鲍鱼、海龟甲及海蒿子等提取物对凝血和纤溶系统的影响

采用家兔为实验动物,对６种海洋生物提取液分别进行了家兔体内和体外凝血及纤溶系统的实验。试验证明：鲍鱼２号、海龟甲及海蒿子提取液对家兔（体内、外）有非常显著的抗凝作用,海龟甲、鲍鱼１号对增强家兔纤维蛋白溶解活性有非常显著的作用。这对“活血化瘀”药物的研究提供了资料,具有一定的临床应用价值。     

低分子肝素的抗血栓作用

研究了低分子肝素 (lowmoleculerweightheparin ,LMWH)的抗血栓作用 .研究表明 ,静脉注射LMWH (40 0、2 0 0IU/kg)能明显降低家兔高、中、低切比粘度 (P <0 .0 1) ,并显著降低家兔体内实验性血栓湿重及干重 (P <0 .0 0 1) ;静脉注射LMWH 40 0、2 0 0IU/kg及 30 0、15 0IU/kg能分别抑制家兔及小鼠ADP诱导的血小板聚集作用 (P <0 .0 0 1) .实验证明 ,相对分子质量为 6 40 0的低分子肝素有抗血栓作用 .     

铜锤玉带草的抗炎镇痛作用

目的研究铜锤玉带草的抗炎镇痛作用。方法健康小鼠192只,每48只随机分为4组(n=12),分别为空白对照(生理盐水)组,水提取液(1 g·mL^(-1))组,醇提取液(1g·mL(-1))组,醇提取液(1g·mL^(-1))组以及阿司匹林(0.02 g.mL(-1))组以及阿司匹林(0.02 g.mL^(-1))组,分别采用二甲苯致小鼠耳廓肿胀法和10%蛋清致小鼠足跖肿胀法研究铜锤玉带草的抗炎作用。应用醋酸致小鼠扭体法、小鼠热板法研究其镇痛作用。结果醋酸致小鼠扭体实验中,空白对照组与水提取液组、醇提取液组比较有显著差异(P<0.05或P<0.01);与阿司匹林组比较有非常显著差异(P<0.01)。二甲苯致小鼠耳廓肿胀实验中,空白对照组与水提取液组、醇提取液组比较有非常显著差异(P<0.01);与阿司匹林组比较有非常显著差异(P<0.01)。铜锤玉带草可抑制二甲苯致小鼠耳廓肿胀和10%蛋清致小鼠足跖肿胀,能提高热板法小鼠的痛阈值,减少醋酸致小鼠扭体反应的次数。结论中药铜锤玉带草有一定的镇痛、抗炎作用。     

溶栓1号抗血小板聚集及抗血栓形成作用

溶栓 1号是从蚯蚓中提取的酸性蛋白酶 ,并经进一步纯化 ,可静脉给药考察对ADP诱导的家兔血小板聚集的抑制作用 ;并采用小鼠肺血栓模型 ,电刺激致家兔颈动脉血栓模型及穿线法形成家兔颈动脉血栓模型 3种实验性血栓模型 ,考察溶栓 1号的抗血栓形成作用。实验结果表明 :溶栓 1号静脉注射给药 (1 5 0、3 0 0、60 0u/kg)可明显抑制ADP诱导的家兔血小板聚集作用 ,并可明显抑制小鼠肺血栓、家兔颈动脉血栓的形成。溶栓 1号抑制血栓形成可能与抑制血小板活性有关     

肚痛丸体内抗菌作用研究

目的：对肚痛丸提取液进行体内抗菌活性试验。方法：采用体外抗菌试验方法。结果：肚痛丸提取液对志贺菌、金黄色葡萄球菌、沙门菌、大肠杆菌和绿脓杆菌等感染的小鼠均有较好的治疗作用。结论：肚痛丸提取液在体内对肠道常见细菌具有显著的抗菌作用。     

胃炎Ⅰ号和胃炎Ⅱ号药用有效成份对乙酰胆碱酯酶和Na~+-K~+ATP酶活性的影响

以水为溶剂,在50℃和100℃条件下提取胃炎Ⅰ号和胃炎Ⅱ号的药用有效成份。提取液中含生物碱、甙类、黄酮类和多糖等化合物。体外酶学实验表明,该提取液在10mg/ml和1mg/ml时对乙酰胆碱酯酶有抑制作用;而在1×10~(-2)mg/ml和1×10~(+3)mg/ml时则对乙酰胆碱酯酶有明显的激活作用;不同浓度的提取液对Na~+-K~+ATP酶均呈抑制作用。对这种激活作用和抑制作用的生理生化及临床意义进行了讨论。     

退热Ⅲ号制剂的药效试验

目的：对退热Ⅲ号口服液的药理作用进行实验研究。方法：以发热、炎症及咳嗽多种动物模型观察了退热Ⅲ号口服液的药效作用。结果：退热Ⅲ号口服液对致热家兔及大鼠体温升高均有明显的退热作用,并能抑制小鼠耳廓的炎性肿胀,并有止咳祛痰作用。结论：证实了退热Ⅲ号口服液治疗感冒、发热、止咳等疾病的作用及其机理,为临床应用提供实验依据。     

绿豆对动物的降血脂作用

本文研究了绿豆对动物的降血脂作用。结果表明,绿豆水醇提取液连续口服7天,对正常小鼠(100g/kg·天)、大鼠(16g/kg·天)血清胆固醇含量有明显的降低作用(P<0.05)。对实验性高胆固醇血症的家兔,绿豆水醇提取液连续口服7天(11.16g/kg·天),也极显著地降低了其血清中胆固醇含量(P<0.01)。急性、亚急性毒理实验表明,本品没有任何毒副作用。     

注射用蝰蛇巴曲酶对家兔凝血功能的影响

目的研究注射用蝰蛇巴曲酶对家兔体内、外凝血功能的影响。方法采用家兔肝脏创伤止血实验观察注射用蝰蛇巴曲酶对家兔体内凝血功能的影响;通过测定血液凝血系统相关参数指标观察注射用蝰蛇巴曲酶对家兔体外凝血功能的影响。结果注射用蝰蛇巴曲酶（0．05～0．20kU·kg^-1）可明显减少家兔肝脏切口的失血量,缩短切口出血时间;并可明显缩短全血凝血时间（CT）、活化部分凝血活酶时间（APTT）及凝血酶原时间（PT）、凝血酶时间（TT）。结论注射用蝰蛇巴曲酶有明显的止血作用,能加强体内凝血系统活性：     

银杏叶提取物制剂、阿司匹林及氯吡格雷抗血小板聚集作用比较及对血小板活化因子含量的影响

目的:观察银杏叶提取物(EGB)制剂、阿司匹林及氯吡格雷对家兔血小板聚集率及血小板活化因子(PAF)含量的影响。方法:采用体内实验,观察EGB制剂、阿司匹林及氯吡格雷对由花生四烯酸(AA)、二磷酸腺苷(ADP)和PAF诱导的家兔血小板聚集作用的影响,以及对给药前后家兔PAF含量的影响。结果:与生理盐水组比较,EGB制剂抑制AA、ADP、PAF诱导的家兔血小板聚集有统计学差异(P<0.05,P<0.01),并能够降低血清中PAF的含量(P<0.05),阿司匹林对AA诱导的血小板聚集有统计学差异(P<0.01),氯吡格雷对ADP诱导的血小板聚集有统计学差异(P<0.01),而阿司匹林和氯吡格雷对PAF的含量没有显著影响。结论:EGB制剂具有抗血小板聚集作用,抗PAF诱导的血小板聚集作用最强,并能显著降低PAF含量。     

海洋生物提取物抗紫外线作用研究

目的从海洋生物组织中提取制备对紫外线具有较强吸收作用的成分,为建立紫外线损伤的防护提供新方法。方法高压液相纯化海洋生物组织的提取物,观察其紫外吸收特征并绘制曲线,优选出有较强紫外吸收作用的样品,采用细胞培养法观察其对菌落及细胞的保护作用。结果优选出提取物的紫外吸收波长范围在220～300nm,且保持了较高的紫外吸收能力;经菌落抗紫外线和细胞抗紫外线实验证实,该提取物对菌落和细胞具有明显的紫外防护作用,菌落和细胞计数与对照组比较差异均有显著性(P<0.05)。结论本研究制备的海洋生物提取物具有明显的紫外防护作用。     

海洋生物中抗氧化活性成分的研究进展

近30年来，从海洋生物中分离到许多具有抗氧化活性的物质，本文按这些抗氧化活性物质的种类。综述了来自海洋生物的抗氧化活性物质的研究进展。     

Screening of Some Marine Organism Extracts for cAMP Phosphodiesterase Inhibition,Cytotoxicity, and Antiviral Activity against HSV-1

Methanol and hot water extracts of 71 samples of 56 kinds of marine products were subjected to inhibitory test for cyclicAMP phosphodiesterase (cAMP PDE), cytotoxic and anti-viral screening tests. Among them, 7 extracts of marine products showed a significant inhibition for cAMP PDE and 5 extracts showed a significant cytotoxicity against KB cells at concentrations under 20 µg/ml. Eight extracts of marine products showed higher therapeutic indexes against herpes simplex virus type 1 (HSV-1).     

Ultrasensitive detection of domoic acid in mouse blood by competitive ELISA using blood collection cards.

Domoic acid (DA), an analog of the excitatory amino acid glutamate, is produced by the diatom genus Pseudo-nitzschia and acts as a neurotoxin in humans. During diatom blooms, DA can contaminate shellfish, as well as other filter feeding organisms, and can be transferred by ingestion to higher trophic levels, including marine mammals and humans. The prevalence of this algal toxin and its effects on protected species makes measurement of domoic acid in living animals a necessary biomonitoring tool for the near future. Blood collection cards have already been used for the sampling, extraction and detection of brevetoxin in blood from exposed laboratory animals and, more recently, marine mammals. However, a difficulty unique to measuring DA in blood is the rapid rate (>95% in 2h) at which it is cleared from blood. To meet this challenge, a direct competitive ELISA (cELISA), a method of detection with extremely high sensitivity and specificity, was used to analyze the blood of DA-exposed mice after extraction from the blood collection cards. More than 99% of DA was cleared from blood within 4h post dosage; however, domoic acid was still quantifiable (>0.7ngml(-1)) at 4h from blood spot extracts and still detectable at 24h when compared to control blood spots. By using this highly sensitive assay in conjunction with the use of blood spot cards for easy blood sample extraction, this method could be a very effective means of biomonitoring domoic acid in marine mammals in the field, as well as human populations.     

青岛沿海海洋附着生物抗肿瘤活性的筛选

对青岛沿海海洋附着生物资源进行调查，采用海虾细胞毒性法及流式细胞术对已鉴定的18种附着生物进行抗肿瘤活性筛选。结果表明，星座美洲海鞘Amaroucium ecostellatum Verril、大菊海鞘Botryllus magnicoecus Hartmeyer、山形海绵Mycale macilenta、海黍子Sargassum kjellmanianum Yendo、裙带菜Undaria pinnatifida(Harv．)Sur．甲醇提取物具有较强的抗肿瘤活性。并进一步进行活性成分追踪研究，确定星座美洲海鞘、大菊海鞘、山形海绵、海黍子、裙带菜的活性部位。     

Marine natural products influencing larval settlement and metamorphosis of marine sessile organisms]

Most marine sessile organisms have a planktonic larval phase in their life cycles, and then larvae settle and metamorphose into their adult forms. The selection of settlement sites is a critical event for these organisms because settlement on unsuitable places affects their survivorship severely. Ascidians live gregariously, and conspecific chemical cues are thought to play an important role in gregarious settlement of larvae. The extracts of conspecific adults or larvae have been claimed to contain "natural metamorphosis inducers." Little is known, however, about their chemical properties. To discover natural signal substances for larval metamorphosis in ascidians, we surveyed the metamorphosis-inducing activity of the medium conditioned by ascidian larvae, and succeeded in isolating a metamorphosis-inducing substance from the conditioned medium of Halocycthia roretzi larvae and found that it was identical to lumichrome. We have also isolated more than 40 active metabolites, which may mimic lumichrome, from marine sponges. On the contrary, marine sessile organisms cause serious problems by settling on fishing nets, hulls of ships, and cooling systems of power plants. Organotin compounds have been widely used for the control of these organisms, but they are known to be toxic to marine biota. Therefore, nontoxic antifouling substances are urgently needed. Marine sessile organisms possess chemical defense systems using their secondary metabolites, which might be potential by nontoxic antifouling agents. We have attempted to obtain antibarnacle substances from marine sponges and isolated 26 antifoulants.     

Abstracts

Abstract

In order to develop new drugs from underutilized marine sources, the chemistry and medicinal chemistry of pharmacologically active metabolites obtained from these sources were investigated. Marine organisms, including algae, sponges, bryozoans, soft corals, tunicates, etc., were collected. Fresh samples were also examined for the presence of marine microorganisms. Marine microorganisms deserve special attention for secondary metabolite production, because of their biosynthetic diversity and culturability. Their lipophilic extracts were screened using a variety of pharmacological assays. Bioassay-directed separation of active extracts by chromatography didentified many structurally diverse compounds. The isolation, characterization and structure-activity relationships are desribed here for inhibitors of inflammation, 5-lipoxygenase, lipid peroxide formation, and PAF binding.     

Comparative study on plant latex proteases and their involvement in hemostasis: a special emphasis on clot inducing and dissolving properties

In the present study we compared the clot inducing and dissolving properties of Calotropis gigantea R. Br. (Asclepiadaceae), Synadenium grantii Hook. f. (Euphorbiaceae) and Wrightia tinctoria R. Br. (Apocynaceae) latex extracts. All the three latex extracts hydrolyzed casein, fibrinogen and crude fibrin dose-dependently. The proteolytic action on fibrinogen subunity was in the order of Aalpha > Bbeta > gamma. All extracts exhibited procoagulant activity as assayed by re-calcification time. However, thrombin like activity is restricted to C. gigantea. In addition, the extracts dose-dependently hydrolyzed blood and plasma clots. Furthermore, the hydrolyzing pattern of fibrin in the plasma clot was substantiated by SDS-PAGE. The extracts hydrolyzed all the subunits (alpha polymer, alpha-chains, gamma-gamma dimer and beta-chain) of fibrin efficiently. Both fibrinogenolytic and fibrinolytic activity potency of the extracts were in the order of C. gigantea > S. grantii > W. tinctoria. Among the three latices, C. gigantea is toxic with a minimum hemorrhagic dose (MHD) of > 75 microg, whereas S. grantii and W. tinctoria latex extracts were non-toxic and did not induce any hemorrhagic effect at the tested dose (> 200 microg). The proteolytic activity of C. gigantea latex extract on different substrates was inhibited by IAA. On the other hand, the proteolytic activities of S. grantii and W. tinctoria were inhibited by PMSF. Thus, this study provides the basis for the probable action of plant latex proteases to stop bleeding and effect wound healing as exploited in folk medicine.     

21世纪,中国的海洋药物

海洋是一个巨大的药源宝库,本世纪６０年代以来,从海洋动物、植物及微生物中已分离获得新化合物１００００多种,其中１／２以上具有抗肿瘤、抗菌、抗病毒、抗凝血等药理活性;这些新型化合物为药物设计提供了可贵的分子模型,为海洋药物的开发提供了重要的先导化合物库,然而将这些活性化合物开发成药、用于临床可贵的分子模型,为海洋药物的开发提供了重要的先导化合物库,然而将这些活笥化合物开发成药、用于临床的并不多,究其