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Formulation of nano spray preparation from Purslane Leaf Extract (Portulaca oleracea l.) as sunscreen 马齿苋叶提取物纳米喷雾制剂作为防晒剂的配方
Pub Date : 2024-02-29 DOI: 10.55522/jmpas.v13i1.5890
Elmiawati Latifah
Purslane plant (Portulaca oleracea L.) is a type of wild plant that grows abundantly, but its benefits are rarely known. Purslane contains saponins, which have high antioxidant and biological activity. Skin that is sensitive to sun exposure is the issue this nanospray is targeting. The aim of this research is to determine the optimal formulation of herbal nanospray products with Purslane sunscreen to treat skin problems caused by sun exposure. The research method used was an experimental method with research stages starting from plant determination, extract making, nanospray formulation determination, preparation evaluation, in vivo UV protection activity test, and in vitro SPF test. Quantitative descriptive analysis was carried out using Microsoft Excel and SPSS Version 24. There were significant differences in erythema (lesions on the skin) between the 4 treatment groups, with significant differences in the negative control and positive control groups, as well as the group given dose treatment (the amount of extract in the nanoparticles) of 0.8 g and 0.4 g of purslane extract with the negative control. So, it can be concluded that doses of 0.8 g (SPF value: 9.9) and 0.4 g (SPF value: 8.43) of purslane extract have the potential to be sunscreens with maximum category and extra protective power. Purslane extract nanospray sunscreen has the advantage of being made from herbal ingredients, which have less potential for irritation than chemical sunscreen products.
马齿苋(Portulaca oleracea L.)是一种生长茂盛的野生植物,但其功效却鲜为人知。马齿苋含有皂甙,具有很高的抗氧化性和生物活性。对阳光照射敏感的皮肤正是这种纳米喷雾剂所针对的问题。本研究的目的是确定含有马齿苋防晒剂的中草药纳米喷雾产品的最佳配方,以治疗日晒引起的皮肤问题。采用的研究方法是实验法,研究阶段从植物确定、提取物制作、纳米喷雾配方确定、制剂评估、体内紫外线防护活性测试和体外 SPF 测试开始。使用 Microsoft Excel 和 SPSS Version 24 进行了定量描述性分析。4 个处理组之间的红斑(皮肤上的病变)存在明显差异,阴性对照组和阳性对照组以及给予 0.8 克和 0.4 克马齿苋提取物剂量处理(纳米颗粒中的提取物量)的组与阴性对照组之间存在明显差异。因此,可以得出结论,0.8 克(SPF 值:9.9)和 0.4 克(SPF 值:8.43)的马齿苋提取物有可能成为具有最大类别和额外保护能力的防晒剂。马齿苋提取物纳米喷雾防晒剂的优点是由草本成分制成,与化学防晒产品相比,刺激性较小。
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引用次数: 0
Assessing the toxicity and anti-anemia of Beta Vulgaris L.: in silico, phytochemical and antioxidant analysis 评估黄花菜的毒性和抗贫血性:硅学、植物化学和抗氧化分析
Pub Date : 2024-02-29 DOI: 10.55522/jmpas.v13i1.5882
S. E. Nugraha
The objective of this investigation was to determine the toxicity, anti-anemia activity, betanin content, flavonoid content, and antioxidant capacity of Beta vulgaris L. Microwave-assisted extraction (MAE) was implemented to optimize the extraction procedure. The total phenolic content (TPC) and total flavonoid content (TFC) of the extracts were determined using the Folin-Ciocalteu colorimetric and aluminum chloride methods, respectively. Furthermore, the 2,2-diphenyl-1-picrylhydrazyl (DPPH) method was employed to ascertain antioxidant capacity, whereas thin-layer chromatography was used to identify betanin content. The toxicity and anti-anemia properties were assessed in silico. The in-silico methods encompass several steps: ligand and target protein synthesis, docking of betanin compounds with the erythropoietin receptor (EpoR) target protein via SwissDock, docking data visualization via USCF Chimera, and toxicity analysis via the pkCSM and Protox online tools. The findings indicated that the beetroot extract contained a total of 34.96 ± 3.97 mg GAE/g sample of phenol. The flavonoid content of beetroot was 4.93 ± 0.33 mg QE/g sample. Qualitative analysis conducted using thin-layer chromatography yielded results indicating the presence of betanin in the extract. The IC50 value for the antioxidant activity was 97.31 μg/ml. The docking study revealed the effective interaction of betanin with several amino acid residues, suggesting a low toxicity potential, supported by toxicity class 4 and an LD50 of 305 mg/kg, and the absence of liver and Ames toxicity. It concluded that betanin is a promising anti-anemia agent. levels.
微波辅助萃取(MAE)优化了萃取过程。采用 Folin-Ciocalteu 比色法和氯化铝法分别测定了提取物中的总酚含量(TPC)和总黄酮含量(TFC)。此外,还采用了 2,2-二苯基-1-苦基肼(DPPH)法来确定抗氧化能力,而薄层色谱法则用来鉴定甜菜宁的含量。对毒性和抗贫血特性进行了硅学评估。硅学方法包括几个步骤:配体和靶蛋白合成、通过 SwissDock 将甜菜苷化合物与促红细胞生成素受体(EpoR)靶蛋白对接、通过 USCF Chimera 将对接数据可视化,以及通过 pkCSM 和 Protox 在线工具进行毒性分析。研究结果表明,甜菜根提取物中总共含有 34.96 ± 3.97 毫克 GAE/克样品酚。甜菜根的类黄酮含量为 4.93 ± 0.33 mg QE/g。使用薄层色谱法进行的定性分析结果表明,提取物中含有甜菜苷。抗氧化活性的 IC50 值为 97.31 μg/ml。对接研究显示,甜菜苷与几个氨基酸残基有效地相互作用,毒性等级为 4 级,半数致死剂量为 305 毫克/千克,没有肝脏和阿姆斯毒性,这表明甜菜苷具有低毒性。研究得出结论,白桦脂素是一种很有前途的抗贫血药物。
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引用次数: 0
In-silico studies and docking of n-substituted isoindoline-1, 3-dioine analogues as anti-proliferative agents 作为抗增殖剂的正代异吲哚啉-1, 3-二环类似物的分子内研究和对接
Pub Date : 2024-02-29 DOI: 10.55522/jmpas.v13i1.4651
Shailendra Saraf
Recently,isoindoline-1,3-dione compounds based folpet, phosmet, captonand thalidomide were developed because they have a comparable degree of anti-proliferative efficacy owing to their diverse mechanisms such as HDAC inhibitors, tryptase inhibitors, inhibits the mode of tnf-α, and angiogenesis inhibitors. It was investigated how the phthalimide pharmacophore interacted with molecules such tnf-α, HDAC, VEGF, EGF, and Tyrosine Kinase Angiogenesis. In order to assess the inhibitory activity against enzyme assay, a series of phthalimidepharmacophores with various substituent’s (Schiff's base) at the N-phenyl ring were submitted to protein-ligand docking investigations using the lib-dock method in the current work. All of the compounds' chemical structures were designed using Cambridge software, ChemBioOffice Ultra 12.0, and their molecular characteristics were determined using the online molecular modelling tool Molinspiration. Utilizing the Discovery Studio Client version 4.1, ADMETlab 2.0, and Lazar 1.4.2 softwares, ADME, Toxicity, and Molecular Docking investigations using the lib-dock method were carried out to evaluate the binding mode and interactions of synthetic hits at the binding site of receptors. Docking studies demonstrated that these sorts of ligands interacted mostly with TNF-α, HDAC, VEGF, EGF, Tyrosine kinase, and angiogenesis reports, among others, by forming hydrogen bonds and interacting hydrophobically with the domain. Our docking results indicate that compounds A1, A10, A11, A22, A26, and A28 demonstrated the greatest binding affinity with the corresponding proteins based on the predicted binding energy. These computer simulations have shown that phthalimide compounds with N-phenyl rings replaced can effectively suppress enzymatic assay.
近来,以氟派特、酞酰亚胺、卡普顿和沙利度胺为基础的异吲哚啉-1,3-二酮化合物被开发出来,因为它们具有不同的机制,如 HDAC 抑制剂、胰蛋白酶抑制剂、tnf-α 抑制剂和血管生成抑制剂,因而具有相当程度的抗增殖功效。研究人员对邻苯二甲酰亚胺的药理结构与 tnf-α、HDAC、血管内皮生长因子、表皮生长因子和酪氨酸激酶血管生成等分子之间的相互作用进行了研究。为了评估酞酰亚胺类药物对酶的抑制活性,本研究采用 lib-dock 方法对一系列在 N-苯基环上具有不同取代基(希夫碱)的酞酰亚胺类药物进行了蛋白质配体对接研究。所有化合物的化学结构都是用剑桥软件 ChemBioOffice Ultra 12.0 设计的,其分子特征则是用在线分子建模工具 Molinspiration 确定的。利用 Discovery Studio Client 4.1 版、ADMETlab 2.0 和 Lazar 1.4.2 软件,采用 lib-dock 方法进行了 ADME、毒性和分子对接研究,以评估合成药物在受体结合部位的结合模式和相互作用。Docking 研究表明,这些配体主要与 TNF-α、HDAC、VEGF、EGF、酪氨酸激酶和血管生成报告等相互作用,形成氢键并与结构域发生疏水作用。我们的对接结果表明,根据预测的结合能,化合物 A1、A10、A11、A22、A26 和 A28 与相应蛋白质的结合亲和力最大。这些计算机模拟结果表明,替换了 N-苯基环的邻苯二甲酰亚胺化合物可以有效抑制酶测定。
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引用次数: 0
Decoding the aging nexus: unravelling genetic networks and pharmacological strategies for lifespan extension and the methuselah paradox 解码衰老关系:揭示延长寿命的基因网络和药理学策略以及甲苏拉悖论
Pub Date : 2024-02-29 DOI: 10.55522/jmpas.v13i1.6243
Anamitra Goswami
We are all interested in knowing- whether genes and drugs can increase our life-span. As per Bible, Methuselah's lifespan lasted for a total of 969 years. Recent research has identified the Methuselah gene, a specific DNA segment that holds the potential to promote robust and healthy aging. This discovery opens new avenues for the development of pharmaceutical interventions aimed at extending human lifespan. Aging, a complex process influenced by natural selection, has evolved over time, adapting to factors such as cellular senescence and genetic instability. Research on aging has extensively employed invertebrate models like cnidarians, worms, flies, and yeast. Utilizing genetic methodologies with these organisms has resulted in the identification of numerous aging genes. Remarkably, there is compelling evidence of evolutionary conservation within longevity pathways across diverse species, including mammals. In search of omic study, we would consider data from another set of experiments performed on Cnidarians and show that there has a great advanced on the `biology of aging’ in an indirect way. Cnidarians, like Turritopsis dohrnii, showcase "ontogeny reversal," reverting to earlier stages, thus achieving biological immortality through repeated rejuvenation after reproduction. Alternatively, compounds like resveratrol and rapamycin, have been identified as having the ability to decelerate aging in model organisms. However, as of now, only rapamycin has demonstrated an impact on longevity in experiments on mice. The opportunity to postpone human aging currently exists, whether through established groups of tiny molecules or numerous emerging alternatives. In this context, we explore the approaches to convert findings from age-related research into pharmaceuticals.
我们都想知道--基因和药物是否能延长我们的寿命。根据《圣经》记载,玛土撒拉的寿命长达 969 年。最近的研究发现了玛土撒拉基因,这是一个特定的DNA片段,具有促进健康茁壮成长的潜力。这一发现为开发旨在延长人类寿命的药物干预开辟了新途径。衰老是一个受自然选择影响的复杂过程,随着时间的推移,衰老逐渐适应了细胞衰老和遗传不稳定性等因素。有关衰老的研究广泛采用了无脊椎动物模型,如刺胞动物、蠕虫、苍蝇和酵母。利用这些生物的遗传方法,发现了许多衰老基因。值得注意的是,有令人信服的证据表明,包括哺乳动物在内的不同物种的长寿途径具有进化保护性。在寻找奥米克研究的过程中,我们将考虑在无脊椎动物身上进行的另一组实验数据,并以间接的方式说明 "衰老生物学 "的巨大进步。蛇尾目动物,如 Turritopsis dohrnii,展示了 "本体逆转",即恢复到早期阶段,从而通过繁殖后的反复返老还童实现生物永生。另外,白藜芦醇和雷帕霉素等化合物已被确认具有延缓模式生物衰老的能力。不过,到目前为止,只有雷帕霉素在小鼠实验中显示出对长寿的影响。目前,无论是通过已有的微小分子组,还是通过众多新兴的替代品,都有机会延缓人类衰老。在此背景下,我们探讨了将与衰老相关的研究成果转化为药物的方法。
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引用次数: 0
Anti-inflammatory and antioxidant properties of Agelas sp., Ircinia sp., and Aaptos suberitoides Agelas sp., Ircinia sp.和Aaptos subsubtioides的抗炎和抗氧化特性
Pub Date : 2023-10-31 DOI: 10.55522/jmpas.v12i5.5640
Aileen May G Ang, Mylene M Uy
Reactive oxygen species (ROS) and cyclooxygenase-2 (COX-2) can be therapeutic targets for inflammatory diseases. COX-2 expression which can be triggered by ROS might consequently promote inflammation. Inhibition of ROS by the antioxidant, however, may prevent or decrease the expression of COX-2. In this study, the antioxidant and anti-inflammatory properties of the hexane (H), dichloromethane (DCM), and methanol-water (MW) extracts of marine sponges Agelas sp. (Asp), Ircinia sp. (Isp), and Aaptos suberitoides (As) were determined. The correlation between their antioxidant properties and ability to inhibit COX enzymes was also established. The MW extracts of the marine sponges and the AsDCM contain a significant (p<0>50% of the COX-2 and gave a selectivity index (COX-2/COX-1) >1.0. This suggests that the extracts can be sources of compounds with promising and selective inhibitory properties against COX-2. Correlation analysis further showed a positive linear correlation between the extracts’ inhibitory activity against the COX enzymes and their TPC, reducing power, and DPPH radical scavenging activity. Thus, the antioxidant activity of the extracts may have influenced their anti-inflammatory property via COX inhibition.
活性氧(ROS)和环氧合酶-2 (COX-2)可作为炎症性疾病的治疗靶点。ROS触发的COX-2表达可能因此促进炎症。然而,抗氧化剂对ROS的抑制可以阻止或降低COX-2的表达。本研究测定了海绵Agelas sp. (Asp)、Ircinia sp. (Isp)和Aaptos subellioides (As)的己烷(H)、二氯甲烷(DCM)和甲醇-水(MW)提取物的抗氧化和抗炎性能。还建立了其抗氧化性能与抑制COX酶的能力之间的相关性。海绵和AsDCM的MW提取物含有显著的COX-2 (p<0>50%),选择性指数(COX-2/COX-1) >1.0。这表明,这些提取物可能是对COX-2有选择性抑制作用的化合物的来源。相关分析进一步表明,提取物对COX酶的抑制活性与其TPC、还原能力、DPPH自由基清除能力呈线性正相关。因此,提取物的抗氧化活性可能通过抑制COX影响其抗炎特性。
{"title":"Anti-inflammatory and antioxidant properties of Agelas sp., Ircinia sp., and Aaptos suberitoides","authors":"Aileen May G Ang, Mylene M Uy","doi":"10.55522/jmpas.v12i5.5640","DOIUrl":"https://doi.org/10.55522/jmpas.v12i5.5640","url":null,"abstract":"Reactive oxygen species (ROS) and cyclooxygenase-2 (COX-2) can be therapeutic targets for inflammatory diseases. COX-2 expression which can be triggered by ROS might consequently promote inflammation. Inhibition of ROS by the antioxidant, however, may prevent or decrease the expression of COX-2. In this study, the antioxidant and anti-inflammatory properties of the hexane (H), dichloromethane (DCM), and methanol-water (MW) extracts of marine sponges Agelas sp. (Asp), Ircinia sp. (Isp), and Aaptos suberitoides (As) were determined. The correlation between their antioxidant properties and ability to inhibit COX enzymes was also established. The MW extracts of the marine sponges and the AsDCM contain a significant (p<0>50% of the COX-2 and gave a selectivity index (COX-2/COX-1) >1.0. This suggests that the extracts can be sources of compounds with promising and selective inhibitory properties against COX-2. Correlation analysis further showed a positive linear correlation between the extracts’ inhibitory activity against the COX enzymes and their TPC, reducing power, and DPPH radical scavenging activity. Thus, the antioxidant activity of the extracts may have influenced their anti-inflammatory property via COX inhibition.","PeriodicalId":16445,"journal":{"name":"Journal of Medical pharmaceutical and allied sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-10-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135869949","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: 0
Analysis of correlation between insulin resistance and severity of acne vulgaris 胰岛素抵抗与寻常性痤疮严重程度的相关性分析
Pub Date : 2023-10-31 DOI: 10.55522/jmpas.v12i5.5165
Shalabh Singla, Rajwinder Singh, Vinay Shanker, Harpreet Kaur Walia, Parul Goyal
Blood glucose levels in the disease activate the free IGF-1 which promotes lipogenesis of sebaceous glands thus leading to acne formation. The study was aimed to analyze the correlation between insulin resistance and the severity of acne vulgaris. A total of 100 patients clinically diagnosed with acne vulgaris were enrolled in the study. The severity of the acne was evaluated using the GAGS system. The HOMA-IR index was used for the analysis of insulin resistance. The mean age of the patients was 22.13 years with a predominance of females i.e., 76%. GAGS score revealed 89% of patients had mild acne, 9% of patients had moderate acne and 2% of patients had severe acne. As per the HOMA-IR index cutoff value of 2.5, 35% of patients in our study had insulin resistance. A significant positive correlation was observed between the acne vulgaris and insulin resistance. Early treatment of insulin resistance can help evaluate a patient’s metabolic aspects that should be helpful in the diagnosis and treatment of various other skin conditions associated with it apart from acne vulgaris such as acanthosis nigricans, acrochordons, etc., and improving the health and the quality of care for these patients.
糖尿病患者的血糖水平会激活游离的IGF-1,它会促进皮脂腺的脂肪生成,从而导致痤疮的形成。本研究旨在分析胰岛素抵抗与寻常性痤疮严重程度之间的关系。共有100名临床诊断为寻常性痤疮的患者参加了这项研究。使用GAGS系统评估痤疮的严重程度。采用HOMA-IR指数分析胰岛素抵抗。患者平均年龄22.13岁,以女性居多,占76%。GAGS评分显示89%的患者为轻度痤疮,9%的患者为中度痤疮,2%的患者为重度痤疮。根据HOMA-IR指数临界值2.5,我们研究中35%的患者存在胰岛素抵抗。寻常痤疮与胰岛素抵抗呈显著正相关。胰岛素抵抗的早期治疗可以帮助评估患者的代谢方面,这应该有助于诊断和治疗除寻常性痤疮(如黑棘皮病、肢索病等)外与胰岛素抵抗相关的各种其他皮肤状况,并改善这些患者的健康和护理质量。
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引用次数: 0
Green synthesis of copper oxide nanoparticles using christia vespertilionis aerial parts extract: A sustainable approach for antibacterial efficacy assessment 绿色合成氧化铜纳米颗粒利用大葱地皮提取物:一个可持续的抗菌效果评估方法
Pub Date : 2023-10-31 DOI: 10.55522/jmpas.v12i5.5688
Ravindran Muthukumarasamy, Nur Zulaiqah binti Abd Rahman, Shahnaz Majeed, Enrico Magosso, Sreenivas Patro Sisinthy, Sengamalam Radhakrishnan
Metal nanoparticles typically exhibit sizes ranging from 1 to 100 nanometers and can be produced by several techniques, such as green synthesis and chemical synthesis. This study focuses on the green synthesis of copper oxide nanoparticles (CuO-NPs) using aerial extract of Christia vespertilionis. The observation of CuO-NPs formation was made based on the variations in colour exhibited by the extract mixture following the introduction of copper (II) sulphate (CuSO4). The synthesised nanoparticles underwent characterization utilising various instrumentation techniques, including UV-Vis spectrophotometry, FTIR, TEM, SEM, EDX, and TGA. The antibacterial activity of these nanoparticles was assessed by using disc diffusion method, against selected Gram-positive and Gram-negative bacteria. The investigation also encompassed an examination of the combined effect of the nanoparticles and the antibiotic Ciprofloxacin on antibacterial activity. In this study, it was noted that the maximum absorbance of the CuO-NPs occurred at a wavelength of 253nm. The functional groups of the CuO-NPs were confirmed through FTIR spectrum. TEM analysis revealed the average particle size of the CuO-NPs as 62.16 nm. Additionally, examination of SEM images revealed that the particles exhibited irregular shapes while maintaining a homogeneous distribution. The nanoparticles exhibited enhanced antibacterial efficacy against Gram-positive bacteria in comparison to the Gram-negative bacteria that were examined. Significant synergistic effect was shown when the CuoNPs were used with the antibiotic against the bacteria tested. In conclusion, the study conducted demonstrates favourable outcomes as an antibacterial agent and recommended to conduct additional research to investigate the mechanism of action and toxicity of this agent.
金属纳米颗粒的尺寸通常从1纳米到100纳米不等,可以通过几种技术生产,例如绿色合成和化学合成。本研究主要研究了绿色合成氧化铜纳米颗粒(CuO-NPs)的方法。在引入硫酸铜(CuSO4)后,根据萃取混合物所表现出的颜色变化,观察了CuO-NPs的形成。合成的纳米颗粒进行了各种仪器技术的表征,包括紫外可见分光光度法,FTIR, TEM, SEM, EDX和TGA。采用圆盘扩散法测定纳米颗粒对选定的革兰氏阳性菌和革兰氏阴性菌的抑菌活性。研究还包括纳米颗粒和抗生素环丙沙星对抗菌活性的联合作用。在本研究中,我们注意到CuO-NPs的最大吸光度出现在253nm波长处。通过FTIR光谱确定了CuO-NPs的官能团。TEM分析表明,所制备的CuO-NPs的平均粒径为62.16 nm。此外,对扫描电镜图像的检查显示,颗粒在保持均匀分布的同时呈现不规则形状。与检测的革兰氏阴性细菌相比,纳米颗粒对革兰氏阳性细菌的抗菌效果增强。当CuoNPs与抗生素一起使用时,显示出显著的协同效应。综上所述,本研究显示了作为抗菌药物的良好效果,并建议进一步研究该药物的作用机制和毒性。
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引用次数: 0
Design and evaluation of herbal tablet formulation (HTF) of leaves of Carica papaya linn, Moringa oleifera linn and fruit of Carrissa carandus lam 番木瓜叶、辣木叶和红桃果实的中药片剂配方设计与评价
Pub Date : 2023-10-31 DOI: 10.55522/jmpas.v12i5.5480.
Suraj Singh, Saravanan K
The objective of the research paper to design and development of herbal tablet formulation (HTF) of leaves of Carica Papaya Linn (LCPL) & Moringao leiferaLinn (LMOL) and fruit part of Carrissa CarandusLam (FCCL).Powdered leaves of Carica Papaya Linn & Moringao leifera Linn and fruit part of Carrissa Carandus Lam was macerated in 80% hydro-ethanolic solution for 72 hours .To identify the active constituents, phyto-chemical screening was performed. The extracts were evaluated for the flavonoid and phenolic content by qualitative and quantitative measurement. The Leaves of LCPL& LMOL and fruit of FCCL was extracted by maceration process. Preliminary phytochemical screening was performed. The LCPL showed the presence of flavonoids, phenol, proteins, glycosides, and alkaloids. The LMOL has shown the presence of phenolic compounds, flavonoids, carbohydrates, proteins, amino acids, terpenoids and tannins. The FCCL has shown the presence of phenolic compounds, flavonoids, carbohydrates, terpenoids, glycosides, alkaloids and tannins. Total flavonoid content and phenolic content was present as gallic acid and Iso-quercetin respectively. The herbal tablet formulation was prepared by wet granulation method utilizing the different proportion of the plant extract. The evaluation of Herbal tablet formulation stated that HTF-3 formulation has shown the best result in pre-compression and post-compression parameters. The hydro ethanolic extract of LCPL, LMOL and FCCL show the presence of different flavonoid and phenolic content i.e., Iso-quercetin, gallic acid. The Three different batches of HTF were prepared and result data indicates that developed formulation has been approved, suitable for oral administration and pharmacological evaluation.
本研究的目的是设计和开发番木瓜叶(Carica Papaya Linn, LCPL)的中药片剂。Carrissa CarandusLam (FCCL)的辣木精(LMOL)和果实部分。番木瓜叶粉;采用80%水乙醇浸泡法,对辣木和山茱萸果实部分进行72 h的植物化学筛选,鉴定其有效成分。采用定性和定量的方法对提取物的类黄酮和酚类含量进行评价。lcpl的叶片采用浸渍法提取枸杞子中LMOL和果实。初步进行了植物化学筛选。结果表明,黄酮类化合物、酚类化合物、蛋白质、糖苷类化合物和生物碱类化合物均存在。LMOL中含有酚类化合物、黄酮类化合物、碳水化合物、蛋白质、氨基酸、萜类化合物和单宁。FCCL中含有酚类化合物、类黄酮、碳水化合物、萜类、苷类、生物碱和单宁。总黄酮含量和酚类含量分别以没食子酸和异槲皮素的形式存在。以不同比例的植物提取物为原料,采用湿造粒法制备中药片剂。中药片剂制剂评价结果表明,HTF-3制剂在预压缩和后压缩参数上效果最佳。LCPL、LMOL和FCCL的水乙醇提取物显示出不同的类黄酮和酚类含量,即异槲皮素、没食子酸。制备了3个不同批次的HTF,结果表明所研制的制剂已获批准,适合口服给药和药理评价。
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引用次数: 0
A case of vaccine associated paralytic poliomyelitis in an immune competent child in Morocco 摩洛哥一名免疫能力儿童发生疫苗相关麻痹性脊髓灰质炎病例
Pub Date : 2023-10-31 DOI: 10.55522/jmpas.v12i5.5482
Sanae Lemrabet, Abdelkarim Filali-Maltouf, Leila Medraoui, Hicham Oumzil
This article describes the case of a previously healthy immune-competent child who, despite having received full protection against poliomyelitis with OPV, developed severe flaccid paralysis which eventually led to his death. Poliovirus testing of his contacts revealed the presence of Sabin-like type 3 poliovirus in one of them. The patient developed paralysis and respiratory distress and deceased a few months after the onset of paralysis with respiratory failure. This tragic case report demonstrates the emergence of VAPP and emphasizes the significance of early diagnosis of VAPP infections to enhance the clinical management of VAPP-infected patients.
这篇文章描述了一个以前健康的免疫能力儿童的病例,尽管接种了口服脊髓灰质炎疫苗,得到了预防脊髓灰质炎的充分保护,但他患上了严重的弛缓性麻痹,最终导致他死亡。对其接触者进行的脊髓灰质炎病毒检测显示,其中一人体内存在萨宾样3型脊髓灰质炎病毒。患者出现麻痹和呼吸窘迫,在麻痹并呼吸衰竭发作几个月后死亡。这一悲剧性病例报告证明了VAPP的出现,并强调了VAPP感染的早期诊断对加强VAPP感染患者的临床管理的意义。
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引用次数: 0
Identification of potential CDK 8 inhibitor from pyrimidine derivatives via In-Silico approach 从嘧啶衍生物中鉴定潜在的cdk8抑制剂
Pub Date : 2023-10-31 DOI: 10.55522/jmpas.v12i5.4784
Pramod Baburao Patil, Subhash Trimbakrao Kumbhar
Pyrimidinesare six-membered heterocyclic scaffold present naturally in nucleic acid components and are promising leads for the synthesis of medicinally important compounds. Cyclin-dependent kinases (CDKs) with a serine/threonine catalytic core are important druggable targets for cancer therapy and the binding of regulatory subunits controls them. In the present study series of virtually designed pyrimidine derivatives were screened using molecular docking techniques against the cyclin-dependent kinase-8 (CDK8) as a targeted protein. The density functional theory calculation of compounds having good binding affinity was done to estimate the orbital energy. The molecular dynamics simulation of the best-docked compound with the CDK8 was simulated to estimate the effect of mobility on the interactions.Themolecular docking provided insights regarding the binding ability of the designed compounds with the targeted CSK8 structure. As a result, the docked compounds exerted good interactions with the CDK8, and the compound PB129 showed the highest negative binding affinity of -12.4 kcal/mol with the formation of two hydrogen bonds. The results of the simulation study indicated that the complex of CDK-8 and PB129 hasa tight binding with constant hydrogen contacts. Moreover, the density functional theory indicated that PB129 has strong orbital energy and this compound will show tight interactions by either donating or accepting the electron with protein structure. Studied compounds showed good results for the docking study by exerting tight binding with the CDK-8 (PDB 6T41). Compound PB129 showed stable confirmation over the simulation run and has good orbital energies. Compound PB129 may act as a lead against the CDK8.
嘧啶是天然存在于核酸组分中的六元杂环支架,是合成重要药用化合物的有希望的先导物。具有丝氨酸/苏氨酸催化核心的细胞周期蛋白依赖性激酶(CDKs)是癌症治疗的重要药物靶点,调控亚基的结合控制着它们。在本研究中,利用分子对接技术筛选了一系列虚拟设计的嘧啶衍生物,以对抗细胞周期蛋白依赖性激酶-8 (CDK8)作为靶蛋白。用密度泛函理论计算了具有良好结合亲和力的化合物的轨道能量。通过模拟最佳对接化合物与CDK8的分子动力学,估计迁移率对相互作用的影响。分子对接提供了关于设计的化合物与靶向CSK8结构的结合能力的见解。结果表明,对接的化合物与CDK8具有良好的相互作用,其中PB129的负结合亲和力最高,为-12.4 kcal/mol,并形成两个氢键。模拟研究结果表明,CDK-8与PB129配合物结合紧密,具有恒定的氢接触。此外,密度泛函理论表明,PB129具有较强的轨道能,该化合物与蛋白质结构的电子相互作用紧密。所研究的化合物通过与CDK-8 (PDB 6T41)紧密结合,在对接研究中表现出良好的效果。化合物PB129在模拟运行中得到了稳定的证实,具有良好的轨道能。化合物PB129可能作为抗CDK8的先导物。
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Journal of Medical pharmaceutical and allied sciences
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