Treatment with coumarin to prevent or delay recurrence of malignant melanoma

Both coumarin (1,2-benzopyrone) and warfarin (4-hydroxycoumarin) have been shown to prevent the recurrence of malignant melanoma. Their action is macrophage-dependent and the dosage is critical. In 1984 a multicentre, prospective, randomised, double-blind trial of coumarin, given as a daily 50-mg dose for 2 years after surgery in patients with high-risk melanoma, was started. The patients had lesions greater than 1.70 mm thick and TNM stage IB or stage II disease. To date there are 4 recurrences in the coumarin-treated group of 13 patients, and 10 recurrences in the placebo-treated group of 14 patients (P<>There were no toxic effects.     

Coumarin induced acral skin necrosis associated with hereditary protein C deficiency

Summary Hemorrhagic skin necrosis of the toes was observed in a patient with heterozygous protein C deficiency (protein C:Ag 32% and protein C activity 30%) on the 4^th day of coumarin treatment overlapping with effective intravenous anticoagulation with heparin. Family studies revealed protein C deficiency in two sisters of the proposita without a history of thromboembolic disease. Immunologic studies in the proposita at the time of coumarin necrosis revealed slight depression of complement factor C4 and the presence of immune complexes. The present case and review of the literature show that the pathogenetic mechanism leading to coumarin necrosis in patients with protein C deficiency seems not yet to be fully understood.     

白芷根中香豆素类成分的组织化学定位研究

目的：确定香豆素在白芷药用部位根中的积累部位,为进一步揭示白芷活性成分香豆素类及其积累规律与白芷内部结构及发育的关系奠定基础。方法：结合冰冻切片技术、荧光显微技术对白芷根中香豆素类成分进行组织化学定位研究。结果：白芷木栓层、木质部和栓内层、韧皮部中分布的分泌组织在紫外光的激发下,均有明显的蓝色荧光发生,其中分泌组织的荧光与对照品欧前胡素的荧光相同,而同步阴性对照实验中分泌组织的荧光消失。结论：在白芷根中,香豆素类成分分布于分泌组织内。     

退黄藤中东莨菪内酯的分离纯化及含量测定

目的 分离纯化退黄藤中的东莨菪内酯并测定其含量.方法 采用硅胶柱色谱分离纯化退黄藤中的东莨菪内酯,并根据理化性质及光谱数据鉴定其结构;采用HPLC法测定其含量,色谱柱为Zorbax Eclipse XDB-C1s柱(250 mm ×4.6 mm,5μm),流动相为甲醇-0.1％冰乙酸(39∶61),流速1.0 mL·min-1,检测波长345 nm.结果 东莨菪内酯3.11 ～31.1 μg·mL-1与峰面积呈良好的线性关系(r =0.9999),平均回收率为99.29％,RSD=1.40％(n=6).结论 所用方法简便、准确、快速,可用于退黄藤药材的质量控制.     

(3S,4S)-3-氨基-4-氨羰氧甲基-2-吖叮啶酮-1-磺酸钠衍生物的合成与抗菌活性

以(3S,4S)-3-氨基-4-氨羰氧甲基-2-吖叮啶酮-1-磺酸钠为母核,选择D-(-)-2-(7或8-甲氧基香豆素-3-甲酰胺基)-2-苯或4-羟基苯乙酸和D-(-)-α-(4-乙基-2,3-二氧-1-哌嗪甲酰胺基)-2-苯或4-羟基苯乙酸作为边链,合成6个新的单胺菌素衍生物:(3S,4S)-3-[D-(-)-2-(8或7-甲氧基香豆素-3-甲酰胺基)-2-(苯或4-羟基苯)乙酰胺基]-4-氨羰氧甲基-2-吖叮啶酮-1-磺酸钠Ⅳ_(1-4);(3S,4S)-3-[D-(-)-α-(4-乙基-2,3-二氧-1-哌嗪甲酰胺基)-2-(苯或4-羟基苯)乙酰胺基]-4-氨羰氧甲基-2-吖叮啶酮-1-磺酸钠Ⅳ_(5-6)。初步体外抑菌试验表明,化合物Ⅳ_5,Ⅳ_6对革兰氏阴性菌有较强的抗菌活性。     

大丁草中抗菌活性成分的研究

从菊科植物大丁草Gerbera anandvia(L.)Sch Bip.(Leibnitzia anandria(L.)Nakai)全草中分离出十二种化合物。经化学反应及光谱分析鉴定、确定了其中九个化合物的结构。共中晶Ⅷ(大丁纤维二糖甙,5-methyl-coumarin-4-cellobioside)和晶Ⅸ(大丁龙胆二糖甙,5-methyl-coumarin-4-gentiobioside)为二个新的天然产物。其它七种化合物为大丁双香豆特(Ⅰ)、大丁甙元(Ⅱ)、琥珀酸(Ⅲ)、大丁甙(Ⅴ)、木犀草素7-β-D-葡葡糖甙(Ⅵ)、蒲公英赛醇(Ⅺ)和β-谷甾醇(Ⅻ)。其中晶Ⅰ,Ⅱ,Ⅲ,Ⅷ和Ⅸ显示了不同程度的抗菌活性。     

Synthesis,in‐vitro Antimicrobial and Cytotoxic Studies of Novel Azetidinone Derivatives

Developing novel antimicrobial drugs is increasingly important in the modern pharmaceutical industry. A series of novel 3‐chloro‐4‐[4‐(2‐oxo‐2H‐chromen‐4‐ylmethoxy)phenyl]‐1‐phenylazetidin‐2‐ones 5a–o have been synthesized from 4‐bromomethylcoumarins 1a–e and 4‐aryliminomethyl‐phenols 3a–c . These compounds were screened for their in‐vitro antibacterial activity against two Gram‐positive (Staphylococcus aureus and Vancomycin resistant enteroccoccus) and two Gram‐negative (Escherichia coli and Shigella dysentery) bacterial strains and antifungal activity against Aspergillus fumigatus, Candida albicans, and Penicillium. Results revealed that compounds 5c , 5f , 5h , 5j , and 5m showed excellent activity against a panel of microorganisms. The brine‐shrimp bioassay was also carried out to study their in‐vitro cytotoxic properties and two compounds, 5h and 5m , possessing LD₅₀ = 7.154×10^–4 M and 5.782×10^–4 M, respectively, displayed potent cytotoxic activity against Artemia salina. The presence of a chlorine group in the coumarin moiety, its effect on their antibacterial, antifungal, and cytotoxic activities is discussed. All newly synthesized compounds were characterized by elemental analysis, IR, ¹H‐NMR, ¹³C‐NMR, and MS.     

正交试验法优选秦皮提取工艺

目的:优选秦皮提取工艺。方法:采用L9(34)正交试验设计,以秦皮甲素、秦皮乙素、出膏率为考察指标,考察溶媒倍量、提取时间和提取次数等因素对秦皮甲素、秦皮乙素提取转移率的影响。结果:秦皮最佳提取工艺为A3B3C3,即加10倍量水回流提取3次,每次2h。结论:提取工艺简便可行。     

大丁草中抗菌活性成分的研究Ⅳ

从秋季采收的菊科植物大丁草Gerbera anandria(L.)Sch Bip.全草中共分出十三种成分。本文报道其中三个新化合物的结构鉴定.它们分别是3,8-dihydroxy-4-methoxy-coumarin(ⅪⅩ),3,8-dihydroxy-4-methoxy-2-oxo-2 H-1-benzopyran-5-carboxylic acid(ⅩⅦ),和5,8-dihydroxy-7-(4-hydroxy-5-methyl-coumarin-3-)-coumarin(ⅩⅪ)。     

(3S,4S)-3-氨基-4-氨羰氧甲基-2-吖叮啶酮-1-磺酸钠衍生物的合成与抗菌活性

以(3S,4S)-3-氨基-4-氨羰氧甲基-2-吖叮啶酮-1-磺酸钠为母核,选择D-(-)-2-(7或8-甲氧基香豆素-3-甲酰胺基)-2-苯或4-羟基苯乙酸和D-(-)-α-(4-乙基-2,3-二氧-1-哌嗪甲酰胺基)-2-苯或4-羟基苯乙酸作为边链,合成6个新的单胺菌素衍生物:(3S,4S)-3-[D-(-)-2-(8或7-甲氧基香豆素-3-甲酰胺基)-2-(苯或4-羟基苯)乙酰胺基]-4-氨羰氧甲基-2-吖叮啶酮-1-磺酸钠Ⅳ_(1-4);(3S,4S)-3-[D-(-)-α-(4-乙基-2,3-二氧-1-哌嗪甲酰胺基)-2-(苯或4-羟基苯)乙酰胺基]-4-氨羰氧甲基-2-吖叮啶酮-1-磺酸钠Ⅳ_(5-6)。初步体外抑菌试验表明,化合物Ⅳ_5,Ⅳ_6对革兰氏阴性菌有较强的抗菌活性。