Antioxidant Defense System Induced by a Methanol Extract of Caesalpinia bonducella. in Rat Liver

ABSTRACT

The antioxidant defense system dramatically controls hepatocellular carcinoma induced by N.-nitrosodiethylamine (NDEA). In order to assess the anticarcinogenic activity of a methanol extract of Caesalpinia bonducella. (MECB) leaves containing flavonoids and triterpenoids, the antioxidant defense system has been evaluated. The effect of MECB on lipid peroxidation end-product malondialdehyde (MDA), enzymatic antioxidants such as superoxide dismutase (SOD) and catalase (CAT), and nonenzymatic antioxidants glutathione (GSH), vitamin E, and vitamin C levels were analyzed in the liver of control and experimental animals. Serum was also analyzed for transaminase activity (SGOT and SGPT), alkaline phosphatase (SALP), bilirubin, total protein, and uric acid. Depletion of all these antioxidants was recorded in cancer conditions. These deleterious effects are controlled by the administration of MECB. After drug administration, there was a marked increase in antioxidant levels and a dramatic decrease in lipid peroxidation levels. MECB also produced a protective effect by decreasing the activity of serum enzymes, bilirubin, and increased the protein and uric acid levels. From the above results, it can be concluded that the observed anticarcinogenic properties of MECB may also be explained by its strong antioxidant capacity and capability to induce an in vivo. antioxidant system.     

In vivo immunomodulatory activities of the aqueous extract of bonduc nut Caesalpinia bonducella seeds

This study evaluated the in vivo immunomodulatory activities of the aqueous extract of Caesalpinia bonducella Fleming (Caesalpiniaceae) seeds. C. bonducella is a plant widely used in the traditional medicinal systems of India. In the present investigation, the aqueous extract of C. bonducella seeds was tested for its effect on cell mediated and humoral components of the immune system in rats. Administration of C. bonducella seed extract produced an increase of 93.03?±?4 mean hemagglutinating antibody (HA) titer and a change of 0.56?±?0.058?mm in delayed type hypersensitivity (DTH) as compared to control at a dose of 400?mg/kg body weight. Thus, the results of this study indicate that C. bonducella extract could be a promising immunostimulatory agent.     

通气颗粒对小鼠胃肠功能的影响

目的：验证通气颗粒的主要功效。方法：采用小鼠胃酚红排空法,正常和脾虚小鼠炭末推进法,醋酸扭体法。结果：通气颗粒中、高剂量组（４,８ｇ．ｋｇ＾－１）灌胃给药可显著促进正常小鼠胃酚红排空运动（Ｐ〈０．０１）;通气颗粒中、高２个剂量组（４,８ｇ．ｋｇ＾－１）灌胃给药可显著促进正常小鼠小肠推动功能（Ｐ〈０．０５,Ｐ〈０．０１）;通气颗粒低、中、高３个剂量组（２,４,８ｇ．ｋｇ＾－１）连续灌胃给药５ｄ,可显     

Irritant potential of some constituents from the seeds of Caesalpinia bonducella (L.) Fleming

The irritant potential of four triterpenoids, isolated for the first time from the seeds of Caesalpinia bonducella, identified as f -amyrin [12-ursen-3 g -ol], g -amyrin [12-oleanex-3 g -ol], lupeol [lup-20(29)-en-3 g -ol] and lupeol acetate [lup-20(29)-en-3 g -yl acetate] was investigated by open mouse ear assay, evaluating their ID₅₀ (irritant dose in 50% animals) after acute effects and by irritant units (IU) after chronic effects. f -Amyrin, lupeol acetate and g -amyrin were the most potent and persistent irritant compounds with red weals of 1.5-2.1 cm diameter areas of the animal skin and with lowest ID₅₀ =0.078, 0.186 and 0.190 mg/10 w l after 1.5, 2.10 and 3.5 h, respectively. Their reactions lasted for 24 h with IU=2.5; 0.312 and 1.25 mg/10 w l, respectively. Lupeol was the least irritant and least persistent compound with ID₅₀ =0.603 mg/10 w l after 4.5 h. Its reaction subsided before 24 h.     

The antinociceptive effects of magnesium sulfate and MK-801 in visceral inflammatory pain model: The role of NO/cGMP/K+ATP pathway

Abstract

Context: Magnesium and MK-801 (dizocilpine), antagonists of N-methyl-d-aspartate receptors, are involved in the processing of pain.

Objective: This study determines whether magnesium sulfate (MS) and MK-801 affects visceral inflammatory pain and determines a possible mechanism of action.

Materials and methods: Analgesic activity was assessed using the acetic acid-induced writhing test in rats. MS (1–45?mg/kg) or MK-801 (0.005–0.03?mg/kg) was administrated subcutaneously (s.c.). To assess possible mechanisms of action, we examined the effects of l-NAME (10?mg/kg, intraperitoneal), methylene blue (0.5?mg/kg, s.c.), and glibenclamide (3?mg/kg, s.c.) on the effect of MS or MK-801.

Results: MS and MK-801 showed biphasic and linear dose–response pattern, respectively. MS reduces the number of writhing on the dose of 1, 5, and 15?mg/kg by 60, 50, and 78%, respectively, while it has no effects on the doses of 30 and 45?mg/kg. MK-801 (0.005–0.03?mg/kg) showed decrease in the number of writhing by 33–79%. The mean effective doses of MS and MK-801 were 6.6 (first phase) and 0.009?mg/kg, respectively. Both drugs did not impair the rotarod performance. l-NAME, methylene blue, and glybenclamide reduced the effect of MK-801 by 100, 43, and 64%, respectively, but not the effect of MS.

Conclusions: The results suggest that MS and MK-801 may be useful analgesics in the management of visceral inflammatory pain, at doses that do not induce motor impairment. The modulation of NO/cGMP/K+ATP pathway plays an important role in the antinociceptive mechanism of MK-801, but does not contribute to the antinociceptive effect of MS.     

Oral Hypoglycemic Effect of Caesalpinia bonducella

The blood sugar lowering efficacy of the aqueous extract of Caesalpinia bonducella F. (seed shell) was evaluated in fasted, fed, glucose loaded, streptozotocin diabetic, and alloxan diabetic rat models. The extract was administered orally at a dose of 250 mg/kg of rat body weight. It produced very significant blood sugar lowering (at least P < 0.005) in glucose loaded, streptozotocin diabetic, and alloxan diabetic models. However, effects were not so pronounced in fasted and fed models. As a whole, Caesalpinia bonducella can be regarded as a good oral hypoglycemic agent in rat.     

陆英煎剂对小鼠镇痛作用的实验研究

目的 通过实验研究陆英煎剂对小鼠的镇痛作用.方法 镇痛实验采用小鼠热板法和醋酸扭体法,实验分为陆英煎剂组、盐酸曲马多组、生理盐水组,灌胃给药.结果 与生理盐水组比较,陆英煎剂组和盐酸曲马多组对小鼠热板致痛的痛阈值均有不同程度的提高,对小鼠醋酸致痛引起的扭体次数均有明显的降低作用.结论 陆英煎剂具有明显的镇痛作用,其镇痛作用比盐酸曲马多弱.     

中华眼镜蛇毒口服给药镇痛作用的研究

目的：研究中华眼镜蛇毒灌服给药对小鼠的镇痛作用。方法：将ICR和昆明种小鼠,采用3种致疼痛模型,即冰醋酸所致扭体反应、小鼠热板法致痛实验和甲醛致炎性疼痛反应;中华眼镜蛇毒经热变性复性处理,将其灌胃给药30-270μg／kg。结果：中华眼镜蛇毒粗毒灌服给药能减少腹腔注射醋酸引起的扭体次数,延长热引起的疼痛反应潜伏期和减少甲醛引起的舔足反应。结论：中华眼镜蛇毒灌服给药具有良好的镇痛作用,且给药途径方便、安全范围大,具有进一步开发成新型镇痛药的潜力。     

牙痛灵喷雾剂对小鼠实验性疼痛的镇痛作用

目的：观察牙痛灵喷雾剂的镇痛作用,为其临床应用提供一定的实验依据。方法：制备小鼠实验性疼痛模型,观察牙痛灵喷雾剂的镇痛作用。（1）扭体法：取昆明种小鼠50只,随机分为5组,每组10只,雌雄各半。空白对照组灌胃给予生理盐水10mL／kg;牙痛灵喷雾剂低、中、高剂量组分别灌胃牙痛灵喷雾剂0．36、1．08、3．24g／kg。阳性对照组灌胃阿司匹林0．4g／kg。每日用药1次,10d后观察各组动物腹腔注射醋酸后5～20min内的扭体反应次数。（2）热板法：将小鼠放在（55±1）℃的热板上,以小鼠舔后足为疼痛反应指标,观察小鼠的热痛阈值。选用痛觉阈值在5～30s的雌性小鼠50只,随机分为5组,每组10只,分组与给药方法与（1）同。给药10d后记录各组小鼠热板法痛阂值,比较各组间的差异。结果：（1）扭体法实验结果显示,牙痛灵喷雾剂0．36、1．08、3．24g／kg灌胃10d使腹腔注射醋酸所致的小鼠扭体反应次数较空白对照组明显减少,对扭体反应次数的抑制率分别为25．6％、30．6％和43．5％（P〈0．05,P〈0．01）。（2）热板法实验结果显示,给药前各组小鼠热痛阈值无统计学差异（P〉0．05）;给药10d后牙痛灵喷雾剂各剂量组小鼠热痛阂值均较给药前显著提高,与空白对照组比较,牙痛灵喷雾剂组给药后热痛阈值显著延长（P〈0．05,P〈0．01）。结论：牙痛灵喷雾剂对小鼠实验性疼痛具有良好的镇痛作用。     

Antiinflammatory, Analgesic and Antipyretic Activity of Certain Thiazolidinones

The thiazolidin-4-one derivatives and the corresponding spiro compounds were synthesized from sulphanilamide and were evaluated for anti-inflammatory and analgesic activity in acute and sub acute models. Compounds were also evaluated for antipyretic and cyclooxygenase enzyme inhibitory activity. All the compounds showed significant antiinflammatory, analgesic and antipyretic activity at 100 mg/kg in all the models. The compounds B1, B2, B5, B6, and B8 showed maximum inhibition of COX-2 activity without inhibiting the COX-1 activity. The nimesulide was used as standard drug for comparison. The substitution at R, R₁ and R₂ with the functional groups Cl, OCH₃, NO₂ and OH in the aromatic ring resulted in increased activity as compared to unsubstituted thiazolidin-4-ones. However the substitution at R₃ with spiro group did not improve the activity. The study suggests that COX-2 binding site may not be a rigid structure but might adopt to various related molecules.     

(-)-Linalool produces antinociception in two experimental models of pain

Linalool is a monoterpene compound commonly found as a major component of the essential oils of several aromatic plant species, many of which are used in traditional medical systems as analgesic and anti-inflammatory remedies. We previously reported that (-)-linalool, the natural occurring enantiomer, plays a major role in the anti-inflammatory activity displayed by different essential oils, suggesting that linalool-producing species are potentially anti-inflammatory agents. In this study, the antinociceptive activity of (-)-linalool was examined in two different pain models in mice: the acetic acid-induced writhing response, a model of inflammatory pain, and the hot plate test, a model of supraspinal analgesia. Moreover, the effect of (-)-linalool on spontaneous locomotor activity (25, 50, 75 and 100 mg/kg) was evaluated. The results show that this compound induced a significant reduction of the acid-induced writhing at doses ranging from 25 to 75 mg/kg. Such effect was completely reversed both by the opioid receptor antagonist naloxone and by the unselective muscarinic receptor antagonist atropine. In the hot plate test, only the dose of 100 mg/kg of (-)-linalool resulted in a significant effect. (-)-Linalool induced a dose dependent increase of motility effects, thus ruling out the confounding influence of a possible sedative effect. The more pronounced effect of (-)-linalool on the writhing test with respect to the hot plate test is consistent with the observation that (-)-linalool possesses anti-inflammatory activity. Finally, the activation of opioidergic and cholinergic systems appears to play a crucial role in (-)-linalool-induced antinociception.     

白术醇提物的抗炎镇痛活性研究

目的 探讨白术醇提物的抗炎镇痛活性,为进一步研究白术抗炎镇痛的作用机制提供基础。方法 采用热板法测定白术不同剂量组小鼠的痛阈值,腹腔注射0.6%醋酸刺激致痛模型(扭体法)观察白术3个不同剂量的镇痛作用;采用二甲苯致小鼠耳廓肿胀实验和角叉菜胶致大鼠足肿胀实验观察白术3个不同剂量的抗炎作用。结果 高、中剂量的白术醇提物可显著增加小鼠的热板痛域值(P<0.01,P<0.01),减少腹腔注射醋酸引起的小鼠扭体反应次数(P<0.01,P<0.01),而白术低剂量组不能有效的提高小鼠的痛阈值(P>0.05)和减少扭体反应次数(P>0.05)。在抗炎试验中,高、中剂量的白术醇提取可显著抑制小鼠耳廓肿胀度(P＜0.01,P＜0.01),而低剂量组对小鼠耳廓肿胀抑制效果不明显(P＞0.05);高剂量组在2h后能显著抑制大鼠足跖肿胀,中剂量组(除6h时间点)与白术低剂量组(除3h时间点)在药后0.5-6h之间与模型组比较均无显著性差异(P＞0.05)。结论 白术醇提物具有较好的抗炎、镇痛作用,并且随着剂量的增大,抗炎镇痛活性增强。     

Chemical constituents from the the twigs and leaves of Caesalpinia enneaphylla

Fifteen compounds were isolated from the twigs and leaves of Caesalpiniaenneaphylla. Their structures were identified to be: (E)-3-(4-hydroxybenzylidene)- 5,7-dihydroxychroman-4-one (1), 8-methoxybonducellin (2), (E)-3-(3,4- dihydroxybenzylidene)-5,7-hydroxychroman-4-one (3), 2′,4′-dihydroxychalcone (4), oxyfadichalcone B (5), 7-hydroxyflavonone (6), pinocembrin (7), kaempferol (8), quercitrin (9), kaempferol 3-O-α-L-rhamnopyranoside (10), quercetin 3-O-α-D-arabinoside (11), trans-2,3-diacetoxy-1-[(benzoyloxy)methyl]-cyclohexa-4,6-diene (12), 3-hydroxybenzyl benzoate (13), 2-acetoxybenzyl benzoate (14), and glutinol (15). All the compounds were isolated from C. enneaphylla for the first time.     

喙荚云实的化学成分

目的喙荚云实的化学成分研究。方法采用多种色谱方法分离纯化,依据理化性质、波谱数据分析进行结构鉴定。结果从喙荚云实的体积分数为95%的乙醇溶液提取物中分离纯化得到7个化合物,分别鉴定为-βamyrin(1)、Caffeine(2)、Caesalmin C(3)、Caesalmin D(4)、Caesalpin F(5)、β-谷甾醇(-βsitosterol,6)、胡萝卜苷(Daucosterol,7)。结论化合物1,2为首次从该属植物中分离得到的化合物,化合物6,7为首次从该植物中分离得到的化合物。     

Two new diterpenes from the seeds of Caesalpinia minax Hance

Molecules with diterpene skeletons often possess valuable medicinal properties. Two new diterpenes 1α,6α,7β-triacetoxy-5α-hydroxy-14β-ethyl-O-vouacapane (1) and 2α-acetoxy-14,15-cyclopimara-7β,16-diol (2) were isolated from the seeds of Caesalpinia minax Hance. Their structures were established on the basis of extensive spectroscopic analyses, including HR-ESI-MS, UV, IR, 1D, and 2D NMR (HSQC, HMBC, NOESY) methods. The stereochemical structure of 1 was confirmed via the circular dichroism spectrum and calculated ECD experiment. The inhibitory activity of nitric oxide production of RAW264.7 macrophages stimulated by lipopolysaccharide of compounds 1 and 2 was evaluated, and compound 1 was found to show significant inhibitory effect.     

壮药红鱼眼三萜类成分镇痛和抗炎活性实验研究

目的研究壮药红鱼眼三萜类成分的镇痛和抗炎活性。方法采用扭体法观察镇痛作用;用二甲苯使小鼠致炎和醋酸致小鼠腹腔毛细血管通透性增加观察抗炎作用。结果红鱼眼三萜类成分对醋酸致痛具有明显的镇痛作用,对二甲苯所致炎性水肿也有显著的抑制作用。结论红鱼眼三萜类成分具有较好的镇痛、抗炎活性。     

喙荚云实种子中的新二萜

目的研究喙荚云实的化学成分。方法采用多种色谱方法分离纯化,依据理化性质、波谱数据分析进行结构鉴定。结果从喙荚云实的体积分数为95%的乙醇回流提取物中分离鉴定了1个二萜类化合物。结论此二萜类化合物为新化合物。     

Two new cassane-type diterpenes from the seeds of Caesalpinia crista

Two new cassane-type diterpenes, phangininoxys D and E (1 and 2), together with five known compounds were isolated from the seeds of Caesalpinia crista Linn. The structures of these compounds were elucidated by means of various spectroscopic analyses. All the isolated compounds were evaluated for cytotoxicity activities against HeLa, HT-29 and KB cell lines, and compound 7 showed moderate selective activities against KB cell line with an IC₅₀ value of 17.1 μM.     

Arginase Inhibition by Ethylacetate Extract of Caesalpinia sappan Lignum Contributes to Activation of Endothelial Nitric Oxide Synthase

Caesalpinia sappan (C. sappan) is a medicinal plant used for promoting blood circulation and removing stasis. During a screening procedure on medicinal plants, the ethylacetate extract of the lignum of C. sappan (CLE) showed inhibitory activity on arginase which has recently been reported as a novel therapeutic target for the treatment of cardiovascular diseases such as atherosclerosis. CLE inhibited arginase II activity prepared from kidney lysate in a dose-dependent manner. In HUVECs, inhibition of arginase activity by CLE reciprocally increased NOx production through enhancement of eNOS dimer stability without any significant changes in the protein levels of eNOS and arginase II expression. Furthermore, CLE-dependent arginase inhibition resulted in increase of NO generation and decrease of superoxide production on endothelium of isolated mice aorta. These results indicate that CLE augments NO production on endothelium through inhibition of arginase activity, and may imply their usefulness for the treatment of cardiovascular diseases associated with endothelial dysfunction.