补骨脂素、异补骨脂素和补骨脂酚急性毒性的性别差异研究

[目的] 探究补骨脂素、异补骨脂素和补骨脂酚对小鼠急性毒性的性别差异。[方法] 补骨脂素给药剂量为雌性（1 125、843、633、475、356 mg/kg）、雄性（633、475、356、267、200 mg/kg）,异补骨脂素给药剂量为雌性（404、343、292、248、210 mg/kg）、雄性（317、292、269、248、229 mg/kg）,补骨脂酚雌、雄剂量均为2 000、1 765、1 500、1 200、1 020 mg/kg。一次性灌胃给予受试药,连续观察并记录14 d小鼠的毒性反应、体质量和死亡情况,应用SPSS统计学软件,采用Probit回归法计算半数致死量（LD₅₀）和95%可信区间。[结果] 给药后小鼠毒性反应主要表现为抽搐、四肢强直,部分动物口眼周围有分泌物,剂量越高反应越明显。与对照组比较,补骨脂素、异补骨脂素给药组随给药剂量增大,小鼠体质量呈现降低趋势。补骨脂素雌性小鼠的LD₅₀为514.35mg/kg,雄性小鼠LD₅₀为421.37 mg/kg,雌性小鼠LD₅₀值比雄性高出22%。异补骨脂素雌性小鼠LD₅₀为258.02 mg/kg,雄性小鼠LD₅₀为255.26 mg/kg。补骨脂酚雌性小鼠LD₅₀超出2 000 mg/kg,雄性小鼠LD₅₀为1 679.4 mg/kg。[结论] 补骨脂素和补骨脂酚对小鼠的急性毒性存在一定性别差异,但无统计学意义。     

过氧乙酸消毒剂的毒性试验

目的：对一元包装过氧乙酸消毒剂的急性和亚急性毒性进行研究,为其安全使用提供依据。方法依据卫生部《消毒技术规范》（2002年版）进行试验：（1）急性毒性试验：选用健康Wistar大鼠60只,随机分组,一次性经口灌胃不同剂量消毒剂,观察大鼠的中毒症状和死亡情况,计算半数致死量（LD50）。（2）亚急性毒性试验：选用健康Wistar大鼠40只,随机分为3个剂量组和阴性对照组,连续经口灌胃（33～342）mg/kg体重消毒剂28d,试验结束后检测大鼠体重、脏/体比值、血液学指标及血清生化指标,并进行病理组织学检查。结果对雌性、雄性大鼠LD50分别为1470mg/kg体重、1710mg/kg体重;大鼠亚急性试验各剂量组体重、血液学指标、生化指标、脏/体比值,与阴性对照组比较,统计学上均差异无显著性;大体解剖观察未见异常,未见与受试物有关的病理组织学改变。结论该过氧乙酸消毒剂对大鼠急性经口毒性为低毒级,且在本试验剂量范围内,未观察到明显的亚急性经口毒性。     

细辛脑注射制剂异常毒性检查标准研究

目的测定细辛脑注射制剂静脉给药的小鼠LD50值,同时起草本品异常毒性检查标准。方法采用加权回归机率单位法(Bliss法)对小鼠静脉给药测定LD50值,同时按照《中国药典》2010年版要求确定异常毒性检查限值,起草异常毒性标准。结果测定细辛脑注射制剂的小鼠LD50为51.9-153.1 mg/kg,为标准中拟增加异常毒性检查项,异常毒性检查项的限值建议定为15 mg/kg,按此限值检查结果符合规定。结论细辛脑注射制剂毒性较大,各企业生产工艺不同毒性也差异较大,为减少本品临床使用不良反应的发生,应在其质量标准中增加异常毒性检查项。     

护肝中药“五田保肝液”急性毒性实验研究

[目的]明确护肝中药"五田保肝液"的用药安全剂量范围,为临床用药安全提供实验依据。[方法]依据中药、天然药物急性毒性实验研究技术指导原则设计实验,观察小鼠急性毒性反应,并记录其死亡情况,确定急性毒性实验中五田保肝液半数致死量(LD50)或最大给药量。[结果]半数致死量实验中未测得LD50,最大给药量实验获得小鼠最大给药量折合生药228 g/(kg·d),相当于成人临床用药量的120倍。[结论]护肝中药"五田保肝液"急性毒性反应低,临床常用药物剂量安全可靠。     

In vivo antiplasmodial activity of Bombax buonopozense root bark aqueous extract in mice infected by Plasmodium berghei

Objective

To evaluate the in vivo antiplasmodial activity and the oral acute toxicity of the Bombax buonopozense root bark aqueous extract.

方剂配伍增加中药方剂活性——一项来自毒理学的实验研究

[目的] 比较不同制备方法对清热解毒方水煎剂毒性的影响。[方法] 清热解毒方中各味药材分别制备成不同待测样品：合煎样品、分煎样品及单味药给药样品,采用简化机率法测定各样品对小鼠灌胃给药的半数致死量（LD₅₀）,并比较测定结果。[结果] 所测得合煎样品和分煎样品的LD₅₀分别为（91.26±7.92）g/kg 和（111.47±9.12）g/kg,与合煎样品比较,分煎样品的毒性显著降低（P<0.05）,且动物死亡时间及死前表现不同。单味药样品给药后多未出现明显毒性反应。[结论] 与单味中药比较,复方配伍确能提高中药的生物活性。     

蟾酥抗肿瘤有效成分的活性追踪分离及急性毒性研究

目的 从传统中药蟾酥中寻找抗肿瘤活性强而毒性低的化合物。方法 采用追踪分离的方式,以体外肿瘤细胞生长抑制强度为活性指标,同时结合小鼠急性毒性实验,对蟾酥的主要化学成分进行初步研究。结果 采用活性追踪分离方式,从蟾酥中分离得到具有抑制肿瘤细胞生长活性同时对小鼠急性毒性较低的化合物蟾毒它灵,其对人非小细胞肺癌A549细胞具有较好的生长抑制作用,小鼠iv给药的LD₅₀约为蟾毒灵的4倍,而且稳定性较好。结论 综合化合物的活性、毒性及稳定性等因素,初步判断蟾毒它灵较其他同类化合物具有更好的抗肿瘤药物开发前景。     

季节性流感疫苗对小鼠感染H7N9禽流感病毒的保护效力

目的 评价季节性流感裂解疫苗对流感病毒H7N9的免疫保护效力。方法 用我国2012～2013年度季节性流感裂解疫苗,以腹腔注射方式免疫BALB/c小鼠,并设PBS免疫模型组,末次免疫14 d后以5 LD₅₀ A/Anhui/1（H7N9）进行攻试验。感染后观察记录小鼠临床表现,体重变化,并分别于第2天和第4天每组处死3只小鼠,取肺组织和鼻甲骨测病毒滴度和载量。结果 感染后疫苗与模型组小鼠体重下降明显,疫苗组存活率为10%,模型组全部死亡。感染后第4天疫苗组鼻甲骨滴度显著低于模型组。血凝抑制试验及中和实验表明免疫小鼠血清无中和H7N9病毒抗体。结论 季节性流感疫苗在小鼠中对于H7N9流感病毒感染无明显保护作用。     

小鼠急性铊中毒半数致死剂量的测定

目的 测定硝酸亚铊急性中毒小鼠的半数致死剂量(median lethal dose,LD50).方法 130只小鼠随机分为13组,每组10只,雌雄各半,给小鼠经口灌入不同剂量的硝酸亚铊水溶液,观察并记录2周内各组小鼠症状、毒性反应及死亡情况,观察死亡小鼠肠道的组织病理学变化.以小鼠死亡率为指标,按改良寇氏法计算其LD5...     

Effects of melatonin on changes in cognitive performances and brain malondialdehyde concentration induced by sub–chronic co–administration of chlorpyrifos and cypermethrin in male Wister rats

ObjectiveTo evaluate the ameliorative effect of melatonin on sub-chronic chlorpyrifos (CPF) and cypermethrin (CYP)-evoked cognitive changes in male Wistar rats.MethodsFifty adult male Wistar rats, divided into five groups of ten rats each, were used for the study. Groups 1 and II were given distilled water and soya oil (2 mL/kg) respectively. Group III was administered with melatonin at 0.5 mg/kg only. Group IV was administered with CPF [7.96 mg/kg (1/10th LD₅₀)] and CYP [29.6 mg/kg (1/10th LD₅₀)], and Group V was administered with CPF [7.96 mg/kg (1/10th LD₅₀)] and CYP [29.6 mg/kg (1/10th LD₅₀)] 30 min after melatonin (0.5 mg/kg). The regimens were administered by gavage once daily for 12 weeks. Thereafter, cognitive performances were determined and the brain was evaluated for malonaldehyde concentration.ResultsCPF and CYP induced cognitive deficits and increased brain malonaldehyde concentration, which were all ameliorated by melatonin.ConclusionCognitive deficits elicited by CPF and CYP was mitigated by melatonin due to its antioxidant property.     

芒果叶中芒果苷含量的测定

[目的]建立芒果叶中芒果苷含量的测定方法;测定不同时期芒果叶中芒果苷的含量。[方法]采用高效液相色谱法(HPLC),Cosmosil ODS柱分离,流动相:乙腈-1%冰醋酸溶液(15∶85)为流动相,流速1.0 mL/min,柱温25℃,检测波长254 nm。从海南采集不同时期的芒果叶,测定其中芒果苷含量。[结果]芒果苷在0.069 5~2.224 0μg范围内进样量与峰面积呈良好的线性关系,平均回收率96.77%,RSD=1.19%。[结论]所建立的芒果苷含量测定方法灵敏度高,准确度高,重现性好。     

基于斑马鱼幼鱼模型的甘遂毒性评价

[目的]以模式生物斑马鱼幼鱼为模型,评价甘遂不同溶剂连续提取物毒性差异及毒性特征。[方法]采用索氏提取法获得甘遂不同溶剂连续提取物。通过预实验,确定各提取物72 h最大不致死浓度和最小全致死浓度。在此区间设定6~8个药物浓度,建立致死曲线,计算半数致死浓度（LC₅₀）。以毒性最大提取物的10%致死浓度（LC₁₀）、最小致死浓度（LC₁）、1/3 LC₁和1/10 LC₁为给药浓度,同时设立空白组和溶剂对照组,连续给药72 h,观察甘遂毒性特征。停药后将幼鱼置于养殖水中恢复48 h,观察毒性可逆性。[结果]甘遂不同提取部位毒性顺序为石油醚 > 二氯甲烷 > 乙酸乙酯 > 乙醇提取物。甘遂的主要毒性为肝毒性和胃肠道刺激性。肝毒性既可造成肝肿大,又可导致肝变性,肝肿大不可逆,而肝变性具有可逆性。[结论]本实验首次利用单个模型以相同浓度单次给药,同时评价了甘遂对心脏、肝脏、肾脏、神经系统和胃肠道等脏器系统的毒性作用及可逆性。实验结果证实了甘遂的毒性集中于石油醚提取部位,并可对肝脏和胃肠道造成实质性损伤。本实验为斑马鱼模型在中药毒性评价中的应用提供了参考。     

Antioxidant,antimicrobial, cytotoxic and analgesic activities of ethanolic extract of Mentha arvensis L.

ObjectiveTo investigate potential antioxidant, antimicrobial, cytotoxic and analgesic activities of ethanolic extract of Mentha arvensis L. in different in vivo and in vitro experimental models.MethodsIn vitro DPPH radical scavenging assay was used to evaluate the antioxidant activity of the plant extract. In vivo analgesic activity was carried out by acetic acid-induced writhing test in Swiss albino mice. All studies in mice were undertaken at the doses of 250 and 500 mg/kg body weight. Antibacterial activity was studied by disk diffusion assay against some Gram-positive and Gram-negative bacterial strains. Brine shrimp lethality assay was used to investigate cytotoxicity effects of the plant extract.ResultsThe extract showed free radical scavenging activity in the DPPH assay (IC₅₀∼41 μg/mL) compared to the standard antioxidant ascorbic acid (IC₅₀∼19 μg/mL). The extract also produced prominent antimicrobial activity against Salmonella typhi, Salmonella paratyphi, Shigella boydii, Streptococcus pyogenes and Streptococcus aureus compared to standard drug kanamycin at the dose of 30 μg/disc. The extract exhibited lethality against the brine shrimp nauplii with the LC₅₀ values of 40 μg/mL, and also 90% mortality (LC₉₀) value was found to be 160 μg/mL. In analgesic test, the extract demonstrated statistically significant (P<0.01) analgesic effect in acetic acid induced writhing in white albino mice at both dose levels.ConclusionsThese results suggest that the ethanolic extract of Mentha arvensis L. has potential antioxidant, antibacterial, cytotoxic and analgesic activities that support the ethnopharmacological uses of this plant.     

SF型消洗灵毒性研究

SF型消洗灵(Na_3PO_4、1/4NaOCl、12H_2O)经成都市与北京市卫生防疫站对其消毒性能进行了鉴定,证明其对细菌及病毒均有良好的消毒效果。我们对其进行了急性毒性、蓄积毒性及诱变性的研究。结果小鼠经口LD_(50)为6937mg/kg 体重;雌、雄生大鼠的经口LD_(50)分别为6810及5010mg/kg 体重,属于基本无毒物质。蓄积系数大于12.8,表明无明显蓄积作用。小鼠骨髓微核试验、睾丸染色体畸变分析及Ames 试验均为阴性,未发现有诱变性。我们认为SF 型消洗灵用于食具及水果的洗涤与消毒,如果其残留量不大,是一种有前途的优良消毒洗涤剂。     

茶多酚急性、慢性毒性实验研究☆

ObjectiveThe study was to observe the acute and chronic toxicity of Tea Polyphenols(TP).Methodsthe mice were divided into five groups and TP was given orally for 7 days.The method of Bliss was used to determine the LD₅₀ of the TP.The rats was divided into control group,TP high dosage group,TP middle dosage group and low dosage group(0.4,0.6,0.8g/kg^.d^-1)to observe the chronic toxicity.ResultThe LD₅₀ of TP is 2.499g/kg.The rats have showed no toxicity reaction in weight,blood,the internal organs,liver and kidneys function after the using of the drug.ConclusionThe TP has low toxicity,the dosage of 0.8g/kg.d^-1 in rat is equivalent to 100 times of the dosage used in clinic for an adult.It indicates that the clinical using of TP is safe.     

知母水、醇提取液的急性毒性实验研究

[目的] 观察知母水、醇提取液的急性毒性反应。[方法] 选择昆明种小鼠为受试对象,采用急性经口毒性实验测定知母水、醇提取液的的最大耐受量。[结果] 知母水提液的小鼠经口最大耐受量为35.0g/kg。知母80%乙醇提取液的小鼠经口最大耐受量为37.5g/kg。[结论] 知母水、醇提取液的毒性较低,临床给药安全可靠。     

金莲花汤不同提取物对细胞增殖的影响及体外抗病毒活性研究

目的 探讨不同提取方法的金莲花汤提取物（金莲花汤不同提取物）对小鼠巨噬细胞Raw264.7增殖以及对小鼠H1N1流感病毒活性的影响方法 通过MTT法观察药物处理后对小鼠巨噬细胞Raw264.7生长增殖情况的影响;利用小鼠H1N1流感病毒感染MDCK细胞,进行病毒扩增并测定病毒效价;利用小鼠H1N1流感病毒感染小鼠巨噬细胞Raw264.7,采用MTT法结合CPE方法确定金莲花汤不同提取物的抗病毒效果。结果 MTT结果发现,金莲花汤不同提取物（20%、40%、60%、80%、95%、二次80%、二次95%及粗提取物）均对小鼠巨噬细胞Raw264.7增殖具有明显的抑制作用,IC₅₀分别为0.063、0.064、0.145、0.065、0.064、0.064、0.105、0.2mg/ml;MTT结果结合CPE分析显示,60%金莲花汤提取物IC₂₅及IC₅₀的药物剂量有轻微的抗病毒效果;80%金莲花汤提取物IC₀及二次95%金莲花汤提取物IC₂₅的药物剂量抗病毒效果较好,差异有统计学意义。结论 不同提取方法的金莲花汤提取物对小鼠巨噬细胞Raw264.7增殖有一定的抑制作用;在体外抗病毒实验中,一定提取纯度的金莲花汤提取物对小鼠H1N1流感病毒有抑制作用。     

Control of human filarial vector,Culex quinquefasciatus Say 1823 (Diptera: Culicidae) through bioactive fraction of Cayratia trifolia leaf

Objective

To investigate the mosquito larvicidal activity of Cayratia trifolia (L.) Domin (Vitaceae: Vitales) (C. trifolia) which is distributed in many parts of India with medicinal properties as vector control is facing threat due to the emergence of resistance to synthetic insecticides.

Methods

Young and mature leaves of C. trifolia were investigated for larvicidal activity against 3rd instars larvae of Culex quinquefasciatus in different seasons throughout the year. The active fractions were extracted using six different solvents in a non-polar to polar fashion viz petroleum-ether, benzene, chloroform: methanol (1:1 v/v), acetone, absolute alcohol and distilled water. Dose dependent mortality was recorded against each solvent extract. Determination of LD₅₀ and LD₉₀ were executed through log-probit analysis using the most bioactive fraction. The fluctuations in mortality were statistically co-related through ANOVA analyses concerning different seasons and types of leaves as random variables. Justification of larvicidal activity was established through student''s t-test. Costing effects were evaluated on the non-target water fauna under laboratory conditions. Thin layer chromatographic techniques were performed for phytochemical analysis and categorization of chemical personality of the active fractions using the most effective solvent extract following standard methods.

Results

Significant variations in mortality rate were noted with respect to the type of leaves (mature and senescence), concentration of leaf extract and between seasons. The water extract among all the solvent extracts was found to induce cent percent mortality at 50 mg/L in test mosquito species within 24 h with a LD₅₀ and LD₉₀ value of 10.70 mg/L and 27.64 mg/L respectively. No significant mortality was recorded in non-target water population. Chromatographic analyses of the water extract revealed the presence of steroids, triterpene glycosides, essential oil, phenolics and diterpenes as secondary phytochemicals.

Conclusions

Water extract of C. trifolia leaf promised as a cost effective and potent larvicidal agent against Culex quinquefasciatus.     

月腺大戟水提物对小鼠的毒性作用

目的：探讨月腺大戟水提物的毒性作用。方法:以实验用一级标准昆明种近交系小鼠为实验对象,随机分为5组。阴性对照组,给予蒸馏水灌胃;阳性对照组,腹腔注射环磷酰胺50mg·kg^-1;低、中、高剂量组,分别给予77、144、288g·kg^-1月腺大戟水提物灌胃,观察微核率、精子畸变率以及高剂量组的肝、脾、肾、心、脑、肺病理切片。结果:高剂量(288g·kg^-1) 月腺大戟水提物对脾脏、肾脏和心脏具有毒性作用;中、高剂量组的微核率和精子畸变率与阴性对照组均有统计学差异(P＜0.01, P＜0.005),低剂量组与阴性对照组无统计学差异(P＞0.05)。结论:月腺大戟水提物在较高剂量下有致突变和生殖毒性,但在低剂量下未发现明显毒性。     

Acute and Sub-chronic Toxicity of Tetrandrine in Intravenously Exposed Female BALB/c Mice

Objective: To evaluate the acute and sub-chronic toxicity of intravenously administered tetrandrine(TET) in female BALB/c mice. Methods: The median lethal dose(LD_(50)) of intravenously administered TET was calculated in mice using Dixon's up-and-down method. In the acute toxicity study, mice were intravenously administered with TET at a single dose of 20, 100, 180, 260 and 340 mg/kg, respectively and were evaluated at 14 days after administration. In the sub-acute toxicity study, mice were intravenously administered various doses of TET(30, 90 and 150 mg/kg) each day for 14 consecutive days. Clinical symptoms, mortality, body weight, serum biochemistry, organ weight and histopathology were examined at the end of the experiment, as well as after a 1-week recovery period. Result: LD_(50) was found to be 444.67±35.76 mg/kg. In the acute toxicity study, no statistically significant differences in body weight, blood biochemistry, or organ histology were observed between the administration and control groups when mice were intravenously administered with single dose at 20, 100, 180, 260 and 340 mg/kg of TET(P0.05). In the sub-acute toxicity study, no significant changes in body weight, biochemistry and organ histology were observed with up to 90 mg/kg of TET compared with the control group(P0.05), however, in the 150 mg/kg administered group, TET induced transient toxicity to liver, lungs and kidneys, but withdrawal of TET can lead to reversal of the pathological conditions. Conclusions: The overall findings of this study indicate that TET is relatively non-toxic from a single dose of 20, 100, 180, 260 or 340 mg/kg, and that up to 90 mg/kg daily for 14 consecutive days can be considered a safe application dose.