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Preliminary toxicity and gastroprotective potential of flavonoid-rich fractions of leaves from Opilia celtidifolia (Guill. & Perr.) Endl. ex Walp (Opiliaceae) 黄酮类化合物的初步毒性和胃保护作用。&穗青葱)。Endl。原蛇麻(蛇麻科)
Pub Date : 2018-12-18 DOI: 10.26510/2394-0859.PBE.2018.07
Konaté Kiessoun, D. I. Crepin, Diao Mamounata, Yomalan Kassi, A. Souza, M. Dicko
Objective : In Burkina Faso as in other developing countries, the diarrheal diseases constitute a serious problem of public health. To treat diarrhea, most Burkina Faso people living in the rural areas do rely on medicinal plants. To evaluate the traditional use of Opilia celtidifolia , scientific validation is needed. Methods : The collected plant materials were dried, pulverized, and aqueous acetone extracts were prepared. The serially diluted fractions of the extracts and finally reach the flavonoid-rich fractions which assayed for antibacterial activities against selected enteropathogens by agar well diffusion method, minimum inhibitory concentration and minimal bactericidal concentration respectively. The anti-diarrheal activity was evaluated using castor oil induced diarrhea, magnesium sulphate-induced diarrhea and gastrointestinal transit test examined in animal models respectively. Results : Flavonoid-rich fractions has positive effects in a dose dependent manner against diarrhoea induced by castor oil, magnesium sulphate-induced diarrhea and gastrointestinal transit test examined in animal models. The bioactive fraction also showed good antimicrobial activity against all bacteria strains and compared to the ciprofloxacin. Conclusions : These findings indicate that the flavonoid-rich fraction possesses antidiarrheal property in rats and confirm the ethnomedicinal use of Opilia celtidifolia a valuable natural remedy for the treatment, management and/or control of diarrhea. The results provided some insight into the gastroprotective potential of this plant traditionally used by the people of Burkina Faso to treat diarrhea.
目的:与其他发展中国家一样,腹泻病在布基纳法索构成了一个严重的公共卫生问题。为了治疗腹泻,大多数生活在农村地区的布基纳法索人确实依靠药用植物。要评价槐的传统用途,还需要科学的验证。方法:将采集的植物材料进行干燥、粉碎,制备丙酮水提物。通过琼脂孔扩散法、最小抑菌浓度法和最小杀菌浓度法对选定的肠道病原菌进行抑菌活性测定。采用蓖麻油致泻法、硫酸镁致泻法和动物胃肠运输法分别评价其抗泻活性。结果:富黄酮类成分对蓖麻油致腹泻、硫酸镁致腹泻及动物胃肠运输试验均有剂量依赖性的积极作用。与环丙沙星相比,生物活性部分对所有菌株均表现出良好的抑菌活性。结论:这些研究结果表明,黄酮类化合物在大鼠体内具有止泻作用,证实了蛇毛是一种治疗、管理和/或控制腹泻的宝贵天然药物。这些结果为这种植物的胃保护潜力提供了一些见解,这种植物传统上被布基纳法索人民用于治疗腹泻。
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引用次数: 0
Molecular structure, HOMO, LUMO, MEP, natural bond orbital analysis of benzo and anthraquinodimethane derivatives 苯并和蒽醌二甲烷衍生物的分子结构、HOMO、LUMO、MEP、天然键轨道分析
Pub Date : 2018-04-01 DOI: 10.26510/2394-0859.PBE.2018.04
Tahar Abbaz, A. Bendjeddou, D. Villemin
Objective: Optimized molecular structures have been investigated by DFT/B3LYP method with 6-31G (d,p) basis set. Stability of Benzo and anthraquinodimethane derivatives 1-4, hyperconjugative interactions, charge delocalization and intramolecular hydrogen bond has been analyzed by using natural bond orbital (NBO) analysis. Electronic structures were discussed and the relocation of the electron density was determined. Molecular electrostatic potential (MEP), local density functional descriptors has been studied. Nonlinear optical (NLO) properties were also investigated. In addition, frontier molecular orbitals analyses have been performed from the optimized geometries. An ionization potential (I), electron affinity (A), electrophilicity index (ω), chemical potential (µ), electronegativity (χ), hardness (η), and softness (S), have been investigated. All the above calculations are made by the method mentioned above.Methods: The most stable optimized geometries obtained from DFT/B3LYP method with 6-31G(d,p) basis set were investigated for the study of molecular structures, nonlinear properties, natural bond orbital (NBO), molecular electrostatic potential (MEP) and frontier molecular orbital of Benzo and anthraquinodimethane derivatives.Results: Reactive sites of electrophilic and nucleophilic attacks for the investigated molecule were predicted using MEP at the B3LYP/6-31G(d,p). Compound 4 possesses higher electronegativity value than all compounds so; it is the best electron acceptor; the more reactive sites for electrophilic attacks are shown in compounds 1 and 4, for nucleophilic attacks are indicated in compounds 2 and 3 and the more reactive sites in radical attacks are detected in compounds 2 and 4.Conclusions: Compound 1 is softest, best electron donor and more reactive than all compounds. The calculated first order hyperpolarizability was found much lesser than reported in literature for urea.
目的:以6-31G (d,p)为基组,采用DFT/B3LYP方法研究优化后的分子结构。利用自然键轨道(NBO)分析了苯并和蒽醌二甲烷衍生物1-4的稳定性、超共轭相互作用、电荷离域和分子内氢键。讨论了电子结构,确定了电子密度的重新定位。对分子静电势、局部密度泛函描述符进行了研究。非线性光学(NLO)性质也进行了研究。此外,对优化后的结构进行了前沿分子轨道分析。研究了其电离势(I)、电子亲和性(A)、亲电性指数(ω)、化学势(µ)、电负性(χ)、硬度(η)和柔软度(S)。以上计算均采用上述方法进行。方法:以6-31G(d,p)基为基础,采用DFT/B3LYP方法对苯并和蒽醌二甲烷衍生物的分子结构、非线性性质、自然键轨道(NBO)、分子静电势(MEP)和前沿分子轨道进行了研究。结果:利用MEP在B3LYP/6-31G上预测了所研究分子亲电和亲核攻击的反应位点(d,p)。化合物4具有较高的电负性;它是最好的电子受体;亲电攻击的活性位点较多见于化合物1和4,亲核攻击的活性位点较多见于化合物2和3,自由基攻击的活性位点较多见于化合物2和4。结论:化合物1最柔软,是最好的电子供体,反应性较好。尿素的一阶超极化率比文献报道的要小得多。
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引用次数: 29
Evaluation of analgesic activity of ethanolic and aqueous extracts of leaf of Plumeria rubra in albino rat 白化大鼠黄花鸡蛋花叶乙醇提取物及水提物的镇痛作用评价
Pub Date : 2018-04-01 DOI: 10.26510/2394-0859.PBE.2018.06
Dhanapal Venkatachalam, B. Thavamani, Muddukrishniah
Objective : Plumeria rubra is an important traditional medicinal plant used in various ailments and the indigenous plant as a medicament for treatment of various inflammatory conditions is well documented in literature. The analgesic activity was evaluated by hot-plate and acetic acid induced writhing methods. Methods : The leaves of P. rubra were collected from the local area in and around Palakkad, Kerala (India). About 1500 g of the powder was extracted using Soxhlet apparatus for 12 h using 5.0 L of Ethanol as solvent. The test extracts was administered intraperitoneally at a dose of 100 and 200 mg/kg while Pentazocine (5 mg/kg) and diclofenac sodium (10 mg/kg) served as standards. Results : The ethanolic extract of 200 mg/kg having significant analgesic activity in Acetic acid induced abdominal writhing response and percentage of inhibition (PI) (p<0.01 )when compared to control.. The Ethanolic extract of 100 mg/kg and 200 mg/kg exhibited significant analgesic activity in the hot plate method (p<0.001) by increasing the pain reaction time (PAT) of the rats to  sec 7.25±0.38 at 45 min after treatment in comparison to control (4.08±13). Conclusions : The results suggest that ethanolic extracts of P. rubra possesses potent analgesic properties, which support its use in traditional medicine and suggesting that the plant should be further investigated for its pharmacological active natural products.
目的:红鸡蛋花是一种重要的传统药用植物,用于治疗各种疾病,其作为治疗各种炎症的药物已有文献记载。采用热板法和醋酸扭体法评价其镇痛活性。方法:在印度喀拉拉邦Palakkad及周边地区采集红叶。以5.0 L乙醇为溶剂,用索氏仪提取约1500 g粉末,提取12 h。实验提取液分别以100和200 mg/kg的剂量腹腔注射,并以Pentazocine (5 mg/kg)和双氯芬酸钠(10 mg/kg)为标准。结果:与对照组相比,200 mg/kg乙醇提取物对醋酸诱导的大鼠扭腹反应和抑制率(PI)均有显著的镇痛作用(p<0.01)。100 mg/kg和200 mg/kg乙醇提取物在热板法中表现出显著的镇痛活性(p<0.001),治疗后45 min大鼠的疼痛反应时间(PAT)为7.25±0.38秒,对照组为4.08±13秒。结论:红颜草乙醇提取物具有较强的镇痛作用,支持其在传统医学中的应用,建议对其活性天然产物进行进一步的药理研究。
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引用次数: 2
Polycystic ovarian syndrome: a curse to young women’s 多囊卵巢综合征:年轻女性的诅咒
Pub Date : 2018-04-01 DOI: 10.26510/2394-0859.PBE.2018.03
N. Srivastava, Shashi Pratap Singh, A. Shukla, K. Gupta
The endocrine system is the group of glands that secrete hormone directly into the circulatory system moves towards distant target organs and affects them. This system release hormones that help control many important body functions. Dysfunctioning in the endocrine system may develop many disorders like diabetes, thyroid, growth disorders and sexual dysfunction. Poly cystic ovarian syndrome is one of the common endocrine disorder. PCOS is a common condition that causes a range of symptoms including irregular periods, unwanted hair growth, acne and weight problems. Increased circulating levels of testosterone can be considered as the major cause of development of polycystic ovarian syndrome. It is a male hormone, but women’s bodies make it too. Higher than normal testosterone level, makes women to experience PCOS. The physicians target on regular menstruation. In order to maintain the regular periods physicians basically administer Estrogen and Progesterone injection. Metformin is used during PCOS to treat insulin resistance developed in those women. Insulin resistance means that their bodies do not respond well to the hormone insulin that controls blood sugar levels. This causes blood sugar level to rise and this may lead to greater production of testosterone. Corticosteroids, vitamins, contraceptives pills are also prescribed for symptomatic treatment of PCOS. Changing of lifestyles may greatly help in management of poly cystic ovarian disorder. Regular exercise and weight management is the key for complete treatment of PCOS. This review contains all the information regarding PCOS.
内分泌系统是一组腺体,它们直接向循环系统分泌激素,并向远处的目标器官移动并影响它们。这个系统释放激素,帮助控制许多重要的身体功能。内分泌系统的功能失调可能导致许多疾病,如糖尿病、甲状腺、生长障碍和性功能障碍。多囊卵巢综合征是一种常见的内分泌疾病。多囊卵巢综合征是一种常见的疾病,它会导致一系列症状,包括月经不规律、多余的毛发生长、痤疮和体重问题。循环睾酮水平升高可被认为是多囊卵巢综合征发展的主要原因。它是一种男性荷尔蒙,但女性的身体也会分泌。睾丸激素水平高于正常水平,使女性患上多囊卵巢综合征。医生以月经规律为目标。为了维持正常的月经周期,医生主要给她们注射雌激素和黄体酮。二甲双胍在多囊卵巢综合征期间用于治疗这些妇女的胰岛素抵抗。胰岛素抵抗意味着他们的身体对控制血糖水平的激素胰岛素反应不佳。这会导致血糖水平上升,这可能会导致更多的睾丸激素的产生。皮质类固醇、维生素、避孕药也可用于多囊卵巢综合征的对症治疗。生活方式的改变对多囊卵巢疾病的治疗有很大的帮助。有规律的运动和体重管理是全面治疗多囊卵巢综合征的关键。这篇综述包含了关于多囊卵巢综合征的所有信息。
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引用次数: 0
Synthesis and evaluation trypanosomicidal activity of new derivatives of megazol 甲甲脲新衍生物的合成及杀锥虫活性评价
Pub Date : 2018-04-01 DOI: 10.26510/2394-0859.PBE.2018.05
Helena Braga Leites, F. S. Damasceno, A. Silber, R. Mendonça, C. N. Albuquerque
Objective : This work aims at the synthesis of megazol analogs with antitrypanosomicidal activity. Chagas’disease is caused by Trypanosoma cruzi and is a debilitating disease that has both acute and chronic forms. Many South Americans suffer from the chronic form of Chagas’disease, and there is no treatment currently available. Methods : In the chemical part, classical techniques of heterocyclic synthesis as well as usual methods of identification were used. In the biological part the cell proliferation test was used in vitro and the IC 50. Results : We synthesized a series of derivatives of 2-(1-methyl-5-nitro-2-imidazolyl)-5-substituted-1,3,4-thiadiazoles where 1-acetyl, 1-propyl and 1-nonyl were used as the substituent (4,6,7). Derivatives without nitro group were also synthesized (3,12) along with thiosemicarbazones (8,9,10) and a 5-(5-nitro-2-furanyl)-1,3,4-thiadiazol-2-amine (11). These compounds were evaluated using an in vitro test where were measured the cell proliferation. The derivatives that obtained the best results underwent further tests, in which their IC50 was calculated. The data revealed that two compounds (4,6) were effective against the parasite (IC50= 0.354 µM; IC50= 2.13 µM) and besides that, obtained the same results as the positive control, antimycim and rotenone. All proposed structures were obtained in satisfactory yields and purities. Conclusions : In conclusion, the in vitro trypanocidal activity makes these compounds promising leads in the development of an effective therapeutic agent. However, this study must be completed by additional tests with in vitro amastigote/macrophage models or in vivo mouse models. Analyzing the amide derivatives, compounds (4) and (6) were the ones that presented the best results.
目的:合成具有抗锥虫活性的甲脲类似物。恰加斯病是由克氏锥虫引起的,是一种使人衰弱的疾病,有急性和慢性两种形式。许多南美人患有慢性恰加斯病,目前尚无治疗方法。方法:在化学部分,采用杂环合成的经典技术和常用的鉴定方法。生物部分采用体外细胞增殖试验和ic50法。结果:我们合成了一系列以1-乙酰基、1-丙基和1-壬基为取代基的2-(1-甲基-5-硝基-2-咪唑基)-5-取代-1,3,4-噻二唑衍生物(4,6,7)。不含硝基的衍生物也与硫代氨基脲(8,9,10)和5-(5-硝基-2-呋喃基)-1,3,4-噻二唑-2-胺(11)合成(3,12)。这些化合物是评估使用体外试验,其中测量细胞增殖。获得最佳结果的衍生物进行了进一步的测试,并计算了它们的IC50。结果表明,两种化合物(4,6)对疟原虫有较好的抑制作用(IC50= 0.354µM;IC50= 2.13µM),结果与阳性对照、抗真菌素和鱼藤酮相同。所有提出的结构都获得了令人满意的产率和纯度。结论:该化合物具有良好的体外杀锥虫活性,有望成为一种有效的治疗药物。然而,这项研究必须通过体外无尾线虫/巨噬细胞模型或体内小鼠模型的额外测试来完成。对酰胺类衍生物进行分析,化合物(4)和(6)的效果最好。
{"title":"Synthesis and evaluation trypanosomicidal activity of new derivatives of megazol","authors":"Helena Braga Leites, F. S. Damasceno, A. Silber, R. Mendonça, C. N. Albuquerque","doi":"10.26510/2394-0859.PBE.2018.05","DOIUrl":"https://doi.org/10.26510/2394-0859.PBE.2018.05","url":null,"abstract":"Objective : This work aims at the synthesis of megazol analogs with antitrypanosomicidal activity. Chagas’disease is caused by Trypanosoma cruzi and is a debilitating disease that has both acute and chronic forms. Many South Americans suffer from the chronic form of Chagas’disease, and there is no treatment currently available. Methods : In the chemical part, classical techniques of heterocyclic synthesis as well as usual methods of identification were used. In the biological part the cell proliferation test was used in vitro and the IC 50. Results : We synthesized a series of derivatives of 2-(1-methyl-5-nitro-2-imidazolyl)-5-substituted-1,3,4-thiadiazoles where 1-acetyl, 1-propyl and 1-nonyl were used as the substituent (4,6,7). Derivatives without nitro group were also synthesized (3,12) along with thiosemicarbazones (8,9,10) and a 5-(5-nitro-2-furanyl)-1,3,4-thiadiazol-2-amine (11). These compounds were evaluated using an in vitro test where were measured the cell proliferation. The derivatives that obtained the best results underwent further tests, in which their IC50 was calculated. The data revealed that two compounds (4,6) were effective against the parasite (IC50= 0.354 µM; IC50= 2.13 µM) and besides that, obtained the same results as the positive control, antimycim and rotenone. All proposed structures were obtained in satisfactory yields and purities. Conclusions : In conclusion, the in vitro trypanocidal activity makes these compounds promising leads in the development of an effective therapeutic agent. However, this study must be completed by additional tests with in vitro amastigote/macrophage models or in vivo mouse models. Analyzing the amide derivatives, compounds (4) and (6) were the ones that presented the best results.","PeriodicalId":19998,"journal":{"name":"Pharmaceutical and Biological Evaluations","volume":"96 1","pages":"40-51"},"PeriodicalIF":0.0,"publicationDate":"2018-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78956406","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 1
Development and statistically validated UV spectrophotometric determination of testosterone in gel formulation 开发和统计验证紫外分光光度法测定凝胶制剂中的睾酮
Pub Date : 2018-02-01 DOI: 10.26510/2394-0859.PBE.2018.02
Kartik Bhagat, A. V. Ganorkar, A. Hemke, K. Gupta
Objective : A simple, precise and accurate UV-spectrophotometric method is developed and statistically validated for estimation of Testosterone in gel formulation. The proposed method includes using regression equation, area under curve (AUC), first order derivative and second order derivative spectroscopic method. Methods : based on measurement of absorbance at a selected wavelength using UV-visible spectrophotometer with 1cm matched quartz cell and acetonitrile as a solvent. All developed methods obeyed Beer’s-lambert’s law in the concentration range of 5-25μg/mL, with correlation coefficient value less than 1. Results : The percent amount of drug estimated was nearly 100%, found to be a good agreement with label claim of marketed gel formulation. The recovery study was carried out at three different levels, the validation study data was found to be statistically significant as all the statistical parameters are within the acceptance range (% RSD <2.0 and S.D. <±2.0). Conclusions : The results of estimation and validation parameters like accuracy, precision, ruggedness, linearity and range were studied for all the developed methods and were found to be within limits. The results obtained were statistically compared using paired t-test and one way ANOVA analysis. The proposed method can be adopted for routine quality control for estimation of drug in formulation.
目的:建立一种简便、精确、准确的紫外分光光度法测定凝胶制剂中睾酮含量的方法。该方法包括回归方程法、曲线下面积法、一阶导数法和二阶导数光谱法。方法:采用紫外可见分光光度计,以乙腈为溶剂,用1cm匹配的石英池测定在选定波长处的吸光度。所建立的方法在5 ~ 25μg/mL浓度范围内均符合比尔-朗伯定律,相关系数值均小于1。结果:所估算的药量百分比接近100%,与上市凝胶制剂的标签声明吻合较好。回收率研究分三个不同水平进行,所有统计参数均在可接受范围内(% RSD <2.0, sd <±2.0),验证研究数据具有统计学意义。结论:对所建立方法的准确度、精密度、稳健性、线性度、范围等参数的估计和验证结果进行了研究,均在限定范围内。所得结果采用配对t检验和单因素方差分析进行统计学比较。该方法可用于制剂中药物的常规质量控制。
{"title":"Development and statistically validated UV spectrophotometric determination of testosterone in gel formulation","authors":"Kartik Bhagat, A. V. Ganorkar, A. Hemke, K. Gupta","doi":"10.26510/2394-0859.PBE.2018.02","DOIUrl":"https://doi.org/10.26510/2394-0859.PBE.2018.02","url":null,"abstract":"Objective : A simple, precise and accurate UV-spectrophotometric method is developed and statistically validated for estimation of Testosterone in gel formulation. The proposed method includes using regression equation, area under curve (AUC), first order derivative and second order derivative spectroscopic method. Methods : based on measurement of absorbance at a selected wavelength using UV-visible spectrophotometer with 1cm matched quartz cell and acetonitrile as a solvent. All developed methods obeyed Beer’s-lambert’s law in the concentration range of 5-25μg/mL, with correlation coefficient value less than 1. Results : The percent amount of drug estimated was nearly 100%, found to be a good agreement with label claim of marketed gel formulation. The recovery study was carried out at three different levels, the validation study data was found to be statistically significant as all the statistical parameters are within the acceptance range (% RSD <2.0 and S.D. <±2.0). Conclusions : The results of estimation and validation parameters like accuracy, precision, ruggedness, linearity and range were studied for all the developed methods and were found to be within limits. The results obtained were statistically compared using paired t-test and one way ANOVA analysis. The proposed method can be adopted for routine quality control for estimation of drug in formulation.","PeriodicalId":19998,"journal":{"name":"Pharmaceutical and Biological Evaluations","volume":"25 1","pages":"1-9"},"PeriodicalIF":0.0,"publicationDate":"2018-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81506743","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 1
Comparative efficacy of herbal anti-diarrheal products for treatment of diarrhea in calves 中药止泻产品治疗犊牛腹泻的疗效比较
Pub Date : 2018-02-01 DOI: 10.26510/2394-0859.PBE.2018.01
N. Ranaut, Pranshu Sharma, K. Ravikanth, B. Ganguly
Objective : The present study was undertaken to compare the efficacy of herbal drugs, Diaroak ® and Salcochek ® (M/s Ayurvet Limited), against antibiotic drugs in the treatment of calf diarrhea. Methods : 15 calves suffering from diarrhea were divided into 3 groups: T 0 ,receiving ciprofloxacin (250 mg) and tinidazole (300 mg) twice daily for three days, T 1 , receiving 15 gm Diaroak twice daily till recovery, and T 3 , receiving 15 gm Salcochektwice daily till recovery. The parameters evaluated included average number of doses required for complete recovery, total number of animals completely recovered per group, number of animals in morbid state per group, mortality recorded per group, frequency of defecation per group, presence or absence of mucus in feces along with appetite of animals, and incidence of diarrhea and mortality during post-treatment period. Results : Complete recovery was seen in all the treated animals with no recurrence. After recovery, animals treated with herbals had better consistency of feces than those treated with antibiotics. Conclusions : Herbal anti-diarrheals Diaroak and Salcocheck can be used for treating non-specific diarrhea in calves.
目的:比较中草药Diaroak®和Salcochek®(M/s Ayurvet Limited)治疗小牛腹泻的抗菌药物疗效。方法:15头腹泻犊牛分为3组:t0组,给予环丙沙星(250 mg)和替硝唑(300 mg)每日2次,连用3 d; t1组,给予Diaroak 15 gm,每日2次,连用3 d; t3组,给予salcochek 15 gm,每日2次,连用3 d。评估的参数包括完全恢复所需的平均剂量,每组完全恢复的动物总数,每组处于病态状态的动物数量,每组记录的死亡率,每组排便频率,粪便中是否存在粘液以及动物的食欲,以及治疗后期间腹泻的发生率和死亡率。结果:所有治疗动物均痊愈,无复发。康复后,用草药治疗的动物比用抗生素治疗的动物粪便具有更好的一致性。结论:中药止泻剂Diaroak和Salcocheck可用于犊牛非特异性腹泻的治疗。
{"title":"Comparative efficacy of herbal anti-diarrheal products for treatment of diarrhea in calves","authors":"N. Ranaut, Pranshu Sharma, K. Ravikanth, B. Ganguly","doi":"10.26510/2394-0859.PBE.2018.01","DOIUrl":"https://doi.org/10.26510/2394-0859.PBE.2018.01","url":null,"abstract":"Objective : The present study was undertaken to compare the efficacy of herbal drugs, Diaroak ® and Salcochek ® (M/s Ayurvet Limited), against antibiotic drugs in the treatment of calf diarrhea. Methods : 15 calves suffering from diarrhea were divided into 3 groups: T 0 ,receiving ciprofloxacin (250 mg) and tinidazole (300 mg) twice daily for three days, T 1 , receiving 15 gm Diaroak twice daily till recovery, and T 3 , receiving 15 gm Salcochektwice daily till recovery. The parameters evaluated included average number of doses required for complete recovery, total number of animals completely recovered per group, number of animals in morbid state per group, mortality recorded per group, frequency of defecation per group, presence or absence of mucus in feces along with appetite of animals, and incidence of diarrhea and mortality during post-treatment period. Results : Complete recovery was seen in all the treated animals with no recurrence. After recovery, animals treated with herbals had better consistency of feces than those treated with antibiotics. Conclusions : Herbal anti-diarrheals Diaroak and Salcocheck can be used for treating non-specific diarrhea in calves.","PeriodicalId":19998,"journal":{"name":"Pharmaceutical and Biological Evaluations","volume":"37 1","pages":"10-13"},"PeriodicalIF":0.0,"publicationDate":"2018-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88186518","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 5
Antimicrobial evaluation of flowering stalks of Cistanche violacea, a holoparasitic plant collected from arid region in Qassim, Saudi Arabia 产自沙特阿拉伯卡西姆干旱区全寄生植物紫肉苁蓉花茎的抗菌评价
Pub Date : 2017-12-03 DOI: 10.26510/2394-0859.PBE.2017.37
E. Abdallah
Objective : Cistanche violacea has been found in Qassim region (Saudi Arabia), growing as a parasitic plant on Haloxylon salicornicum . The flowering stalk part of this plant was evaluated for antimicrobial potential against various referenced bacteria and fungi. Methods : The flowering stalk parts were collected from the field, dried, extracted by maceration in 80% methanol and 80% Ethanol, The crude extracts were examined against the tested microorganisms using agar-well diffusion method. Results : The antimicrobial testing showed that among 10 referenced bacterial isolates, only one exhibited significant susceptibility to the methanol and ethanol extracts of C. violacea , which was Staphylococcus epidermidis ATCC ® 12228 TM , recorded 15 and 16 mm inhibition zones, respectively. While other bacteria recorded weak or no susceptibility and no antifungal activity was detected. Conclusions : In general, the methanolic and ethanolic extracts of the flowering stalks of C. violacea exhibited weak or no antimicrobial properties except with one bacterial strain, further studies on the other biological activities are recommended as well as investigating the chemical constituents. To the best of the author’s knowledge, this is the first report evaluating the antimicrobial potential of the flowering stalks of C. violacea in Qassim area, Saudi Arabia.
目的:在沙特阿拉伯卡西姆地区发现紫肉苁蓉作为寄生植物生长在盐角梭梭上。对该植物的开花茎部分进行了抑菌活性评价。方法:田间采集花茎部分,干燥,80%甲醇和80%乙醇浸渍提取,粗提物采用琼脂孔扩散法对被试微生物进行检测。结果:10株参考菌株中,只有1株表皮葡萄球菌ATCC®12228 TM对紫紫葡萄球菌甲醇和乙醇提取物有显著的敏感性,分别有15 mm和16 mm的抑菌区。而其他细菌的敏感性较弱或无敏感性,无抗真菌活性。结论:总体而言,堇菜花茎甲醇和乙醇提取物除对一株菌株的抑菌作用外,其余生物活性的研究均较弱或无抑菌作用,值得进一步深入研究。据作者所知,这是第一份评估沙特阿拉伯卡西姆地区堇菜花茎抗菌潜力的报告。
{"title":"Antimicrobial evaluation of flowering stalks of Cistanche violacea, a holoparasitic plant collected from arid region in Qassim, Saudi Arabia","authors":"E. Abdallah","doi":"10.26510/2394-0859.PBE.2017.37","DOIUrl":"https://doi.org/10.26510/2394-0859.PBE.2017.37","url":null,"abstract":"Objective : Cistanche violacea has been found in Qassim region (Saudi Arabia), growing as a parasitic plant on Haloxylon salicornicum . The flowering stalk part of this plant was evaluated for antimicrobial potential against various referenced bacteria and fungi. Methods : The flowering stalk parts were collected from the field, dried, extracted by maceration in 80% methanol and 80% Ethanol, The crude extracts were examined against the tested microorganisms using agar-well diffusion method. Results : The antimicrobial testing showed that among 10 referenced bacterial isolates, only one exhibited significant susceptibility to the methanol and ethanol extracts of C. violacea , which was Staphylococcus epidermidis ATCC ® 12228 TM , recorded 15 and 16 mm inhibition zones, respectively. While other bacteria recorded weak or no susceptibility and no antifungal activity was detected. Conclusions : In general, the methanolic and ethanolic extracts of the flowering stalks of C. violacea exhibited weak or no antimicrobial properties except with one bacterial strain, further studies on the other biological activities are recommended as well as investigating the chemical constituents. To the best of the author’s knowledge, this is the first report evaluating the antimicrobial potential of the flowering stalks of C. violacea in Qassim area, Saudi Arabia.","PeriodicalId":19998,"journal":{"name":"Pharmaceutical and Biological Evaluations","volume":"49 1","pages":"239-244"},"PeriodicalIF":0.0,"publicationDate":"2017-12-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79918723","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 1
Synthesis and biological evaluation of new aryl substituted Schiff’s bases 新的芳基取代席夫碱的合成及生物学评价
Pub Date : 2017-12-03 DOI: 10.26510/2394-0859.PBE.2017.39
V. Parcha, J. Kaur
Objective : Chemical substances employed to treat various infections caused by various types of microorganism are termed as antimicrobials and natural chemical compounds produced by specific types of bacteria are termed as antibiotics. Unlimited use of antibiotics in humans and animals and in areas other than the treatment and prophylaxis of disease have resulted in a serious problem of drug resistance. Various attempts have been adopted to cope with the resistance problem and enhance the activity, or broaden the spectrum of drugs . Based on structure-activity relationship synthesis of new compounds has been one of the best approaches for better results. It has been demonstrated that Schiff base of some leading molecules and antibiotics possess good potential as more effective and safe drugs. Encouraged by reports on potential of Schiff’s bases as antimicrobial agents and to cope up with the current requirements of developing newer, safer and broad spectrum agents attempts were made to synthesize new Schiff’s bases. Methods : Our earlier in which structure activity relationship studies revealed that substitution by nitro and amino gp in Schiff’s base moiety resulted in the enhancement of activity. So further attempts were made to extend the series with incorporation of nitro and amino moiety by condensing o,m dinitro substituted acid hydrazide with various nitro/amino substituted benzaldehydes for increasing their antimicrobial potential. Results : Synthesized compounds were characterized on the basis of spectral studies (like UV, IR, and NMR). All the synthesized derivatives were screened further for their antibacterial effect. All the synthesized derivatives were screened further for their antibacterial effect. Conclusions : Highest activity was observed in the derivative with nitro substitution in both the aryl rings.
目的:用于治疗由各种微生物引起的各种感染的化学物质称为抗菌剂,由特定类型的细菌产生的天然化合物称为抗生素。在人类和动物身上以及在治疗和预防疾病以外的领域无限制地使用抗生素,造成了严重的耐药性问题。已经采取了各种尝试来应对耐药性问题,提高药物的活性,或拓宽药物的范围。基于构效关系合成新化合物已成为获得较好效果的最佳途径之一。研究表明,一些先导分子和抗生素的希夫碱具有成为更有效、更安全的药物的良好潜力。受到希夫碱作为抗菌剂潜力的报道的鼓舞,以及为了适应开发更新、更安全、广谱抗菌剂的当前要求,人们尝试合成新的希夫碱。方法:我们早期的结构活性关系研究表明,在希夫碱基上取代硝基和氨基gp可以提高活性。因此,进一步尝试通过与各种硝基/氨基取代的苯甲醛缩合o,m二硝基取代的酸肼,以增加其抗菌潜力,以加入硝基和氨基部分来扩展该系列。结果:合成的化合物在光谱研究(如紫外、红外和核磁共振)的基础上进行了表征。对所有合成的衍生物进行了进一步的抗菌效果筛选。对所有合成的衍生物进行了进一步的抗菌效果筛选。结论:两个芳基环上都有硝基取代的衍生物活性最高。
{"title":"Synthesis and biological evaluation of new aryl substituted Schiff’s bases","authors":"V. Parcha, J. Kaur","doi":"10.26510/2394-0859.PBE.2017.39","DOIUrl":"https://doi.org/10.26510/2394-0859.PBE.2017.39","url":null,"abstract":"Objective : Chemical substances employed to treat various infections caused by various types of microorganism are termed as antimicrobials and natural chemical compounds produced by specific types of bacteria are termed as antibiotics. Unlimited use of antibiotics in humans and animals and in areas other than the treatment and prophylaxis of disease have resulted in a serious problem of drug resistance. Various attempts have been adopted to cope with the resistance problem and enhance the activity, or broaden the spectrum of drugs . Based on structure-activity relationship synthesis of new compounds has been one of the best approaches for better results. It has been demonstrated that Schiff base of some leading molecules and antibiotics possess good potential as more effective and safe drugs. Encouraged by reports on potential of Schiff’s bases as antimicrobial agents and to cope up with the current requirements of developing newer, safer and broad spectrum agents attempts were made to synthesize new Schiff’s bases. Methods : Our earlier in which structure activity relationship studies revealed that substitution by nitro and amino gp in Schiff’s base moiety resulted in the enhancement of activity. So further attempts were made to extend the series with incorporation of nitro and amino moiety by condensing o,m dinitro substituted acid hydrazide with various nitro/amino substituted benzaldehydes for increasing their antimicrobial potential. Results : Synthesized compounds were characterized on the basis of spectral studies (like UV, IR, and NMR). All the synthesized derivatives were screened further for their antibacterial effect. All the synthesized derivatives were screened further for their antibacterial effect. Conclusions : Highest activity was observed in the derivative with nitro substitution in both the aryl rings.","PeriodicalId":19998,"journal":{"name":"Pharmaceutical and Biological Evaluations","volume":"17 1","pages":"252-257"},"PeriodicalIF":0.0,"publicationDate":"2017-12-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85518560","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 1
Effect of lopinavir and efavirenz on pharmacokinetics and pharmacodynamics of glibenclamide in diabetic rats 洛匹那韦和依非韦伦对糖尿病大鼠格列苯脲药动学和药效学的影响
Pub Date : 2017-12-03 DOI: 10.26510/2394-0859.PBE.2017.38
Prashanth Vennapanja, A. Ramarao
Objective : The aim of the study is whether the impact of Efavirenz and Lopinavir will increase the plasma level of Glibenclamide or not. Efavirenz and Lopinavir is an antiretroviral drug to treat HIV AIDS and inhibits cytochrome P450-3A4. Multiple CYP isoforms are involved in the metabolism of Glibenclamide like CYP2C8 and CYP3A4. Hence there is more possibility of Efavirenz and Lopinavir to inhibit the metabolism of Glibenclamide by inhibiting CYP 3A4. Methods : Efavirenz and Lopinavir (10 mg/kg,p.o.) alone and along with Glibenclamide (10 mg/kg, p.o.) was given to normal and diabetic rats. PK/PD parameters were studied. In the rats co-treated with Efavirenz and Lopinavir and Glibenclamide. Results : The pharmacokinetic parameters like clearance of Glibenclamide was reduced, peak plasma concentration, area under the plasma concentration time curve and elimination half-life were significantly increased when compared to pioglitazone treated rats. Conclusions : This study revealed that lopinavir and efavirenz affected the disposition of Glibenclamide in rats probably by the inhibition of CYP3A4, leading to increasing Glibenclamide concentrations that could increase the efficacy of Glibenclamide or it may causes severe hypoglycemia. Therefore, its warrants to use relatively less dose of Glibenclamide than the normal dose.
目的:研究依非韦伦和洛匹那韦是否会增加格列本脲的血浆水平。依非韦伦和洛匹那韦是一种治疗艾滋病的抗逆转录病毒药物,可以抑制细胞色素P450-3A4。多种CYP亚型参与格列本脲的代谢,如CYP2C8和CYP3A4。因此,依非韦伦和洛匹那韦更有可能通过抑制CYP 3A4来抑制格列本脲的代谢。方法:分别给药依非韦伦、洛匹那韦(10 mg/kg,口服)和格列本脲(10 mg/kg,口服)。研究了PK/PD参数。用依非韦伦、洛匹那韦和格列本脲联合治疗大鼠。结果:与吡格列酮治疗大鼠相比,格列本脲的清除率降低,血药浓度峰、血药浓度时间曲线下面积、消除半衰期等药动学参数明显增加。结论:本研究揭示洛匹那韦和依非韦伦可能通过抑制CYP3A4影响大鼠对格列本脲的配置,导致格列本脲浓度升高,从而提高格列本脲的疗效,也可能导致严重的低血糖。因此,使用相对较少剂量的格列本脲是合理的。
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Pharmaceutical and Biological Evaluations
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