Screening of Bauhinia purpurea Linn. for analgesic and anti-inflammatory activities

Objectives:

Ethanol extract of the stem of Bauhinia purpurea Linn. was subjected to analgesic and anti-inflammatory activities in animal models.

Materials and Methods:

Albino Wistar rats and mice were the experimental animals respectively. Different CNS depressant paradigms like analgesic activity (determined by Eddy''s hot plate method and acetic acid writhing method) and anti-inflammatory activity determined by carrageenan induced paw edema using plethysmometer in albino rats) were carried out, following the intra-peritoneal administration of ethanol extract of Bauhinia purpurea Linn. (BP) at the dose level of 50 mg/kg and 100 mg/kg.

Results:

The analgesic and anti-inflammatory activities of ethanol extracts of BP were significant (P < 0.001). The maximum analgesic effect was observed at 120 min at the dose of 100 mg/kg (i.p.) and was comparable to that of standard analgin (150 mg/kg) and the percentage of edema inhibition effect was 46.4% and 77% for 50 mg/kg and 100 mg/kg (i.p) respectively. Anti-inflammatory activity was compared with standard Diclofenac sodium (5 mg/kg).

Conclusion:

Ethanol extract of Bauhinia purpurea has shown significant analgesic and anti-inflammatory activities at the dose of 100 mg/kg and was comparable with corresponding standard drugs. The activity was attributed to the presence of phytoconstituents in the tested extract.     

鹅掌柴叶挥发油的成分分析及抗炎镇痛活性

目的 探讨鹅掌柴新鲜叶挥发油的化学成分及其抗炎镇痛作用。 方法 采用水蒸气蒸馏法得到鹅掌柴叶挥发油(SOLEO),用气相色谱-质谱联用技术(GC-MS)进行SOLEO成分的定性定量分析,并用醋酸扭体法、二甲苯致小鼠耳郭肿胀法两种模型评价SOLEO的抗炎镇痛活性。 结果 GC-MS法测出SOLEO中55个组分,其中组分1~16共占84.28%,为SOLEO的主要成分。4-萜品醇、(-)-斯巴醇、氧化石竹烯、芳樟醇4种成分占总含量的51.86%。SOLEO可明显减少醋酸所致小鼠的扭体次数,可明显缓解二甲苯所致小鼠的耳郭肿胀程度,SOLEO经灌胃给药10 g生药/(kg.d)剂量组的抑制率分别为52.5 %和59.6 %。 结论 SOLEO为鹅掌柴抗炎镇痛药理作用的活性成分之一,为民间以鹅掌柴新鲜叶入药提供科学依据。     

青藤碱衍生物的合成及其抗炎镇痛活性青藤碱衍生物的合成及其抗炎镇痛活性

目的为定向设计合成高效低毒的新一代青藤碱类药物提供线索。方法以青藤碱为先导物,对C环进行结构改造。结果共合成7个衍生物,进行了抗炎镇痛活性的筛选,结果表明,化合物2和5具有较好的抗炎镇痛作用。结论C环结构修饰值得进一步研究。     

黑骨藤镇痛抗炎作用活性部位筛选

目的 研究苗药黑骨藤镇痛抗炎作用的活性部位。方法 小鼠随机分为空白组、阿司匹林组及黑骨藤水、正丁醇、氯仿、醋酸乙酯、石油醚提取部位的低、高剂量组。除空白组外,各组ig给药,空白组ig生理盐水。采用扭体法观察记录给药后15 min内小鼠扭体次数。采用热板法测定小鼠的痛觉反应时间。采用耳廓肿胀法检测小鼠耳廓肿胀度。采用棉球肉芽肿法：观测小鼠肉芽湿质量和干质量。结果 黑骨藤各提取部位对醋酸诱发小鼠扭体反应有显著的镇痛作用,其中黑骨藤正丁醇提取部位高剂量组效果最好,其疼痛抑制率为80.2%。黑骨藤正丁醇提取部位对热板法致痛有显著的镇痛作用,与空白组比较,能显著提高小鼠的痛阈值（P<0.05、0.01）。黑骨藤水、醋酸乙酯、石油醚提取部位对二甲苯致小鼠耳廓肿胀的急性炎症有显著的抗炎作用,能明显减少小鼠耳廓肿胀度。黑骨藤各提取部位对小鼠肉芽湿质量和干质量均有抑制作用,其中正丁醇提取部位效果最好。结论 黑骨藤具有良好的镇痛抗炎作用。其中,正丁醇部位镇痛作用最好。     

Synthesis and analgesic and anti-inflammatory activities of 1,2-benzothiazine derivatives

Three 1,2-benzothiazine derivatives were synthesized, and their analgesic/anti-inflammatory efficacy and their effects on gastric irritation were evaluated. Among the three compounds, 39 exhibited the most potent analgesic action, but the effect was weaker than that of piroxicam. Nonetheless, the compound showed 4 times more potent analgesic action with less gastric damage than did ibuprofen. These compounds did not show anti-inflammatory effect at an oral dose of 5 mg/kg.     

Synthesis and anti-inflammatory and analgesic activities of phenoxyalkanoic acid derivatives

The synthesis of phenoxyalkanoic acid derivatives and their anti-inflammatory and analgesic activities are described. Analysis of structure-activity relationships shows that in trichlorophenoxy derivatives anti-edematous potency is associated with the presence of 1-thiopropyl moiety and 2 or 4-aminopyridyl moiety at R′ position contributes to the analgesic activity.     

草乌甲素脂质体的皮肤渗透性及抗炎镇痛作用

目的：考察草乌甲素脂质体的皮肤渗透性及抗炎镇痛效果。方法：采用正交设计详细考察了处方中各因素对透皮速率的影响；比较了脂质体与饱和水溶液的经皮渗透性；研究了脂质体对二甲苯所致急性炎症以及醋酸所致扭体反应的影响。结果：处方中磷脂、油酸、油酸钠对透皮速率有极显著性影响。脂质体可以明显加快草乌甲素的透皮吸收，缩短时滞。本品对炎症和疼痛均有明显的抑制作用，优于双氯芬酸钠乳胶剂对照组。结论：脂质体是草乌甲素透皮吸收的优良载体，有利于充分发挥药物的疗效。     

Anti-amnesic effect of Ficus religiosa in scopolamine-induced anterograde and retrograde amnesia

Context:?Ficus religiosa Linn (Moraceae) is a variety of fig tree. Its figs are known to contain a high serotonergic content, and modulation of serotonergic neurotransmission plays a crucial role in the pathogenesis of amnesia. Thus, the present study was envisaged.

Objective:?To investigate the effect of the methanol extract of figs of Ficus religiosa (FRFE) on scopolamine-induced anterograde and retrograde amnesia in mice.

Materials and methods:?Transfer latency (TL) to the preferred niche in the elevated plus-maze (EPM) and learning avoidance of passive behavior to avoid punishment in the modified passive avoidance paradigm (MPA) served as behavioral models for the assessment of memory. Scopolamine (1?mg/kg, i.p.) was administered before training for induction of anterograde amnesia and before retrieval for induction of retrograde amnesia in both models. TL in the EPM, step down latency (SDL), number of trials, and number of mistakes in the MPA were determined in vehicle control, FRFE treated (10, 50, and 100?mg/kg, i.p.), and standard groups (piracetam 200?mg/kg, i.p.). Cyproheptadine, a non-selective 5-HT_1/2 blocker (4?mg/kg, i.p.), was administered along with the FRFE to investigate the involvement of serotonergic pathways in the anti-amnesic effect of FRFE.

Results and discussion:?FRFE resulted in a significant improvement of memory, as its treatment attenuated the scopolamine-induced anterograde and retrograde amnesia dose-dependently. Further, cyproheptadine pretreatment significantly reversed the anti-amnesic effect of FRFE.

Conclusion:?FRFE has anti-amnesic activity against scopolamine-induced amnesia, in a dose-dependent manner. Inhibition of the anti-amnesic effect of FRFE by cyproheptadine substantiates the involvement of serotonergic pathways for its activity.     

黄荆叶不同溶剂提取物的抗炎镇痛作用研究

目的:观察黄荆叶不同溶剂(氯仿、乙酸乙酯、水)提取部分的抗炎、镇痛作用.方法:采用二甲苯诱导小鼠耳廓肿胀和角叉菜胶诱导大鼠足肿胀建立炎症模型观察黄荆叶不同溶剂提取物的抗炎作用;采用扭体法和热板法观察黄荆叶不同溶剂提取物的镇痛作用.结果:乙酸乙酯提取部分(16g·kg<'-1>、8g·kg<'-1>)对二甲苯诱导的小鼠耳肿胀抑制作用最为显著(P<0.01);氯仿提取部分(16g·kg<'-1>)能明显抑制角义菜胶诱导的大鼠足肿胀(P<0.01).对热刺激和醋酸刺激引起的小鼠疼痛,乙酸乙酯提取部分(16g.k<'-1>、8g.<'-1>)和水提物各剂量组具有显著的镇痛作用(P<0.01),氯仿提取部分各剂量组镇痛作用不明显(P>0.05).结论:黄荆叶不同溶剂提取部位的抗炎镇痛作用有差异,乙酸乙酯提取物具有明显的抗炎和镇痛作用.而氯仿提取物抗炎作用较强,水提取物的镇痛作用较强.     

In vivo anti-inflammatory and analgesic activities of strictosamide from Nauclea officinalis

Context: Strictosamide is the main representative constituent of Nauclea officinalis Pierre ex Pitard (Rubiaceae), which has been used for a long time in China to treat diseases related to infection and inflammation, but its pharmacological activities are not well studied.

Objective: This work evaluates the anti-inflammatory and analgesic activities of strictosamide by in vivo experiments.

Materials and methods: The anti-inflammatory activity was assessed in mice by models of 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced ear edema, acetic acid-elevated vascular permeability, and carboxymethylcellulose sodium (CMC–Na)-induced leukocyte migration. The analgesic activity was estimated in mice using acetic acid-induced writhing and hot-plate tests. Compound was injected to mice twice a day for 3?d at doses of 10, 20, and 40?mg/kg.

Results: At 20 and 40?mg/kg, strictosamide obviously decreased the TPA-induced mice ear edema (24.7 and 28.1% inhibition, respectively), and significantly inhibited acetic acid-stimulated peritoneal vascular permeability in mice (23.3 and 33.4% inhibition, respectively). It also significantly decreased the leukocytes in the mice peritoneal cavity induced by CMC–Na at all the tested doses (46.0, 49.1, and 58.7% inhibition, respectively). To acetic acid-induced writhing test in mice, strictosamide markedly prolonged the pain latency at 20 and 40?mg/kg and decreased the writhing counts at 40?mg/kg (49.7% inhibition). However, it did not obviously improve the pain threshold of mice in hot-plate test.

Discussion and conclusion: Strictosamide may have important effects on inflammation and inflammatory pain. The results provide scientific support for the role of strictosamide in the use of N. officinalis to treat inflammatory diseases.     

滇白珠抗菌抗炎和镇痛活性的实验研究

滇白珠根挥发油对金黄葡萄球菌、绿脓杆菌、大肠杆菌和变形杆菌均有抑制作用;滇白珠根醋酸乙酯和正丁醇提取物显著抑制小鼠腹腔毛细血管通透性而具有抗炎作用,对热致疼痛具有明显的镇痛作用。     

Synthesis and anti-inflammatory and analgesic activities of pyridyloxy- and phenoxyalkanoic acid derivatives

Synthesis of pyridyloxy-, pyridyloxyphenoxy- and phenoxylphenoxyalkanate derivatives and their anti-inflammatory and analgesic activities were investigated. Analysis of structure-activity relationships showed that in pyridyloxyalkanoic acid derivatives anti-edematous potency was associated with the presence of chlorophenoxypropionic acid moiety and 2-nitrated methyl propionates contributed to the analgesic activity.     

Chemical study and anti-inflammatory, analgesic and antioxidant activities of the leaves of Aristotelia chilensis (Mol.) Stuntz, Elaeocarpaceae

Objectives Aristotelia chilensis leaves (Elaeocarpaceae) are used in Chilean folk medicine to treat pain and inflammation. A bioguided study was carried out on serial extracts (hexane, dichloromethane, methanol, aqueous extract (INFU) and a crude mixture of alkaloids (ALK‐MIX). All extracts were evaluated for (1) topical administration against both arachidonic acid and 12‐deoxyphorbol‐13‐decanoate (TPA)‐induced inflammation in mice and (2) per‐os administration against inflammation by λ‐carrageenan‐induced paw oedema in guinea‐pigs and (3) topical analgesia in tail flick and formalin models and per‐os writhing test in mice. Methods Greater anti‐inflammatory effects were obtained against TPA with dichloromethane extract and methanol extract (63.9 and 66.0%, respectively). INFU showed the most potent effect (56.2%) against arachidonic acid. Greater effects were obtained in the writhing test with hexane and dichloromethane extracts (89.2% both). In the topical analgesia models, all the extracts and ALK‐MIX were active with exception of the hexane extract in the formalin assay. In tail flick test, ALK‐MIX and the methanol extract were the most active (58.2 and 55.2%, respectively). In relation to the tail formalin assay, the methanol extract (74.1%) was the most active. Concerning antioxidant activity, both INFU and the methanol extract were the most active either in the inhibition of xanthine oxidase (52.9 and 62.7%, respectively) or in the DPPH free radical scavenging activity (EC50 (concentration that produced 50% of activity) = 12.1 and 9.7 µg/ml, respectively). Key findings Aristoteline, aristone, serratoline and hobartinol were isolated from ALK‐MIX. Ursolic acid, friedelin and quercetin 5,3′‐dimethyl ether were present in the dichloromethane extract while quercetin 3‐O‐β‐d ‐glucoside and kaempferol were present in the methanol extract. From INFU were isolated protopine, aristoteline and caffeic and ferulic acids. Conclusions The effects of A. chilensis are herein demonstrated, validating its use in traditional medicine. Protopine is reported for the first time in Elaeocarpaceae.     

冬凌草抗炎有效部位筛选及初步表征

目的:筛选冬凌草的抗炎有效部位并对有效部位进行初步表征.方法:冬凌草采用梯度极性溶剂水、25%乙醇、50%乙醇、75%乙醇及100%乙醇分别提取,提取物通过蛋清致大鼠足跖肿胀试验以确定抗炎有效部位;并对有效部位采用MS分析,HPLC测定主成分冬凌草甲素的含量.结果:冬凌草100%乙醇提取物对大鼠足跖肿胀有明显的抑制作用,MS分析提取物中明显含有冬凌草甲素及其他贝壳杉烷类二萜,HPLC测定无水乙醇提取冬凌草甲素的提取率为0.174 6%.结论:冬凌草100%乙醇提取物组分具有明显的抗炎作用,为冬凌草的抗炎有效部位,为其临床抗炎提供依据.     

Synthesis of new imidazolyl acetic acid derivatives with anti-inflammatory and analgesic activities

We synthesized 2-(4-(4-fluorobenzylidene)-2-(4-fluorophenyl) 5-oxo-4,5-dihydroimidazol-1-yl) acetic acid 3. Chlorination afforded the chloro derivative 4, which reacted with different amines and hydrazine to afford compounds 5–8. Pyrazole, pyrazolone, and thiazolidinone derivatives were also synthesized from Imidazol-1-ylacetic acid hydrazide 8 to give compounds 9–12. Compounds were then evaluated for their anti-inflammatory activity against carrageenan-induced rat paw edema and their analgesic activity using the writhing test in albino mice. Compounds 5, 9, 10, 12 exhibited maximum anti-inflammatory activity, and all the compounds inhibited writhing, with 10 and 12 being two times more effective than the reference standard.     

Screening for antidepressant, sedative and analgesic activities of novel fused thiophene derivatives

This study was aimed at the synthesis of fused benzothiophene derivatives containing heterocyclic moiety. The reaction of the tetrahydrobenzo[b]thiophene derivatives 1a,b with ethoxycarbonylisothiocyanate afforded the thiourea derivatives 2a,b. Cyclization of the latter products gave the annulated benzo[b]thienopyrimidine derivatives 3a,b. Compounds 2a,b and 3a underwent a series of heterocyclization reactions through the reaction with some chemical reagents to give the new benzo[b]thienopyrimidine derivatives 5a,b to 8a-c. Also, this work was extended to study the potential role of the novel synthesized thiourea derivative 2a and benzo[b]thienopyrimidine derivatives 3a, 5b, 6a and 8b as antidepressant, sedative or analgesic agents at two doses (15 or 30 mg kg(-1) body mass). Some compounds (2a, 3a and 5b) showed mild antidepressant activity in the forced-swimming test. No compound showed sedative effect. Visceral pain evoked by i.p. injection of acetic acid in mice was significantly inhibited by all compounds at a high doses.