Bioactive monoterpene indole alkaloids from Nauclea officinalis

Two new monoterpene indole alkaloids, naucleaoffines A (1) and B (2), together with six known alkaloids (3–8), were isolated from the stems and leaves of Nauclea officinalis. The structures of 1 and 2 were elucidated by extensive spectroscopic methods and the known compounds were identified by comparisons with the data reported in literature. All isolated compounds were evaluated for their anti-inflammatory activities and anti-HIV-1 activities. Compounds 1–8 exhibited significant inhibitory activities on nitric oxide (NO) production induced by lipopolysaccharide in mouse macrophage RAW 264.7 cells in vitro with IC₅₀ values comparable to that of hydrocortisone. In addition, compounds 1–8 showed significant anti-HIV-1 activities with EC₅₀ ranged from 0.06 to 2.08 µM. These findings suggest that the discoveries of these indole alkaloids with significant anti-inflammatory activities and anti-HIV-1 activities isolated from N. officinalis could be of great importance to the development of new anti-inflammatory and anti-HIV agents.     

半夏总生物碱对帕金森病大鼠的学习记忆及氧化应激反应的影响

目的 探讨半夏总生物碱(total alkaloids from Pinellia Ternate,TAPT)对帕金森病模型大鼠的防治作用及其抗氧化机制.方法 采用脑内定位注射6-羟基多巴胺(6-OHDA)建立帕金森病大鼠模型,在模型建立成功的同时给予半夏总生物碱预防性治疗.采用Morris水迷宫进行帕金森病大鼠的行为学检测,用化学比色法检测大脑皮质及血清超氧化物歧化酶(SOD)活力、丙二醛(MDA)、过氧化氢(H2O2)和还原型谷胱甘肽(GSH)的含量.结果 与正常组比较,帕金森病模型组大鼠的逃避潜伏期明显延长(P＜0.01),跨越平台次数明显减少(P＜0.01);经半夏总生物碱治疗组,大鼠逃避潜伏期明显缩短(P＜0.05,P＜0.01),跨越平台次数明显增加(P＜0.01).帕金森病模型组大鼠脑皮质及血清中MDA、H2O2的含量增加,SOD活性及GSH的含量降低(P＜0.01);经半夏总生物碱治疗组,脑皮质MDA、H2O2的含量显著减少(P＜0.01),皮质GSH、SOD含量显著增加(P＜0.01);半夏总生物碱给药组中低浓度组、中浓度组血清MDA的含量无统计学意义(P＞0.05),高浓度组血清MDA含量下降(P＜0.01),各治疗组中血清H2O2含量明显下降(P＜0.01),血清GSH含量显著增加(P＜0.01).结论 半夏总生物碱具有改善学习记忆能力,对抗大鼠神经系统的退行性变有一定的作用,可能通过改变帕金森病模型大鼠皮质部分及血清SOD、GSH的含量,而抑制了MDA和H2O2的产生.     

蕤核叶片解剖结构和组织化学定位研究

采用解剖学和组织化学方法,研究了蕤核(Prinsepia uniflora Batal.)叶片的解剖结构,并对叶片中的黄酮类、生物碱类及多糖的组织化学定位进行了研究。结果表明:蕤核叶片上表皮有角质层,下表皮有气孔分布,气孔密度为278个·mm-2,近轴面栅栏组织细胞2～3层,排列紧密而整齐,含有许多晶体;叶片主脉木质部发达,由多列导管组成。上述特征说明蕤核叶片的解剖结构与环境之间的适应性。组织化学定位显示黄酮多分布于栅栏组织和厚角组织,生物碱含量少,多糖均匀分布于叶肉中。     

Natural neuroprotective alkaloids from Stephania japonica (Thunb.) Miers

Modulating inflammatory responses after stroke can prevent brain injury and, therefore, improve neurological outcome. Stephania japonica (Thunb.) Miers is a Chinese folk medicine with the function of dispelling the “wind and blockage” in the human body according to the Chinese medicine theory, in which the symptoms of stroke are caused by the “wind and blockage” in the body. In this paper, we for the first time linked S. japonica to stroke by clarifying fifteen alkaloidal constituents including five undescribed (1–5) ones and screening out six hasubanan type alkaloids (1–4, 7, 15) that elicited stronger anti-neuroinflammatory activities than the positive drug. Moreover, the total alkaloid fraction (ASJ) with previously undescribed 3 as the main component was subject to the in vivo evaluation of the protective effect in the MCAO-induced brain injury. The results showed that ASJ exhibited potent protective effect against brain injury in the MCAO rat model. The results reported in this paper suggested that the hasubanan alkaloids from S. japonica would be an important molecular source for discovering novel therapeutic agents for neuroinflammation-related diseases, such as stroke diseases.     

碎米莎草茎总生物碱对植物和病原菌的生物活性

以水稻(Oryza sativa)等5种植物和水稻稻瘟病(Magnaporthe grisea)等6种植物病原真菌为试验对象,测定了碎米莎草(Cyperus iria)茎总生物碱对植物和病原菌的生物活性.结果表明,250～4000 μg mL-1的总生物碱对水稻种子的萌发无显著影响,对千金子(Leptochloa chinensis)幼苗的苗高有显著抑制作用.4000μmL-1的总生物碱对烟草(Nicotiana tabacum)、鳢肠(Eclipta prostrate)和车前草(Plantago asiatica)种子的萌发、烟草幼苗的苗高以及水稻、烟草和鳢肠幼苗的鲜重有显著抑制作用,相对较低浓度总生物碱对千金子种子萌发、千金子和车前草幼苗的鲜重以及5种植物幼苗的根长和苗高(烟草幼苗的苗高除外)有显著抑制作用.25～400 μg mL-1的碎米莎草茎总生物碱对小麦赤霉病菌(Fusarium gramblearum)的生长无显著影响,而对苹果轮纹病菌(Physalospora piricola)的生长有显著抑制作用,100～400μg mL-1的总生物碱对稻瘟病菌、油菜菌核病菌(Sclerotinia sclerotiovum)和番茄早疫病菌(Alternaria solani)的生长有显著抑制作用,200～400 μg mL-1的总生物碱对杨树溃疡病菌(Dothiorella gregaria)的生长有显著抑制作用,400μg mL-1的总生物碱对上述病原真菌的抑菌率分别为8.20%、74.87%、40.93%、60.91%、52.70%和16.28%.     

Cyclopeptide alkaloids from Scutia buxifolia Reiss

Scutianene E (1), 3,4,28-tris-epi-scutiaene E (2), 28-epi-scutianene E (3) and scutianene L (4), four neutral cyclopeptide alkaloids, were isolated from Scutia buxifolia Reiss, together with four known cyclopeptide alkaloids, scutianines B, C, D and E. Scutianenes 1-3 are diastereoisomeric compounds, with 3-hydroxyleucine as a β-hydroxy amino acid unit, which is connected to the styryl fragment via an ether bridge, β-phenylserine, as a common ring-bonded amino acid residue. Attached to the amino group of β-hydroxyamino acid is a side chain [trans-CH = CH-Ph]. The structures of the peptides were elucidated by means of spectroscopic analysis, including extensive 2D NMR studies. The stereochemistry for the diastereomeric 3,4,28-tris-epi-scutiaene E and 28-epi-scutianene E was confirmed by X-ray diffraction analysis of their O-acetyl derivatives.     

新疆药用延胡索资源调查

作者对新疆维吾尔自治区的9个市、县进行了药用延胡索的资源调查,采集植物标本70余份,弄清药用种类主要是3种,即Corydalis glaucescens Regel,C.ledebouriana Kir.et Kar.和C.schanginii(Pall.)Fedtsch.;初步了解了3种药用延胡索植物的分布状况,并对块茎中总生物碱的含量作了分析。     

Four New C19-Diterpenoid Alkaloids from Aconitum nagarum Stapf

Four new aconitine-type C₁₉-diterpenoid alkaloids, were isolated from the roots of Aconitum nagarum Stapf which were named as nagarutines A–D ( 1–4 ), together with eleven known compounds ( 5–15 ). The structures of the compounds were identified by IR, HR-ESI-MS, 1D and 2D NMR spectra. All compounds were tested for the inhibitory effect on LPS induced NO production in RAW 264.7 macrophages, compound 7 showed moderate anti-inflammatory activity effect and Inhibition rate is about 44.50%.