Activity study of a hydroxynaphthoquinone fraction from Arnebia euchroma in experimental arthritis

Although various drugs for the treatment of rheumatoid arthritis (RA) have been used in clinics, RA is not completely curable to date. Thus, to seek new drugs for the treatment of RA has been a hotspot. Hydroxynaphthoquinones are the major anti-inflammatory active constituents in Arnebia euchroma (Royle) Johnst. The present study aims to evaluate the anti-arthritic activity of a hydroxynaphthoquinone mixture (HM) of A. euchroma (Royle) Johnst, including its anti-inflammatory and analgesic effects. The anti-arthritic efficacy of HM was examined using complete Freund's adjuvant- and bovine type II collagen-induced arthritic models. The paw edema, polyarthritis index and histopathological change were evaluated. The analgesic effect was assessed using the chemical and thermal models of nociception. Results found that HM administered prophylactically and curatively showed marked anti-arthritic activity by suppressing the paw swelling and development of inflammation, lowering the levels of TNF-α and IL-1β and protecting cartilage and bone from damage. The protection of HM was superior to that of reference drugs such as prednisone acetate or etanercept, and showed no direct deleterious effect. Similarly, HM showed significant analgesic effects. In summary, HM possessed potent anti-arthritic activity. It could relieve inflammatory symptoms and protect against joint destruction. These findings indicate that HM would be a potential therapeutic agent for arthritic disease, which provide pharmacological evidence for its clinical application.     

Analgesic activity of methanol extract of Aegle marmelos leaves

The methanol extract of leaves of Aegle marmelos at a dose level of 200 and 300 mg/kg showed significant analgesic activity on acetic acid-induced writhing and tail flick test in mice.     

Pharmacokinetic Assessment of the Marker Active Metabolites 4-Methyl-amino-antipyrine and 4-Acetyl-amino-antipyrine After Intravenous and Intramuscular Injection of Metamizole (Dipyrone) in Healthy Donkeys

Metamizole (MT) is an analgesic and antipyretic drug labelled for use in humans, horses, cattle, swine, and dogs in some countries. Metamizole is rapidly hydrolyzed to the active primary metabolite 4-methyl-amino-antipyrine (MAA). MAA is formed in much larger amounts compared to other minor metabolites. Among the other secondary metabolites, 4-amino-antipyrine (AA) is also relatively active. The aim of this research was to evaluate the pharmacokinetic profiles of MAA and AA after administration of 25 mg/kg MT by intravenous (IV) and intramuscular (IM) routes in healthy donkeys. Six jennies were randomly allocated to two equally sized treatment groups according to a 2 × 2 crossover study. Blood was collected at predetermined times within 24 hours, and plasma was analyzed by a validated HPLC UV method. Plasma concentrations of MAA after IV and IM administrations of MT were detectable from 5 minutes to 10 hours in all the donkeys. Plasma concentrations of AA were detectable from 5 minutes to 8 hours, but in smaller amounts. C_max (P < .01), AUC_0-last, AUC_0-∞, AUMC_0-last, and MRT (P < .05) were statistically different between the IV and IM groups. The AUC_IM/AUC_IV ratio of MAA was 1.37. The AA concentrations were lower than those found for MAA. The AA plasma versus time curves profiles after the two routes of administration of MT were variable (within the groups) and different (between the groups). T_max, λz, and AUC_0-last were found to be statistically different between the groups (P < .05). The AUC_IM AA/AUC_IV AA ratio was 2.26.     

大马勃抗炎镇痛及体外抑菌作用的研究

探讨大马勃子实体、菌丝体、发酵液不同提取物的抗炎、镇痛以及体外抑菌活性，为大马勃的进一步开发利用提供基础研究。实验结果显示，大马勃各部分提取物均能明显抑制二甲苯致小鼠耳肿胀度和对醋酸诱发的小鼠扭体反应，其中大马勃发酵液抗炎镇痛效果最佳，抑制率最高，分别为42．9％和43．69％；同时各种提取物均有不同程度的抑制作用，并且MIC最小值为3．15mg·mL-1。结果表明大马勃子实体及液体发酵代谢产物具有明显的抗炎、镇痛及抑菌作用，本着合理利用资源，走工业化生产道路，可利用发酵代谢产物来代替大马勃子实体的相关临床作用。     

The studies of anti-inflammatory and analgesic activities and pharmacokinetics of Oxytropis falcate Bunge extraction after transdermal administration in rats

The aim of this study was to evaluate the activities of anti-inflammatory and analgesic of the total flavonoids extraction from Oxytropis falcate Bunge (FEO) after transdermal administration. The pharmacokinetics and absolute bioavailability of FEO in rat, furthermore, was studied. Firstly, the anti-inflammatory and analgesic effects of the FEO were studied by xylene-induced ear edema, adjuvant-induced joint inflammation law in rats, acetic acid-induced writhing and hot-plate tests in mice. Secondly, we developed a sensitive and specific HPLC method to analyze 2′, 4′-dihydroxychalcone (TFC, the mainly ingredient of FEO) in rat plasma to study the pharmacokinetic of TEC. The results showed FEO has anti-inflammatory and analgesic property in a dose-dependent manner, and that the high dose group (90.6 mg/kg) of FEO appeared more significantly effective than the positive drug. From the pharmacokinetic studies of TFC in rats, we got the main pharmacokinetic parameters of TFC, providing a basis for the future studies in clinic.     

抗病毒合剂的解热镇痛作用研究

抗病毒合剂由具有抗病毒、清热、滋阴凉血等作用的中草药,经水煎醇沉,浓缩制备而成,以家兔和小鼠为动物模型研究该合剂的解热和镇痛作用。结果表明,抗病毒合剂对松节油和猪瘟活疫苗引起的家兔发热有显著的抑制作用(P<0.05或P<0.01);对小白鼠的热板法致痛试验仅0.8mL剂量组给药后30min较对照组差异显著(P<0.05),而对醋酸所致小鼠扭体镇痛作用抑制率为零,由此可见抗病毒合剂的镇痛作用不明显。     

Anti-inflammatory and analgesic properties of cis-mulberroside A from Ramulus mori

This study examined the analgesic and anti-inflammatory actions of cis-mulberroside A isolated from Ramulus mori in several models of inflammatory pain in mice. Cis-mulberroside A (25 and 50 mg/kg) given by p.o. route 30 min before challenge produced a dose-dependent inhibition of the acetic acid-induced pain and Evans blue leakage in mice. In addition, this compound exhibited significant systemic anti-inflammatory activity in carrageenan-induced mouse paw edema in a concentration-related manner (33.1–68.5% inhibition), and similar results were achieved in formalin test. Suppressive effects of cis-mulberroside A on the production of NO and expression of inducible nitric oxide synthase (iNOS) in lipopolysaccharide (LPS)-stimulated macrophages were also assessed. Collectively, cis-mulberroside A showed high analgesic and anti-inflammatory activities. The above results will be the supporting evidence for the potential anti-rheumatoid activity of R.mori in Chinese traditional medicine.     

胆红素含量不同的培植牛黄的镇静、镇痛及抗惊厥作用研究

采用活动记数法，热板法、电刺激法和扭体法，电惊厥法和化学惊厥法，观察胆红素含量不同的培植牛黄和天然牛黄的镇静、镇痛和抗惊厥作用。经实验研究证明，胆红素含量不同的培植牛黄与天然牛黄具有相近的镇静、镇痛和抗惊厥作用。中、低胆红素培植牛黄和天然牛黄均能明显减少小鼠自发活动次数，延长戊巴比妥钠的作用时间；显著降低醋酸所致小鼠的疼痛反应，但对电、热物理因素所致小鼠疼痛反应无明显抑制作用。此外，这３种药物对小鼠由电及苯甲酸钠咖啡因所致惊厥具有保护作用。因而表明，培植牛黄和天然牛黄的镇静，镇痛及对惊厥的保护作用与其胆红素含量无明显的相关性。     

Determination of oral tramadol pharmacokinetics in horses

The determination of the pharmacokinetic parameters of tramadol in plasma and a better characterization of its metabolites after oral administration to horses is necessary to design dosage regimens to achieve target plasma concentrations that are associated with analgesia. The purpose of this study was to determine the pharmacokinetics and elimination pattern in urine of tramadol and its metabolites after oral administration to horses. Tramadol was administered orally to six horses and its half-life, T_max and C_max in plasma were 10.1, 0.59 h, and 132.7 ng/mL, respectively. The half-life, T_max and C_max for M1 in plasma were 4.0, 0.59 h, and 28.0 ng/mL, respectively. Tramadol and its metabolites were detectable in urine between 1 and 24 h after the administration. In conclusion, the PK data reported in this study provides information for the design of future studies of tramadol in horses.