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Antibacterial Potential of Aqueous Extracts and Compounds from Selected Brown Seaweeds 某些褐藻的水提取物和化合物的抗菌潜力
Pub Date : 2019-09-24 DOI: 10.26689/itps.v2i1.804
Sujitra Raj Genga Raj, Chean Hui Ng, S. Mohd-Said, Kent Yu
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引用次数: 3
Approaches in Theranostics and Pharmacological Sciences 治疗学和药理学方法
Pub Date : 2019-09-24 DOI: 10.26689/itps.v2i1.883
S. Gopinath
It is our pleasure to release the second issue (Volume 2, Issue 1) of INNOSC Theranostics and Pharmacological Sciences. In line with the journal’s primary scope – “therapeutic and diagnosis,” this issue published articles pertaining to the major aspects such as therapeutics, medical diagnosis, medicinal chemistry, drug metabolism and transport, nanomedicine, translational medicine, and molecular and cellular pharmacology. This issue has five original articles and one review article that was submitted by authors from different countries of origin. One of the research articles entitled “Formulation Development and in vitro Characterization of Zolmitriptan Controlled Release Drug Delivery Systems” by Pandala et al., made an effort in developing the extended-release of zolmitriptan matrix to treat migraine [1]. Authors used the formulations from natural polymers/gums and have shown a promising delivery system which can enhance the bioavailability and has potential for greater therapeutic efficacy. The second article by Katagi et al. worked on “Schiff Base Oxime Derivatives Reactivate Chlorpyrifos-induced Acetylcholinesterase Inhibition” [2]. This study is primarily aimed at synthesizing a series of Schiff base oximes and assessing the in vitro reactivating potency against chlorpyrifosinhibited acetylcholinesterase. Based on the study, authors concluded that compounds with chloroand nitro-substitution on the 4th position yielded a better activity against chlorpyrifosinhibited acetylcholinesterase. In addition, the above Schiff base oximes are claimed to be promising, because of their sufficient reactivation strength at lower concentration. The third article was authored by Razalli et al. on “Antimicrobial Potential of Andrographis paniculata Conjugated Gold Nanoparticle” which delineates the carrier potential of gold nanoparticle [3]. To demonstrate their notion, the herbal extracts were capped on the gold nanoparticle and tested against the bacterial strains. The nanoparticle used in this study was characterized morphologically, chemically, and biologically. Authors demonstrated the inhibition potential of desired plant extracts and their higher antimicrobial activity mediated by the gold nanoparticle conjugation. Regarding the fourth article, Teh et al. have studied on “Toxicity Effect of Bougainvillea glabra (Paper Flower) Water Extracts on Zebrafish Embryo” [4]. This article assessed the acute toxicity and the potential teratogenic activity of water extracts of B. glabra bracts on zebrafish embryos. The researchers participated in this work concluded that the water extracts derived from the pink, purple, and dark pink bracts of B. glabra have mild toxicity toward embryo, a model for studies in pharmacology in the future. The next article under the technical aspect is on “Antibacterial Potential of Aqueous Extracts and Compounds from Selected Brown Seaweeds” by Genga Raj et al., in which authors took a great effort to demonstrate the antimicrobial
我们很高兴出版《INNOSC治疗学与药理科学》第二期(第2卷第1期)。根据该杂志的主要范围-“治疗和诊断”,这一期发表的文章涉及治疗学,医学诊断,药物化学,药物代谢和运输,纳米医学,转化医学以及分子和细胞药理学等主要方面。本期有来自不同国家的作者提交的5篇原创文章和1篇综述文章。Pandala等人在《佐米曲坦控释给药系统的配方开发及体外表征》一文中,对佐米曲坦基质缓释治疗偏头痛进行了研究[1]。作者使用天然聚合物/树胶的配方,并展示了一种有希望的递送系统,可以提高生物利用度,具有更大的治疗效果。Katagi等人的第二篇文章“希夫碱肟衍生物重新激活毒死蜱诱导的乙酰胆碱酯酶抑制”[2]。本研究主要目的是合成一系列希夫碱肟,并评估其体外对毒死蜱抑制的乙酰胆碱酯酶的再激活能力。在此基础上,作者得出结论,氯代和硝基取代4位的化合物对氯吡虫啉抑制的乙酰胆碱酯酶具有较好的活性。此外,由于上述希夫碱肟在较低浓度下具有足够的再活化强度,因此被认为是有前途的。第三篇文章由Razalli等人撰写,题为“穿心莲共轭金纳米粒子的抗菌潜力”,描述了金纳米粒子的载体潜力[3]。为了证明他们的观点,草药提取物被盖在金纳米颗粒上,并对细菌菌株进行了测试。本研究中使用的纳米颗粒在形态、化学和生物学上进行了表征。作者证明了金纳米粒子偶联介导的植物提取物的抑制潜力及其较高的抗菌活性。第四篇文章,Teh等人研究了“三角梅(纸花)水提取物对斑马鱼胚胎的毒性作用”[4]。本文研究了光斑草苞片水提取物对斑马鱼胚胎的急性毒性和潜在致畸活性。参与本研究的研究人员得出结论,从紫、粉色和深粉色的光苞叶中提取的水提取物对胚胎有轻微的毒性,为今后的药理学研究提供了一个模型。技术方面的下一篇文章是Genga Raj等人的“精选褐藻水萃取物和化合物的抗菌潜力”,作者花了很大的精力证明了褐藻水萃取物的抗菌活性[5]。本刊唯一的一篇综述文章由Enjamoori等人撰写,阐述了用于植物药理学研究的沙芦综述[6]。作者收集了植物医学的重要性,特别关注植物化学和药理学方面。有了这些,我们编制了第二期的文章,围绕着期刊的主要目标和范围,在接下来的几期中将有更多关于这个主题的文章。
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引用次数: 1
Toxicity Effect of Bougainvillea glabra (Paper Flower) Water Extracts on Zebrafish Embryo 九重葛(纸花)水提取物对斑马鱼胚胎的毒性效应
Pub Date : 2019-07-31 DOI: 10.26689/itps.v2i1.780
Lu E Teh, C. S. Kue, Chean Hui Ng, B. F. Lau
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引用次数: 5
Antimicrobial Potential of Andrographis paniculata Conjugated Gold Nanoparticle 穿心莲共轭金纳米颗粒的抗菌潜力
Pub Date : 2019-07-17 DOI: 10.26689/itps.v2i1.744
N. Razalli, S. Gopinath, F. Kasim, Ahmad Radi Wan Yaakub, P. Anbu
Background: Herbal extracts have been traditionally used as antibacterial agents, and different strategies have been proposed to enhance their antimicrobial activities. This research aimed to assess the antimicrobial potential of Andrographis paniculata conjugated gold nanoparticle (GNP) compounds against Escherichia coli and Bacillus subtilis.Methods: Herbal extract was conjugated with GNP through electrostatic interaction, and characterization was carried out by Fourier-transmission infrared spectroscopy, screening electron microscopy, and transmission electron microscopy and supported by energy-dispersive X-ray spectroscopy. Antibacterial activity of the herbal extract and GNP conjugation was evaluated by disc diffusion assay.Results: Chemical and morphological characterizations of the GNP and herbal extract conjugate revealed intactness of the GNP. In disc diffusion assay, the inhibition zone formed by these compounds was measured for both microorganisms, and they were in the range of 0.6-0.9 cm for the herbal extract. When the herbal extract conjugated with GNP, the zone was between 0.8 and 1.1 cm.Conclusion: This study demonstrated the potentiality of GNP to carry the antibacterial compounds from the herbal extract.
背景:传统上,草药提取物一直被用作抗菌药物,人们提出了不同的策略来提高其抗菌活性。本研究旨在评价穿心莲偶联金纳米颗粒(GNP)化合物对大肠杆菌和枯草芽孢杆菌的抑菌潜力。方法:通过静电相互作用将中药提取物与GNP偶联,采用傅里叶红外光谱、筛选电镜和透射电镜对其进行表征,并采用能量色散x射线光谱进行表征。采用圆盘扩散法对中药提取物和GNP偶联物进行抑菌活性评价。结果:GNP和草药提取物偶联物的化学和形态特征显示GNP的完整性。在圆盘扩散法中,测定了这些化合物对两种微生物形成的抑制带,对草药提取物的抑制带在0.6 ~ 0.9 cm范围内。当与GNP偶联时,该区域在0.8 ~ 1.1 cm之间。结论:本研究证明了国产GNP具有携带中药提取物中抗菌化合物的潜力。
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引用次数: 2
Schiff Base Oxime Derivatives Reactivate Chlorpyrifos-induced Acetylcholinesterase Inhibition 希夫碱肟衍生物重新激活毒死蜱诱导的乙酰胆碱酯酶抑制
Pub Date : 2019-07-02 DOI: 10.26689/itps.v2i1.499
M. Katagi, Jennifer Fernandes, Shivalingrao MamleDesai, M. Sujatha, A. Rekha, Girish Bolakatti
Background: The biological effects of organophosphorus (OP) compounds are connected with the irreversible inhibition of acetylcholinesterase (AChE), an important neuromediator acetylcholine (ACh) splitting enzyme in the human body at the synaptic clefts. Due to this inhibition, AChE is unable to fulfil its physiological function resulting in the accumulation of ACh, which, in turn over stimulates the parasympathetic nerve receptors, and causes fatal cholinergic crisis. Objective: The objective of the study was to synthesize a series of Schiff base oximes and to assess their evaluating for their in vitro reactivating potency against chlorpyrifos inhibited AChE. Methods: The amino group of 4-amino acetophenone exploited by treating with substituted benzaldehyde in the presence of glacial acetic acid to form Schiff base (1a-1f). The titled compounds (2a-2f) were prepared by treating Schiff base with hydroxylamine hydrochloride in the presence of alcohol. Through structural and spectral analysis, the structure of compounds was confirmed. The synthesized compounds were evaluated for their reactivation efficacy against chlorpyrifos-inhibited rat brain AChE by Ellman's method. Results: The pralidoxime (2-PAM) was potent reactivation against chlorpyrifos-inhibited AChE at the concentration tested (0.001 M). In this case, the compounds 2a (40.4%, 60 min) and 2d (37.9%, 60 min) showed promising reactivation as compared to 2-PAM (40.6%, 60min) against chlorpyrifos-inhibited AChE. Conclusion: Compounds having chloro (2a) and nitro (2d) substitution on 4th position gave good activity against chlorpyrifos-inhibited AChE. Moreover, these Schiff base oximes seem to be very promising because of their sufficient reactivation strength at lower concentration (10-3 M).
背景:有机磷化合物的生物学效应与乙酰胆碱酯酶(AChE)在突触间隙处的不可逆抑制有关。AChE是人体重要的乙酰胆碱分裂酶的神经介质。由于这种抑制作用,乙酰胆碱能无法发挥其生理功能,导致乙酰胆碱能积累,进而刺激副交感神经受体,引起致命的胆碱能危象。目的:合成一系列希夫碱肟,并评价其对毒死蜱抑制乙酰胆碱酯酶活性的体外再激活能力。方法:在冰醋酸存在下,用取代苯甲醛处理4-氨基苯乙酮的氨基,形成希夫碱(1a-1f)。在醇的存在下,用盐酸羟胺处理希夫碱制备了标题化合物(2a-2f)。通过结构和光谱分析,确定了化合物的结构。采用Ellman法评价合成的化合物对毒死蜱抑制大鼠脑乙酰胆碱酯酶的再激活作用。结果:普拉多肟(2-PAM)在浓度为0.001 M时对毒死蜱抑制的乙酰胆碱酯(AChE)具有较强的活性,其中化合物2a (40.4%, 60min)和2d (37.9%, 60min)对毒死蜱抑制的乙酰胆碱酯(AChE)具有较强的活性。结论:含有氯(2a)和硝基(2d)取代4位的化合物对毒死蜱抑制的乙酰胆碱酯酶具有良好的活性。此外,由于这些希夫碱肟在较低浓度(10-3 M)下具有足够的再活化强度,因此看起来非常有前景。
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引用次数: 1
Formulation Development and In Vitro Characterization of Zolmitriptan Controlled Release Drug Delivery Systems 佐米曲坦控释给药系统的配方开发及体外表征
Pub Date : 2019-03-11 DOI: 10.26689/ITPS.V2I1.550
Shambhavi Pandala, V. Bakshi, R. Jadi
Background: Zolmitriptan is an artificial tryptamine, employed for the acute cure of migraine attack with or exclusive of aura and cluster headaches. Objective: It is an attempt to develop the extended release (ER) of Zolmitriptan matrix (ZMT) tablets to treat migraine safely and effectively. Methods: All formulations were prepared with natural polymers or gums like guar gum, xanthan gum, karaya gum through direct compression method using 6mm punch. Results: Powder blend of all formulations (F1 - F12) using different ratios of the above mentioned gums (5%, 10%, 15% and 20%) were characterized with pre-compression parameters (angle of repose, bulk density, tapped density, compressibility index, hausner ratio, compatibility studies) and post-compression parameters (weight variation, thickness, friability, hardness, assay, in vitro dissolution studies). F1 - F4 formulations were prepared with gum karaya and compared with remaining gums; gum karaya shows more retardance capacity. F9 - F12 (with guar gum) formulations were unable to produce the desired release, whereas F5 - F8 formulations containing with xanthan gum exhibited more retarding effect with increasing concentration of polymer. Conclusion: All prepared formulations (F1 - F12) were characterized and F3 formulation was optimized (97.3% drug released in 8 hours). All prepared formulations (F1 - F12) showed good flow properties and release patterns. Hence, formulations of ZMT matrix tablets have a promising delivery system which will enhance bio-availability and achieve greater therapeutic efficacy.
背景:佐米曲坦是一种人工色胺,用于急性治疗伴有或不伴有先兆和丛集性头痛的偏头痛发作。目的:研制安全有效治疗偏头痛的佐米曲坦基质缓释片(ZMT)。方法:采用天然聚合物或瓜尔胶、黄原胶、卡拉亚胶等胶,采用6mm冲孔直接加压法制备。结果:采用不同比例(5%、10%、15%和20%)的配方(F1 - F12)的粉末共混物进行了预压缩参数(休歇角、容重、攻丝密度、压缩指数、豪斯纳比、相容性研究)和压缩后参数(重量变化、厚度、脆度、硬度、含量、体外溶出度研究)的表征。用卡拉亚胶制备F1 - F4配方,并与剩余胶进行比较;Gum karaya表现出更强的迟滞能力。加瓜尔胶的F9 ~ F12不能达到理想的缓释效果,而加黄原胶的F5 ~ F8随着聚合物浓度的增加表现出较好的缓释效果。结论:对制备的配方(F1 - F12)进行了表征,并对F3配方进行了优化(8 h释药97.3%)。所有制备的配方(F1 - F12)均表现出良好的流动性能和释放模式。因此,ZMT基质片的制剂具有很好的给药系统,可以提高生物利用度,获得更大的治疗效果。
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引用次数: 3
A Review on Leucas aspera for Phytopharmacological Studies 关于天南星植物药理研究的综述
Pub Date : 2018-12-26 DOI: 10.26689/ITPS.V2I1.436
Vijay Kumar Enjamoori, Avinash Nampalli, B. Vasudha, Kiran Gangarapu, Narender Boggula
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引用次数: 5
A Foreword from the Editor 编辑的前言
Pub Date : 2018-12-11 DOI: 10.26689/ITPS.V1I1.512
S. Gopinath
Human health poses severe problems caused by various factors; which includes disease-causing agents that have been raised due to the emergence and re-emergence of diseases.  In the past, different classes of diseases were reported and they are infectious, non-infectious and contagious created a threat to the public health and economy.   To overcome these hurdles, theranostics, a fast-growing discipline has become a tool with the advancements of therapeutics and medical diagnosis. Achievement with theranostics was driven by different input from various angles of medical researches. These approaches were attested with the novel creations of a complete platform for the clinic analysis and therapy. Eventually, the involvement of all levels of stakeholders and their acquired knowledge sharing were expanded to the theranostics approaches.  On the other hand, Pharmacological sciences generate the remedies to a wide range of diseases with the demonstration of different pharmacological products.  This discipline delineates the mode of drug action, including natural and man-made compounds that show the influence on the human tissues and organs.
各种因素对人类健康造成严重问题;其中包括由于疾病的出现和再次出现而增加的致病物质。在过去,报告了不同类别的疾病,它们有传染性、非传染性和传染性,对公共卫生和经济构成威胁。为了克服这些障碍,随着治疗学和医学诊断的进步,治疗学这一快速发展的学科已经成为一种工具。治疗学的成就是由不同医学研究角度的不同投入推动的。这些方法被证明与一个完整的平台的临床分析和治疗的新创造。最终,各级利益相关者的参与和他们所获得的知识共享扩展到治疗学方法。另一方面,药理学产生的补救措施,以广泛的疾病与不同的药理产品的示范。这门学科描述了药物作用的模式,包括对人体组织和器官有影响的天然和人造化合物。
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引用次数: 0
Review on Chronic Exposure of Acrylamide Causes a Neurotoxicity Risk 慢性接触丙烯酰胺导致神经毒性风险的研究进展
Pub Date : 2018-12-11 DOI: 10.26689/ITPS.V1I1.416
N. Maddu, S. F. Begum
The exposure and inhalation of acrylamide (ACR) are not safe to the human health leading to the potential neurotoxicity. ACR is widely used in biochemical techniques and highly occurs in processing foods such as potato chips prepared at high temperatures. ACR is formed from reducing sugars and asparagine through the Maillard reaction. It exerts various harmful and toxic effects such as neurotoxicity both in humans and animal studies. The extensive damage of synaptic proteins, the formation of ACR-DNA adducts, degeneration of motor neurons, neurofilament reduction, are the most common neurological symptoms. The main metabolite of ACR metabolism is glycidamide, and it causes harmful effects as same as ACR. The main purpose of this study is to analyze the neurotoxic effects of ACR on various regions of the brain and its different mechanistic pathways that are involved in ACR neurotoxicity. The consumption of ACR-containing foods and its exposure are reduced by the human, leading to the reduction of toxic effects associated with ACR.
丙烯酰胺(ACR)暴露和吸入对人体健康不安全,可导致潜在的神经毒性。ACR在生物化学技术中有广泛的应用,在诸如薯片等高温食品的加工中也经常发生。ACR是由还原糖和天冬酰胺通过美拉德反应形成的。在人类和动物研究中,它具有各种有害和毒性作用,如神经毒性。突触蛋白的广泛损伤、ACR-DNA加合物的形成、运动神经元变性、神经丝减少是最常见的神经症状。ACR代谢的主要代谢物是甘油酰胺,其危害性与ACR相同。本研究的主要目的是分析ACR对大脑各区域的神经毒性作用及其参与ACR神经毒性的不同机制途径。人类减少了对含ACR的食物的摄入和接触,从而减少了与ACR相关的毒性作用。
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引用次数: 5
Aptamer: A Versatile Probe in Medical Diagnosis 多聚物:医学诊断中的多功能探针
Pub Date : 2018-12-06 DOI: 10.26689/ITPS.V1I1.511
T. LakshmiPriya, S. Gopinath
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引用次数: 3
期刊
INNOSC Theranostics and Pharmacological Sciences
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