不同干燥方法对桂枝药材中苯丙素类成分的影响及评价

目的:研究不同干燥方法对桂枝药材中苯丙素类(香豆素、肉桂醇、肉桂酸、桂皮醛、邻甲氧基肉桂醛)化学成分的影响,为桂枝适宜干燥方法的确定提供依据。方法:以苯丙素类化学成分含量为评价指标,分别对晒干、阴干及3种现代加工干燥方法后桂枝的质量进行评价,通过SPSS软件进行主成分分析,利用主成分得分进行综合评价。结果:不同干燥处理方法后有效成分含量差异较大,其中微波干燥使有效成分损失最多,阴干、晒干、低温热风干燥有利于桂枝有效成分的保留。结论:以干燥时间、化学成分含量、外观性状、气味等为评价指标,确定热风干燥50℃为桂枝药材较为适宜的现代干燥加工方法。     

Ferulic acid enhances insulin secretion by potentiating L-type Ca2+ channel activation

Objective: To investigate the effect of ferulic acid, a natural compound, on pancreatic beta cell viability,Ca²⁺ channels, and insulin secretion.Methods: We studied the effects of ferulic acid on rat insulinoma cell line viability using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide viability assay. The whole-cell patch-clamp technique and enzyme-linked immunosorbent assay were also used to examine the action of ferulic acid on Ca²⁺ channels and insulin se...     

我国水生药用动物资源调查与产业发展策略探讨

在第四次全国中药资源普查药用动物专项调研基础上,针对具有多样性的水体生态环境及种类丰富的水生药用动物资源,结合现代生物学技术与传统调查方法,开展了水生药用动物野生资源和养殖资源调查,为水生药用动物资源普查技术规范的制定和完善提供参考。针对我国水生药用动物养殖过程中存在的种质退化、饲料供应短缺、养殖环境污染等问题及形成原因进行分析,提出以野生资源保护为基础、水生药用动物研究为核心、生态化养殖为方向的产业可持续发展策略。     

基于TCMSP数据库中药成分的新型冠状病毒3CL水解酶抑制剂虚拟筛选

目的运用分子对接技术模拟预测TCMSP数据库中药成分对新型冠状病毒(SARS-Co V-2)3CL水解酶的作用。方法基于SARS-Co V-2 3CL水解酶的PDB晶型结构(6LU7),构建虚拟靶标模型,以TCMSP数据库中的13 143个化合物为配体筛选对象,以6LU7原配体分子为对照,采用薛定谔2018软件,以Glide程序建立6LU7分子对接体系。然后以原配体分子的对接打分结果为阈值,口服生物利用度(OB)≥30%或类药性(DL)≥0.18为标准筛选候选化合物。最后建立"成分-药材-归经-功效"网络,对候选成分的主要药材归属和作用功效进行总结。结果按照对接打分、OB、DL筛选标准,共筛选得到60个化合物。受体-配体相互作用结果显示,候选化合物主要与靶点蛋白的GLU166、GLY143、ASP187、CYS145、GLN189和LEU141等发生氢键作用。网络预测结果显示,所筛选化合物主要归属药材为甘草、桑白皮、满山红、虎杖和车前草等,肺脏是作用的关键靶器官,其作用功效以清热解毒、止咳祛痰、泻肺平喘等为主。结论对TCMSP数据库化合物进行虚拟分子对接得到的结果为SARS-CoV-2 3CL水解酶抑制剂筛选提供了相关数据。     

药用菊非药用部位的资源化利用现状与展望

菊花Chrysanthemum morifolium是我国传统中药材,其非药用部位的产量远远高于花序,仅菊茎叶产量就为药用部位的3.5倍;长期以来,菊非药用部位未得到充分利用,造成了极大的资源浪费和环境污染,因此,药用菊非药用部位的深入研究与开发值得关注。研究表明,菊非药用部位富含挥发油类、黄酮类、酚酸类以及多糖类等成分,具有抗菌、抗炎、抗氧化、抗惊厥和改善肠道失调等功效。通过对药用菊在栽培和生产过程中所产生的茎、叶、根等非药用部位的化学成分、药理作用及其资源利用现状进行归纳分析,以期为药用菊非药用部位的资源价值发现与产业化提供科学依据和参考。     

Investigation of the central and peripheral actions of clonidine and methoxamine using a new in vivo rat preparation

A cross-circulation technique was developed in rats to distinguish central from peripheral cardiovascular actions of drugs. The right common carotid arteries were ligated, and the left common carotid arteries and left and right external jugular veins of two pentobarbital-anesthetized rats were connected with PE tubing so that peripheral blood from one rat. A, supplied the head of another rat, B, and then returned to the body of A, and vice versa, for peripheral blood from rat B. Each rat was artificially ventilated with O₂, the chest was opened, and both subclavian arteries were ligated. The distribution of blood flow was verified by the microsphere technique. Prior to ligation of the subclavian arteries, blood flow from rat A supplied its own brain and both brain hemispheres but not the brain stem of rat B. Following subclavian artery ligation, blood flow from rat A did not supply A's brain, but supplied both hemispheres and the brain stem of rat B. The head of each rat was, therefore, rendered dependent on the carotid arterial blood supply from another rat. The i.v. injection of clonidine (25 μg/kg) into rat A significantly increased mean arterial pressure and slightly, but not significantly, decreased heart rate in rat A, whereas it significantly decreased mean arterial pressure and slightly, but not significantly, decreased heart rate in rat B. Conversely, i.v. injection of methoxamine (25 μg/kg) in rat A significantly increased mean arterial pressure and decreased heart rate in rat A, and significantly increased mean arterial pressure and slightly, but not significantly, increased heart rate in rat B. Therefore, this rat cross-circulation preparation can be used to separate the central and peripheral cardiovascular actions of drugs.     

整合代谢组学和网络药理学探究蕲艾的安全性与毒理学机制

目的 基于代谢组学和网络药理学分析相结合的方法探究蕲艾Artemisia argyi的安全性与毒理学机制。方法 采用气相色谱-质谱（gas chromatography-mass spectrometry,GC-MS）和超高效液相色谱串联四极杆飞行时间质谱（ultra performance liquid chromatography coupled to tandem quadrupole time-of-flight mass spectrometry,UPLC-Q-TOF-MS）技术分析蕲艾挥发油组分（essential oil from A. argyi,AAEO）、石油醚组分、醋酸乙酯组分、正丁醇组分和水组分的化学组成;利用KM小鼠连续7 d给药评价AAEO和4个非挥发性组分的安全性;代谢组学技术检测AAEO干预前后肝脏内源性代谢物的变化;网络药理学分析AAEO肝毒性的潜在成分和作用靶点;整合代谢组学和网络药理学并构建“代谢物-反应-酶-基因”相互作用网络揭示AAEO肝毒性的毒理学机制。结果 共鉴定出AAEO中39个成分,占挥发油含量的89.30%;从4个非挥发性组分中共鉴定出34个成分。与对照组比较,AAEO显著增加小鼠肝脏指数（P＜0.05、0.01）,上调肝脏丙氨酸氨基转移酶（alanine aminotransferase,ALT）和天冬氨酸氨基转移酶（aspartate aminotransferase,AST）的活性（P＜0.01）,并损伤肝脏组织病理结构呈现出明显肝毒性。代谢组学结果显示给予AAEO后肝脏的17个代谢物水平发生显著变化,包含9种氨基酸,主要涉及苯丙氨酸、酪氨酸和色氨酸生物合成,丙氨酸、天冬氨酸和谷氨酸代谢等途径;网络药理学分析提示樟脑、侧柏酮、石竹素、(−)-宁酮等10个成分是AAEO中潜在的肝毒性物质;整合代谢组学和网络药理学分析筛选出苯丙氨酸羟化酶（phenylalanine hydroxylase,PAH）为AAEO肝毒性的关键靶点,且PAH mRNA和蛋白表达在AAEO高、低剂量组均显著降低（P＜0.05、0.01）,揭示AAEO通过下调PAH表达抑制酪氨酸生物合成产生肝毒性。分子对接结果显示10个潜在毒性物质与PAH结合能均小于−20.00 kJ/mol。结论 结合代谢组学和网络药理学阐明了蕲艾的毒性组分、可能的毒性物质及毒理学机制,为蕲艾产业的发展和临床应用提供了依据。     

Models of drug-induced liver injury for evaluation of phytotherapeutics and other natural products

Extracts from medicinal plants, many of which have been used for centuries, are increasingly tested in models of hepatotoxicity. One of the most popular models to evaluate the hepatoprotective potential of natural products is acetaminophen (APAP)-induced liver injury, although other hepatotoxicity models such as carbon tetrachloride, thioacetamide, ethanol and endotoxin are occasionally used. APAP overdose is a clinically relevant model of drug-induced liver injury. Critical mechanisms and signaling pathways, which trigger necrotic cell death and sterile inflammation, are discussed. Although there is increasing understanding of the pathophysiology of APAP-induced liver injury, the mechanism is complex and prone to misinterpretation, especially when unknown chemicals such as plant extracts are tested. This review discusses the fundamental aspects that need to be considered when using this model, such as selection of the animal species or in vitro system, timing and dose-responses of signaling events, metabolic activation and protein adduct formation, the role of lipid peroxidation and apoptotic versus necrotic cell death, and the impact of the ensuing sterile inflammatory response. The goal is to enable researchers to select the appropriate model and experimental conditions for testing of natural products that will yield clinically relevant results and allow valid interpretations of the pharmacological mechanisms.     

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??OBJECTIVE To study the effects of anti-inflammatory active fraction (AF) from the tuber of Scirpus yagaraohwi in mice with intracerebral haemorrhage(ICH). METHODS A 25 ??L volume of autologous nonanticoagulated blood was collected from the tail artery of the mouse and then injected into the striatum using a syringe pump. Neurological deficits of the mouse was assessed 1, 3 and 5 days after ICH using a 28-point neurological deficit scale, and brain water content of the mouse cerebral tissues after ICH was measured at third day. The concentrations of pro-inflammatory cytokines in perihematoma tissues, including interleukin-6, interleukin-1?? and tumor necrosis factor-??, were measured by ELISA assay. RESULTS The results show that AF significantly reduced the neurological deficit scores and the brain water content after ICH. AF also markedly inhibited the levels of IL-6, IL-1?? and TNF-?? at first day and third day after ICH. CONCLUSION Anti-inflammatory active fraction of Scirpus yagaraohwi can improve the brain injury in mouse induced by ICH. The mechanism may involve decreased expression of pro-inflammatory cytokines of mouse after ICH.