach neurons had low IC₅₀s for fipronil. Two types of glutamate-induced chloride current were observed: desensitizing and non-desensitizing, with fipronil IC₅₀s of 800 and 10 nM, respectively. We have developed methods to separately record these two types of GluCls. The non-desensitizing and desensitizing currents were selectively inhibited by trypsin and polyvinylpyrrolidone, respectively. In conclusion, in addition to GABA receptors, GluCls play a crucial role in selectivity of fipronil to insects over mammals. GluCls form the basis for development of selective and safe insecticides.     

水稻4种功能营养成分与SSR标记关联分析

以108份水稻种质组成的自然群体为试验材料,鉴定水稻中抗性淀粉(RS)、谷蛋白(Glu)、总黄酮(Tfl)、γ-氨基丁酸(GABA)等4种功能成分含量的性状。利用69个SSR标记分析群体结构,通过TASSEL3.0的GLM和MLM模型作性状和标记关联分析,进一步挖掘优异等位变异及相关载体材料。结果表明,共检测到31个与水稻中4种功能成分含量显著相关的位点,其中13个位点在两种模型中均被检测出显著关联。进一步得到29个优异等位变异。两年两个模型中均检测出RM1374、RM1379和RM27850。     

Insecticidal activity of Sikimi extract and its modulation of the GABAA receptor channel

Sikimi plant (also known as Japanese star anise), Illicium anisatium, is toxic to mammals. Extracts of Sikimi were studied for their insecticidal activity against the larvae of mosquito, Culex quinquefasciatus, and for their mechanism of action on ion channels. Crude methanol extract and its ethyl acetate-soluble fractions were insecticidally active, with EC₅₀ values of 63·0 μg ml^-1 and 43·7 μg ml^-1, respectively. The ethyl acetate-soluble fraction was perfused through the bathing solution and the current induced by a brief (10 ms) application of GABA by pressure ejection through pipette electrode was recorded by the whole-cell patch clamp technique. The extract suppressed GABA-induced currents irreversibly with an EC₅₀ value of 0·42 μg ml^-1. The time constant of current fitted to the single exponential function was shortened by the ethyl acetate-soluble fraction at concentrations ranging from 0·1 μg ml^-1 to 10 μg ml^-1 in a concentration-dependent manner. It was concluded that Sikimi extracts decreased the affinity of GABA for its binding site on the GABA receptor, thereby suppressing GABA-induced currents. © 1998 SCI     

Review: Approaches to New Parasiticides

Intensive use of parasiticides has sometimes led to severe resistance in arthropods and helminths of veterinary importance. In the context of the growing awareness of parasitic diseases, this has created a public demand for effective and safe control agents. During the last two decades considerable knowledge in parasite neurophysiology and endocrinology has accumulated which allows the development of new screening procedures and target-site-directed approaches for the discovery of new drugs. The suitability of this strategic approach is discussed on the basis of recent discoveries of new chemical and natural compounds. In particular, target sites such as GABA_A receptors, muscarinic and nicotinic acetylcholine receptors, cuticle synthesis and degradation, ecdysteroid receptors, the calcium release channel and semiochemicals have been selected in order to demonstrate the current approaches to identify new chemical entities, biologically active against nematodes and arthropods.     

茶叶中γ-氨基丁酸的研究进展

茶叶中γ-氨基丁酸(GABA)是一种非蛋白质氨基酸,具有抗抑郁、降血压、增强记忆力、抗癌等功效,因此受到较多学者的关注。文章对近年来茶树中GABA的代谢机理、富集技术和GABA对人体健康作用等方面进行综述与展望,以期为系统研究茶叶中GABA和GABA茶产品开发提供理论依据。     

Simultaneous HPLC determination of gamma amino butyric acid (GABA) and lysine in selected Pakistani rice varieties by pre-column derivatization with 2-Hydroxynaphthaldehyde

A selective and sensitive HPLC method for the simultaneous determination of gamma amino butyric acid (GABA) and lysine in Pakistani rice varieties was developed. Both analytes were detected in rice varieties as Schiff base derivatives with 2-hydroxynaphthaldehyde. The derivatives were analyzed on a reverse phase C-18 column with Diode Array Detector (DAD) at 254 nm. The calibration curves were found linear over a concentration range of 3.83–34.58 μg/mL for GABA and 5.16–48.68 μg/mL for lysine with a correlation coefficient of 0.998 for both standards. GABA and lysine contents were found higher in brown rice varieties (4.1–6.58 mg/100 g for GABA and 15.1–27.6 mg/100 g for lysine) than the polished varieties (0.32–0.47 mg/100 g GABA and 13.1–19.8 mg/100 g lysine). This method could be used for separation and quantification of GABA and lysine simultaneously in food samples, especially in cereal seeds.     

Suppression of Progesterone-enhanced Hyperactivation in Hamster Spermatozoa by γ-aminobutyric Acid

It has been recently shown that mammalian spermatozoa were hyperactivated by steroids, amines and amino acids. In the present study, we investigated whether hyperactivation of hamster sperm is regulated by progesterone (P) and γ-aminobutyric acid (GABA). Although sperm hyperactivation was enhanced by P, GABA significantly suppressed P-enhanced hyperactivation in a dose-dependent manner. Suppression of P-enhanced hyperactivation by GABA was significantly inhibited by an antagonist of the GABA_A receptor (bicuculline). Moreover, P bound to the sperm head, and this binding was decreased by GABA. Because the concentrations of GABA and P change in association with the estrous cycle, these results suggest that GABA and P competitively regulate the enhancement of hyperactivation through the GABA_A receptor.     

氮气厌氧处理对茶叶γ-氨基丁酸及主要化学成分含量的影响

为生产出富含γ-氨基丁酸(GABA)降压功能茶,采用氮气厌氧处理茶鲜叶后再进行微波杀青等方法,研究了氮气厌氧处理对茶叶品质及γ-氨基丁酸含量的影响。结果表明:真空充氮2h和除氮充氧2h,循环4次,成茶中GABA含量达1.89mg/g,是未经氮气厌氧处理茶叶中GABA含量的37.8倍;成茶中的茶多酚、咖啡碱和儿茶素含量基本不变;氨基酸和可溶性糖含量呈下降趋势。     

籼型巨胚水稻新品系莲塘巨胚红的选育与应用

介绍了"莲塘巨胚红"的选育过程、品系特性及栽培技术要点,是"91-308"与"巨胚1号"杂交选育而成的红米类籼型巨胚水稻新品系,分蘖力强,生育期112～114 d,单产4500 kg/hm2左右,适宜在江西赣抚平原、赣中南丘陵山区作二晚种植。该品系稻米具有胚巨大、种皮呈红色的特点,富含γ-氨基丁酸、铁以及多种必需氨基酸等成分,可作为降血压功能性稻米的原料进行综合开发利用。     

Larval settlement of the tropical abalone, Haliotis asinina Linnaeus, using natural and artificial chemical inducers

Many kinds of chemical and biological materials have been used as inducers of settlement of abalone larvae, as well as other species of marine gastropods, with responses being highly variable, even to the same chemical cue. The present study tested chemical inducers, γ-aminobutyric acid (GABA), δ-aminovaleric acid (5-AVA) and l -glutamic acid (GA) and the effects they have on larval settlement of Haliotis asinina . Additionally, a relatively inexpensive commercial substance, monosodium glutamate (MSG), was trialed. The datum provided shows all chemicals to be active inducers of settlement in this study, in order of effectiveness of 5-AVA, GABA, MSG to GA. Induction as adjudged from larval numbers settled was best at 6 h 62%, with 10⁻¹ mM 5-AVA. At 24 h, induction was the highest at 78% when exposed to 10⁻² mM 5-AVA. Larvae that were allowed to settle up to 72 h showed the highest numbers of settled larvae, and declined back to 60% when exposed to 10⁻² 5-AVA and 10⁻¹ mM GABA respectively. Monosodium glutamate, although third in settlement standings would bypass the other chemicals, with regard to cost versus yield. The assessment of settlement surface, rough or smooth proved to be irrelevant, which had no significant impact on larval settlement.