国药中黄酮类的研究(Ⅵ) 桑寄生化学成分的研究(第二报) 广寄生中槲皮素及其配糖体的分离

国产桑寄生品种甚多,而常作藥用的有北寄生、杜寄生、广寄生三种,前二种系同科同属,后一种是同科异属,作者巳报告了北寄生成分的研究,本报則从后者广寄生分离出有强烈利尿作用的結晶成分,特报告于后.按广寄生产于我国粤桂諸省,本实驗所用材料由本院华南植物研究所供給,并紲鑒定其学名为Loranthus paraciticus L(Merr.)是为桑寄生屬Loranthus L.与槲寄生屬Viscum L.不同即与北寄生为同科不同屬的植物,由于作者曾在北寄生的乙醚浸出液中     

从本草考证论桑寄生和槲寄生

目的:让中医药专业人员能更清楚理解、识别并正确使用桑寄生与槲寄生,以取得良好的临床疗效。方法:从历代本草文献及现代药典标准角度考察分析其药用历史沿革,以正本清源。分析历代本草相关记述、化学成分、药理作用及临床应用等内容,综合认识二者来源、性状特征以及功效的异同。结果:从本草考证结合药典标准来看原桑(上)寄生实指今槲寄生,主产我国北方及中部地区,现桑寄生实为同科不同种的另一种(类)半寄生植物广寄生,主产两广及云南。结论:从历史沿革来看桑寄生之名其实更应该属于现在药典之槲寄生,药典之桑寄生建议更名为寄生或广寄生。     

桑寄生化学成分的研究广寄生叶中d-儿茶素及檞皮甙的分离和鉴定

桑寄生为常用中药,广寄生(Taxillus Chinensis(DC.)Danser)为桑寄生主流品种之一,中国药典各版均有收载。据文献报道叶中含广寄生甙(Avicullarin)及檞皮素(Quercetin)。作者从叶中分得二种结晶,理化鉴定及光谱分析证明晶Ⅰ为d-儿茶素(d-Catechin),晶Ⅱ为檞皮甙(Quercitrin),收率分别为0.013％和0.14％。为进一步考察广寄生叶中黄酮成分的组成,取夏季、冬季采收的广寄生及两种市售的寄生茶作叶的总黄丽层折鉴定,用檞皮甙、广寄生甙、d-儿茶素、槲皮素纯品对照,结果均含以上成分,但以檞皮甙为主,广寄生甙含量很低。     

益肾又安胎的桑寄生

桑寄生也称“广寄生”,为常绿寄生小灌木植物。始载于《神农本草经》,名“桑上寄生”,列入上品。     

桑寄生化学成分的研究(第一报)

中药桑寄生是我国古代常用药品之一,早在2300年前的“神农本草经”已有关于它的记载,当初以寄生在桑树上的作药用,后来发现并不是专寄生在桑树的,而且不容易分别。到了唐朝的“新修本草”(西纪659年)著者苏敬等,干脆说桑寄生并不是专寄生在桑树上而多寄生在槲、欅、柳、水杨、枫等树上,直到现在巳有1500年左右桑寄生的名字已成了历史上的惯用名词并非指桑上寄生,而是寄生在各种可能寄生的树上了。刘慎谔谓中国产的槲寄生科(Loranthaceae)有5属30种,东北产1属1种。在崔友     

基于时空变化的桑寄生中广寄生苷、槲皮苷、槲皮素含量分析

目的：研究基于时空变化的桑寄生中广寄生苷、槲皮苷、槲皮素含有量的影响。方法：采用双波长切换法测定来源于不同产地、不同采收期的桑寄生样品中广寄生苷、槲皮苷、槲皮素含量,样品采用甲醇超声提取方法制备。色谱条件：Ultimate^®XB-C₁₈色谱柱（250 mm×4.6 mm,5 μm）,流动相为乙腈（A）-甲醇（B）-0.1%磷酸溶液（C）,梯度洗脱（0~25 min,3% A,39% B;25~45 min,3% A~23% A,39% B~19% B）,流速：1.0 mL·min^-1,柱温：25℃,双波长切换检测（0~25 min,254 nm;25~45 min,365 nm）。结果：广寄生苷、槲皮苷、槲皮素的线性范围分别为0.099 2~1.984 0 μg（r=0.999 9）,0.225 4~4.458 0 μg（r=0.999 9）和0.125 8~2.516 0 μg（r=0.999 7）,平均加样回收率（n=5）分别为98.39%,97.08%和98.15%。不同产地桑寄生药材茎枝中广寄生苷、槲皮苷、槲皮素含量分别为0.000 0~0.021 5,0.214 3~0.892 0和0.000 0~0.023 1 mg·g^-1,叶中为0.000 0~0.096 3,2.265 3~5.998 7和0.000 0~0.156 9 mg·g^-1;不同采收期桑寄生药材茎枝中广寄生苷、槲皮苷、槲皮素含量分别为0.000 0~0.022 5,0.159 6~0.825 3和0.000 0~0.040 9 mg·g^-1,叶中为0.021 8~0.095 5,2.261 0~5.998 7和0.026 3~0.210 3 mg·g^-1。结论：该方法准确度高、简便快捷、重复性好,可作为桑寄生药材的质量控制标准。     

药理学及毒物学

Ⅶ-70 广寄生之利尿作用李蘊山傅紹萱 韓銳 曾广方药学学报,1959,7,1 作者等就曾广方氏自广寄生(Loranthus Paracticus L.C.Meer)中分离出的兩种結晶,取其中之一为黃酮类甙,暫名广寄生甙,对血压和利尿作用初步地做了研究。 (一)对血压的作用:用21只麻醉犬由靜脉注射0.05—2mg/kg的广寄生甙溶液,均显示降压作用,維持3—4分鐘,再次注射則出現急速耐受現象。     

谈中药材桑寄生与槲寄生的混用现象与建议

为加强对中药材在流通领域中的监督管理 ,我省对易混淆中药材品种进行了重点监督抽验 ,从监督抽验情况看 ,中药材在部分经营单位和医疗使用单位仍有混用现象 ,其中以桑寄生与槲寄生的混用现象为多。其他如山豆根与北豆根、五加皮与香加皮、金钱草与连钱草、白头翁与委陵菜等混用现象亦发现。现以桑寄生与槲寄生为例 ,谈一下二者的区别和混用的主要原因及几点建议 ,以引起有关方面中药专业人员的重视。1 桑寄生与槲寄生的区别　桑寄生来源于桑寄生科植物桑寄生Taxilluschinensis(DC )Danser的干燥带叶茎枝。别名广寄生等。主产于广东、广西…     

马桑寄生黄酮成分的研究

用马桑寄生叶提取分离马桑内酯混合结晶时,从水母液中析出黄酮类物质,经分离得到三种结晶,理化鉴定和光谱分析证明晶Ⅰ为槲皮素,晶Ⅱ为广寄生甙即萹蓄甙,晶Ⅲ为檞皮甙。按常法用醋酸乙酯从马桑寄生叶中提取的总黄酮层析鉴定尚含有D—儿茶素。     

桑寄生和槲寄生的鉴别

寄生类药物广泛应用于中医临床,作为常用药物有祛风湿、补肝肾、强筋骨、安胎作用。但是寄生按基源分为桑寄生和槲寄生两种不同来源,应分别按处     

Release of oxytocin contributes to the natriuretic action of aminophylline in rats

Aminophylline, 0·25 to 2·0 mg intramuscularly, caused diuresis, natriuresis and increase in the Na/K of the urine in the 1 hr period after injection into normal hydrated or unhydrated rats. The urinary changes induced by 2 mg aminophylline and by 8 mU oxytocin equated. Salt-maintained adrenalectomized rats were fully sensitive to the diuretic, natriuretic action of aminophylline. The Na/K in the urine decreased at the 2 mg dose level. Hypophysectomy abolished and neuro-hypophysectomy markedly decreased the diuretic natriuretic action of aminophylline in unanaesthetized rats. Under ethanol-pentobarbitone anaesthesia the diuretic natriuretic action of 0·4 mg aminophylline intravenously lasted 30–40 min in normal rats, and for less than 10 min in neurohypophsectomized rats. The duration of the cardiovascular response to aminophylline was 7–8 min. Thioglycollate-labile oxytocic activity, not detectable in the arterial plasma of control animals, was demonstrable in the arterial plasma of normal rats 8–12 min after 0·5 mg aminophylline intravenously.     

Studies on the diuretic effect of haloperidol in adult rats

An increase in urinary flow has been observed in rats during cataleptic response to haloperidol. The present experiment was carried out to study the mechanism of haloperidol-induced diuresis. Wistar-Imamichi adult female rats were injected i.p. with haloperidol in a dose of 0.1, 1 or 10 mg/kg, and the time course of changes in urine volume was observed. The dose-dependent diuretic effect of 1 or 10 mg/kg haloperidol was significant from 4 hr afterward, and the haloperidol-induced diuresis was prevented by pretreatment with phenoxybenzamine, prazosin or yohimbine. Chlorpromazine but not spiperone and pimozide induced a significant increase in urine volume, though the effect of chlorpromazine was less marked as compared with that of haloperidol. Clonidine in a dose of 0.125-1.0 mg/kg enhanced urine flow markedly from 30 min, and the same alpha-adrenergic blockers were also effective in blocking the diuretic effect of clonidine. Urinary osmolarity in 1 mg/kg haloperidol- and 0.125 mg/kg clonidine-treated rats decreased significantly, whereas only clonidine stimulated urinary Na and K excretion. Plasma osmolarity and negative free water clearance did not change in both haloperidol- and clonidine-treated rats. The present results suggest that the haloperidol-induced diuretic effect could be due to the central alpha-adrenoceptor blocking action of haloperidol.     

General pharmacological studies on N-(2,6-dimethylphenyl)-8-pyrrolizidineacetamide hydrochloride hemihydrate. 3rd communication: effect on cardiovascular system

In this general pharmacological study of N-[2,6-dimethylphenyl)-8-pyrrolizidineacetamide hydrochloride hemihydrate (SUN 1165), its effects on the cardiovascular and respiratory systems were studied. SUN 1165, at doses of up to 1.0 mg/kg i.v., had almost no effect. SUN 1165, at doses of 3.0 and 6.0 mg/kg i.v., caused dose-dependent decreases in blood pressure, common carotid, vertebral, coronary, hepatic and femoral artery and portal vein blood flows, cardiac contractility, heart rate and myocardial oxygen consumption. SUN 1165 increased urine volume and urinary excretion of electrolytes in rats at a dose of 100 mg/kg p.o. SUN 1165 decreased renal plasma flow and urinary excretion of electrolytes in anesthetized dogs at 6.0 mg/kg i.v., but at the antiarrhythmic doses (1.0-3.0 mg/kg i.v. in dogs), it had almost no effects on renal function. SUN 1165 had almost no effect on the autonomic nervous systems in anesthetized dogs. These results suggest that SUN 1165 at the antiarrhythmic doses do not have any effects on the respiratory and cardiovascular systems, renal function and autonomic nervous systems in rats and dogs, but that when administered at high doses, it has inhibitory effects on respiratory and cardiovascular system and renal function. In conclusion, SUN 1165 seems to be a novel antiarrhythmic drug relatively free of cardiovascular, respiratory, renal and autonomic effects.     

黄耆的利尿与降压作用

给大白鼠皮下注射及麻醉狗静脉注射黄耆0.5克/公斤后,均可产生显著的利尿作用;给正常人口服0.2克/公斤后亦可产生显著的利尿作用.黄耆的利尿作用持续时间较长,给大白鼠皮下注射后,利尿作用可持续7天,连续给药7天后无耐受性.大白鼠皮下注射0.5克/公斤的利尿效价与氨茶碱0.05克/公斤及双氢氯噻嗪0.2毫克/公斤者相当.给麻醉狗静脉注射或灌胃黄耆0.5克/公斤后,均可引起明显的降压作用,重复静脉注射时出现快速耐受性.黄耆的毒性很小,给小白鼠灌胃75克/公斤无异常症状,小白鼠的半数致死量(腹腔注射)为40±5克/公斤,大白鼠慢性毒性试验未出现不良反应.     

Pharmacological and toxicological properties of the saluretic xipamide (4-chloro-5-sulfamoyl-2',6'-salicyloxylidide)]

Xipamide (4-chloro-5-sulfamoyl-2',6'-salicyloxylidide, Aquaphor), a new compound is a derivate of salicylic acid with marked sodium and water excreting potency. Its effect is dosage dependent. Dosages as low as 0.001 mg/kg p.o. in rats and 0.04 mg/kg p.o. in dogs lead to a statistically significant increase of sodium and water excretion. Potassium excretion was less affected and showed to be rather constant in a dosage range between 0.01 and 10.0 mg/kg. In rats a maximum of sodium and water excretion could be reached by a dose of 200 mg/kg duration of action in rats was approximately 10 h. In dogs a statistically significant sodium and chloride excretion could be detected after oral application of 0.04 mg/kg. Xipamide increased diuresis started with an oral dose of 0.1 mg/kg. Intravenous application of xipamide in a dose of 0.2 mg/kg in dogs accompanied by permanent infusion of 5 per cent mannit solution clearly showed the diuretic profile of the substance: increased diuresis started within 40 min. A peak was reached within 40-60 min post injectionem. Then excretion decreased slowly. Even 120 min post injectionem a diuretic action could be detected. Diuresis and sodium excretion could be demonstrated in rats with experimentally predamaged kidneys and with steroid dependent sodium retention. As could be demonstrated in hypertensive rats xipamide had a hypotensive effect, normotensive rats were not affected. In animal studies xipamide was excellently tolerated. The therapeutic range of the substance was high in single doses as well as when the drug administered over 6 weeks.     

Pharmacological properties of the novel highly potent diuretic 7-chloro-2,3-dihydro-1-(2-methylbenzoyl)-4(1H)-quinolinone 4-oxime-O-sulfonic acid potassium salt.

7-Chloro-2,3-dihydro-1-(2-methylbenzoyl)-4(1H)-quinolinone 4-oxime-O-sulfonic acid potassium salt (M17055, CAS 114417-20-8) showed potent diuretic and saluretic effects dose-dependently, in rats (p.o.), mice (p.o.) and dogs (i.v.), at doses of 0.1-100 mg/kg, 0.3-100 mg/kg and 0.01-30 mg/kg, respectively. The efficacy of M17055 for diuresis, natriuresis and chloruresis was much higher than that of hydrochlorothiazide and almost the same as that of furosemide. These results indicate that this compound may be classified as a "high ceiling diuretic". The potencies of M17055 for natriuresis in rats (p.o.), mice (p.o.) and dogs (i.v.) calculated with ED50 values were 38, 34 and 24 times, respectively, more potent than those of furosemide. Urinary excretions of sodium, chloride and potassium increased in parallel with urinary volume with the administration of M17055 or furosemide, whereas an apparent dissociation with urinary calcium and sodium excretion was observed with M17055 alone. In rats, the increase of urinary calcium excretion with M17055 was significantly lower than that with furosemide under comparable conditions of natriuresis. Moreover, in mice, M17055 decreased urinary calcium excretion at doses with low effectiveness. In clearance studies using anesthetized dogs, M17055 suppressed negative free water clearance (CH2O) under saline loaded conditions, and it decreased positive CH2O under water diuretic conditions. These changes in the effects on CH2O induced by M17055 resemble those of loop diuretics. However, M17055 could not shift negative CH2O to positive, while furosemide was able to do so. Moreover, positive CH2O decreased to nearly zero with M17055, while urine remained dilute with furosemide even at 30 mg/kg.(ABSTRACT TRUNCATED AT 250 WORDS)     

中国萝芙木的药理研究,Ⅱ.海南岛萝芙木的降压作用和毒性试验

在发现广东大陆部分出产蘿芙木后,植物学家又相继在海南岛、云南和广西发现了蘿芙木,经鉴定和广东所产为同一品种,即Rauwolfia verticillata (Lour.) Baill. 我们在肯定了广东所产蘿芙木叶的粗制剂和生物硷的降压作用后,首先用海南岛所产叶的粗制剂物和生物硷进行实验,结果也发现它们有显著的降压作用。由于化学研究指出根含生物硷较多,因而又进行试验,肯定了根的生物硷的降压作用。此外,又进行     

PHARMACOLOGICAL PROFILE OF ORALLY ADMINISTERED YM087, A VASOPRESSIN ANTAGONIST, IN CONSCIOUS RATS

1. YM087 is a newly synthesized non-peptide arginine vasopressin (AVP) antagonist that shows high affinity for both V1A and V2 receptors. In the present study, the V1A and V2 receptor antagonist effects of orally administered YM087 were assessed in conscious rats. 2. In conscious rats, orally administered YM087 (0.1, 0.3 and 1.0 mg/kg) did not affect basal blood pressure, but YM087 dose-dependently inhibited 30 mU/kg, i.v., AVP-induced pressor responses. This inhibition lasted for over 8 h following the oral administration of the highest dose of YM087 (1 mg/kg). 3. In rats deprived of water and food for 16-18 h, oral administration of YM087 (0.1, 0.3, 1 and 3 mg/kg) dose-dependently increased urine volume and reduced urine osmolality, with associated increases in urinary sodium and potassium excretion. However, these increases in electrolyte excretion were lower than those seen at comparable diuretic doses of furosemide (3, 10, 30 and 100 mg/kg, p.o.). 4. Oral administration of YM087 (0.3, 1 and 3 mg/kg) produced a dose-dependent increase in urine volume in rats allowed free access to water, with the diuretic effect peaking 2-4 h post-dosing at all dose levels. The diuretic effect of YM087 was sustained 8-10 h after a dose of 3 mg/kg; this is in contrast with the transient diuresis seen after furosemide (100 mg/kg, p.o.) dosing. 5. The present results demonstrate that YM087 is an orally active AVP antagonist with potent and long-lasting effects. YM087 suppressed V1A receptor-mediated pressor responses to AVP with minimal effects on basal haemodynamics and exerted a diuretic effect without increased electrolyte excretion by inhibiting V2 receptor-mediated water reabsorption.     

Effect of yohimbine on xylazine-induced diuresis in rats

Intraperitoneal (ip) administration of xylazine (1-6 mg/kg) in male rats significantly increased urine flow over a 2-hr period in a dose-dependent manner, while urine osmolality was significantly decreased. Xylazine at 4.5 and 6 mg/kg significantly increased sodium excretion, whereas the 3 and 6 mg/kg doses of xylazine significantly increased potassium excretion. Yohimbine injected ip at 0.5 or 1 mg/kg 15 min before xylazine (6 mg/kg, ip) significantly decreased urine flow by 44% and 64% respectively. Yohimbine also prevented the increase in sodium and potassium excretion induced by xylazine. The data indicate that yohimbine is of value in controlling the diuretic effect of xylazine in rats.     

Diuretic activity of leaves of garcinia cambogia in rats

The present study was undertaken to establish the diuretic activity of ethanol and aqueous extract of dried leaves of Garcinia cambogia in rats. Aqueous and ethanol extracts of leaves were administered to experimental rats orally at doses of 100 and 200 mg/kg and compared with furosemide (20 mg/kg, intraperitoneally) as the standard. The parameters measured for diuretic activity were total urine volume, urine concentration electrolytes such as sodium, potassium and chloride have been evaluated . The rats treated with ethanol extract of Garcinia cambogia and aqueous extract of Garcinia cambogia in a dose of 100 and 200 mg/kg showed higher urine output when compared to the respective control. Both ethanol and aqueous extracts have showed a significant dose-dependent increase in the excretion of electrolytes when compared to the control group.