红毛五加粗多糖的抗肿瘤作用及免疫作用

 红毛五加粗多糖（AGCEM)200mg/kg能抑制S₁₈₀肿瘤生长，当剂量为100mg/kg和50mg/ kg时能增加小鼠和环磷酰胺所致免疫功能抑制的小鼠的足垫厚度。但红毛五加粗多糖100mg/kg和50 mg/kg对正常小鼠的溶血素生成无显著作用。此外，红毛五加粗多糖100mg/kg，50mg/kg和25mg/ kg能明显增加小鼠静注碳粒廓清速率。     

白边岛衣多糖抗肿瘤作用的研究

白边岛衣多糖腹腔注射200mg/kg(1/5LD₅₀)能显著抑制小鼠肉瘤180、艾氏腹水癌和宫颈癌-u14等肿瘤的生长,但不能延长白血病L7217小鼠的存活时间,50mg/kg和100mg/kg(1/10和1/20 LD₅₀)能增加小鼠网状内皮系统的吞噬功能。     

懈皮素磷酸酷钾对冠脉流量及心肌耗氧量的影响

 iv懈皮素磷酸酯钾（potassium quercetin phosphate,简称PQP)20mg/kg能增加猫的冠脉流量，对血压、心率及心肌耗氧量均无显著影响。小鼠ipPQP 200mg/kg能显著增加心肌营养性血流，但对小鼠心肌耐缺氧时间无明显影响。小鼠ivPQP的LD₅₀为238.5±26.5mg/kh。     

蝉花总多糖对细胞免疫和体液免疫反应的促进作用

目的：研究蝉花总多糖（CCP）体内外对细胞免疫和体液免疫的影响。方法：首先用MTT法和ELISA法测定小鼠脾细胞增殖和IgG抗体的生成水平,以研究CCP体外对细胞免疫和体液免疫的影响;然后通过DNFB诱导的小鼠迟发型超敏（DTH）反应和绵羊红细胞（SRBC）诱导的小鼠血清抗体生成实验进一步观察CCP体内对特异性细胞免疫和体液免疫反应的影响。结果：CCP 0.16~100μg/mL各浓度不仅能直接刺激小鼠脾细胞的增殖和IgG抗体生成,对Con A或LPS诱导的小鼠T、B淋巴细胞增殖和IgG抗体生成也具有显著的促进作用,并呈现良好的浓度依赖性。CPP 20 mg/kg可显著提高小鼠的DTH反应;10和20 mg/kg可剂量依赖性地显著提高抗SRBC抗体的生成。结论：CCP在体内外均能有效促进细胞免疫和体液免疫反应。     

西洋参茎叶皂甙及单体对心脏的作用

西洋参茎叶皂甙(0.03～3mg/ml)可抑制豚鼠乳头肌缩力,对高钾去极化标本,西洋参茎叶皂甙(0.03～0.3mg/ml)可使缩力增加。西洋参单体皂甙-Re10mg/kg,-Rb₃30mg/kg可抑制大鼠血流动力学LVSP,土dp/dtmax等指标,单体P-F₁₁10mg/kg与上述作用相反。证明西洋参茎叶皂甙中存在作用相反的成分。     

乌蕨对砷和铵的解毒作用

观察了乌蕨的4种提取物对小鼠砷和氯化铵急性中毒的解毒作用。结果表明:乌蕨提取物B及C能明显降低小鼠的死亡率,提取物C尚可使小鼠对砷耐受量提高,使其LD₅₀从31.1±4.3mg/kg提高到38.2±5.9mg/kg。4种提取物对小鼠NH₄Cl中毒虽可降低其死亡率,但与对照组相比,差异无显著意义(P>0.05)。     

国产哌仑西平对大鼠胃溃疡的防治作用

 本文报告了哌仑西平（pirenzepine，P)和阿托品对大鼠5种胃溃疡模型的防治作用。大鼠预先1次给予P 1 h后，对结扎大鼠幽门24h或冷水应激18h或ip利血平5 mg/kg形成的大鼠胃溃疡，P的ED₅₀分别为47.2; 0.88和45.3 mg/kg。大鼠灌服300 mg/kg阿司匹林加0.15mol HC 1 所致的胃溃疡，P的ED₅₀为6.6mg/kg。大鼠胃壁注射99%醋酸0.05ml形成慢性胃溃疡，灌服p25mK/kg 14d能促进溃疡愈合。     

群体药动学参数法预测丁胺卡那霉素的个体化给药方案

 本文依据群体药动学参数和丁胺卡那霉素的消除特点，建立了一种预测丁胺卡那霉素个体化给药方案的方法。临床应用结果表明，20例病人预测的个体化剂量为6.3±0.8mg/kg,预浏的峰、谷浓 度分别为22.97±2.20mg/L和3.75±2.13mg/L,与临床监测结果23.70±3. 49mg/L和3.24±2.05mg/L非常接近(P>0.05).药动学参数预测值为，CL86. 5±31.6m1·h_{-1(/sub)·kg-1，Vd O.2488 ±0.0026L/kg, T1/22.19 0.62h；与实际值CL89.3±37.1m1 h^-1．Kg^-1, Vd O.2412± 0.0695L/kg, T1/2 2.18± 1.23h比较，差异均无显著意义（P> 0. 05）。}     

脑芬泰软胶囊对实验性脑缺血损伤的保护作用

目的:研究脑芬泰软胶囊对小鼠及大鼠实验性脑缺血损伤的保护作用。方法:采用小鼠断头法致全脑缺血缺氧模型,测定小鼠断头后呼吸持续时间;小鼠双侧颈总动脉结扎致急性全脑缺血模型,观察小鼠6h内的存活时间;线栓法复制局灶性脑缺血模型,评价动物行为功能,测定脑梗死范围及脑组织中乳酸脱氢酶的活性;双侧颈总动脉结扎制备大鼠急性全脑缺血模型,干湿重法测定脑组织含水量,伊文思蓝法测定血脑屏障的损伤程度,HE染色观察脑组织的病理改变。结果:脑芬泰软胶囊(60mg/kg)能显著延长小鼠断头后张口喘气时间,各剂量组(60mg/kg、30 mg/kg、15 mg/kg)能剂量依赖性地延长小鼠的存活时间,但尚无统计学差异。在局灶性脑缺血模型上,脑芬泰软胶囊(48mg/kg、24mg/kg)能显著改善大鼠脑缺血造成的行为缺陷;48mg/kg剂量组明显提高脑组织中乳酸脱氢酶的活性;显著缩小梗死范围,并在12～48 mg/kg范围内呈一定的剂量依赖性。48、12mg/kg剂量组可抑制脑水肿的发生;12mg/kg组显著降低脑血管通透性;病理学组织检查显示,脑芬泰软胶囊(48mg/kg、24 mg/kg、12mg/kg)能改善脑缺血大鼠的神经细胞损伤,减少组织坏死,尤以48、24mg/kg剂量组改善显著。结论:脑芬泰软胶囊对小鼠及大鼠实验性脑缺血损伤有明显的保护作用。     

绞股蓝总皂甙和人参总皂甙对大鼠急性心肌缺血心脏舒张功能保护作用的比较

 目的：评价绞股蓝总皂甙(Gyp)对大鼠急性心肌缺血心脏舒张功能保护作用，并同人参总皂甙(Gin)做比较。方法：用SMUP-160心功能测定软件，分别测定正常对照，提前给予Gyp(iv,40 mg/kg)和Gin(iv，40 mg/kg)组大 鼠心脏的舒张功能。结果:Gyp(iv,40mg/kg)对麻醉大鼠基础心功能无影响。Gin(iV,40 mg/kg)可显著降低心室收 缩崃压（LVSP）和心率（HR）（P<0.05或P<0.01),一过性降低心室压最大上升和下降速率（士dP/dt_max)和心肌纤维零负荷下最大缩短速率(V_max)，对等容舒张期压力下降时间常数T无影响。结扎大鼠冠脉左前降支即刻引起左室舒张功能损伤并于10min达到峰值，表现为等容收缩相T值显著延长，-dP/dt_max和-dP/dt_max·LVSP^-1明显降低，心室舒张末压（LVEDP)则明显升高。冠脉结扎前给予Gyp或Gin可显著（P<0.05或P<0.01)拮抗T值的延长，LVEDP的抬高和-dP/dt_max,-dP/dt_max·LVSP^-1的降低。结论:Gyp和Gin对大鼠实验性心肌缺血心脏舒张功能均有明显的保护作用。同Gyp相比,Gin似能更有效地改善急性心肌缺血所致LVEDP的抬高。     

Antiinflammatory activity and effects on isolated smooth muscle of extracts from different Teucrium species

The present study analyses the antiinflammatory effects and the action on in vitro motility of methanol and dichloromethanol extracts and stems of four Teucrium species (T. flavum, T. cartaginenses, T. buxifolium and T. pumillum). The antiinflammatory activity was tested in the carrageenan-induced paw oedema in rats. T. flavum methanol (200 mg/kg, i.p.) and dichloromethanol (138 mg/kg, i.p.) extracts showed a significant anti-inflammatory effect through the 24 h experimental period and reduced the E_max induced by histamine and serotonin in vitro on guinea-pig ileum and rat uterus respectively. These extracts did not modify the contractile effects induced by acetylcholine on rat duodenum and noradrenaline on rat vas deferens. The methanol extracts of T. pumillum (50 mg/kg, i.p.) and T. buxifolium (26 mg/kg, i.p.) exhibited significant antiinflammatory effects only in the acute phase of the oedema (2 h) without affecting the chronic phase (24 h). In guinea-pig ileum, rat uterus and rat vas deferens, the methanol extract of T. pumillum reduced the maximal effect induced by histamine, serotonin and noradrenaline, respectively, whereas the methanol extract of T. buxifolium lacked any effect on the contractile activity induced by various agonists in vitro. When tested for antiinflammatory activity the methanol (200 mg/kg, i.p.) and dichloromethanol (200 mg/kg, i.p.) extracts of T. cartaginenses did not modify the oedematous response induced by carrageenan administration.     

Physalis angulata extract exerts anti-inflammatory effects in rats by inhibiting different pathways

Physalis angulata is a popular medicine used in Brazil due to its anti-inflammatory effects, but the pharmacological mechanisms underlying these actions remain to be better understood. In the present work, lyophilized aqueous extract from the roots of Physalis angulata Linneu (AEPa) was used to control the inflammatory response induced by the injection of 1% carrageenan into subcutaneous rat's air pouches. Adenosine deaminase (ADA) activity, nitrite level, and prostaglandin E₂ (PGE₂) level were used to evaluate the action of inflammatory mediators. Tumor growth factor-β (TGF-β) level was used as a bioindicator of immunomodulatory response. Rats were injected with vehicle, indomethacin, or AEPa (0.5 mg/kg, 1 mg/kg, and 5 mg/kg i.p.), 1 h before carrageenan administration. AEPa at 0.5 mg/kg had no effect. However, 1 mg/kg of AEPa showed significant anti-inflammatory effects, decreasing exudate volume, total number of inflammatory cells, ADA activity, nitrite level, and PGE₂ level in 50%, 41%, 20%, 60%, and 41%, respectively. The anti-inflammatory effects of 5 mg/kg AEPa appeared to be more effective than those of 1 mg/kg AEPa (84%, 80%, 43%, 70%, and 75%, respectively). In addition, TGF-β level was upregulated to 9700 pg/ml after 5 mg/kg AEPa, in comparison with 160 pg/ml in the vehicle-treated group, and 137 pg/ml in the indomethacin-treated group. The results indicate that AEPa exerts powerful anti-inflammatory and immunomodulatory activities, interfering with the cyclooxygenase pathway, lymphocyte proliferation, NO, and TGF-β production.     

Isolation and identification of an antiinflammatory principle from santolina chamaecyparissus

The chloroform extract from Santolina chamaecyparissus squarrosa exhibited a potent anti-inflammatory effect on carrageenan-induced oedema in the rat hind paw. β-Sytosteryl 3-β-D-glucoside, isolated by fractionating this extract, was anti-inflammatory in the above test, with intraperitoneal and oral ED₅₀ values of 70 and 146 mg/kg, respectively.     

Anti-inflammatory action of hydroalcoholic extract,dichloromethane fraction and steroid α-spinasterol from Polygala sabulosa in LPS-induced peritonitis in mice

Ethnopharmacological relevance

Polygala sabulosa A. W. Bennett is a small herb popularly known as “timutu-pinheirinho” that is widely distributed in southern Brazil and that is used to treat disorders of the bowel and kidney and as a topical anesthetic and expectorant in folk medicine. This study was designed to investigate the anti-inflammatory properties of the hydroalcoholic extract (HEPs), CH₂Cl₂ fraction and the steroid α-spinasterol obtained from the aerial parts of Polygala sabulosa in a model of acute inflammation induced by intraperitoneal injection of bacterial lipopolysaccharide in mice.

Materials and methods

The anti-inflammatory effect of HEPs (3–300 mg/kg, i.g.), CH₂Cl₂ fraction (0.003–30 mg/kg, i.g.) and steroid α-spinasterol (0.001–1 mg/kg, i.p. or 1–10 mg/kg, i.g.), were evaluated in mice subjected to the acute inflammation caused by intraperitoneal (i.p.) injection of lipopolysaccharide (LPS, 0.02 µg/kg). The anti-inflammatory activity of the HEPs, CH₂Cl₂ fraction and steroid were assessed by determining the total numbers of leukocytes and differential cell counts (neutrophils and mononuclear cells) and levels of pro-inflammatory (IL-1β, TNF-α, IL-6) or anti-inflammatory (IL-10) cytokines in peritoneal fluid.

Results

The administration of HEPs (3–300 mg/kg, i.g.) completely inhibited inflammatory cell infiltration (300 mg/kg, i.g.) and it reduced TNF-α (100–300 mg/kg) and IL-1β (100 mg/kg) levels in LPS-injected mice. Furthermore, the administration of CH₂Cl₂ fraction (0.003–30 mg/kg, i.g.) or α-spinasterol (0.001–10 mg/kg, by i.p. or i.g.) significantly reduces inflammatory cell infiltration in LPS-injected mice. Moreover, dexamethasone (0.5 mg/kg, i.p., used as a positive control) inhibited inflammatory cell infiltration and reduced the levels of TNF-α, IL-1β and IL-6 in LPS-injected mice.

Conclusions

Taken together, these results provide the first experimental evidence demonstrating that HEPs have significant anti-inflammatory effects on LPS-induced inflammation. These effects appear to be, at least in part, due to the presence of α-spinasterol. These findings support the widespread use of Polygala sabulosa in popular medicine and demonstrate that this plant has therapeutic potential for the development of phytomedicines with anti-inflammatory properties.     

Hypoglycaemic activity of Anthocleista vogelii (Planch) aqueous extract in rodents

The hypoglycaemic effect of Anthocleista vogelii was studied in mice, rats and rabbits. Aqueous extract of the plant obtained by infusion from finely pulverized root was used. The extract (100, 400 and 800 mg/kg) induced significant hypoglycaemic activity in a dose-related fashion at 2 h after oral administration in mice and rats with ED₂₅ of 250 mg/kg and 350 mg/kg respectively. The extract (800 mg/kg, orally) similarly induced statistically significant lowering of blood glucose levels at 8 h in normoglycaemic rabbits. The extract (400 mg/kg and 800 mg/kg, orally) also caused reduction of blood glucose levels in alloxan-induced diabetic animals. The results of this study indicate that the aqueous extract of the roots of Anthocleista vogelii possess favourable hypoglycaemic activity both in normo and hyperglycaemic animals compared to chlorpropamide as a standard.     

Pharmacological studies on the crude drug ‘Hwang-Jin-Guey’ from Taiwan (1)

Three different crude drugs take the same name ‘Hwang-jin-guey’ on the Taiwan market, they are (1) Cudrania cochinchinensis var. gerontogea (Moraceae), (2) Ventilago leiocarpa (Rhamnaceae) and (3) Viscum multinerve (Loranthaceae). To clarify and compare the pharmacological actions of these folk medicines, the antiinflammatory and liver-protective effects of their aqueous and ethanol extracts were investigated. The results showed that the aqueous extracts of C. cochinchinensis (300 mg/kg), V. leiocarpa (300 mg/kg) and ethanol extract of C. cochinchinensis (100 mg/kg) displayed marked antiinflammatory activity compared to indomethacin. An ethanol extract of V. leiocarpa (300 mg/kg) exhibited a comparable inhibitory effect to indomethacin in the paw oedema induced by carrageenan. As to the liver-protective effect, the statistical analysis (ANOVA) indicated that the aqueous (100 mg/kg) and ethanol (300 mg/kg) extracts of C. cochinchinensis presented pronounced activities against CCI₄-induced acute liver damage. However, treatment with V. multinerve offered no protection against CCI₄-induced hepatotoxicity, whether aqueous or ethanol extracts. These phenomena were also confirmed by histological observation.     

Pharmacological screening of the methanol and dichloromethanol extracts of Genista patens

The pharmacological effects of the dichloromethanol and methanol extracts obtained from leaves and stems of Genista patens DC were analysed in in vitro and in vivo models. Both extracts showed low acute toxicity (LD₅₀ > 3 g/kg), CNS depressor and antiinflammatory activity, and similar analgesic effect in models of chemical and thermal stimulation. Furthermore, the dichloromethanol extract (1–20 mg/kg) induced a pronounced dose-dependent decrease on blood pressure. On isolated organs, the dichloromethanol extract (1, 10, 100 μg/mL) shifted the concentration-effect curve to the right for ACh and reduced the E_max induced by histamine without modifying responses induced by noradrenaline and serotonin.     

Hypnotic, anticonvulsant and muscle relaxant effects of Rubus brasiliensis. Involvement of GABAA-system

Rubus brasiliensis hexanic fraction induced anxiolysis in rodents, which was reversed by flumazenil, a specific GABA_A-benzodiazepine receptor antagonist (Nogueira and Nogueira). Then, we investigated if this hexanic fraction was able to induce hypnotic, anticonvulsant and muscle relaxant effects, and the involvement of GABA_A-system. The hexanic fraction (50, 100, 150 and 300 mg/kg, vo) was administered to male Swiss mice, 30 min before the tests. Only the dose of 300 mg/kg of this fraction decreased the latency and increased sleeping time in the barbituric-hypnosis test (sodium pentobarbital, 30 mg/kg, ip), prevented the pentylenetetrazol seizures (70 mg/kg, ip) and induced muscle relaxant (inclined plane) in 100% of animals. These effects were reversed by flumazenil (3 mg/kg, ip). In conclusion: (1) R. brasiliensis hexanic fraction induced hypnotic, anticonvulsant and muscle relaxant effects, in mice, and the GABA_A–benzodiazepine receptor may play an important role in the effects of this fraction; (2) it is strongly suggested that this fraction contains a benzodiazepine-like principle.     

A preliminary study of the biological activities of the bark extract of Piliostigma thonningii (schum) in mice

The biological activities of the stem bark of Piliostigma thonningii were studied in mice. The oral LD₅₀ of the 70% ethanol extract was 1862 mg/kg. It significantly reduced pentobarbitone-induced sleeping time after an intraperitoneal injection (p < 0.05). The extract induced persistent contractions on the guineapig ileum which were completely blocked by atropine. Mice intubated with varying doses (100,200,400 mg/kg) of the extract had diarrhoea. The extract appeared to mediate its action through a cholinergic mechanism.     

Preventive and curative effects of Berberis aristata Fruit extract on paracetamol- and CCl4-induced hepatotoxicity

The effect of an aqueous-methanol extract of Berberis aristata fruits (Berberidaceae) was investigated against paracetamol- and CCl₄-induced hepatic damage. Paracetamol produced 100% mortality at a dose of 1 g/kg in mice while pre-treatment of animals with crude extract (500 mg/kg) reduced the death rate to 10%. Pre-treatment of rats with fruit extract (500 mg/kg, orally twice daily for 2 days) prevented (p<0.05) the paracetamol (640 mg/kg) as well as CCl₄ (1.5 mL/kg)-induced rise in serum transaminases (GOT and GPT). Post-treatment with three successive doses of extract (500 mg/kg, 6h) restricted the hepatic damage induced by acetaminophen (p<0.01) but CCl₄-induced hepatotoxicity was not altered (p>0.05). Plant extract (500 mg/kg) caused significant prolongation (p<0.01) in pentobarbital (75 mg/kg)-induced sleep as well as increased strychnine-induced lethality in mice suggestive of inhibitory effect on microsomal drug metabolizing enzymes (MDME). These results indicate that the crude extract of Berberis aristata fruits exhibits hepatoprotective action partly through MDME inhibitory action.