Assessment of Bioactive Potential of Aqueous Protein Extracts from Diatoms Nitzschia laevis,Spirulina platensis,and Chlorella vulgaris

The bioactivities of protein extracts from Nitzschia laevis, Spirulina platensis, and Chlorella vulgaris were evaluated in vitro. Free radical scavenging potential, reducing power, oxygen radical absorbance capacity, superoxide anion radical, xanthine oxidase inhibition, and potential to inhibit angiotensin 1-converting enzyme (ACE) and acetylcholinesterase enzyme (AChE) were studied. Nitzschia protein extracts showed the highest 2,2-diphenyl-1-picrylhydrazyl (DPPH) scavenging activities, reducing power, and ACE inhibitory activity. Spirulina’s proteins showed the highest 2,2′-Azino-bis (3 ethylbenzothiazoline-6-sulfonic acid) (ABTS) scavenging activity, xanthine oxidase, and AChE inhibition activities. Aqueous protein extracts from Nitzschia, Spirulina, and Chlorella showed in vitro antioxidant, anti-ACE, and anti-AChE activities, suggesting possible new sources of bioactive proteins of different phyla with nutraceutical and pharmaceutical potentials.     

甲氰菊酯对尼罗罗非鱼组织乙酰胆碱酯酶、谷丙转氨酶和谷胱甘肽活性的影响

用急性染毒法研究6种浓度(0、0.4、0.6、0.8、1.0、1.5 μg/L)的甲氰菊酯对(34.89±9.99)g的尼罗罗非鱼(Tilapia nilotica)分别处理6、12、24、48、96 h后,其组织内乙酰胆碱酯酶(AChE)、谷丙转氨酶(GPT)和谷胱甘肽( GSH)的动态变化.结果显示:AChE活性在...     

丹皮、泽泻混和物对黄粉虫幼虫体内蛋白酶和乙酰胆碱酯酶活性的影响

以中药材丹皮、泽泻及其混和物为饲料对黄粉虫幼虫体内蛋白酶和乙酰胆碱酯酶活性的影响进行了研究结果表明:丹皮能显著抑制幼虫体内的蛋白酶活性,在处理5d后,也抑制幼虫的乙酰胆碱酯酶活性;而丹皮泽泻饮片混和物与泽泻相比,幼虫体内蛋白酶和乙酰胆碱酯酶活性没有受到显著影响,但与面粉相比,在一定时间内幼虫的蛋白酶活性受到了影响,说明丹皮影响了幼虫对蛋白质的水解作用,随着时间的延长对幼虫的神经传导也有影响;而混和物在一定时间内可影响幼虫对蛋白质的水解作用而对幼虫的神经传导没有显著影响     

汞离子胁迫对红鳍笛鲷抗氧化酶及乙酰胆碱酯酶活性的影响

为探讨鱼体抗氧化系统以及神经系统对水体中汞胁迫的响应机制,在实验条件下研究了汞离子对红鳍笛鲷幼鱼[体长为(4.95±0.79)cm,体重为(4.57±2.02)g]的急性毒性及对鱼体肝脏、鳃组织的超氧化物歧化酶(SOD)、丙二醛(MDA)及脑组织乙酰胆碱酯酶(AChE)活力的影响。结果表明:半静水实验条件下,汞离子对红鳍笛鲷幼鱼的安全浓度为0.040mg/L。汞离子暴露6h时,各浓度组的肝脏SOD酶活均比对照组有显著升高(P<0.05)。随暴露时间的增加,低浓度组SOD的活性变化较小,而高浓度组鱼体肝脏SOD的活性出现被诱导或被抑制的现象,表明鱼体在高浓度汞胁迫下抗氧化系统出现一定程度的紊乱。鳃的SOD活力在暴露6h亦显著升高,随时间的延长,各浓度组SOD的活性具不同程度的下降趋势。MDA含量的变化表明,鳃组织在暴露6h时已开始受到显著损伤(P<0.05),而肝在6h时无显著变化,在12h时开始受损伤。脑组织AChE活性在暴露6h时略受抑制(P>0.05);暴露12h时高浓度组显著增加(P<0.05),诱导率平均为36%;汞离子暴露24h时,鱼脑AChE的抑制率分别为28%～38%;暴露48h、96h时抑制率...     

Marine-Derived Compounds with Anti-Alzheimer’s Disease Activities

Alzheimer’s disease (AD) is an irreversible and progressive brain disorder that slowly destroys memory and thinking skills, and, eventually, the ability to perform simple tasks. As the aging population continues to increase exponentially, AD has become a big concern for society. Therefore, neuroprotective compounds are in the spotlight, as a means to tackle this problem. On the other hand, since it is believed—in many cultures—that marine organisms in an individual diet cannot only improve brain functioning, but also slow down its dysfunction, many researchers have focused on identifying neuroprotective compounds from marine resources. The fact that the marine environment is a rich source of structurally unique and biologically and pharmacologically active compounds, with unprecedented mechanisms of action, marine macroorganisms, such as tunicates, corals, sponges, algae, as well as microorganisms, such as marine-derived bacteria, actinomycetes, and fungi, have been the target sources of these compounds. Therefore, this literature review summarizes and categorizes various classes of marine-derived compounds that are able to inhibit key enzymes involved in AD, including acetylcholinesterase (AChE), butyrylcholinesterase (BuChE), β-secretase (BACE-1), and different kinases, together with the related pathways involved in the pathogenesis of AD. The compounds discussed herein are emerging as promising anti-AD activities for further in-depth in vitro and in vivo investigations, to gain more insight of their mechanisms of action and for the development of potential anti-AD drug leads.     

诱杀植物香根草对稻蛀茎夜蛾幼虫解毒酶和乙酰胆碱酯酶的影响

香根草能够有效诱集水稻害虫稻蛀茎夜蛾Sesamia inferens雌成虫在其上产卵,但孵化出的幼虫在香根草上不能完成生活史。为了初步明确香根草对稻蛀茎夜蛾幼虫生理生化水平的影响,本研究分析测定了取食香根草后稻蛀茎夜蛾幼虫体内解毒酶和乙酰胆碱酯酶AChE活性的变化。结果表明:与取食水稻的幼虫相比,取食香根草后幼虫解毒酶谷胱甘肽硫转移酶GSTs和AChE活性显著提高。其他两种解毒酶,羧酸酯酶CarE和细胞色素P450酶活性无显著差异。取食香根草后,4龄幼虫GSTs比活力约为取食水稻的2.1倍;2龄幼虫AChE比活力约为取食水稻的2.9倍。本研究结果表明香根草可能存在某些有毒活性物质或者次生代谢物质,诱导了稻蛀茎夜蛾体内GSTs和AChE的活性,这可能是稻蛀茎夜蛾取食香根草后的应急防御机制之一。此研究结果为深入阐明香根草在生理、生化水平上对稻蛀茎夜蛾幼虫的影响奠定了基础,为开发以香根草为基础的稻蛀茎夜蛾绿色防控新技术提供了理论依据。     

Acetylcholinesterase point mutations in European strains of Tetranychus urticae (Acari: Tetranychidae) resistant to organophosphates

BACKROUND: In Tetranychus urticae Koch, acetylcholinesterase insensitivity is often involved in organophosphate (OP) and carbamate (CARB) resistance. By combining toxicological, biochemical and molecular data from three reference laboratory and three OP selected strains (OP strains), the AChE1 mutations associated with resistance in T. urticae were characterised. RESULTS: The resistance ratios of the OP strains varied from 9 to 43 for pirimiphos‐methyl, from 78 to 586 for chlorpyrifos, from 8 to 333 for methomyl and from 137 to 4164 for dimethoate. The insecticide concentration needed to inhibit 50% of the AChE1 activity was, in the OP strains, at least 2.7, 55, 58 and 31 times higher for the OP pirimiphos‐methyl, chlorpyrifos oxon, paraoxon and omethoate respectively, and 87 times higher for the CARB carbaryl. By comparing the AChE1 sequence, four amino acid substitutions were detected in the OP strains: (1) F331W (Torpedo numbering) in all the three OP strains; (2) T280A found in the three OP strains but not in all clones; (3) G328A, found in two OP strains; (4) A201S found in only one OP strain. CONCLUSIONS: Four AChE1 mutations were found in resistant strains of T. urticae, and three of them, F331W, G328A and A201S, are possibly involved in resistance to OP and CARB insecticides. Among them, F331W is probably the most important and the most common in T. urticae. It can be easily detected by the diagnostic PCR‐RLFP assay developed in this study. Copyright © 2009 Society of Chemical Industry     

Biological Activities of Aqueous and Organic Extracts from Tropical Marine Sponges

We report on screening tests of 66 extracts obtained from 35 marine sponge species from the Caribbean Sea (Curaçao) and from eight species from the Great Barrier Reef (Lizard Island). Extracts were prepared in aqueous and organic solvents and were tested for hemolytic, hemagglutinating, antibacterial and anti-acetylcholinesterase (AChE) activities, as well as their ability to inhibit or activate cell protein phosphatase 1 (PP1). The most interesting activities were obtained from extracts of Ircinia felix, Pandaros acanthifolium, Topsentia ophiraphidites, Verongula rigida and Neofibularia nolitangere. Aqueous and organic extracts of I. felix and V. rigida showed strong antibacterial activity. Topsentia aqueous and some organic extracts were strongly hemolytic, as were all organic extracts from I. felix. The strongest hemolytic activity was observed in aqueous extracts from P. acanthifolium. Organic extracts of N. nolitangere and I. felix inhibited PP1. The aqueous extract from Myrmekioderma styx possessed the strongest hemagglutinating activity, whilst AChE inhibiting activity was found only in a few sponges and was generally weak, except in the methanolic extract of T. ophiraphidites.     

Acetylcholinesterase-Inhibiting Activity of Pyrrole Derivatives from a Novel Marine Gliding Bacterium, Rapidithrix thailandica

Acetylcholinesterase-inhibiting activity of marinoquinoline A (1), a new pyrroloquinoline from a novel species of a marine gliding bacterium Rapidithrix thailandica, was assessed (IC₅₀ 4.9 μM). Two related pyrrole derivatives, 3-(2′-aminophenyl)-pyrrole (3) and 2,2-dimethyl-pyrrolo-1,2-dihydroquinoline (4), were also isolated from two other strains of R. thailandica. The isolation of 3 from a natural source is reported here for the first time. Compound 4 was proposed to be an isolation artifact derived from 3. The two isolated compounds were virtually inactive in the acetylcholinesterase-inhibitory assay (enzyme inhibition < 30% at 0.1 g L⁻¹).