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Design, Optimization and In vitro Evaluation of Mesalazine 400 mg Delayed Release Tablet for Colon Specific Delivery 用于结肠给药的美沙拉秦 400 毫克缓释片的设计、优化和体外评估
Pub Date : 2023-12-26 DOI: 10.3329/dujps.v22i2.69325
Diponkor Kumar Shill, U. Kumar, Asm Monjur Al Hossain, Dilshad Noor Lira, A. S. Rouf
Ulcerative colitis is a chronic inflammatory disease, and patients would get benefit more if the drug is given directly to the colon. Mesalazine is intended to deliver to the colon for treating ulcerative colitis. Here, we aimed to design and optimize mesalazine 400 mg delayed release tablet for colon-specific delivery using a quality by design (QbD) approach. The tablet was first formulated as an optimized core tablet and then coated with Eudragit S 12.5 for ensuring colonic delivery. The experimental design for the core tablet was constructed using a 32 full factorial design, where the percentages of sodium starch glycolate (SSG) and polyvinylpyrrolidone (PVP K-30) were independent variables and the tablet hardness (kg/cm2) and cumulative percentage of drug release at pH 7.2 phosphate buffer after 1.5 hours were treated as responses. Responses obtained from the initial exploratory formulations were evaluated to develop an optimized formulation to have a hardness value of 7-8 kg/cm2 and the maximum amount of drug release at pH 7.2 buffer. The optimized formulation involved the use of SSG and PVP K-30 at 3.05% and 1.69%, respectively. Hardness and cumulative percent of drug release obtained for the optimized core tablet were 7.8 kg/cm2 and 91.76%, respectively. The compatibility of drug and excipients was studied utilizing XRD, FTIR and TGA. The optimized core tablet was then coated with Eudragit S 12.5 to deliver the drug selectively to the colon and further assessed for its in vitro dissolution. Dissolution studies indicated that coated tablets with a weight gain of 7.4% exhibited the maximum cumulative percent of drug release (91.19 ± 0.11%), with a zero-order drug release profile (R2 = 0.943). A stability study performed according to ICH Q1A (R2) guidelines at accelerated storage conditions identified that there was no significant change in drug content over the storage period, indicating the stability of the formulated tablet batches. Together, these data suggest that the mesalazine tablet developed through the QbD approach offers excellent physical properties and drug release profile and, therefore, could be recommended for commercial manufacturing. Dhaka Univ. J. Pharm. Sci. 22(2): 189-201, 2023 (December)
溃疡性结肠炎是一种慢性炎症性疾病,如果直接在结肠中给药,患者将获得更多益处。美沙拉嗪可直接进入结肠治疗溃疡性结肠炎。在此,我们旨在采用质量源于设计(QbD)的方法,设计并优化美沙拉秦 400 毫克缓释片,用于结肠特异性给药。首先将片剂配制成优化的核心片剂,然后用 Eudragit S 12.5 包衣,以确保结肠给药。核心片剂的实验设计采用 32 全因子设计,其中淀粉乙醇酸钠(SSG)和聚乙烯吡咯烷酮(PVP K-30)的百分比为自变量,片剂硬度(kg/cm2)和 1.5 小时后在 pH 值为 7.2 的磷酸盐缓冲液中的累积药物释放百分比为响应变量。通过对初步探索配方的反应进行评估,开发出一种优化配方,使其硬度值达到 7-8 公斤/平方厘米,并在 pH 值为 7.2 的缓冲液中达到最大的药物释放量。优化配方中使用了 SSG 和 PVP K-30,含量分别为 3.05% 和 1.69%。优化芯片的硬度和累积药物释放率分别为 7.8 kg/cm2 和 91.76%。利用 XRD、FTIR 和 TGA 研究了药物与辅料的相容性。然后用 Eudragit S 12.5 包衣优化后的核心片剂,以将药物选择性地输送到结肠,并进一步评估其体外溶出度。溶出度研究表明,增重 7.4% 的包衣片剂具有最大的累积药物释放率(91.19 ± 0.11%),药物释放曲线为零阶(R2 = 0.943)。根据 ICH Q1A (R2) 指南,在加速储存条件下进行了稳定性研究,结果表明药物含量在储存期间没有显著变化,这表明配制的片剂批次具有稳定性。这些数据共同表明,通过 QbD 方法开发的美沙拉嗪片剂具有优异的物理性质和药物释放特性,因此可推荐用于商业生产。Dhaka Univ.22(2):189-201,2023 年(12 月)
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引用次数: 0
Anti-viral Activity of 62 Medicinal Plants, Herbs and Spices Available in Bangladesh: A Mini Review 孟加拉国 62 种药用植物、草药和香料的抗病毒活性:小型综述
Pub Date : 2023-12-26 DOI: 10.3329/dujps.v22i2.67408
Adiba Firuj, F. Aktar, Tahmina Akter, J. A. Chowdhury, A. A. Chowdhury, Shaila Kabir, Sultan Mehtap Büyüker, Md. Shah Amran
Microorganisms can cause devastating diseases leading to a pandemic, such as COVID-19 which has created a devastating situation throughout the world. The SARS-CoV-2 or severe acute respiratory syndrome coronavirus-2 is the major concern for creating this pandemic situation. Viruses are the major pathogenic microorganisms that have the potential to be detrimental to human beings and animals in many ways. By entering the human body through different routes and commanding different machinery of the body to generate a higher number of their genomic copies and proteins they create pathogenesis. Phytomedicines may act as suitable weapons to halt the reproduction of such viruses and combat diseases caused byBangladesh is the habitat of about 500 medicinal and aromatic plants. Many of these plants have been found to show anti-viral activity. The anti-viral activity of Terminalia chebula, a well-known Bangladeshi medicinal plant has been proven to combat Newcastle Disease virus, Herpes Simplex Virus, Adenovirus type 5, Measles virus, Echovirus type 11, Rotavirus, Influenza A virus, Hepatitis B virus and Enterovirus. This review article was aimed to search available medicinal plants as novel anti-viral drugs. Dhaka Univ. J. Pharm. Sci. 22(2): 213-232, 2023 (December)
微生物可引发毁灭性疾病,导致大流行,如 COVID-19 在全世界造成了破坏性局面。SARS-CoV-2 或严重急性呼吸系统综合症冠状病毒-2 是造成这种大流行的主要原因。病毒是主要的病原微生物,有可能在许多方面对人类和动物造成危害。它们通过不同途径进入人体,并指挥人体的不同机制产生更多的基因组拷贝和蛋白质,从而产生致病作用。植物药可以作为适当的武器,阻止这些病毒的繁殖,并防治由这些病毒引起的疾病。孟加拉是大约 500 种药用植物和芳香植物的栖息地。其中许多植物被发现具有抗病毒活性。Terminalia chebula 是一种著名的孟加拉药用植物,其抗病毒活性已被证实可防治新城疫病毒、单纯疱疹病毒、腺病毒 5 型、麻疹病毒、埃可病毒 11 型、轮状病毒、甲型流感病毒、乙型肝炎病毒和肠道病毒。这篇综述文章旨在寻找可用作新型抗病毒药物的药用植物。Dhaka Univ.22(2):213-232,2023 年(12 月)
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引用次数: 0
Formulation and Evaluation of Ledipasvir Nano-suspension Through QbD Approach 通过 QbD 方法配制和评估来地帕韦纳米悬浮剂
Pub Date : 2023-12-26 DOI: 10.3329/dujps.v22i2.69324
Md Rezowanur Rahman, Diponkor Kumar Shill, U. Kumar, Asm Monjur Al Hossain, S. C. Bachar, A. S. Rouf
Ledipasvir, belonging to the BCS class II, is a directly acting anti-viral agent used to treat Hepatitis C virus infections. Due to poor water solubility and oral bioavailability, developing an effective delivery system for this drug has been an enormously challenging issue for the formulators. Moreover, suitable dosage forms for pediatric and geriatric patients and patients having difficulty in swallowing as well pose an added burden. Therefore, the present study aims to formulate a nanosuspension, via a solid dispersion technique, based on liquid oral suspension using the Quality by Design (QbD) method. Primarily, the compatible polymers for Ledipasvir were screened using FT-IR and DSC, and finally, the polymers- poloxamer 188, poloxamer 407, HPC and HMPC were selected, considering their ability to turn the API into amorphous state in solid dispersions. The design of formulation and analysis with the D-Optimal design using Design Expert® Software revealed that poloxamer 188 and poloxamer 407 at 0.3:0.7 ratio of Ledipasvir:Polymer produced the optimized nanosuspension formulations with a statistically significant mathematical model. Subsequently, the formulations were stabilized using a suspension vehicle optimized via Box-Behnken design using the amount of xanthan gum (gm), avicel® RC-591 (gm) and citric acid monohydrate (gm) as independent variables, and viscosity (cp) and zeta potential (mv) as responses. The dissolution profiles revealed that the prepared suspensions of Ledipasvir had much faster dissolution than the market products available as the tablet dosage form. In-vivo simulation studies using PKSolver® suggested that the absorption of the drug from the formulated suspensions was comparable to that of market product up to a single dose level (90 mg) and superseded in triplicate dose level (270 mg). The formulated suspensions were found to be stable over three- and six-month periods, as identified via accelerated stability studies. Interestingly, the dissolution profile of the stabilized suspensions was found to be similar after six months to that of the initial. Dhaka Univ. J. Pharm. Sci. 22(2): 173-188, 2023 (December)
来地帕韦属于 BCS II 类药物,是一种直接作用的抗病毒药物,用于治疗丙型肝炎病毒感染。由于水溶性和口服生物利用度较差,为这种药物开发有效的给药系统一直是配方设计师面临的巨大挑战。此外,适合儿童和老年患者以及吞咽困难患者的剂型也是一个额外的负担。因此,本研究旨在采用质量源于设计(QbD)的方法,通过固体分散技术,在口服液悬浮剂的基础上配制纳米悬浮剂。首先,使用傅立叶变换红外光谱(FT-IR)和电热恒温(DSC)对与莱迪帕韦相容的聚合物进行了筛选,最后,考虑到聚合物--poloxamer 188、poloxamer 407、HPC 和 HMPC--在固体分散体中能将原料药变成无定形状态的能力,选择了这些聚合物。配方设计和使用 Design Expert® 软件进行的 D-Optimal 设计分析表明,莱迪帕韦与聚合物的比例为 0.3:0.7 时,poloxamer 188 和 poloxamer 407 可制成优化的纳米悬浮配方,其数学模型具有显著的统计学意义。随后,以黄原胶(gm)、avicel® RC-591(gm)和一水柠檬酸(gm)的用量为自变量,以粘度(cp)和ZETA电位(mv)为响应变量,通过Box-Behnken设计优化悬浮载体,稳定制剂。溶解曲线显示,制备的莱迪帕韦悬浮剂比市场上的片剂产品溶解速度快得多。使用 PKSolver® 进行的体内模拟研究表明,配制的混悬液在单剂量水平(90 毫克)的药物吸收率与市售产品相当,而在三剂量水平(270 毫克)的药物吸收率则高于市售产品。通过加速稳定性研究发现,配制的混悬液在三个月和六个月的时间内都很稳定。有趣的是,稳定悬浮液在六个月后的溶解情况与初始悬浮液相似。Dhaka Univ.22(2):173-188,2023 年(12 月)
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引用次数: 0
Phytochemical and Biological Investigations of Bacopa monnieri L. Bacopa monnieri L.的植物化学和生物学研究
Pub Date : 2023-12-26 DOI: 10.3329/dujps.v22i2.67407
Md Abu Huraira, Muhammad Abdullah Al Mansur, M. Kuddus
Bacopa monnieri L. (Family: Scrophulariaceae), a medicinal herb of Bangladesh, has been used in traditional medicine to increase memory and brain power. The present research was aimed to investigate the phytochemical composition and biological activities of whole plant of B. monnieri. Through phytochemical analysis, two triterpenes, taraxerone and betulinic acid were obtained from B. monnieri. The crude methanol extract of the whole plant of Bacopa monnieri and its petroleum ether, dichloromethane, chloroform and aqueous fractions were screened for determination of several in vitro biological activities. In DPPH assay for antioxidant test, the dichloromethane fraction showed strong DPPH radical quenching activity (IC50 = 3.78 μg/ml). The chloroform fraction exhibited the maximum lethal concentration, LC50 value of 5.5 μg/ml against brine shrimp. In membrane stabilization assay, the crude extract and all solvent fractions revealed significant anti-inflammatory activity by inhibiting hemolysis of RBC induced by both hypotonic solution and heat. In thrombolytic assay, the petroleum ether fraction demonstrated highest thrombolytic activity (39.24%), when compared to the standard streptokinase (64.22%). In antimicrobial screening, the chloroform fraction displayed reasonable activity against most of the tested microorganisms. This study concludes that B.  monnieri has potential antioxidant, anti-inflammatory and thrombolytic activities. Dhaka Univ. J. Pharm. Sci. 22(2): 155-161, 2023 (December)
Bacopa monnieri L.(科:景天科)是孟加拉国的一种药材,在传统医学中被用于增强记忆力和脑力。本研究旨在调查孟加拉鼠尾草全株的植物化学成分和生物活性。通过植物化学分析,从 B. monnieri 中获得了两种三萜类化合物:蒲公英萜酮和白桦脂酸。研究人员对猴面包树全株的粗甲醇提取物及其石油醚、二氯甲烷、氯仿和水馏分进行了筛选,以测定几种体外生物活性。在 DPPH 抗氧化试验中,二氯甲烷馏分显示出很强的 DPPH 自由基淬灭活性(IC50 = 3.78 μg/ml)。氯仿馏分对盐水虾的致死浓度最高,LC50 值为 5.5 μg/ml。在膜稳定试验中,粗提取物和所有溶剂馏分都显示出显著的抗炎活性,抑制了低渗溶液和热引起的红细胞溶血。在溶栓试验中,与标准链激酶(64.22%)相比,石油醚馏分的溶栓活性最高(39.24%)。在抗菌筛选中,氯仿馏分对大多数受试微生物显示出合理的活性。本研究得出结论,单叶榕具有潜在的抗氧化、抗炎和溶栓活性。Dhaka Univ.22(2):155-161,2023 年(12 月)
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引用次数: 0
Isolation, Molecular Characterization, Optimization and Purification of Amylase Enzyme from Locally Isolated Bacillus Species in Different Regions of Munshiganj, Bangladesh 孟加拉 Munshiganj 不同地区当地分离的芽孢杆菌淀粉酶的分离、分子特征、优化和纯化
Pub Date : 2023-12-26 DOI: 10.3329/dujps.v22i2.67406
Md. Fuadh-Al-Kabir, Julia Ferdouse, A.N.M. Hamidul Kabir
Amylase is a kind of enzyme that facilitates the breakdown of carbohydrates in the body. This enzyme has many applications in different industries. Generally, in pharmaceutical sector it is used for the treatment of pancreatic disorder, pancreatic enzyme replacement therapy (PERT) and as a digestive aid. In this study, the bacterial strain was isolated from soil samples collected from potato dumpsites in different areas of Munshiganj, Bangladesh. After subculturing on the nutrient agar plate, 31 colonies were obtained, of which 9 isolates were found as amylase producer on starch agar medium. Of these, 2 isolates (MC-04 and MC-15) were selected based on the starch hydrolysis clear zone ratio. The isolate MC-04 showed crude enzyme activity of 2.82 IU/ml and specific enzyme activity of 3.42 IU/mg, and isolate MC-15 showed crude enzyme activity of 3.16 IU/ml and specific enzyme activity of 3.77 IU/mg. The best isolate, MC-15, was then identified by morphology, biochemical and molecular characterization and confirmed by 16S-rRNA gene sequencing. After 16S-rRNA sequencing, the isolate (MC-15) was identified as Bacillus subtilis. This amylase production of this strain had also been optimized under certain conditions such as different incubation periods, pH, temperatures and different carbon sources. We found that the best incubation period was 48 h, the optimum pH-7.0, the optimum temperature at 40°C and 2% starch was considered as the best source of carbon. Finally, the crude amylase enzyme was purified by precipitation with ammonium sulfate, dialysis, and single-step gel filtration chromatography. The enzymatic activity of the purified amylase was found to be 8.91 IU/ml, that was 2.82-fold greater enzymatic activity than the raw enzyme. The experiments confirmed that Bacillus subtilis may be a good source of amylase enzyme for industrial application in Bangladesh. Dhaka Univ. J. Pharm. Sci. 22(2): 147-154, 2023 (December)
淀粉酶是一种促进体内碳水化合物分解的酶。这种酶在不同行业有许多应用。一般来说,在制药领域,它被用于治疗胰腺疾病、胰酶替代疗法(PERT)和消化辅助剂。在这项研究中,细菌菌株是从孟加拉国 Munshiganj 不同地区的马铃薯倾倒地采集的土壤样本中分离出来的。在营养琼脂平板上进行亚培养后,获得了 31 个菌落,其中 9 个分离菌株在淀粉琼脂培养基上可产生淀粉酶。根据淀粉水解透明区比率,选出了其中的 2 个分离物(MC-04 和 MC-15)。MC-04 分离物的粗酶活为 2.82 IU/ml,特异酶活为 3.42 IU/mg;MC-15 分离物的粗酶活为 3.16 IU/ml,特异酶活为 3.77 IU/mg。随后,通过形态学、生化和分子特征鉴定,并通过 16S-rRNA 基因测序确认了最佳分离物 MC-15。经过 16S-rRNA 测序,该分离株(MC-15)被确定为枯草芽孢杆菌。在不同的培养期、pH 值、温度和不同碳源等条件下,对该菌株的淀粉酶产量也进行了优化。我们发现,最佳培养期为 48 小时,最佳 pH 值为 7.0,最佳温度为 40°C,2% 的淀粉被认为是最佳碳源。最后,通过硫酸铵沉淀、透析和单步凝胶过滤色谱法纯化了粗淀粉酶。纯化后的淀粉酶的酶活为 8.91 IU/ml,是原酶的 2.82 倍。实验证实,枯草芽孢杆菌可能是孟加拉国工业应用淀粉酶的良好来源。Dhaka Univ.22(2):147-154,2023 年(12 月)
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引用次数: 0
A Cross-sectional Study on Caffeine Dependency by Drinking Tea and Coffee Among Bangladeshi Students 孟加拉国学生喝茶和咖啡对咖啡因依赖的横断面研究
Pub Date : 2023-12-26 DOI: 10.3329/dujps.v22i2.69326
A. T. Munia, Saif Bin Salam Bondhon, Md Raihan Sarkar, Rabita Rahman, K. Sikdar, Md Abdus Samadd
Too much caffeine consumption might cause physical and mental dependency on the consumer. This study examined the socio-demographic factors, knowledge, behavior, and perception of Bangladeshi students about caffeine which is based on drinking tea and coffee.  This questionnaire-based study included 1020 respondents from primary level to postgraduate level students.  The analysis utilized frequencies, means, percentages, Pearson's chi-square (χ2) statistic and Spearman's rank correlation coefficients. Pearson's chi-square (χ2) statistic test was performed to determine the significance at 5% with a p-value < 0.05. Most of the students (94.8%) consume tea or coffee regularly, and 66.1% drink it daily. A total of 87.5% of students knew that tea and coffee have caffeine. Nearly two-thirds (67.1%) of the students were dependent on tea and coffee, and 35.9% experienced psycho-physiological alterations after a day without drinking those items. About 38% of students noticed side effects after consumption of tea or coffee multiple times in a day. This study also reveals that gender did not alter the knowledge or drinking behavior of tea and coffee. Tea and coffee drinking patterns were not significantly dependent upon the participants’ educational qualifications. Dhaka Univ. J. Pharm. Sci. 22(2): 202-212, 2023 (December)
摄入过多的咖啡因可能会导致消费者在身体和精神上产生依赖性。本研究调查了孟加拉国学生的社会人口因素、知识、行为和对咖啡因的看法,这些因素都以饮用茶和咖啡为基础。 这项基于问卷的研究包括 1020 名受访者,从小学生到研究生。 分析采用了频率、平均值、百分比、皮尔森卡方(χ2)统计和斯皮尔曼等级相关系数。Pearson's chi-square (χ2) 统计检验以 5%为显著性水平,P 值小于 0.05。大多数学生(94.8%)经常饮用茶或咖啡,66.1%的学生每天饮用。87.5%的学生知道茶和咖啡含有咖啡因。近三分之二(67.1%)的学生对茶和咖啡有依赖性,35.9%的学生在一天不喝茶和咖啡后会出现心理生理变化。约 38% 的学生在一天内多次饮用茶或咖啡后发现了副作用。这项研究还显示,性别并没有改变学生对茶和咖啡的认识或饮用行为。茶和咖啡的饮用方式与参与者的学历没有明显的关系。Dhaka Univ.22(2):202-212,2023 年(12 月)
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引用次数: 0
In vitro and In vivo Interaction of Ketorolac Tromethamine and Cefixime Trihydrate 酮咯酸氨丁三醇和三水头孢克肟的体外和体内相互作用
Pub Date : 2023-12-26 DOI: 10.3329/dujps.v22i2.67405
Mokaddas Flora, Rafat Tahsin, J. A. Chowdhury, Shaila Kabir, Md. Shah Amran, A. A. Chowdhury
Drug-drug interaction, a major impediment towards safe and effective pharmacotherapy, often leads to adverse outcome or therapeutic failure if not properly identified. The present study employed a number of in vitro and in vivo methods to conduct a thorough investigation of the interaction potential between ketorolac tromethamine (nonsteroidal anti-inflammatory drug) and cefixime trihydrate (beta-lactam antibiotic). UV-Visible spectrophotometry, FTIR and DSC were carried out to analyze the interaction of ketorolac and cefixime in vitro. UV-visible spectrophotometric study at different pH showed hyperchromic shift and blue shift (hypsochromic shift) in the mixture of the studied drugs compared to ketorolac alone. In contrast, only hyperchromic shift was found in the mixture when compared to cefixime alone. In DSC study, the melting endotherm of ketorolac tromethamine shifted from 169.62°C to 149.99°C in the 1:1 mixture. Again, the FTIR spectrum showed that in 1:1 mixture, the lactam (C=O) band of cefixime trihydrate shifted from 1771.68 cm-1 to 1718.63 cm-1, the amide carbonyl band (-CONH) moved from 1669.45 cm-1 to 1616.4 cm-1 and the -OH band moved from 3296.46 cm-1 to 3397.72 cm-1 which might be indicative of interaction between these two drugs. The in vivo study in rat model was designed to determine whether cefixime has any significant impact on the analgesic activity of ketorolac. In vitro  antimicrobial effect was also performed to evaluate the effect of ketorolac on cefixime. The findings from these study suggested that neither ketorolac nor cefixime imparted any deleterious impact on the biological property of each other which might indicate that co-administration of ketorolac and cefixime are therapeutically effective and safe. Dhaka Univ. J. Pharm. Sci. 22(2): 137-146, 2023 (December)
药物相互作用是实现安全有效药物治疗的主要障碍,如果不能正确识别,往往会导致不良后果或治疗失败。本研究采用了多种体外和体内方法,对酮咯酸氨丁三醇(非甾体抗炎药)和三水合头孢克肟(β-内酰胺类抗生素)之间的相互作用潜力进行了深入研究。采用紫外-可见分光光度法、傅立叶变换红外光谱法和 DSC 分析酮咯酸和头孢克肟在体外的相互作用。在不同 pH 值下进行的紫外-可见分光光度法研究显示,与单独的酮咯酸相比,所研究药物的混合物出现了高色移和蓝移(低色移)。相反,与单独的头孢克肟相比,混合物中只出现了高色移。在 DSC 研究中,在 1:1 的混合物中,酮咯酸氨丁三醇的熔化温度从 169.62°C 下降到 149.99°C。同样,傅立叶变换红外光谱显示,在 1:1 混合物中,头孢克肟三水合物的内酰胺(C=O)带从 1771.68 cm-1 移至 1718.63 cm-1,酰胺羰基带(-CONH)从 1669.45 cm-1 移至 1616.4 cm-1,-OH 带从 3296.46 cm-1 移至 3397.72 cm-1,这可能表明这两种药物之间存在相互作用。大鼠模型体内研究旨在确定头孢克肟对酮咯酸的镇痛活性是否有明显影响。此外,还进行了体外抗菌效果研究,以评估酮咯酸对头孢克肟的影响。这些研究结果表明,酮咯酸和头孢克肟都不会对彼此的生物特性产生任何有害影响,这可能表明酮咯酸和头孢克肟联合用药既有效又安全。达卡大学药学学报》(Dhaka Univ.22(2):137-146,2023 年(12 月)
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引用次数: 0
Isolation and Characterization of Alkaline Proteases Producing Indigenous Bacillus sp. as a Source of Thrombolytic and Fibrinolytic Agents 可作为血栓溶解剂和纤维蛋白溶解剂来源的产碱性蛋白酶本地芽孢杆菌的分离和特征描述
Pub Date : 2023-12-26 DOI: 10.3329/dujps.v22i2.67404
T. Akhtar, M. A. A. Sikder, Tania Yeasmin, Md Arafat Al Mamun, M. Hoq, Md Mustafizur Rahman, Md Rashedul Haque, Md Abdul Mazid
Fibrinolytic enzymes derived from bacteria can be effective as a potent, safe and cost-effective thrombolytic agent for the prevention and treatment of cardiovascular diseases. In this study, microorganisms were isolated from various soil samples and screened for their protease activity and protein concentration. Isolates with higher protease activity were subsequently tested for their thrombolytic and fibrinolytic activity. Of a total 37 isolates, 7 exhibited significant zone in SMA media (zone ratio above 1.3). Of these, 8 isolates showed increased protease activity with values ranging from 120 to 199 U/ml. The highest protease activity was observed for the isolate GST12 obtained from mung bean (green gram) soil. The freeze-dried concentrated crude enzymes were screened by in vitro clot lysis method. Six of these eight concentrated enzymes demonstrated clot lysis above 20%, whereas, enzymes from GST12 and GST21 exhibited the highest clot lysis activity (about 27%), which is comparable with standard drug streptokinase. These two enzymes are also strongly associated with fibrinolytic activity. Our findings identify 8 isolates having potential thrombolytic and fibrinolytic activities that belong to Gram-positive Bacillus. Dhaka Univ. J. Pharm. Sci. 22(2): 125-135, 2023 (December)
从细菌中提取的纤溶酶可作为一种有效、安全和经济的溶栓剂,用于预防和治疗心血管疾病。本研究从各种土壤样本中分离出微生物,并对其蛋白酶活性和蛋白质浓度进行筛选。随后,对蛋白酶活性较高的分离物进行了血栓溶解和纤维蛋白溶解活性测试。在总共 37 个分离菌株中,有 7 个在 SMA 培养基中显示出明显的区域(区域比高于 1.3)。其中,8 个分离菌株的蛋白酶活性有所提高,数值从 120 U/ml 到 199 U/ml 不等。从绿豆(青稞)土壤中分离出的 GST12 蛋白酶活性最高。用体外凝块裂解法对冷冻干燥的浓缩粗酶进行了筛选。在这八种浓缩酶中,有六种的血块裂解率超过 20%,而 GST12 和 GST21 的酶表现出最高的血块裂解活性(约 27%),与标准药物链激酶相当。这两种酶也与纤维蛋白溶解活性密切相关。我们的研究结果确定了 8 种具有潜在血栓溶解和纤维蛋白溶解活性的分离物,它们都属于革兰氏阳性芽孢杆菌。Dhaka Univ.22(2):125-135,2023 年(12 月)
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引用次数: 0
A New Annulenol from Aconitum heterophyllum with Bioactivity and Cytotoxicity against Vero and Lung Cell Line 一种新的异叶乌头环烯醇对Vero和肺细胞具有生物活性和细胞毒性
Pub Date : 2023-06-24 DOI: 10.3329/dujps.v22i1.64141
Md. Saiful Alam, S. Rony, F. Afroz, Abdullah Al Mansur, S. Sharmin, F. Moni, S. Akhter, M. M. Hussain, M. Sohrab
In this research work, a detailed phytochemical and biological investigation of Aconitum heterophyllum was accomplished. The cold methanolic root extract of A. heterophyllum was subjected to VLC for fractionation over silica gel, which led to the isolation of two compounds 1,1,8,8-trimethyl-4-methylene-decahydro- 1H-cyclopenta-[8]-annulen-1-ol (1) and β-stigmasterol (2). The compounds were characterized by analysis of their 1D and 2D NMR spectral data. Compound 1 is first reported from this plant. The crude extract was screened for antimicrobial activity against several gram-positive and gram-negative bacteria, and fungi using disk diffusion method where significant inhibitory activity was observed. The extract was also tested for cytotoxic property using brine shrimp lethality bioassay, which revealed moderate activity in comparison with the standard anticancer drug, vincristine sulphate. Antioxidant property of the crude methanol extract of A. heterophyllum was determined by the scavenging of the DPPH (2,2-diphenyl-1-picrylhydrazyl) free radical and found moderate antioxidant activity (IC50 = 53.25 μg/mL) when compared to standard antioxidant. Total phenolic and flavonoid content and polyphenolic compound content of the crude extract were determined by HPLC. The isolated compounds 1 and 2 showed dosedependent antiproliferation activity against the vero and lung A549 cells.Dhaka Univ. J. Pharm. Sci. 22(1): 1-10, 2023 (June)
本文对乌头进行了较为详细的植物化学和生物学研究。利用凝胶层析液相色谱(VLC)分离得到2个化合物1,1,8,8-三甲基-4-亚甲基-十氢- 1h -环戊-[8]-环烯-1-醇(1)和β-豆甾醇(2)。通过1D和2D NMR数据对化合物进行了表征。化合物1为首次从该植物中分离得到。采用圆盘扩散法筛选粗提物对几种革兰氏阳性和革兰氏阴性细菌和真菌的抑菌活性,观察到明显的抑菌活性。该提取物还使用盐水虾致死性生物测定法进行了细胞毒性测试,与标准抗癌药物硫酸长春新碱相比,其活性中等。通过对DPPH(2,2-二苯基-1-苦味基肼基)自由基的清除作用测定了其抗氧化性能,与标准抗氧化剂相比,其抗氧化活性中等(IC50 = 53.25 μg/mL)。采用高效液相色谱法测定粗提物中总酚、类黄酮含量和多酚类化合物含量。分离得到的化合物1和2对肺A549细胞具有剂量依赖性的抗增殖活性。达卡大学药学院。自然科学22(1):1- 10,2023 (6)
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引用次数: 0
Biological Investigations of Three Marine Algae Enteromorpha intestinalis, Rhizoclonium riparium and Ceratophyllum demersum Collected from the Bay of Bengal 孟加拉湾三种海藻的生物学研究:肠Enteromorpha enterinalis, Rhizoclonium riparium和Ceratophyllum demersum
Pub Date : 2023-06-24 DOI: 10.3329/dujps.v22i1.67098
Md Hanif Biswas, Nasiba Binte Bahar, N. Sharmin, Shiekh Zahir Raihan, S. Halder, Mir Shariful Islam, M. A. Muhit
The ocean consists of versatile domain of lives which can be exploited for human health benefits because of diversified secondary metabolites. Seaweeds, generally called macroalgae, are commonly found in the coastal region of the Bay of Bengal. But none of them were investigated properly for their biological activities. Hence, this study was performed to investigate the antioxidant, antimicrobial, cytotoxic and membrane stabilizing activities along with total phenolic content of the crude methanolic extract of three seaweeds namely, Enteromorpha intestinalis, Rhizoclonium riparium and Ceratophyllum demersum using standard protocols. Among the methanolic extracts of three seaweeds, C. demersum (52.09 ± 1.30 mg of GAE) was found to have the highest phenolic content, followed by E. intestinalis (35.98 ± 1.27 mg of GAE) and then R. riparium (29.94 ± 0.54 mg of GAE). The extractives of these seaweeds also showed promising antioxidant and membrane stabilizing properties compared to the standard. E. intestinalis extract displayed greater reducing power with increasing concentration (EC50 value 7.70 ± 0.27 μg/ml). The same seaweed E. intestinalis was found to have significant free radical (DPPH) scavenging potential (IC50 value 23.46 ± 0.54 μg/ml) compared to the reference standard ascorbic acid (IC50 value 5.76 ±0.13 μg/ml). However, the findings of antimicrobial activity test demonstrated mild antibacterial effects of these seaweeds against Escherichia coli and Aspergillus niger and none of these seaweeds exhibited cytotoxicity when tested against HeLa cell line. These findings will aid in future studies attempting to explore medicinal and therapeutic agents from these readily available seaweeds of Bangladesh. Dhaka Univ. J. Pharm. Sci. 22(1): 81-87, 2023 (June)
海洋由多种多样的生命领域组成,由于次生代谢物的多样性,可以为人类健康利益而加以利用。海藻,通常被称为大型藻类,常见于孟加拉湾的沿海地区。但它们的生物活性都没有得到适当的研究。因此,本研究采用标准方案对肠Enteromorpha ninteinalis、riparium rhizzoclonium riparium和Ceratophyllum demersum三种海藻粗甲醇提取物的抗氧化、抗菌、细胞毒和膜稳定活性以及总酚含量进行了研究。3种海藻的甲醇提取物中,金貂草(52.09±1.30 mg)的酚类含量最高,其次是肠棘草(35.98±1.27 mg),最后是河滨草(29.94±0.54 mg)。与标准品相比,这些海藻提取物也显示出良好的抗氧化和膜稳定性能。随着浓度的增加,肠菊提取物的还原力更强(EC50值为7.70±0.27 μg/ml)。与抗坏血酸的IC50值(5.76±0.13 μg/ml)相比,同一种海藻对DPPH的清除能力(IC50值为23.46±0.54 μg/ml)显著提高。然而,抑菌活性试验结果表明,这些海藻对大肠杆菌和黑曲霉有轻微的抑菌作用,对HeLa细胞株没有细胞毒性。这些发现将有助于未来试图从孟加拉国这些现成的海藻中探索药物和治疗剂的研究。达卡大学药学院。自然科学22(1):81- 87,2023 (6)
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Dhaka University Journal of Pharmaceutical Sciences
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