Hippospongia属海绵化学成分与生物活性研究进展

综述Hippospongia属海绵的化学成分及生物活性。该属海绵次生代谢产物丰富,富含萜类、长链脂肪族类及甾体类化合物,且具有独特的生物活性,包括抗肿瘤、对DNA聚合酶β和HIV逆转录酶抑制作用及冠状血管舒张等作用,具有广阔的开发应用前景。对该属海绵化合物类型进行分类归纳,并对其药理活性研究进行综述,为该属海绵进一步研究开发提供参考。     

掘海绵的化学成分和生物活性研究进展

目的对掘海绵属(Dysidea spp)海绵的化学成分及生物活性进行综述。方法通过检索国内外相关文献,归纳总结了该属海绵的研究情况。结果从该属海绵中已分离鉴定了300个化合物,主要为倍半萜醌类、萜类、甾醇类、溴代衍生物、二酮哌嗪类、多氯取代化合物等;这些化合物具有抗肿瘤、抗炎、抗真菌和抑制HIV-Ⅰ逆转录酶等多种生物活性。结论对掘海绵的化学成分和生物活性的进一步研究提供参考。     

Acanthella属海绵化学成分及生物活性的研究进展

目的对Acanthella属海绵的化学成分及其生物活性进行综述。方法通过综述国内外相关文献,归纳总结了该属海绵的研究概况。结果从该属海绵中已分离鉴定110个化合物,主要为含有异腈基、异硫氰酸酯和甲酰胺等含氮基团的倍半萜、二萜类化合物。这类化合物具有抗疟、抗虫、抗污损、抗肿瘤、抗菌等多样的生物活性。结论为Acanthella属海绵的化学成分及生物活性的进一步研究提供依据。     

Phakellia属海绵次生代谢产物研究进展

海绵是目前海洋天然产物研究中最吸引人的海洋生物之一,海绵中含有丰富的、结构新颖的次生代谢产物,大多数具有显著的生理活性。Phakellia属海绵属于寻常海绵纲软海绵目小轴海绵科,种类较多,分布广泛,在国内外得到了广泛的研究。对近几十年来从Phakellia属海绵中分离鉴定的次生代谢产物进行了系统的归纳整理,这些化学成分主要包括环肽、生物碱、聚醚、萜类、甾醇、炔酸等种类,并对其药理活性进行了简单总结,对Phakellia属海绵的进一步研究开发具有一定的借鉴和指导意义。     

Axinella属海绵化学成分与生物活性研究进展

系统综述了海绵Axinella属的生物碱、三萜、甾体等化学成分,及其抗肿瘤、抗菌、神经保护等生物活性的研究进展,为该属海绵的深入研究提供有用资料。     

Phyllospongia属海绵次级代谢产物及其生物活性研究进展

Phyllospongia属海绵分布较为广泛,其次级代谢产物结构新颖多样,而且活性显著。从该属海绵中发现的次级代谢产物结构类型包括二倍半萜、呋喃萜、溴二苯醚、甾体、磺酸、核苷等类型化合物。其中,二倍半萜类化合物是该属海绵中最为典型的次级代谢产物,而且大多具有较强的生物活性,如细胞毒、抗菌、抗病毒、鱼毒、防附着等,在海绵的化学防御中发挥着重要作用。已有研究对从该属海绵乃至其他海绵中发现活性天然产物及药物先导化合物具有借鉴意义,文中对Phyllospongia属海绵中次级代谢产物的结构及其生物活性进行了简要综述。     

群海绵属化学成分及生物活性研究进展

目的 对Agelas 属海绵化学成分和生物活性进行研究总结。方法 通过文献调研,对该属海绵代谢产物类型进行分类整理,并对其生物活性进行总结报道。结果 目前报道的Agelas 属海绵主要含有溴吡咯生物碱、萜类生物碱、鞘糖脂、甾醇、类胡萝卜素和脂肪酸等类型的代谢产物,许多具有良好的生物活性,包括抗肿瘤、抗疟、抗微生物、抗组织胺及免疫调节等活性。结论 Agelas属海绵次生代谢产物丰富,类型多样,并具有良好的生物活性,因此有广阔的开发应用前景。本文为该属海绵的进一步化学与生物活性研究开发提供参考。     

Dactylospongia属海绵的化学成分及生物活性研究进展

Dactylospongia属海绵中已报道的次生代谢产物主要包括倍半萜醌和倍半萜氢醌类、倍半萜衍生物、大环内酯及甾醇等结构类型,大多具有良好的生物活性,包括抗肿瘤、抗炎及抗菌等。本文根据化合物的结构类型综述了1989-2014年之间经文献报道的Dactylospongia属海绵的化学成分和生物活性,为该属海绵的进一步研究开发提供了参考。     

Phakellia属海绵次生代谢产物研究进展

海绵是目前海洋天然产物研究中最吸引人的海洋生物之一,海绵中含有丰富的、结构新颖的次生代谢产物,大多数具有显著的生理活性。Phakellia属海绵属于寻常海绵纲软海绵目小轴海绵科,种类较多,分布广泛,在国内外得到了广泛的研究。对近几十年来从Phakellia属海绵中分离鉴定的次生代谢产物进行了系统的归纳整理,这些化学成分主要包括环肽、生物碱、聚醚、萜类、甾醇、炔酸等种类,并对其药理活性进行了简单总结,对Phakellia属海绵的进一步研究开发具有一定的借鉴和指导意义。     

锉海绵属海绵Xestospongia sp.甾体类成分研究

目的 对广西涠洲岛北部湾海域来源的锉海绵属（Xestospongia）海绵中获得的结构新颖、活性良好的甾体类成分进行研究。方法 根据甾体类化合物的结构特性，利用多种柱色谱和高效液相色谱（HPLC）等方法，通过高分辨质谱（HRMS）、核磁共振（NMR）和旋光（ORD）等方法并结合文献对照对化合物进行结构鉴定。结果 从锉海绵属海绵中分离得到9个甾体化合物，分别为7-ketocholesterol (1)、3β-Hydroxy-24-methylene-5-cholesten-7-one (2)、(22E)-3β-Hydroxychoiesta-5,22-dien-7-one (3)、(22E)-3β-Hydroxychiest-5,22-diene-7,24-dione (4)、Dictyopterisin G (5)、Dictyopterisins D (6)、Dictyopterisins E (7)、antrocarine E (8)和Fucosterol (9)。结论 化合物2-8均为首次从该属海绵中分离得到，6和7母核上C-7位为少见的甲氧基，8是首次从海绵中分离得到5-OH和7羰基的甾体化合物。     

细薄星芒海绵的三萜成分研究

目的对中国南海海域细薄星芒海绵的三萜成分进行研究。方法采用硅胶柱色谱、Sephadex LH-20凝胶色谱、ODS C18柱色谱、半制备型HPLC等方法进行分离,根据理化性质和波谱分析鉴定化合物的结构。结果分离并鉴定了5个异玛拉巴烷型三萜化合物,分别为stelletinA（Ⅰ）,stelletin B（Ⅱ）,22,23-dihydrostelletin D（Ⅲ）,jaspolide B（Ⅳ）和jaspolide A（Ⅴ）。结论化合物Ⅲ～Ⅴ首次从该种海绵中获得。     

南海细薄星芒海绵抗肿瘤活性成分研究(Ⅱ)

目的研究细薄星芒海绵Stelletta tenuisLindgren的抗肿瘤活性成分。方法利用溶酶萃取和多种层析手段,以体外细胞毒模型跟踪筛选,对南海细薄星芒海绵的抗肿瘤活性成分进行追踪分离,应用波谱技术,并结合文献对照,对所分离得到的化合物进行结构鉴定。结果得到8个异玛拉巴烷(isomalabaricane)型三萜类化合物,其结构分别鉴定为:stellettin B(1),C(2),D(3),E(4),rhabdastrellic acid A(5),stellettin H(6),22,23-dihydrostellettin B(7),geoditin A(8)。结论化合物1-8均系首次从中国南海海绵Stelletta ten-uisLindgren中获得,并归属了它们的1H NMR和13C NMR数据。     

Effects of methysergide, pizotifen and ergotamine in the monkey cranial circulation.

Internal and external carotid vascular resistances were measured, in anaesthetized monkeys, to asses the direct cranial vascular effects of i.v. methysergide, pizotifen and ergotamine, and their effects on the cranial vascular responses to the constrictors 5-hydroxytryptamine and noradrenaline and the dilators histamine, prostaglandin E1 and bradykinin. Methysergide reduced responses to 5-HT, and tended to potentiate the external carotid responses to noradrenaline. Pizotifen blocked responses to histamine; it tended to reduce internal carotid responses to 5-HT, but it potentiated external carotid 5-HT responses. Ergotamine reduced responses to 5-HT and noradrenaline, but this was probably related to its cranial vasoconstrictor effects, especially in the external carotid circulation. Methysergide induced weak transient cranial vasoconstriction and pizotifen had no direct effects. These findings may be relevant to the therapeutic actions of these drugs in migraine, since the doses used approximated to those used clinically.     

Evidence for the presence of P1-purinoceptors on cholinergic nerve terminals in the guinea-pig ileum

The inhibitory effects of adenosine, ATP, 5'-adenylyl methylene diphosphonate (beta, gamma-meATP) and adenosine 5'-alpha, beta-methylene triphosphonate (alpha, beta-meATP) were compared on the cholinergic twitch responses to transmural stimulation of the guinea-pig ileum. Adenosine, ATP and beta, gamma-meATP reduced the twitch responses in a concentration dependent manner. Theophylline antagonized and dipyridamole potentiated the inhibitory responses to adenosine, ATP and beta, gamma-meATP. Inhibitory responses to alpha, beta-meATP were usually preceded by an enhancement in twitch height. Contractions of the unstimulated ileum to alpha, beta-meATP were blocked by atropine and tetrodotoxin while those elicited by ATP were unaffected, which suggests that the initial excitatory effects of alpha, beta-meATP may be due to its ability to release ACh from cholinergic nerve terminals. Use of high pressure liquid chromatography and bioluminescence assay techniques demonstrated the ability of the tissue to degrade ATP and beta, gamma-meATP and, at a much slower rate, alpha, beta-meATP. Inhibitory responses to ATP, AMP and beta, gamma-meATP were reduced by adenosine deaminase, which also abolished responses to adenosine. 5'-AMP deaminase abolished responses to AMP and adenosine, and reduced those to ATP and beta, gamma-meATP. The results suggest that the inhibitory effect of ATP on cholinergic neurotransmission is due to its rapid breakdown to AMP or adenosine, which act on prejunctional P1-purinoceptors.     

Toxicology in the Service of Patient and Medication Safety: a Selected Glance at Past and Present Innovations

Medical and medication errors remain definite threats to patients in US health care. Medical toxicologists frequently encounter patients either harmed by or at risk for harm from adverse drug events, including medication errors and inadvertent exposures. An historical perspective, as viewed through the lens of specific disciplines, can be useful to trace systemic responses to safety threats. Early efforts to address anesthesia perioperative risks and recent actions in medicine, surgery, and obstetrics to introduce checklists, communication tools, and systems approaches are reviewed. Patient safety concepts can be utilized and disseminated by toxicologists to improve medication safety and drive innovative approaches to confront patient harm. Various approaches include simulation of high-risk scenarios which might predispose to medication error, assembling multidisciplinary groups of health care providers to review events and implement mitigation strategies, and proactive patient safety rounds in clinical areas to allow frontline staff to voice concerns and introduce solutions for administration, evaluation, and implementation. We review selected lessons from the past and current innovations to achieve safe medication practice.     

Development of in vitro systems for nanotoxicology: methodological considerations

Due to the rapid development of a diverse array of nanoparticles, used in a wide variety of products, there are now many international activities to assess the potential toxicity of these materials. These particles are developed due to properties such as catalytic reactivity, high surface area, light emission properties, and others. Such properties have the potential to interfere in many well-established toxicity testing protocols. This article outlines some of the most frequently used assays to assess the cytotoxity and biological reactivity of nanoparticles in vitro. The article identifies key issues that need to be addressed in relation to inclusion of relevant controls, assessing particles for their ability to interfere in the assays, and using systematic approaches to prevent misinterpretation of data. The protocols discussed range from simple cytotoxicity assays, to measurement of reactive oxygen species and oxidative stress, activation of proinflammatory signaling, and finally genotoxicity. The aim of this review is to share knowledge relating to nanoparticle toxicity testing in order to provide advice and support for guidelines, regulatory bodies, and for scientists in general.     

Race and Ethnic Differences in Attempts to Cut Down or Quit Substance Use in a High School Sample

Abstract

Much attention has been given to the initiation and progression of substance involvement of youth. Less is known about decrements in substance use and cessation efforts among adolescents from diverse race/ethnic backgrounds. The present study examined substance use and attempts to reduce or quit substance use among adolescents from three race/ethnic groups. Participants were 3,756 Asian-American, Latino, and White high-school students surveyed regarding use of cigarettes, alcohol, illicit drugs, alcohol-related consequences, and substance use cessation efforts. Results indicated that Latino and White students had similar lifetime prevalence rates of alcohol, cigarette, and illicit drug use relative to Asian Americans. Although Latino youths reported lower or comparable rates of alcohol use compared to Whites, they experienced more legal consequences related to their use. A higher proportion of Latinos indicated attempts to reduce or stop alcohol use in comparison to Asian Americans and Whites, and to reduce/stop drug use in comparison to Whites. Adolescents experiencing negative alcohol-related consequences were more apt to attempt to change their substance use than students reporting no consequences. However, few race/ethnic differences were identified in regard to preferred strategies to restrict or cease substance involvement. Implications for adolescent substance use interventions are discussed.     

Further studies on the site of action of nicotinic blocking drugs

The effects of combinations of tubocarine and physostigmine, and of physostigmine and edrophonium alone, have been studied on the responses of the chick biventer cervicis muscle to nerve stimulation and to exogenous acetylcholine. The effects of hexamethonium, tetraethylammonium and triethylcholine have also been studied on the dose-response curves for acetylcholine, determined in the presence of low concentrations of physostigmine.Suitable combinations of tubocurarine and physostigmine reduced responses of the muscle to nerve stimulation, whilst leaving the responses to acetylcholine unaffected, whereas physostigmine and edrophonium augmented responses to acetylcholine, whilst leaving responses to nerve stimulation unaffected. These results indicate that the multiply innervated fibres of the muscle are particularly sensitive to inhibition of cholinesterase.Hexamethonium, tetraethylammonium and triethylcholine, drugs that are known to exhibit actions similar to that of the combination of tubocurarine and physostigmine, and also to possess anticholinesterase activity, depressed responses to acetylcholine determined in the presence of concentrations of physostigmine sufficiently low to possess a specific inhibitory action on cholinesterase. The results indicate that the neuromuscular block produced by large concentrations of these drugs is probably post-junctional in origin.     

A template of information needs for decision-making about delaying remediation on contaminated lands to protect human health

ABSTRACT

The contamination legacy of industrialization, militarization, and nuclear arms race poses current or future risks to populations and the environment. Responsible parties and regulators make decisions regarding which sites to clean up, how, how much, and when. This study aimed to provide an information needs template to evaluate and reduce risks to human health when considering whether to initiate or delay remediation. This investigation focused on four aspects of timing and prioritization: 1) management, planning and implementation, 2) source terms, pathways, and exposures, 3) risks and receptors, and 4) external drivers. Within each type, issues were identified and described. Management class included personnel, health and safety data, funding, equipment, and structural integrity. Source term included contaminant sources, pathways, initiating events, and barriers to exposure. Risk included types and exposures to workers and general public. External drivers included regulatory framework, stakeholders, Congressional mandates, and economic and social contexts. Risk may increase over time as contamination spreads, enters aquifers, and reaches receptors, and may decline as radionuclides decay, and plumes dissipate. The overall objective was to provide a template of information that is useful to managers and regulators, and might be used by the public to understand the risks and benefits of re-prioritization cleanup.     

Perceived risks and benefits of quitting smoking in non-treatment seekers

Little is known about beliefs about quitting and treatment motivation in non-treatment seeking smokers. One hundred eighty-eight daily cigarette smokers not currently motivated to quit smoking completed measures of perceived risks and benefits of quitting and motivation to quit. Self esteem related to quitting was positively related to desire to quit, expected success at quitting, confidence in quitting, and motivation to quit. Greater perceived risks of cravings was related to greater expected difficulty of remaining abstinent, and greater perceived risk of increased negative affect was related to decreased expectation of success at quitting, confidence for quitting, and increased expectation for difficulty remaining abstinent. Greater perceived risk of weight gain was related to being less likely to have a goal of complete abstinence. There were no gender, ethnicity, age, or education differences in the relationship of perceived risks and benefits of quitting and motivation. Knowing the risks and benefits that relate to motivation to quit for non-treatment seeking smokers provides the foundation for targeting this group in campaigns to increase quit motivation.