Securinega suffruticosa

This review gives an account of the current knowledge on the chemical constituents, biological activity and pharmacological properties of Securinega suffruticosa. A wide range of chemical compounds have been isolated, mainly alkaloids, flavonoids, tannins and lipids. From the pharmacological point of view the most interesting group are the alkaloids, among which securinine, an indolizidine alkaloids containing a unique tricyclic structure.     

正交设计法优化伏毛铁棒锤根中总生物碱的提取工艺

[目的]考察伏毛铁棒锤根中总生物碱的最佳提取工艺。[方法]采用滴定法测定总生物碱的含量,通过正交设计方法,以总生物碱得率为考察指标,优化总生物碱的提取工艺。[结果]总生物碱最佳提取工艺条件为10倍量60%乙醇在40℃超声提取30min。[结论]在最佳工艺条件下,总生物碱得率为0.51%。     

苦木生物碱体外抑制大肠杆菌效果的研究

[目的]测定苦木生物碱对大肠杆菌C249、WM和YL株的体外抑菌效果。[方法]采用平板培养法制备菌液,用微量稀释法测定最小抑菌浓度,用杯碟法进行体外抑菌试验。[结果]脂溶性苦木生物碱在体外对大肠杆菌有较强的抑制作用,对大肠杆菌C249、WM、YL株的抑菌圈直径分别为19.07±0.232、0.77±0.59、23.00±0.21 mm,属高度敏感,最小抑菌浓度分别为3.2、1.6和1.6 mg/ml。水溶性苦木生物碱对上述菌株几乎无抑菌作用,其抑菌圈直径均小于13 mm,属低度敏感。[结论]脂溶性苦木生物碱对大肠杆菌标准强毒株的体外抑菌效果优于硫酸黄连素,与痢菌净和氧氟沙星相当,比氟苯尼考略差,但对在广西分离到的强毒株WM和YL株的体外抑菌效果也明显优于硫酸黄连素、痢菌净和氧氟沙星,与氟苯尼考相当。     

正交试验优化提取壮药马尾千金草生物碱

[目的]优化马尾千金草生物碱的提取条件。[方法]以马尾千金草的总生物碱含量为指标,运用正交试验设计对酸水浓度、料液比、浸提次数3个因素进行考查,优化最佳提取工艺。[结果]酸水浸泡提取的最佳条件为加入10倍的1%酸水液,浸泡提取3次,每次24 h,生物碱得率为0.0751%,马尾千金草生物碱含量为7.51 mg/g。[结论]该提取方法操作较简单、成本低、生物碱得率高,能有效提取马尾千金草总生物碱。     

Halogenated Indole Alkaloids from Marine Invertebrates

This review discusses the isolation, structural elucidation, and biological activities of halogenated indole alkaloids obtained from marine invertebrates. Meridianins and related compounds (variolins, psammopemmins, and aplicyanins), as well as aplysinopsins and leptoclinidamines, are focused on. A compilation of the ¹³C-NMR spectral data of these selected natural indole alkaloids is also provided.     

Evaluation of Pyridoacridine Alkaloids in a Zebrafish Phenotypic Assay

Three new minor components, the pyridoacridine alkaloids 1-hydroxy-deoxyamphimedine (1), 3-hydroxy-deoxyamphimedine (2), debromopetrosamine (3), and three known compounds, amphimedine (4), neoamphimedine (5) and deoxyamphimedine (6), have been isolated from the sponge Xestospongia cf. carbonaria, collected in Palau. Structures were assigned on the basis of extensive 1D and 2D NMR studies as well as analysis by HRESIMS. Compounds 1–6 were evaluated in a zebrafish phenotype-based assay. Amphimedine (4) was the only compound that caused a phenotype in zebrafish embryos at 30 μM. No phenotype other than death was observed for compounds 1–3, 5, 6.     

Bromopyrrole Alkaloids as Lead Compounds against Protozoan Parasites

In the present study, 13 bromopyrrole alkaloids, including the oroidin analogs hymenidin (2), dispacamide B (3) and dispacamide D (4), stevensine (5) and spongiacidin B (6), their derivatives lacking the imidazole ring bromoaldisin (7), longamide B (8) and longamide A (9), the dimeric oroidin derivatives sceptrin (10) and dibromopalau’amine (11), and the non-oroidin bromopyrrolohomoarginin (12), manzacidin A (13), and agelongine (14), obtained from marine sponges belonging to Axinella and Agelas genera have been screened in vitro against four parasitic protozoa, i.e., two Trypanosoma species (T. brucei rhodesiense and T. cruzi), Leishmania donovani and Plasmodium falciparum (K1 strain, a chloroquine resistant strain), responsible of human diseases with high morbidity and, in the case of malaria, high mortality. Our results indicate longamide B (8) and dibromopalau’amine (11) to be promising trypanocidal and antileishmanial agents, while dispacamide B (3) and spongiacidin B (6) emerge as antimalarial lead compounds. In addition, evaluation of the activity of the test alkaloids (2–14) against three different enzymes (PfFabI, PfFabG, PfFabZ) involved in the de novo fatty acid biosynthesis pathway of P. falciparum (PfFAS-II) identified bromopyrrolohomoarginin (12) as a potent inhibitor of PfFabZ. The structural similarity within the series of tested molecules allowed us to draw some preliminary structure-activity relationships. Tests against the mammalian L6 cells revealed important clues on therapeutic index of the metabolites. This is the first detailed study on the antiprotozoal potential of marine bromopyrrole alkaloids.     

抗心肌缺血中药有效成分研究进展

对近5年来国内外抗心肌缺血中药有效成分的研究情况进行了综述。大量研究证实许多中药有效成分如黄酮、生物碱、皂苷、糖苷、酚类可能具有较强的抗心肌缺血作用,很可能会为心肌缺血的防治、特别是为抗心肌缺血药物的开发提供新的策略和方向。     

瘤果黑种草化学成分的初步研究

[目的]通过预实验初步了解瘤果黑种草的化学成分,以对其中的有效成分进行进一步的研究.[方法]采用试管系统预试法和专项检查相结合,对水提物、醇提物、酸性乙醇提取液和石油醚提取部分通过各种显色剂、指示剂的反应,初步确定瘤果黑种草的成分.[结果]瘤果黑种草中含有生物碱、黄酮类化合物、皂甙、强心苷、植物甾醇、还原糖、有机酸、内酯、挥发油、油脂等多种成分.[结论]研究为瘤果黑种草的进一步研究及开发利用提供了一定的科学依据.     

Two new amide alkaloids with anti-leukaemia activities from Aconitum taipeicum

Two new amide alkaloids, named 3-isopropyl-tetrahydropyrrolo [1,2-a] pyrimidine-2,4(1H,3H)-dione (1) and 1-acetyl-2,3,6-triisopropyl-tetrahydropyrimidin-4(1H)-one (2), were isolated from the roots of Aconitum taipeicum. Their chemical structures were characterized on the basis of MS, 1D- and 2D NMR. The anti-leukaemia activities of the compounds were also tested. The results indicated that the compounds exhibited more significant cell growth inhibitory activities against HL-60 cells than adriamycin, with the IC₅₀ of 1.1 ± 0.03 μg/mL and 1.6 ± 0.07 μg/mL respectively. In addition, two compounds showed anti-tumor activities against K562 cells as well.