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Pancreatic lipase inhibitory and anti‐acne activity of Piper betle: Kinetic studies, in silico docking, and chemical characterization of bioactive compounds 胡椒槟榔的胰脂肪酶抑制和抗痤疮活性:动力学研究、硅学对接和生物活性化合物的化学特征描述
IF 1.3 Q3 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2024-07-22 DOI: 10.1002/vjch.202400030
Rani A. Shinde, Mohini R. Patil, R. Patil, K. S. Vishwakarma, Vijay L. Maheshwari
Lipases play important roles in obesity and skin infections. Piper betle (Piperaceae) is widely cultivated and used in daily life. It is a rich source of lead compounds used in skin infections. This study reveals anti‐acne and pancreatic lipase inhibitory potential of leaf extract of Piper betle using in‐vitro and in‐silico molecular docking. The inhibitory potential of 13 selected plant extracts was evaluated at various concentrations (5–25 µg/mL). Ethyl‐acetate extract of Piper betle with strong pancreatic lipase inhibitory activity was further fractionated by preparative thin layer chromatography and eluted bands showing strong inhibitory activity were characterized by high performance liquid chromatography and gas chromatography. The purified compounds, namely, anodendroside E,2‐monoacetate, and 5H‐cyclopropa (3, 4) benz (1, 2‐ejazulen‐5‐one), were identified and showed over 90% pancreatic lipase inhibition. The isolated compounds showed strong dose‐dependent inhibitory effects on Propionibacterium acnes. These observations were consistent with molecular docking studies, which showed that anodendroside E,2‐monoacetate binds to the allosteric site with a binding energy of –7.0 kcal/mol, and this binding site is stabilized by hydrogen and carbon hydrogen bonds contributed by Phe 354 and Asp130, ser103. These findings suggest that the pancreatic lipase inhibitory and anti‐acne effects of Piper betle are attributed to anodendroside E,2‐monoacetate.
脂肪酶在肥胖症和皮肤感染中发挥着重要作用。胡椒(胡椒科)在日常生活中被广泛种植和使用。它是用于皮肤感染的铅化合物的丰富来源。本研究利用体外和体内分子对接揭示了瓜蒌叶提取物抗痤疮和抑制胰脂肪酶的潜力。研究评估了 13 种选定植物提取物在不同浓度(5-25 µg/mL)下的抑制潜力。制备薄层色谱法对具有较强胰脂肪酶抑制活性的瓜蒌乙酸乙酯提取物进行了进一步分馏,高效液相色谱法和气相色谱法对洗脱出的具有较强抑制活性的条带进行了表征。纯化后的化合物,即anodendroside E、2-monoacetate 和 5H-cyclopropa (3, 4) benz (1, 2-ejazulen-5-one) 被鉴定出,对胰脂肪酶的抑制率超过 90%。分离出的化合物对痤疮丙酸杆菌有很强的剂量依赖性抑制作用。这些观察结果与分子对接研究结果一致,分子对接研究结果表明,anodendroside E,2-monoacetate与异构位点结合的结合能为-7.0 kcal/mol,该结合位点通过Phe 354和Asp130、ser103的氢键和碳氢键而稳定。这些发现表明,胡椒槟榔苷 E,2-单乙酸酯具有抑制胰脂肪酶和抗痤疮的作用。
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引用次数: 0
A new cytotoxic saponin from the ethyl acetate extract of Myrsine semiserrata wall Myrsine semiserrata 壁乙酸乙酯提取物中的一种新细胞毒性皂甙
IF 1.3 Q3 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2024-07-10 DOI: 10.1002/vjch.202400143
Thi Binh Yen Nguyen, Thuy Linh Nguyen, V. Vu, Quy Hung Trieu, Thi Mai Huong Doan, Van Cuong Pham
Myrsine semiserrata Wall. (Primulaceae) is an evergreen shrub found in some Asian regions including Northern Vietnam, Southern China, India, Nepal, and Myanmar. Its bark and leaves are utilized in leather tanning while the fruit serves as a commonly used antiseptic agent. Phytochemical study on the ethyl acetate extract from the aerial parts of this plant led to the isolation of a new saponin 3‐O‐α‐L‐arabinopyranosyl juglangenin A (1) and four known triterpenes, lupeol acetate (2), taraxerone (3), cucurbitacin D (4), and cucurbitacin H (5). Their structures were proven by analyzing 1D, 2D NMR, and HR‐ESI‐MS spectroscopic techniques. All isolated compounds were tested for their cytotoxicity on human cancer cell lines: HepG2, KB, MCF7, and A549. Compounds 4 and 5 exhibited potent activity against HepG2 and KB cell lines with IC50 values ranging from 1.06 to 5.99 µm. Saponin substance 1 demonstrated action against all cancer cell lines with IC50 values of 74.26, 42.83, 40.65, and 70.82 µm, respectively.
Myrsine semiserrata Wall.(报春花科)是一种常绿灌木,分布于一些亚洲地区,包括越南北部、中国南部、印度、尼泊尔和缅甸。其树皮和树叶可用于鞣革,而果实则是常用的杀菌剂。通过对该植物气生部分的乙酸乙酯提取物进行植物化学研究,分离出了一种新的皂苷 3-O-α-L-arabinopyranosyl juglangenin A(1)和四种已知的三萜类化合物,即醋酸羽扇豆醇(2)、taraxerone(3)、葫芦素 D(4)和葫芦素 H(5)。通过分析一维、二维核磁共振和 HR-ESI-MS 光谱技术,证明了它们的结构。所有分离出的化合物都对人类癌细胞系进行了细胞毒性测试:HepG2、KB、MCF7 和 A549。化合物 4 和 5 对 HepG2 和 KB 细胞株具有强效活性,IC50 值介于 1.06 至 5.99 µm 之间。皂苷物质 1 对所有癌症细胞株都有作用,其 IC50 值分别为 74.26、42.83、40.65 和 70.82 µm。
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引用次数: 0
Contents: Vietnam Journal of Chemistry 3/2024 目录越南化学杂志》3/2024
IF 0.9 Q3 Chemistry Pub Date : 2024-06-01 DOI: 10.1002/vjch.202390023
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引用次数: 0
Cover 封面
IF 0.9 Q3 Chemistry Pub Date : 2024-06-01 DOI: 10.1002/vjch.202390024
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引用次数: 0
Enhanced solubility and in vitro drug release of diosmetin from soy lecithin based‐diosmetin phytosome 基于大豆卵磷脂的双香叶酮植物胶囊提高了双香叶酮的溶解度和体外药物释放率
IF 0.9 Q3 Chemistry Pub Date : 2024-05-14 DOI: 10.1002/vjch.202300326
T. Huynh, Bich‐Ngoc Duong, Bao‐Tram Ho, Hoang‐Phuc Nguyen, Anh‐Khoa Ton, Thi‐Cam‐Thu Nguyen, Thi‐Hong‐An Nguyen, Kim‐Khanh‐Huy Ngo, Ngoc‐Kim‐Ngan Phan, Quoc‐Tuan Le, Van‐Thanh Nguyen, Thi‐Kim‐Dung Hoang
The Diosmetin Phytosome (Dt‐Ph) was developed to enhance the complex's aqueous solubility and in vitro drug release compared to pure Diosmetin (Dt). The process variables such as the reactants’ molar ratio, reaction time, stirring speed, and reaction temperature were varied to identify the most appropriate conditions for synthesis. The resulting Dt‐Ph possessed a particle size of 213.9 nm, a zeta potential of −115.1 mV, and a 95.6% encapsulation effectiveness, indicating the successful formation of the phytosome. Scanning electron microscopy (SEM) was used to analyze the morphology of the surface of Dt and Dt‐Ph. The in vitro dissolution in 24 h and normal cell cytotoxic activities of the selected formulation were evaluated. The solubility of Dt‐Ph in buffered media was four times higher than Dt, indicating greater hydrophilicity of Dt‐Ph in comparison to the more lipophilic‐free drug. Additionally, the formulation showed a noticeably increased rate and extent of dissolution studies on drug release, which was two times better than Dt. Cytotoxicity results on HEK‐293A cells showed that Dt‐Ph had less impact on normal cells compared to Dt.
与纯的香叶木素(Dt)相比,开发了香叶木素植物胶囊(Dt-Ph)以提高复合物的水溶性和体外药物释放。通过改变反应物摩尔比、反应时间、搅拌速度和反应温度等工艺变量,确定了最合适的合成条件。最终得到的 Dt-Ph 粒径为 213.9 nm,Zeta 电位为 -115.1 mV,封装效率为 95.6%,表明植物胶体的成功形成。采用扫描电子显微镜(SEM)分析了 Dt 和 Dt-Ph 的表面形态,并对所选制剂的 24 小时体外溶解度和正常细胞的细胞毒活性进行了评估。Dt-Ph 在缓冲介质中的溶解度是 Dt 的四倍,这表明与亲脂性更强的无脂药物相比,Dt-Ph 具有更强的亲水性。此外,在药物释放的溶解研究中,该制剂的溶解速率和溶解度明显提高,是 Dt 的两倍。对 HEK-293A 细胞的细胞毒性结果表明,与 Dt 相比,Dt-Ph 对正常细胞的影响较小。
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引用次数: 0
Effect of sodium hydroxide treatment on the fracture toughness of luffa natural fiber reinforced epoxy epikote 828 氢氧化钠处理对丝瓜天然纤维增强环氧树脂 epikote 828 断裂韧度的影响
IF 0.9 Q3 Chemistry Pub Date : 2024-05-10 DOI: 10.1002/vjch.202400010
D. Trung, Doan Thi Yen Oanh
Micro‐sized luffa natural fibers (MLNFs) were derived from raw luffa natural fibers from Vietnam by undergoing treatment with sodium hydroxide. This study examined the impact of sodium hydroxide concentration, temperature, and treatment duration on the fracture toughness of epoxy resin 828 reinforced with MLNFs. The results showed that the fracture toughness of the composite, as measured by the critical‐stress‐intensity factor (KIC) and Izod impact strength, was improved after the treatment of the MLNFs with sodium hydroxide. Specifically, with the optimal sodium hydroxide treatment parameters of 6% NaOH at 70 °C for 6 h, the critical‐stress‐intensity factor increased by 93% (from 2.0 to 3.86 MPa m1/2) and the Izod impact strength rose by 44.6% (from 3.81 to 5.51 kJ/m2). The thermal properties and surface structure of MLNFs treated with NaOH were analyzed using thermogravimetric analysis (TGA) and scanning electron microscopy (SEM) images.
微尺寸丝瓜天然纤维(MLNFs)是从越南的丝瓜天然纤维原料中通过氢氧化钠处理提取出来的。本研究考察了氢氧化钠浓度、温度和处理时间对用 MLNFs 增强的环氧树脂 828 断裂韧度的影响。结果表明,用氢氧化钠处理 MLNFs 后,以临界应力强度因子(KIC)和伊佐德冲击强度衡量的复合材料断裂韧性得到了改善。具体来说,最佳氢氧化钠处理参数为 6% NaOH 70 °C 6 小时,临界应力强度因子提高了 93%(从 2.0 兆帕 m1/2 提高到 3.86 兆帕 m1/2),伊佐德冲击强度提高了 44.6%(从 3.81 kJ/m2 提高到 5.51 kJ/m2)。利用热重分析 (TGA) 和扫描电子显微镜 (SEM) 图像分析了经 NaOH 处理的 MLNFs 的热性能和表面结构。
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引用次数: 0
Stilbene derivatives from Gnetum montanum Markgr. with their xanthine oxidase inhibition activity Gnetum montanum Markgr.的二苯乙烯衍生物及其黄嘌呤氧化酶抑制活性
IF 0.9 Q3 Chemistry Pub Date : 2024-05-10 DOI: 10.1002/vjch.202400069
Nguyen Thi Viet Thanh, Ho Duc Cuong, B. H. Tai, Phan Van Kiem
Phytochemical study on the methanol extract of the trunks of Gnetum montanum Markgr. led to the isolation of one new stilbene derivative, (E)‐2′‐methoxy‐3,5,5′‐trihydroxystilbene (1) and six known compounds, lehmbachol (2), gnetulin (3), trans‐shegansu B (4), cis‐shegansu B (5), (+)‐hannokinol (6), and gnetol (7). Their chemical structures were determined by spectroscopic analyses including HR‐ESI‐MS, 1D and 2D NMR, and circular dichroism methods in comparison with the reported data. In addition, compounds 1–5 showed xanthine oxidase inhibitory activity with IC50 values of 13.6, 35.2, 38.7, 43.4, and 47.7 µm, respectively, compared to the positive control, allopurinol, which showed IC50 value of 2.9 µm.
对 Gnetum montanum Markgr.在对 Gnetum montanum Markgr 树干甲醇提取物进行植物化学研究后,分离出一种新的二苯乙烯衍生物 (E)-2′-methoxy-3,5,5′-trihydroxystilbene (1) 和六种已知化合物 lehmbachol (2)、gnetulin (3)、trans-shegansu B (4)、cis-shegansu B (5)、(+)-hannokinol (6) 和 gnetol (7)。通过光谱分析,包括 HR-ESI-MS、一维和二维核磁共振以及圆二色性方法,并与已报道的数据进行对比,确定了它们的化学结构。此外,化合物 1-5 显示出黄嘌呤氧化酶抑制活性,其 IC50 值分别为 13.6、35.2、38.7、43.4 和 47.7 µm,而阳性对照别嘌呤醇的 IC50 值为 2.9 µm。
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引用次数: 0
Effect of n‐pentanol with novel water hyacinth biodiesel‐diesel ternary blends on diesel engine performance and emission characteristics 正戊醇与新型水葫芦生物柴油-柴油三元混合物对柴油发动机性能和排放特性的影响
IF 0.9 Q3 Chemistry Pub Date : 2024-05-10 DOI: 10.1002/vjch.202300383
Maneesh Singh, Prashant Saini, Divyanshi Srivastava, Srishti Mishra, Saif Nawaz Ahmad
Present research deals with crude oil production from water hyacinth biomass and its biodiesel preparation. Alcohol additive n‐pentanol is mixed with biodiesel and diesel blends to identify their effects on diesel engine performance and emission parameters experimentally. Water hyacinth oil (WHO) is produced through Soxhlet extraction technique, and its biodiesel is prepared by transesterification. n‐pentanol is mixed through magnetic stirring in biodiesel‐diesel blends to improve their combustion quality and efficiency. Prepared fuel blends properties are examined as per ASTM standards. Experimental results reveal that, BSFC and BTE are evaluated as 0.26 kg/kW‐h and 29.5%, respectively, with HC emissions as 29 ppm, CO emissions as 0.28 vol%, NOx emissions as 330 ppm and CO2 emissions as 2.21 vol% for WHB20D75P5 fuel at maximum load. The comparison of D100 and WHB20D80 with respect to WHB20D75P5 reveals 3.27% reduction and 7.27% improvement in BTE, respectively. Both HC and CO are reduced by 14.70% and 22.22% for WHB20D75P5 fuel compared to diesel. NOx and CO2 emissions are increased by 6.79% and 12.75% for WHB20D75P5 fuel compared to diesel. Overall, WHB20D75P5 fuel is the best performer.
本研究涉及从布袋莲生物质中提取原油并制备生物柴油。酒精添加剂正戊醇与生物柴油和柴油混合物混合,通过实验确定其对柴油发动机性能和排放参数的影响。通过磁力搅拌将正戊醇混入生物柴油-柴油混合物中,以提高其燃烧质量和效率。根据 ASTM 标准对制备的混合燃料性能进行了检测。实验结果表明,WHB20D75P5 燃料在最大负荷下的 BSFC 和 BTE 分别为 0.26 kg/kW-h 和 29.5%,HC 排放量为 29 ppm,CO 排放量为 0.28 vol%,NOx 排放量为 330 ppm,CO2 排放量为 2.21 vol%。与 WHB20D75P5 相比,D100 和 WHB20D80 的 BTE 分别降低了 3.27% 和 7.27%。与柴油相比,WHB20D75P5 燃料的 HC 和 CO 分别减少了 14.70% 和 22.22%。与柴油相比,WHB20D75P5 燃料的 NOx 和 CO2 排放量分别增加了 6.79% 和 12.75%。总体而言,WHB20D75P5 燃料的性能最佳。
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引用次数: 0
Evaluation of vat blue removal by Aspergillus niger using scanning electron microscopy and glucose oxidase enzyme activity 利用扫描电子显微镜和葡萄糖氧化酶活性评估黑曲霉去除蝙蝠蓝的效果
IF 0.9 Q3 Chemistry Pub Date : 2024-05-10 DOI: 10.1002/vjch.202300374
Juana Lira Pérez, Juan Carlos Figueroa Estrada, Mayola García Rivero, Refugio Rodríguez Vázquez
The use of fungi to reduce dye removal in water from diverse industries can be an efficient option for solving environmental problems. However, the mycoremediation processes involved in color removal are unknown. In this article, Aspergillus niger CDBB‐H‐175 was applied for vat blue discoloration (DC). Hence, inactive biomass by two methods (metabolic inhibitor and heat) and active biomass were studied by scanning electron microscopy and enzyme activities to determine the vat blue DC. When using active biomass, 62% of DC, glucose oxidase (GOX) enzyme activity, 1.19 U/mL and 1.43 mg/L of H2O2 were obtained. It was observed that 68% of DC was due to the degradation process and 32% was due to biomass sorption. When the biomass was inactivated with sodium azide, DC increased by 90% (1.45‐fold), low GOX activity (0.138 U/mL), and H2O2 (0.25 mg/L) were detected. High DC might be due to a high dye sorption in hyphae, since an increase in the thickness and morphology of the hyphae were observed by SEM. Inactivated biomass through heating, showed a 69.5% of DC, where 0.01 U/mL GOX and 0.25 mg/L H2O2 were reached, demonstrating that inactivation of A. niger biomass by sodium azide can be considered as an alternative treatment for colored wastewater.
利用真菌减少各种工业用水中的染料去除量,是解决环境问题的一种有效选择。然而,脱色过程中涉及的真菌修复过程尚不清楚。本文将黑曲霉 CDBB-H-175 应用于大桶蓝脱色(DC)。因此,通过两种方法(代谢抑制剂和加热)研究了非活性生物质,并通过扫描电子显微镜和酶活性研究了活性生物质,以确定还原蓝脱色效果。在使用活性生物质时,得到了 62% 的 DC、葡萄糖氧化酶(GOX)酶活性、1.19 U/mL和 1.43 mg/L 的 H2O2。据观察,68%的 DC 是由于降解过程造成的,32%是由于生物质吸附造成的。用叠氮化钠灭活生物质后,DC 增加了 90%(1.45 倍),检测到的 GOX 活性(0.138 U/mL)和 H2O2(0.25 mg/L)较低。用扫描电镜观察到菌丝的厚度和形态有所增加,因此高 DC 可能是由于菌丝对染料的高吸附性造成的。通过加热灭活的生物质显示出 69.5% 的直流电,达到 0.01 U/mL GOX 和 0.25 mg/L H2O2,这表明用叠氮化钠灭活黑僵菌生物质可被视为处理有色废水的一种替代方法。
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引用次数: 0
Unveiling the potential of Satureja calamintha nepeta: A study on its phytochemical composition and antibacterial activity 揭示 Satureja calamintha nepeta 的潜力:关于其植物化学成分和抗菌活性的研究
IF 0.9 Q3 Chemistry Pub Date : 2024-05-10 DOI: 10.1002/vjch.202300174
Mouhcine Hayani, Tariq Benabbouha, Wafaa Nachit, Said Byadi, Khalil Chefira, Aziz Aboulmouhajir, A. Tounsi, T. Zair
Satureja calamintha nepeta is a plant native to northwestern Morocco. The purpose of this investigation is to identify the chemical composition and evaluate the antibacterial of the essential oil extracted from this plant. Firstly, a quality inspection of the plant was carried out to quantify its level of metals, especially the heavier ones, using the ICP technique. Gas chromatography/mass spectrometry was used to characterize the chemical composition of essential oil. The chromatogram analysis shows the presence of 27 compounds, that is, 99.2% of the essential oil, with 1,8‐cineole (34.34%) and cis‐pinocamphone (11.87%) being the most significant. The antibacterial effectiveness of the essential oil was tested using the disc diffusion method against 6 gram‐positive and gram‐negative pathogens. The essential oil shows strong activity against Escherichia coli and Escherichia vekanda strains, with an MIC value of about 2.80 µg/mL. The authors were benefited from the modeling technique to better understand the antibacterial activity.
Satureja calamintha nepeta 是一种原产于摩洛哥西北部的植物。这项研究的目的是确定从这种植物中提取的精油的化学成分并评估其抗菌性。首先,利用 ICP 技术对植物进行了质量检测,以量化其中的金属含量,尤其是重金属含量。气相色谱/质谱法用于确定精油化学成分的特征。色谱分析显示,精油中含有 27 种化合物,占精油总量的 99.2%,其中以 1,8-蒎烯(34.34%)和顺式蒎烷(11.87%)的含量最高。精油的抗菌效果采用了盘扩散法对 6 种革兰氏阳性和革兰氏阴性病原体进行了测试。精油对大肠杆菌和维康达大肠杆菌菌株具有很强的活性,其 MIC 值约为 2.80 µg/mL。作者通过建模技术更好地了解了其抗菌活性。
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引用次数: 0
期刊
Vietnam Journal of Chemistry
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