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1.
目的:研究8-羟基二氢小檗碱和小檗碱与多药耐药基因之间的作用。方法:采用MTT比色法测定药物的细胞毒浓度,适时定量PCR测定不同多药耐药基因的表达。结果:在1~100μM浓度范围内,8-羟基二氢小檗碱和小檗碱对Caco-2细胞无毒性作用;8-羟基二氢小檗碱和小檗碱对mdr1和mrp 1的表达作用一致,在25~100μM范围内,小檗碱能明显降低mrp2的mRNA表达,而8-羟基二氢小檗碱对其无明显影响。结论:8-羟基二氢小檗碱与小檗碱对mrp2的基因表达差异较大,其对MRP2蛋白表达的作用以及与基因调控之间的作用关系还有待更进一步的研究。  相似文献   

2.
Herbal products are popular among women during the perinatal period. St John's wort (SJW), Hypericum perforatum, is a common remedy for mild depression, a problem prevalent in this population. Although the safety of herbal products must be investigated, ethical issues constrain intervention studies in humans. Hence, animal studies often inform clinical decisions. The objective of this study is to systematically review rodent studies assessing the safety of SJW during the perinatal period. A literature search to November 10, 2017, identified 10 rodent studies that met a priori inclusion criteria. Study quality was evaluated according to both the Systematic Review Centre for Laboratory animal Experimentation tool for assessing bias and recommendations for appropriate reporting of herbal medicine research. Significant methodological limitations were found in each of the studies reviewed. These limitations include the lack of botanical verification and omission of extract characterization, inadequate explanation of dosage rationale, and absence of bias limiting protocols. Critical appraisal with contemporary tools indicates that each of the reviewed studies lacks appropriate rigour, rendering the results unreliable. Despite this, these papers are used in the rationale for recommending or contraindicating SJW during pregnancy and lactation.  相似文献   

3.
Classic synthetic antidepressant drugs, as well as St John's wort extract (SJW), directly inhibit the re‐uptake of norepinephrine (NE) and/or serotonin (5‐HT) into pre‐synaptic axons. With chronic treatment they induce adaptive changes in a number of neurotransmitter receptors in synaptic membranes. The immediate effects of SJW Ze 117, an extract low in hyperforin content, on the specific dopamine (DA) uptake were studied in rat striatal brain slices and compared with the effects on NE and 5‐HT uptake in rat cortical brain slices. Specific DA uptake was inhibited in a dose dependent manner. In contrast to the findings in synaptosomal preparations published so far, the extract showed different inhibitory potencies for the respective transporters. The potencies for the uptake inhibition of NA, DA and 5‐HT were 30, 7 and 1, respectively. The results indicate that the SJW Ze 117 extract interferes in three ways with the individual uptakes of the relevant neurotransmitters that are considered to be causal in the development of depression. This observation, the concomitant and potent inhibition of DA re‐uptake by SJW extract, may additionally provide a rationale for the treatment of nicotine or drug addiction with SJW. Copyright © 2009 John Wiley & Sons, Ltd.  相似文献   

4.
The effect of an aqueous extract of fresh floral buds of Jasminum officinale var. grandiflorum Linn. has been studied on female fertility in rats. Parameters included effects on the oestrus cycle, implantation, fetal loss, abortion, teratogenicity and serum progesterone levels on days 5, 12 and 20 of pregnancy. The extract at oral doses of 250 and 500 mg/kg produced a dose dependent significant antiimplantation effect, but failed to produce complete infertility. Treatment of animals during day 8 to day 12 to day 20 of pregnancy did not produce any significant abortifacient activity. There was no significant change in the weight and length of the fetuses delivered by rats treated with extract and no abnormalities were seen in the organs of the offspring. The extract produced a significant decrease in serum progesterone levels on day 5 of pregnancy which may be responsible for the antiimplantation effect observed in this study.  相似文献   

5.
A persistent need exists for effective treatment agents for mycobacterial infections. This research investigated the effectiveness of the Hypericum perforatum herb (commonly known as St John's wort; SJW) in its growth inhibition of mycobacteria. A SJW extract was effective at inhibiting five nonpathogenic Mycobacterium isolates and Bacillus subtilis, but not Escherichia coli. Quantitative studies of concentration sensitivity to the SJW extract were performed with minimal bactericidal concentrations (MBC) ranging from 0.33 to 2.66 mg extract/mL. The SJW compounds hyperforin (Hfn), hypericin (Hpn), and pseudohypericin (Phn) were quantified in the extract using HPLC. The SJW extract solution of 133 mg extract/mL used in this study contained 2.3 mg Hfn/mL, 0.8 mg Hpn/mL, and 2.1 mg Phn/mL. Purified Hfn, Hpn, and Phn were tested for inhibitory activity against Mycobacterium JLS (M. JLS) at similar concentrations used in the crude extract. While Hfn was inhibitory at 46 µg/mL, none of the purified SJW constituents were bactericidal at concentrations corresponding to SJW treatments. Scanning electron microscopy (SEM) analysis of SJW‐treated M. JLS cells showed changes in cell surface morphology. Copyright © 2012 John Wiley & Sons, Ltd.  相似文献   

6.
St John's wort extract (SJW; Hypericum perforatum L.) is taken extensively as a putative herbal antidepressant. It has been shown to induce the activity of cytochrome P-450 3A4 (CYP3A4) and to increase the clearance of numerous drugs and steroids such as cortisol and ethinyl estradiol. This study was conducted to determine if SJW exposure also alters the concentrations of circulating androgenic steroid hormones. The study was conducted using healthy volunteers (6M, 6F) studied before and after a 14-day treatment period with a SJW preparation previously demonstrated to induce the activity of CYP3A4. Plasma concentrations of testosterone, dihydrotestosterone (DHT), dehydroepiandrosterone sulfate (DHEAS), sex hormone-binding globulin (SHBG) and the combined concentrations of androsterone sulfate (AoS) and epiandrosterone sulfate (epiAoS) were measured by immunoassay methods. The results of analysis demonstrated that SJW did not significantly alter the majority of the androgens studied (p > 0.05) although the combined concentrations of the 5alpha-reduced steroids, AoS and epiAoS, significantly declined following treatment in all subjects (p = 0.02), and in males (p = 0.04). Furthermore, the testosterone to DHT ratio was increased in both men and women. Although the latter increase did not reach statistical significance, it is also consistent with the possible inhibition of 5alpha-reductase by SJW. It is concluded that despite significant induction of CYP3A4, short term administration of SJW does not significantly alter the concentrations of most circulating androgens in men and women but may produce a dimunition in some of the circulating 5alpha-reduced androgens.  相似文献   

7.

Ethnopharmacological relevance

There is no evidence in the literature that substantiates the safety of Campomanesia xanthocarpa (Berg.) use during pregnancy.

Materials and methods

Thirty three female rats were randomly assigned to three groups. One group of animals received the Campomanesia xanthocarpa extract via gavage at a dose of 26.3 mg/kg/day from 6 to 15 days of pregnancy (organogenic period, T1) and another group received the same extract throughout the gestational period (from the 1st to the 20th day of pregnancy, T2). Control groups received distilled water. Euthanasia was done on 20th day, when the liver, kidney, spleen ovaries, fetuses and their respective placentas were removed. Implantations, reabsorptions, live and dead fetuses were recorded.

Results and conclusions

Campomanesia xanthocarpa, in these experimental conditions, did not disturb the reproductive function of female rats and did not interrupt the progress of the embryofetal development. Moreover, our results provide further evidence that the Campomanesia xanthocarpa treatment reduces reabsorption sites, increases placenta weight and the number of live fetuses and may therefore have therapeutic applications.  相似文献   

8.
We aimed to study the effects of gingko biloba extract (EGb) on oxidative stress, astrocyte maturation and cognitive disfunction in offspring of hyperhomocysteinemic rats. Hyperhomocysteinemia was induced in the pregnant rats by administration of methionine (1 gr/kg body weight) dissolved in drinking water throughout pregnancy. One group of animals has received same amount of methionine plus 100 mg/kg/day EGb during pregnancy. On the postnatal day 1, half of the pups from all groups were sacrificed to study the lipid peroxidation (LPO) in different subfractions of brain. Other half of pups were tested in Morris water maze to assess differences in learning and memory performance at the 75 days of age. Maternal hyperhomocysteinemia significantly increased LPO levels especially in mitochondrial subfraction of fetal pup brains. EGb significantly prevented this LPO inrease. Methionine administration to animals reduced glial fibrillary acidic protein (GFAP) expression in pup brains significantly. EGb administration improved GFAP expression significantly. Offspring of hyperhomocysteinemic animals had poor long term spatial memory performance on Morris water maze and EGb administration had no effect on impaired spatial memory. In conclusion, maternally induced hyperhomocysteinemia significantly increased oxidative stress, decreased expression of GFAP and impaired learning performance. Copyright © 2011 John Wiley & Sons, Ltd.  相似文献   

9.
The effect of the leaf extract of Biophytum sensitivum, an annual herb used in traditional Nepalese folk medicine for the treatment of hyperglycemic patients, was studied on glucose homeostasis in rabbits. In the first set of experiments, an acute effect of the extract on fasting plasma glucose (fpg) levels and serum insulin response was examined in non-diabetic and alloxan-diabetic rabbits. Initial dose-response studies showed that a dose of 200 mg/kg body weight (b.w.) was optimum for hypoglycemia. A single administration of this dose to 16-h fasted non-diabetic rabbits brought about a 16.1% fall in fpg at the end of 1 and 2 h, and the hypoglycemic effect persisted at the end of 6 h (13.8% fall). Serum insulin levels showed a significant rise in the treated animals, which suggested a pancreatic mode of action (i.e. insulinotropic effect) of B. sensitivum. The study of an acute effect of the extract in alloxan-diabetic rabbits, however, showed that it failed to produce such hypoglycemic or serum insulin response. In another set of experiments, administration of the above dose of the leaf extract attenuated the plasma glucose response to oral administration of 3 g/kg b.w. glucose load. The serum insulin levels in the treated animals showed a rise at the end of 2 (13.7% rise) and 6 h (12.6% rise). Taken together, these observations suggest that the hypoglycemic response of B. sensitivum may be mediated through stimulating the synthesis/release of insulin from the beta cells of Langerhans.  相似文献   

10.
猕猴桃水提物诱导二相酶产生及抗氧化的机制研究   总被引:1,自引:1,他引:0  
目的:本实验以人胃腺癌细胞株SGC-7901为模型,用猕猴桃水提物含药血清进行干预,探讨猕猴桃水提物诱导二相酶产生及抗氧化的机制.方法:取正常SD大鼠随机分为猕猴桃水提物高、中、低剂量组(用猕猴桃水提物溶液46.8,31.2,15.6 g·kg-1 ig)和正常对照组(ig给予生理盐水).连续14 d,每天ig 2次,于末次给药1h,腹主动脉取血制备猕猴桃水提物含药血清.取对数生长期的SGC-7901细胞,在不同时间段分别给予相应的含药血清进行干预.用免疫组化法检测SGC -7901细胞内活化状态的核因子相关因子2(Nrf2)的细胞定位;RT-PCR法检测猕猴桃水提物高剂量组含药血清对SGC-7901细胞内二相酶mRNA水平的影响.结果:免疫组化法染色观察结果显示与正常对照组相比,猕猴桃水提物含药血清低、中、高剂量组均可提高Nrf2细胞核内的表达水平,颜色从浅黄色变为棕黄色.经积分统计学分析差异有显著性(P<0.05或P<0.01).RT-PCR检测结果显示与正常对照组相比较,猕猴桃水提物可明显诱导二相酶谷氨酰半胱氨酸合成酶催化亚单位(GCLC)基因的表达(P<0.05),且诱导谷胱甘肽-S-转移酶(GST) -P1和GST-T1基因表达作用差异有高度显著性(P<0.01),但对二相酶GST-M1和醌氧化还原酶(NQ01)基因水平影响不大.结论:猕猴桃水提物可促使Nrf2进入核内,导致二相酶的表达增加,具有诱导细胞解毒抗氧化作用.  相似文献   

11.
目的:阐明长期给药何首乌醇提物 (PME) 和水提物 (PMW) 致大鼠肝损伤的可能机制。方法:分别制备 PME 和 PMW。雄性 SD 大鼠随机分为对照组、阳性对照异硫氰酸 α-萘酯 (ANIT 100 mg·kg–1) 组、PMW组 (15 g·kg–1)、PME 组 (12 g·kg–1)。PME、PMW 组大鼠给药剂量相当于 60 g·kg–1生药量,约为临床最大量的110 倍,灌胃给药 42 d,每日给药 1 次。ANIT 组于第 40 天灌胃给药 1 次。采用试剂盒方法检测大鼠血清生化指标丙氨酸氨基转移酶 (ALT)、天冬氨酸氨基转移酶 (AST)、总胆汁酸 (TBA)、碱性磷酸酶 (ALP)、总胆红素(TBIL) 水平;采用苏木素-伊红 (HE) 染色法检测大鼠肝脏病理变化;采用实时荧光定量聚合酶链式反应 (qRT-PCR) 测 定 给 药 后 大 鼠 肝 脏 组 织 中 胆 汁 酸 、 胆 红 素 代 谢 相 关 转 运 体 有 机 阴 离 子 转 运 多 肽 1a1 (OATP1a...  相似文献   

12.
The aim of this study was to demonstrate the effects of single and repeated oral administration of the aqueous rhizomes extract of Triticum repens (TR) (20 mg/kg) on lipid metabolism in normal and streptozotocin-induced diabetic rats. In normal rats, the aqueous extract of TR induced a significant decrease in the plasma triglycerides concentrations 4 days (P<0.05) and 1 week after repeated oral administration (P<0.05). This reduction was abolished 2 weeks after once daily repeated oral administration. A significant decrease of plasma cholesterol levels was observed only 1 week (P<0.05) after repeated oral administration.

In diabetic rats, TR treatment caused a significant decrease in plasma triglycerides levels after a single (P<0.01) and repeated (P<0.001) oral administration. A strong decrease in cholesterol level was observed 6 h after a single oral administration of the aqueous extract TR (P<0.001). Four days after repeated oral administration of TR aqueous extract, the plasma cholesterol level was significantly decreased (P<0.05) and still dropped after 2 weeks (P<0.001).

On other hand, the repeated oral administration of aqueous TR extract caused a significant decrease in body weight 2 weeks after repeated oral treatment in diabetic rats (P<0.05).

We conclude that the aqueous extract of TR exhibits lipid and body weight lowering activities in severe hyperglycaemic rats after repeated oral administration of aqueous TR extract at a dose of 20 mg/kg.  相似文献   


13.
目的研究白藜芦醇(Res)体外对K562/AO2增殖及凋亡的影响,并探讨与耐药基因mdr1表达的关系。方法用噻唑蓝比色法(MTT)检测对照组、不同剂量Res组(25~200μmol/L)作用48 h后K562/AO2增殖率,用流式细胞仪检测各组凋亡率,并用逆转录-聚合链反应(RT-PCR)法检测各组mdr1 mRNA的表达。结果Res体外对人K562/AO2细胞有显著增殖抑制及凋亡诱导作用,Res组(25μmol/L、50μmol/L、100μmol/L、200μmol/L)作用48 h后其凋亡率均显著高于对照组(P<0.05);mdr1 mRNA表达相对强度均显著低于对照组(P<0.05),且随浓度增加而表达减弱。结论Res体外能诱导K562/AO2细胞的凋亡,且呈一定的浓度依赖性,其作用机制可能与逆转mdr1 mRNA基因表达有关。  相似文献   

14.
目的 基于Ang/Tie-2信号通路,探讨补肾活血方孕前导法给药调控肾虚血瘀-胚胎着床障碍病证结合模型大鼠种植窗期子宫组织血管生成的助孕机制。方法 阴道涂片HE染色法观察,选取动情周期规律的健康未交配雌性SD大鼠60只,随机分为5组:空白组、模型组、阿司匹林组、补肾活血方高剂量组、补肾活血方低剂量组,动情前期时入组,分组给药并合笼,于妊娠第5天处死,腹主动脉采血后,迅速剖取子宫并制片,采用光镜观察各组大鼠子宫内膜组织形态,采用免疫组化法(IHC)检测各组大鼠子宫组织中VEGF、FLK-1表达水平及螺旋动脉数量,采用Western-Blot检测各组大鼠子宫组织中Ang-1、Ang-2、Tie-2蛋白表达水平,采用Real-Time PCR检测各组大鼠子宫组织中Ang-1、Ang-2、Tie-2 mRNA表达水平。结果 给药组能明显改善肾虚血瘀-胚胎着床障碍病证结合模型大鼠种植窗期子宫内膜组织形态,并接近空白组水平;模型组大鼠子宫湿重、子宫脏器指数、螺旋动脉数量、VEGF、FLK-1及子宫组织Tie-2蛋白表达、Ang-1mRNA、Ang-2mRNA和Tie-2mRNA表达等均较空白组降低(P < 0.05);补肾活血方高剂量组大鼠妊娠第5天子宫组织VEGF、FLK-1、螺旋动脉数量、Ang-1蛋白、Tie-2蛋白及Ang-1mRNA、Tie-2mRNA表达量较模型组明显增加(P< 0.01)。结论 补肾活血方孕前导法给药,改善肾虚血瘀-胚胎着床障碍病证结合模型大鼠种植窗期子宫内膜组织形态,促进子宫组织血管生成,改善组织血瘀状态,促进胚胎着床,可能与其提高大鼠子宫组织VEGF、FLK-1、Ang-1、Tie-2表达水平,并维持Ang-2正常表达有关。  相似文献   

15.
Aqueous extract of the root of Momordica angustisepala (Cucurbitaceae) has been studied for abortifacient effects in albino female mice. The aqueous extract containing 0.8 mg dry matter/ml at dosages of 3.5 ml and 4 ml per kg body wt. of the female mice and guinea pig, respectively, was administered i.p. Several hours after administration, the pregnant animals aborted their fetuses. The drug appears to be effective at all stages of pregnancy confirming its use by herbalists to induce abortion in humans in some parts of Nigeria. The mechanism of action appears to be similar to the actions of oxytocics and ergot alkaloids. However, hormonal influence may be implicated.  相似文献   

16.
An aqueous leaf extract of Cassia auriculata (C. auriculata) was found to lower the serum glucose level in normal rats. Maximum reduction in serum glucose level was observed after 4 h at a dose levels of 100, 200, 400 mg/kg body weight of the extract. In normal rats the serum glucose level reduction at 4th h was 23% by 100 mg/kg body weight and 31% by 200 mg/kg body weight. In alloxan-induced diabetic rats, chronic administration of the extract significantly reduced the serum glucose level from third day to till the end of the experiment. The extract was also found to inhibit the body weight reduction induced by alloxan administration. Glucose uptake and glycogen deposition studies suggest that C. auriculata leaf extract probably has no direct insulin like effect which can enhance the peripheral utilization of glucose.  相似文献   

17.
小檗胺对多药耐药K562/Adr细胞作用的研究   总被引:5,自引:0,他引:5       下载免费PDF全文
目的研究小檗胺诱导人白血病K562/Adr细胞凋亡及逆转多药耐药的作用及机理。方法采用MTT法测IC50值,流式细胞仪Annexin V FITC-PI法检测细胞凋亡发生率,PI染色法检测凋亡峰及细胞周期,同时以FCM检测Caspase-3、P-GP蛋白表达及细胞内药物积聚能力,RT-PCR法检测mdr-1基因表达。结果小檗胺能抑制人白血病K562/Adr细胞生长且呈剂量依赖关系,并能诱导细胞凋亡,使Caspase-3蛋白表达及细胞药物外排能力增加,同时降低mdr-1基因mRNA和蛋白表达水平。结论小檗胺能激活Caspase-3以诱导人白血病K562/Adr细胞凋亡,同时能通过降低mdr-1表达逆转多药耐药。  相似文献   

18.
千里光、千柏鼻炎片和总生物碱大鼠胚胎毒性研究   总被引:1,自引:1,他引:1  
目的:探讨千里光及其复方千柏鼻炎片的胚胎毒性及其特点,为妊娠期安全用药提供参考.方法:选取受孕SD雌性大鼠220只,随机分为对照组;环磷酰胺组(10 mg·kg~(-1))、千里光水提物低、中、高剂量组(含生药7.5,15.0,30.0 g·kg~(-1);千柏鼻炎片复方提取物低、中、高剂量组(含生药7.5,15.0,30.0 g·kg~(-1);千里光总生物碱提取物低、中、高剂量组(含生药7.5,15.0,30.0 g·kg~(-1)等11组,于大鼠胚胎器官形成期(妊娠期第6~15天)给药,于妊娠期间定期称量母鼠体重和摄食量,称量子宫质量和胎仔体重,记录早期吸收胎、晚期吸收胎、F吸收胎、死胎、活胎、黄体以及着床腺数目和胎仔性别.对每只胎仔进行外观检查,测量胎仔的身长和尾长,并进行内脏检查和骨骼检查.结果:复方高剂量组的母鼠体重增长减缓,摄食量降低;各种受试物给药组均未见吸收胎明显增高,但水提物和总碱高剂量组的死胎百分数(分别为2.7%,3.36%)较对照组(0.0%)显著升高;总碱高剂量组的胎仔体重和身长明显降低.水提物、复方和总碱各剂鼍组均可见一定程度的骨骼发育异常,主要表现为囟门增大,顶骨、顶间骨、枕骨发育不全或枕骨缺失、颈椎弓发育不全,少数动物出现第14对肋骨等,剂量关系不明显.总碱组骨骼畸形发生的窝百分率高达80%,复方的死胎发生率和骨骼急性发生率相对较低.结论:千里光单味药及其复方均具有一定程度的胚胎毒性,主要表现为骨骼发育异常.尽管复方的胚胎毒性与单味药比较相对较低,但复方仍然能够造成部分动物胎儿骨骼畸形,因此建议千里光以及含千里光的复方在妊娠期禁用.  相似文献   

19.
A developmental toxicity-screening test of valerian   总被引:1,自引:0,他引:1  
Valerian (Valeriana Officinallis) is a perennial plant used as a mild sedative for anxiety and for insomnia. It is also used in the treatment of gastrointestinal cramps and as a diuretic. It is traditionally contraindicated in pregnancy; however, there are no studies to warrant this warning. This study was performed to provide some information to fill this knowledge gap. Female rats were orally dosed with a valerian extract in 45% ethanol (supplied by MediHerb) daily on either gestation days (GD) 1-8 or 8-15. On GD 20, rats were sacrificed and fetuses, placentae and ovaries collected. The fetuses were weighed and examined for external malformations. No signs of maternal toxicity were evident. Results indicated that valerian had no adverse effects on fertility or fetal development. Valerian induced toxicity when GD 10.5 embryos were cultured for 26h in rat serum to which 6 microl/ml of the extract was added. The results of the present preliminary study showed that consumption of up to 65 times the human dose of the valerian extract supplied by Mediherb did not have an adverse reproductive outcome in rats. This may be a result of low pH of the extract removing the potentially cytotoxic epoxide moieties. However, consumption of other preparations of valerian, particularly if they contained considerable levels of valepotriates could have a very different outcome.  相似文献   

20.
A study was designed to elucidate the mechanism of anti-hypertensive effects of danshen in the two-kidney, one clip (2K1C) Goldblatt renovascular hypertensive model, which is the renin-angiotensin system (RAS)-dependent hypertensive model. We investigated the effects of water extracts of danshen on the angiotensin converting enzyme (ACE) activities, systolic blood pressure (SBP), and hormone levels in the plasma of 2K1C rats. ACE activity was inhibited by the addition of danshen extract in a dose-dependent manner. SBP was decreased significantly after administration of danshen extract in 2K1C, whereas plasma renin activity (PRA) was not changed. The plasma concentration of aldosterone (PAC) was decreased significantly in 2K1C group administered with Danshen extract, whereas the plasma concentration of ANP was increased by administration of danshen extract for three weeks. These results suggest that danshen has an anti-hypertensive effect through the inhibition of ACE, an essential regulatory enzyme of RAS.  相似文献   

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