Two-step total synthesis of an anti-MRSA and myosin-inhibiting marine natural product pentabromopseudilin via Suzuki-Miyaura coupling of a MIDA boronate ester

A marine natural product isolated from Pseudoalteromonas sp., pentabromopseudilin, with promising anti-MRSA and myosin ATPase inhibition activities was synthesized in two steps using recently developed MIDA boronate Suzuki-Miyaura coupling technology. Additionally, bromination was shown to be necessary for the antimicrobial activity of pentabromopseudilin.     

Densazalin,a New Cytotoxic Diazatricyclic Alkaloid from the Marine Sponge Haliclona densaspicula

Densazalin, a polycyclic alkaloid, was isolated from the marine sponge Haliclona densaspicula collected in Korea. The complete structure of the compound was determined by spectroscopic methods, including 1D and 2D nuclear magnetic resonance techniques, high-resolution mass spectrometry, and comparison of the calculated and measured electronic circular dichroism spectra. Densazalin possesses a unique 5,11-diazatricyclo[7.3.1.0^2,7]tridecan-2,4,6-triene moiety, which is connected by two linear carbon chains. This compound was derived from the biogenetic precursor bis-1,3-dialkylpyridnium. Densazalin exhibited cytotoxic activity on two human tumor cell lines (AGS and HepG2) in the Cell Counting Kit-8 (CCK-8) bioassay, with IC₅₀ values ranging from 15.5 to 18.4 μM.     

Synthesis of C8-alkyl-substituted purine analogues by direct alkylation of 8-H purines with tetrahydrofuran catalyzed by CoCl_2·6H_2O

C8-Alkyl-substituted purine analogues were synthesized through direct alkylation of 8-H purine with tetrahydrofuran in the presence of Co catalyst in one step. The reactions gave a series of novel C8-oxygen heterocyclic alkyl purine compounds in good yields under mild reaction conditions by the readily available alkylating reagents, providing a complementary route to the classical coupling reactions for the synthesis of C8-alkyl-substituted purine analogues.     

毛细管电泳-电化学检测法用于生物碱电离常数线性模型的研究

依据毛细管区带电泳的特性,推导出在不同pH条件下,有效淌度的倒数(1/μep)与缓冲溶液中氢离子浓度([H^ ])成线性关系,进而建立了用毛细管电泳-电化学检测法测定四种生物碱：苯异丙胺、苯丙醇胺、麻黄碱和甲基麻黄碱电离常数的线性模型和测定方法,测得的pKa值,与紫外分光光度法测定值及文献值比较,结果令人满意．可望在药物离解常数测定的应用中得到推广．     

Anti-Neuroinflammatory Components from Clausena lenis Drake

Clausena lenis Drake (C. lenis) is a folk medicinal herb to treat influenza, colds, bronchitis, and malaria. The 95% and 50% ethanol extract of C. lenis showed significant nitric oxide (NO) inhibition activity in BV-2 microglial cells stimulated by lipopolysaccharide (LPS). Bio-guided isolation of the active extract afforded five new compounds, including a chlorine-containing furoquinoline racemate, (±)-claulenine A (1), an amide alkaloid, claulenine B (2), a prenylated coumarin, claulenin A (3), a furocoumarin glucoside, clauleside A (4), and a multi-prenylated p-hydroxybenzaldehyde, claulenin B (5), along with 33 known ones. Their structures were determined via spectroscopic methods, and the absolute configurations of new compounds were assigned via the electronic circular dichroism (ECD) calculations and single-crystal X-ray diffraction analysis. Compounds 2, 23, 27, 28, 33, and 34 showed potent anti-neuroinflammatory effects on LPS-induced NO production in BV-2 microglial cells, with IC₅₀ values in the range of 17.6–40.9 μM. The possible mechanism was deduced to interact with iNOS through molecular docking.     

一种新手性配体的合成及其锇配合物的催化作用

以1,4-二氯-2,3-二氮杂萘为原料,经两步反应合成了一种新的金鸡纳生物碱衍生物手性配体2,其结构经1H NMR,13C NMR和MS表征。OsO4-2用于催化烯烃的不对称双羟化反应,化学产率91%~94%,e.e.值93%~99%;用于催化烯烃的不对称氨羟化反应,收率45%~63%,e.e.值83%~95%。     

杂环生物碱类化合物的分离及结构鉴定

首次报道从中国南海西沙群岛海绵spongiaobligue中分离得到3个新的含氮生物碱杂环化合物,通过MS,1DNMR,20NMR等波谱数据及元素分析确定它们的结构。     

Alkaloids of Nitraria komarovii. N-Allylnitrarine and Komarovidine N-Oxide

Two new alkaloids, N-allylnitrarine and komarovidinine N-oxide were isolated from the aerial part ofNitraria komarovii.Their structures were established by chemical transformations and spectral data.     

高速逆流制备分离中药黄柏中的生物碱

 利用高速逆流对传统中药黄柏中的生物碱类活性成分进行了制备分离。两相溶剂分离系统采用氯仿 甲醇 0 5mol/LHCl(体积比为 2∶1∶1) ,并对制备物进行了薄层分析。证实了生物碱成分 ,检出了小檗碱。     

鸡尾木生物碱的含量分析

鸡尾木（Excoecaria Venenata S．Lee et F．N.Wei）,大戟科,海漆属,1982年由李树刚、韦发南鉴定为一新树种。鸡尾木的化学成分研究刘绍华等人报道从该植物中分离鉴定出没食子酸、仅一香树脂醇和β-谷甾醇心,作者在该科属植物中发现含有异硫氰酸脂。确定其主要生物碱为2,2,6,6-四甲基-4-哌啶酮、金刚烷胺。本文对鸡尾木叶片中总生物碱及上述两个主要生物碱的含量做了进一步的分析测定。