麦角生物硷的层离研究 Ⅰ.我国野生麦角的成分鉴定及麦角新硷的定量

近年来国内发现几种野生麦角,本院药用植物系进行了调查研究,从分怖地区及麦角外部形态方面作了初步报导,为进一步了解和探讨其中生物硷成分及麦角新硷含量,我们用纸屑离法进行研究。一般化学测定法只能测定麦角总硷含量及水溶性生物硷含量,对于个别生物硷无法测定,自1949年Foster应用纸屑离法后,就大大方便了从事研究麦角复杂成分的方法。 Foster用正丁醇、醋酸、及水的混合液作扩展溶剂,把水溶性及水不溶性生物硷在     

麦角生物硷的层离研究 Ⅱ.麦角生药的柱层离定量

麦角中生物硷的含量测定,一般均按中国药典及 N.F.方法.但这两个方法只能测出总生物硷和水溶性生物硷的含量,对最有效成份——水溶性生物硷中的麦角新硷无法单独测定.Grove 曾用提取方法分离麦角新硷和麦角异新硷,进行个别定量,但手续麻烦,而且提取液体积较大,含量少时测定困难.Carless 用纸纤维柱层离法分别测定麦角中各种生物硷含量,样品用量很少,全部过程需两天.根据作者之一用硅藻土柱层离法自麦角生药中提取麦角新硷的结果,我们认为有可能达到定量目的,因此进行了以下试     

野生麦角调查研究

1957年作者等在华北盛产野生麦角的地区张北及沽源进行了生态因子的调查,并在东北搜集了不同寄主上野生麦角的样本作含硷量的此较分析.张北及沽源禾本科植物对麦角病感染程度由重至轻的顺序为碱草、赖草、大麦草、紫穗大麦草、黑麦、偏穗冰草及披碱草,其平均感染百分数分别为68.48、60.97、60.00、50.00、42.00、14.00及6.59.此外拂子茅亦有轻度感染.大麦、小麦、燕麦及无芒雀麦均未发现感染.野生寄主植物中以赖草和碱草分布最广,其大片单独群落的密度每平方米平均分别为61茎和79茎,披碱草亦有大片羣落,平均密度每平方米为38茎,其他禾草的分布极为零星.估计张北及沽源麦角的年产量至少有12万市斤。张北及沽源盛产野生麦角的生态因子为:(1)有大量的感染寄主,(2)每年积累大量菌源,(3)长期寒冷的冬季,及6、7、8月阴雨气候.麦角形成最盛期为7月下旬至8月上旬,采收最合宜的时期为8月中旬.华北及东北地区各种寄主植物所产麦角含硷量差别很大,由高至低的顺序为:拂子茅(麦角总硷计0.577%),老芒麦(0.44%),披碱草(0.30-0.34%),赖草(0.13-0.15%),碱草(0.115%),黑麦(0.061-0.065%);同一寄主植物在不同地区所产麦角的含硷量差异很少.含硷量的高低与菌核的大小,颜色等关系亦不大.寄生于赖草、碱草、披碱草、老芒麦及黑麦的麦角菌经鉴定均为Clavicepspurpurea,寄生于拂子茅的麦角菌为C.microcephala。     

唐松草属生物硷的研究XIV.从高唐松草中分离具有抗微生物活力的生物硷

本文从高唐松草(Thalictrum polygammum)分离得唐松草硷(Thalicarpine),小蘖红硷(Berberrubine),thaligucinone,deoxythalidastine,thalifendine,小蘖硷,析木兰硷(Magnoflorine)等七种生物硷,同时对六种微生物进行了抗菌活力试验,发现前三种生物硷具有抗微生物活力。     

华北及东北地区野生麦角的调查

前言麦角是妇产科的重要药物,国内每年用量很大,多由外国进口,每年资金外溢很多,所以在国内调查有效的野生麦角资源以代外货,是一件极有意义的工作。此外,麦角在农业上也是著名的黑麦病害,虽然影响黑麦的产量不大,但食用这种含有麦角菌核的面粉,含量如超过0.1%时,即能引起麦角中毒症。野生麦角也寄生在各种禾本科的牧草上,家畜吃了以后,也会产生麦角中毒症。所以麦角不但有医疗上的价值,而且与农业,畜牧业也有莫大的关系。过去对于国内麦角调查作得很少,     

麦角总碱注射液的制备

一、绪言麦角是治疗和预防产后出血不可缺乏的妇科要药。我国对麦角需要量很大,过去完全依赖进口。据近年调查在我国东北、华北地区均产大量野生麦角。对国产麦角的化学分析及药理作用已有研究。近年来在麦角菌的人工接种栽培方面已获得一定的成功。如何利用国产麦角制成制剂以满足临床需用,是迫切需要解决的问题。各国应用的麦角注射制剂有两类:(1)单纯生物碱制剂,如麦角新碱注射液;(2)新     

三尖杉酯硷治疗急性白血病初步总结

三尖杉系我国特产树种,分布较广,民间曾用以治疗肿瘤。无产阶级文化大革命以来,我国许多地方对三尖杉属的抗癌作用,从植化,药理,临床等方面开展了协作研究。临床观察证明,从该属植物分离出的总生物硷对急性白血病有一定疗效。全国三尖杉协作组进一步从总生物硷中分离并合成有效的生物硷单体——三尖杉酯硷,高三尖杉酯硷,异三尖杉酯硷、脱氧三尖杉酯硷等四种,有计划的试用于临床。我院内科血液组于1974年9月至1975年6月,曾用三尖杉酯硷和高三尖杉酯硷混合制剂试用于急性白血病,取得了一定的临床经验。1976年8月至1977年5月又在全国协作组的统一安排下,用三尖杉酯硷(单体)治疗急性非淋巴     

来源于植物的治疗脑病药物及血管活性物质

从植物来源的化合物中,下述药物被推荐用于脑机能不全的治疗:茶碱、罂粟碱、水合麦角生物碱、长春胺和银杏(Gingko biloba)提取物。由于在2/3的病人中,除脑血流不足的症状外,脑代谢紊乱在病原学中占有突出地位。所以那些能改善脑代谢的药物最好同时配有血管活性物质。在临床试验中,茶硷能减少病人的脑血流,因而不应再使用。它对磷酸二酯酶的抑制作用与在体内不能达到的高浓度有关。罂粟碱能短期改善血流,在长期口服高剂量药物时,能抑制磷酸二酯酶,因而导致环磷腺苷的增加,它作为第二信使在脑代谢亦即在旦白质的脂解和磷酸化过程中起重要作用。水合麦角生物硷对人脑血流没有作用,仅一个组(8个人)中有改善。它的作用也是由于抑制磷酸二酯酶所致;与此     

中国萝芙木的药理研究,Ⅳ.萝芙木根生物硷中几个成分的降压作用和毒性

根据动物实验和临床研究证明中国蘿芙木的生物硷具有明显的降压作用后,研究其中的降压有效成分就成为一个重要的问题。赵承嘏曾提取出一种生物硷“蘿芙甲素”,并经动物实验证明有降压作用,主要是由于它的解肾上腺素作用。我们用各地蘿芙木根的生物硷给高血压狗进行实验治疗时,曾见眼睑下垂、瞬膜松弛、瞳孔缩小、镇静、全身颤抖及其他神经症状。说明其中可能含有利血平或具有与利血平类似作用的     

麦角菌发酵物中生物碱的化学研究

利用麦角菌生物合成制取麦角新碱的方法已推广应用于生产。该菌种在小麦种子培养基上培养以后,除麦角新碱外,根据薄层层离鉴定结果证明还产生三种麦角生物碱。为了利用麦角新碱生产过程中母液里的其他麦角生物碱,并为进一步研究生物合成机制提供资料,必须先对母液中所含麦角生物碱进行分离和鉴定。曾采用无粘合剂的氧化鋁薄层层离法,从母液中分离出了四种生物碱。除麦角新碱外,其余三种生物碱通过薄层层离鉴定;熔点、比旋度测定;紫外吸收光谱、红外吸收光谱和元素分析等分别鉴定,证明为麦角异新碱、麦角生碱和麦角异生碱。     

水仙的药理作用

(1)水仙鳞莖之粗浸剂对豚鼠、兎与貓的离体在体子宫,都有强大之兴奋作用,小剂量引致紧張度之增加,大剂量可出現强直收縮,对离体豚鼠子宫更为明显。(2)將水仙注入雄鷄胸肌后在24小时左右,令鷄冠后部变为深黑色,作用可持續20日以上,这一点与石蒜和麦角大有区別。(3)水仙对怀孕豚鼠有明显的墜胎作用。(4)水仙能令鸽發生嘔吐,並能兴奋家兔之十二指腸。     

中药石蒜的药理作用

1、石蒜煎剂与石蒜生物鹼,对豚鼠及兔的子宫,不論离体与在体,都具有明显的兴奋作用,大剂量时可使离体子宫呈現强直性收縮。对大白鼠的未孕子宫則令其节律减少与松弛。在豚鼠子宫上証明,石蒜的兴奋作用不被苯海拉明所对抗。2、石蒜煎剂能使雄鸡鸡冠呈变色反应。此种变色反应与組織胺所致者不同。3、石蒜能兴奋家兔离体十二指腸,对鸽具有催吐作用。     

Studies on the inhibition of adrenaline-induced aggregation of blood platelets.

alpha-Adrenoceptors of platelets seem to differ from those of other cell types. The inhibitory effect of alpha-adrenoceptor-blocking agents on adrenaline-induced aggregation of human platelets does not parallel that on adrenaline-induced contraction of rabbit aortic strips. The most potent inhibitors of adrenaline-induced platelet aggregation are the dihydrogenated ergot alkaloids of the peptide type. Among the other ergoline derivatives testes, only lisuride has a stronger inhibitory effect than those of natural ergot alkaloids.     

STUDIES ON THE SPASMOLYTIC AND UTERINE RELAXANT ACTIONS OF N -ETHYL AND N -BENZYL-1,2-DIPHENYL ETHANOLAMINES: ELUCIDATION OF THE MECHANISMS OF ACTION

The influence of N -ethyl- and N -benzyl-1,2-diphenyl ethanolamines (compounds E and B, respectively) was examined on the spontaneously contracting rabbit jejunum and the rat uterus together with their influence on the contractions induced by some spasmogens in the guinea-pig ileum and oxytocics and CaCl₂in the pregnant rat uterus. Both E and B inhibited the spontaneous contractions of the rabbit jejunum with ID₅₀values of 0.13 and 0.03 μmol ml⁻¹. Their inhibitory activities were not antagonized by α- or β-adrenoceptor blockers but significantly reversed by CaCl₂(0.015 μmol ml⁻¹). The compounds also antagonized nicotine, ACh-, histamine-, 5-HT- and CaCl₂-induced contractions by 44–100%. Compound E seemed to be several times more potent than B in inhibiting the spontaneous uterine contractions with an ID₅₀of (7 nmol ml⁻¹). Their inhibitory effects were not antagonized by β₂-adrenoceptor or H₂-receptor blocking drugs. Both compounds (40 nmol ml⁻¹) antagonized in a competitive manner CaCl₂-induced contractions in the K⁺-depolarised uterus and PGE₂and oxytocin-induced uterine contractions. The ID₅₀values were in the range of 1.6–10.7 nmol ml⁻¹. The results suggest that E and B compounds may be considered as putative L-Ca²⁺channel blockers with certain selectivities. The E compound seemed to be more selective against uterine L-Ca²⁺channels and the B compound against intestinal smooth muscles. Thus, the compounds may be of potential value in treatment of some colics, the irritant bowel syndrome, dysmenorrhoea and premature deliveries. 1999 Academic Press@p$hr     

The analgesic and antiinflammatory activity and pharmacologic properties of bromfenac

Bromfenac sodium (2-amino-3-(4-bromobenzoyl)benzeneacetic acid sodium salt sesquihydrate, AHR-10282B) is a potent long-acting, peripheral, analgesic compound possessing antiinflammatory, antipyretic, and prostaglandin synthetase-inhibiting properties. In the acetylcholine abdominal constriction assay in mice, bromfenac (bromfenac sodium) by the oral route at pretreatment times of 10, 20 and 300 min was respectively 3.7, 6.5 and 2.9 times more potent than zomepirac and 3.4, 6.6., and 44.2 times more potent than suprofen. In dogs bromfenac when given orally was 5.8 times more potent than zomepirac in blocking the nociceptive response to bradykinin. Naloxone did not alter the analgesic properties of bromfenac in mice; and after repeated administration, tolerance to analgesia did not develop. Bromfenac, given orally, was more potent than indometacin in suppressing acute (7.5-20 times) and chronic (3.8 times) inflammation. The gastric and intestinal toxicity potencies of bromfenac, given orally, were comparable with and 1.8 times more potent than indometacin, respectively. Bromfenac was 6.1 to 32.8 times more potent than indometacin in inhibiting the formation of prostaglandin E2 and F2 alpha from microsomes of bovine seminal vesicles, rabbit uteri, and rabbit renal medullae; but it did not block the direct action of prostaglandin E1 (abdominal constriction) and prostaglandin F2 alpha (contraction of the uterus). Bromfenac produced no unwanted central nervous system, cardiovascular, or autonomic effects.     

麦角菌在黑麦品种上的接种栽培

1957年在北京及哈尔滨以各种野生麦角所分离的不同菌种在张北、佳木斯等9个不同的黑麦品种上进行了接种栽培。春黑麦较冬黑麦的感染力强,春黑麦中又以张北及佳木斯最易感病,对自拂子茅(Calamagnostis epigeios(L)Roth)、披碱草(Clinelymus dahuricus Nevski)、老芒麦(Clinelymus sibiricus(L)Nevski)、黑麦(Secale cereale L.)、高滨麦(Clinelymus excelsus Nevski),及Agropyrum sp.6个不同寄主所分离的菌种亦均感染;公主岭及平鲁黑麦感染性较差.不同菌种中以分离自拂子茅的菌种寄生性最强,侵染所有4个春黑麦品种及一个冬黑麦品种.分离自拂子茅的6个不同菌系中以B₅的寄生性最强,公主岭、张北及佳木斯3个品种对B₅的感染率均在70%以上;B₁次之,3个黑麦品种对B₁的感染率均在50%以上;B₇最差,公主岭及张北黑麦对B₇的感染率为5—10%, 不同接种方法以孢子液注射法效果最佳,侵渍法次之,喷雾法最差。每min³接种液中孢子数目在600—9600间浓度愈高致病力愈强。分离自拂子茅麦角(Claviceps microcephala)的不同菌系在各种黑麦品种上所生的菌核较原寄主上的菌核大34倍.B₁与B₅在不同黑麦品种上所生麦角的含硷量为0.22—0.40%,远较自然条件下所产黑麦麦角(C.purpurea Tul.)的含硷量(0.06%)为高,也超过我国药典所规定0.2%的标准。B₅的产硷能力高于B₁。不同品种中以佳木斯黑麦所产菌核的含硷量较高,公主岭及平鲁次之,张北黑麦的麦角含硷量最低。     

Pharmacological screening of some Brazilian plants

Forty-five species of plants from several botanical families growing in North East Brazil have been examined for toxicity on mice and small fishes, cat blood pressure and respiration, isolated toad heart and rectus abdominis muscle, guinea-pig ileum, rabbit duodenum and rat uterus. A high toxicity to mice and fishes was exhibited by aqueous (A) and ethanolic (B) extracts from Luffa operculata, Peschiera affinis, Pithecelobium multiflorum (gall) and Zizyphus joazeiro and by extract B from Pithecelobium multiflorum (stembark). Cardiorespiratory activity was shown by Annona squamosa, Byrsonima sericea, Crataeva tapia, Erythrina velutina, Fagara rhoifolia, Operculina macrocarpa, Perschiera affinis, Pithecelobium multiflorum, Spondias lutea and Zizyphus joazeiro. Extracts A and B from Operculina macrocarpa and Pithecelobium multiflorum, extract A from Luffa operculata and Zizyphus joazeiro and extract B from Crataeva tapia and Peschiera affinis promoted a contraction of the toad rectus abdominis muscle. Both extracts from Annona aquamosa and Fagara rhoifolia (leaf) provoked a spasmogenic effect on guineapig ileum and a spasmolytic one on rabbit duodenum. Extracts A and B from Pithecelobium multiflorum, Vitex gardneriana and Zizyphus joazeiro exhibited a spasmogenic activity on both preparations, while extracts A and B from Peschiera affinis and extract B from Erythrina velutina also evidenced a spasmolytic activity on both preparations. Oxytocic activity was shown by both extracts from Annona squamosa, Byrsonima sericea, Pithecelobium multiflorum and Vitex gardneriana.     

Alkaloids in ergot found on different Gramineae in The Netherlands

The alkaloid content and the composition of the alkaloid complex of thirteen samples of ergot sclerotia from different gramineous host species collected in The Netherlands were investigated. Two samples collected in France were also examined. Ergot ofGlyceria fluitans (L.) R.Br. did not contain alkaloids. The total alkaloid content of ergot found on the other wild grasses was more than 0.2%. The ratio between the contents of water soluble and water insoluble alkaloids of the investigated ergot sclerotia varies between 1∶10 and 1∶20. The composition of the alkaloid complex in the sclerotia was studied by quantitative thin-layer chromatography. The sclerotia could be grouped into three main categories:

sclerotia ofLolium perenne L.,Festuca arundinacea Schreb. andArrhenatherum elatius (L.) P.B. ex J. et C. Presl, containing predominantly ergocornine, α- and β-ergokryptine and ergosine;

sclerotia ofDactylis glomerata L.,Phalaris arundinacea L.,Alopecurus geniculatus L. andHolcus mollis L., containing predominantly ergosine, ergocristine and ergotamine;

sclerotia ofMolinia caerulea (L.) Moench, containing predominantly ergocristine, ergosine and ergqmetrine.

A great similarity was found between the composition of the alkaloid complex in ergot ofLolium perenne L. from different locations and also in ergot ofMolinia caerulea (L.) Moench from different locations. This similarity was less in ergot ofDactylis glomerata L. collected from different locations.     

Comparative bioassay of prostaglandin E2 and its three pulmonary metabolites.

The relative potencies of prostaglandin E2 and its metabolites 15-keto PGE2, 13,14-dihydro-15-keto-PGE2 and 13,14,dihydro-PGE2 were investigated on isolated smooth muscle preparations. These were rat stomach strip, colon and uterus, chick rectum, guinea-pig ileum, trachea and pulmonary artery and rabbit aorta and pulmonary artery. 15-keto PGE2 was equiactive or 1-1.8 times more potent than prostaglandin E2 in relaxing guinea-pig trachea but otherwise the three metabolites were less active than prostaglandin E2 on all preparations.