O,O′-二烷基-O″-(取代苯乙腈肟)磷酸酯、硫代磷酸酯的合成及对氯硝柳胺的灭螺增效作用

合成了20个O,O′-二烷基-O″-(取代苯乙腈肟)磷酸酯、硫代磷酸酯,并分别与杀螺剂氯硝柳胺组成复方,进行室内杀螺试验。初步结果表明,化合物V_4,7,12,18有明显杀螺增效作用,其中V12可使氯硝柳胺的杀螺效果提高3.81倍。同时发现化合物V_2,7,10,13单独使用时,也有良好的杀螺作用。     

血吸虫病化学治疗的研究——ⅩⅩⅩⅣ.α-氯-β-(5-硝基-2-呋喃)丙烯酰胺类及其乙烯噁二唑类衍生物的合成

Synthesis of 35 new compounds of α-chloro-β-(5-nitro-2-furyl) acrylamides and 5-[α-chloro-β-(5-nitro-2-furyl ) vinyl]-oxadiazoles by known methods are reported. In preliminary test in mice 10 compounds were found to possess pronounced activity against Schistosomiasis japonica. Among these Ⅰ₁₂, Ⅰ₁₃, Ⅰ₁₄, Ⅰ₂₀, Ⅱ₁ and Ⅱ₈ were shown to be the most effective.     

国产醋酸甲地孕酮的质量研究:6-羟基-6-甲基-17α-乙酰氧基黄体酮差向异构体的分离与鉴定

用柱层析及薄层层析对国产醋酸甲地孕酮的杂质进行了分析,共分离出7个杂质点:Ⅰ₁,Ⅰ₂,Ⅰ₃,Ⅰ₄,Ⅰ₅,Ⅰ₆,Ⅰ₇,并对其中Ⅰ₃和Ⅰ₄进行分离纯制及光谱分析,确定其结构为6β-羟基-6α-甲基-17α-乙酰氧基黄体酮及其差向异构体6α-羟基-6β-甲基-17α-乙酰氧基黄体酮。本文报道了薄层层析条件(硅胶GF₂₅₄,展开剂:醋酸乙酯-甲苯=7:3)以及光谱鉴别的依据。     

HPLC测定安尔眠胶囊中2,3,5,4’-四羟基二苯乙烯-2-O-β-D-葡萄糖苷

目的 建立安尔眠胶囊中2,3,5,4’-四羟基二苯乙烯-2-O-β-D-葡萄糖苷（C₂₀H₂₂0₉）的含量测定方法。方法 采用高效液相色谱（HPLC）法,以Dionex Acclaim 120^® C₁₈色谱柱（150 mm×4.6 mm,5 μm）为分离柱,以乙腈-1%甲酸溶液（23：77）为流动相,体积流量1.0 mL/min,检测波长320 nm,柱温25 ℃。结果 2,3,5,4’-四羟基二苯乙烯-2-O-β-D-葡萄糖苷在0.010～0.200 μg呈现良好的线性关系（r=0.999 6）,平均回收率为97.35%,RSD为2.07%。结论 该方法<准确可靠,适用于安尔眠胶囊中2,3,5,4’-四羟基二苯乙烯-2-O-β-D-葡萄糖苷的含量测定。     

抗疟新药的研究5-取代苯氧基-6-甲氧基-8-取代氨基喹啉的合成

根据5-(对-氟苯氧基)-6-甲氧基-8-(4-氨基-1-甲基-丁氨基)喹啉(Ⅰ₁)(表1)对猴疟原虫(Plasmodium cynomolgi)的作用略优于伯喹而毒性较低的报道,合成了化合物Ⅰ₁(代号M7844),同时还合成了衍生物5-取代苯氧基-6-甲氧基-8-(4-取代氨基-1-甲基丁氨基)喹啉(Ⅰ_3～17)(表1)以及其同分异构体5-取代苯氧基6-甲氧基-8-(5-取代氨基戊氨基)喹啉(Ⅱ_13～28)(表2)。药理研究证明化合物Ⅰ_1～7、Ⅰ₁₆及Ⅱ₁₈等对鼠疟P.yoelii均有不同程度的作用。化合物Ⅰ₁(M7844)的毒性甚低,对小鼠的毒性比磷酸伯喹低20余倍,对家兔的溶血反应也明显低干伯喹。但在相同剂量下,对猴疟P.cynomolgi的作用不及伯喹。对鼠疟红前期的作用比伯喹低4～5倍。     

灭螺增效剂的合成

药物灭螺是血吸虫病防治的重要环节之一,为了寻找更好的灭螺增效剂,设计合成了O,O′-二烷基-O″-(2-取代-3-苯并呋喃乙腈-α-肟)磷酸酯和硫代磷酸酯(Ⅵ_1～13),O,O′-二烷基-O″-(2-噻吩乙腈-α-肟)磷酸酯(Ⅹ_14,15)等化合物15个。初步试验表明,化合物X₁₅与五氯酚钠合用有较强灭螺增效作用,化合物Ⅹ₁₄及Ⅵ_{1,2,3,6,8,10,12,13}亦有一定的灭螺增效活性,化合物Ⅵ_10,12除增效作用外本身尚有一定的杀螺活性。     

肿瘤的化学治疗 ⅩⅩⅢ.若干[双-(β-卤乙基)-氨基]-吲■-2-羧酸及其乙酯的合成

由5(及7)-[双-(β-羥乙基)-氨基]吲(口朶)-2-羧酸乙酯(Ⅶ_a,b)合成了5(及7)-[双-(β-氯乙基)-氨基]吲(口朶)-2-羧酸乙酯(Ⅱ_a和Ⅱ_b)、5(及7)-[双-(β-溴乙基)-氨基]-吲(口朶)-2-羧酸乙酯(Ⅱ_c和Ⅱ_d)以及5(及7)-[双-(β-碘乙基)-氨基]-吲(口朶)-2-羧酸乙酯(Ⅱ_e和Ⅱ_f)。再經水解制得其相应的羧酸(I_a-f)。此外又合成了5(及7)-乙氧羰氨基-吲(口朶)-2-羧酸乙酯(IX_a,b)和5-乙氧基-7-[双-(β-氯乙基)-氨基]-吲(口朶)-2-羧酸乙酯(Ⅶ)。化合物I_a,I_b,I_c,Ⅱ_a,Ⅱ_b,Ⅱ_c,Ⅱ_e和Ⅱ_f对組織培养Hela細胞有明显的抑制作用。化合物Ⅰ_a,Ⅰ_b,Ⅱ_a和Ⅱ_b口服时对小鼠肉瘤180有明显的抑制作用。化合物Ⅰ_e,Ⅰ_f和Ⅻ对肉瘤180具有中度的抑制作用。     

山野豌豆黄酮类化学成分的研究

自山野豌豆(Vicia amoena Fisch.)全草的乙醇提取物中分得6个化合物,经波谱和化学分析鉴定其中一个为新的黄酮甙,命名为山野豌豆甙(amoenin A₃),其余5个化合物为槲皮素(quercetin D₂)、山奈酚(kaempferol D₁)、槲皮素-3-O-α-L-鼠李糖甙(quercetin-3-O-α-L-rhamnosideC1)、槲皮素-3-O-β-D-葡萄糖甙(quercetin-3-O-β-D-glucosideC2)、山柰酚-3,7-O-α-L-二鼠李糖甙(kaempferol-3,7-O-α-L-dirhamnoside A₂)。以上黄酮类化合物均为首次从山野豌豆中分得。     

HPLC法测定通乐颗粒中2, 3, 5, 4′-四羟基二苯乙烯-2-O-β-D-葡萄糖苷

目的 建立测定通乐颗粒中2, 3, 5, 4′-四羟基二苯乙烯-2-O-β-D-葡萄糖苷的方法。方法 采用HPLC法,色谱柱为Phenomenex C₁₈柱,检测波长为320 nm,流动相为乙腈-水（20∶80）,体积流量为1.0 mL/min。结果 2, 3, 5, 4′-四羟基二苯乙烯-2-O-β-D-葡萄糖苷在10～100 μg/mL与峰面积呈良好线性关系（r＝0.999 7）,平均回收率为99.74%。结论 本方法准确、简便、重复性好,可用于通乐颗粒中2, 3, 5, 4′-四羟基二苯乙烯-2-O-β-D-葡萄糖苷的含量测定。     

川芎有效成份的研究——新的苯酞类化合物4-羟基-3-丁基苯酞的结构测定

从川芎(Ligusticum wallchii Franch)的酚性部分中分离得到一个新的苯酞类化合物Ⅰ,熔点190～191℃,[α]_D—105.5°,C₁₂H₄O₃。化合物Ⅰ的结构经化学和仪器分析测定,鉴定为4-羟基-3-丁基苯酞(4-Hydroxy-3-butyl phthalide),并用合成证实。     

Molluscicidal and antischistosomal activities of Zingiber officinale

Experiments were conducted to study the major constituents of Zingiber officinale responsible for its molluscicidal activity and the effect of the active component on different stages of Schistosoma mansoni. Gingerol and shogaol exhibited potent molluscicidal activity on Biomphalaria glabrata. Gingerol (5.0 ppm) completely abolished the infectivity of Schistosoma mansoni miracidia and cercariae in B. glabrata and mice, respectively, indicating that the molluscicide is capable of interrupting schistosome transmission at a concentration lower than its molluscicidal concentrations.     

The molluscicidal activity of coumarins from Ethulia conyzoides and of dicumarol.

The molluscicidal principles of Ethulia conyzoides were identified as ethuliacoumarin A (1) and isoethuliacoumarin A (2). Ethuliacoumarin A possessed an LC90 between 19 and 23.5 ppm depending on the age of the snail against Biomphalaria glabrata, and between 12 and 15 ppm against Bulinus truncatus. In addition, ethuliacoumarin A was found to be cercaricidal at 25 ppm and ovicidal. Ethuliacoumarin has the structural requirements considered essential for anticoagulant activity. Consequently the anticoagulant dicumarol (4) was tested and found to be molluscicidal in the range from 2.5 to 10 ppm. In contrast, the coumarin anticoagulant warfarin (3) did not show molluscicidal activity.     

Ambrosia maritima L.: study of molluscicidal properties of several generations originating in Egypt and cultivated in Senegal

The authors experiment molluscicidal properties of Ambrosia maritima L. from Egypt and cultivated in Senegal. Four generations are tested. Six plants, on eight tested, had same molluscicidal activity as the strain in Egypt.     

Molluscicidal and antifungal activity of diterpenoids from brown algae of the family dictyotaceae

17 diterpenoids isolated from brown algae of the family DICTYOTACEAE have been evaluated for molluscicidal and antifungal activity. Significant molluscicidal activity is exhibited by the two geometrical isomers 9 and 10. The assessment of structure-activity relationships has been considered.     

Screening of European Fungi for Antibacterial,Antifungal, Larvicidal,Molluscicidal, Antioxidant and Free-Radical Scavenging Activities and Subsequent Isolation of Bioactive Compounds

Crude extracts of 57 species of European fungi have been tested for their bactericidal (Bacillus subtilis, Escherichia coli), fungicidal (Candida albicans, Cladosporium cucumerinum), larvicidal (Aedes aegypti), molluscicidal (Biomphalaria glabrata), antioxidant and free-radical scavenging activities. Connatine and 2(3,4-dihydroxyphenyl)glycine, two compounds with antioxidant and free-radical scavenging properties, were subsequently isolated from the methanolic extracts of Lyophyllum connatum (Tricholomataceae) and Cortinarius hercynicus (Cortinariaceae), respectively. In addition, linoleic acid was shown to be molluscicidal.     

On the molluscicidal activity of tannin containing plants

The aqueous and methanolic extracts of a series of typical tannin containing plants exhibit strong molluscicidal properties against the freshwater snail biomphalaria glabrata, which is the intermediate host of schistosomiasis. The crude extracts of Krameria triandra (Krameriaceae) and Arctostaphylos uvaursi (Ericaceae) were active at concentrations of 50 ppm. Hydrolyzable and condensed tannins are responsable for the molluscicidal activity. This report indicates a new class of plant derived compounds which may have important practical application for the control of schistosomiasis in endemic areas.     

Toxicity of the molluscicidal plant, Ambrosia maritima L., to aquatic non-target organisms

The toxicity of the molluscicidal plant, Ambrosia maritima L., has been evaluated in fish, crustacea and algae. The LC50 for fries of the guppy, Lebistes reticulatus, was respectively 650 and 450 mg/litre using a powder or an ether-methanol-hexane extract from the leaves of the plant. This concentration is much higher than the molluscicidal concentration (LC90) of 35 to 70 mg/litre, which is used in the field (irrigation canals in Egypt). Preliminary tests showed that juveniles of L. reticulatus and Tilapia aurea were as sensitive as the fries. Using the same extract of A. maritima the LC50 for Daphnia magna was 766 mg/litre and no toxic effects could be observed in algae Selenastrum capricornutum at 1 g/litre. It can be concluded that A. maritima has a very low toxicity to aquatic non-target organisms. It is not toxic when used at the molluscicidal concentration of 35 to 70 mg/litre.     

Molluscicidal properties of Acacia nilotica

The acetone, alcohol and aqueous extracts of fruits of Acacia nilotica (L) Willd. ex Del. (Mimosaceae) showed molluscicidal activity against Bulinus truncatus and Biomphalaria pfeifferi, the two snail species which transmit schistosomiasis in the Sudan (S. haematobium and S. mansonii). TAN, a new vegetable molluscicide prepared from the aqueous extract of the fruits of A. nilotica was produced on a pilot scale by using the spray drying procedure. Due to the high content of tannins in the powder (more than 56%), the molluscicidal properties of this plant may well be due to these compounds.     

Molluscicidal Properties of Acacia nilotica.

The acetone, alcohol and aqueous extracts of fruits of ACACIA NILOTICA (L) W ILLD. ex D EL. (Mimosaceae) showed molluscicidal activity against BULINUS TRUNCATUS and BIOMPHALARIA PFEIFFERI, the two snail species which transmit schistosomiasis in the Sudan (S. haematobium and S. mansonii). TAN, a new vegetable molluscicide prepared from the aqueous extract of the fruits of A. NILOTICA was produced on a pilot scale by using the spray drying procedure. Due to the high content of tannins in the powder (more than 56%), the molluscicidal properties of this plant may well be due to these compounds.