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Cytoprotective effect and antioxidant activities of hesperidin against cisplatin-induced fibroblast cell. 橙皮苷对顺铂诱导成纤维细胞的细胞保护作用及抗氧化活性。
IF 1.4 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-04-01 Epub Date: 2025-05-19 DOI: 10.4103/JAPTR.JAPTR_298_24
Anif Nur Artanti, Fea Prihapsara, Faaza Aulia Rahman, Mukh Syaifudin, Muchtaridi Muchtaridi, Endah Puji Septisetyani, Edy Meiyanto, Okid Parama Astirin

Cisplatin (Cisp), a platinum-based compound, is a potent chemotherapy drug that effectively treats various cancers such as lung, breast, bladder, and hepatocellular carcinoma. However, its clinical application is limited due to its fibroblast damage, which is linked to its ability to produce collagen and other extracellular matrix components essential for tissue healing. Enhancing antioxidant capacity offers a potential strategy to reduce Cisp-induced fibroblast damage. Hesperidin (HSD), a flavonoid from Citrus sp., exhibits various pharmacological properties, including anti-inflammatory and antioxidant effects. This study aims to determine HSD as cytoprotective induced by Cisp using the fibroblast cell lines (NIH-3T3). 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay was used to determine antioxidant activity. The viability cell after treatment with HSD, Cisp, and cotreatment HSD-Cisp was evaluated through Mictroculure Tetrazolium Technique (MTT) assay. The evaluation of senescence was performed using the senescence-associated β-galactosidase assay. Gelatin zymography assay was utilized to analyze the activity of matrix metalloproteinases (MMPs). Data were analyzed using one-way ANOVA and Tukey's post hoc test in SPSS (version 20.0). The IC50 of the radical scavenging assay of HSD was found to be 20.967 ± 0.016 µM. HSD showed low cytotoxicity against NIH-3T3 cells, with IC50 values of over 500 µM. HSD showed an antagonistic effect when used as cotreatment HSD with Cisp in NIH-3T3 cells, with a combination index >1. Cotreatment of HSD and Cisp reduces cellular senescence and the expression of MMP-9 and MMP-2. These findings suggest that HSD could be beneficial as a cytoprotective agent, helping to maintain cellular health against chemotherapy.

顺铂(Cisp)是一种以铂为基础的化合物,是一种有效治疗肺癌、乳腺癌、膀胱癌和肝癌等各种癌症的强效化疗药物。然而,它的临床应用受到限制,因为它的成纤维细胞损伤,这与它产生胶原蛋白和其他组织愈合所必需的细胞外基质成分的能力有关。增强抗氧化能力为减少cisp诱导的成纤维细胞损伤提供了潜在的策略。橙皮苷(HSD)是柑橘属植物的一种类黄酮,具有抗炎、抗氧化等多种药理作用。本研究旨在利用成纤维细胞系(NIH-3T3),确定HSD在Cisp诱导下的细胞保护作用。采用2,2-二苯基-1-苦味酰肼(DPPH)自由基清除法测定其抗氧化活性。采用微培养四氮唑法(MTT)测定HSD、Cisp及HSD-Cisp共处理后的细胞活力。衰老评价采用衰老相关β-半乳糖苷酶测定法。采用明胶酶谱法分析基质金属蛋白酶(MMPs)活性。数据分析采用SPSS(20.0版)单因素方差分析和Tukey事后检验。HSD自由基清除实验的IC50为20.967±0.016µM。HSD对NIH-3T3细胞具有较低的细胞毒性,IC50值在500µM以上。HSD与Cisp共处理HSD对NIH-3T3细胞有拮抗作用,联合指数为bbb1。HSD和Cisp共同处理可减少细胞衰老和MMP-9和MMP-2的表达。这些发现表明,HSD可能是一种有益的细胞保护剂,有助于维持细胞健康对抗化疗。
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引用次数: 0
Evaluation of the combined effects of Morinda citrifolia fruit and Averrhoa bilimbi leaves on hair growth in rabbits. 桑葚果与沙棘叶联合对家兔毛发生长影响的评价。
IF 1.4 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-04-01 Epub Date: 2025-05-19 DOI: 10.4103/JAPTR.JAPTR_321_24
Nur Azizah, Imas Maesaroh, Nabila Az Zahra, Syafika Alaydrus

This study was conducted to evaluate the impact of a combination of Morinda citrifolia fruit extract (MCFE) and Averrhoa bilimbi leaf extract (ABLE) on hair growth in rabbits. The study included seven treatment groups: (1) control group (distilled water), (2) positive control (minoxidil 5%), (3) treatment 1 (MCFE 10%), (4) treatment 2 (ABLE 10%), (5) treatment 3 (MCFE 5% + ABLE 5%), (6) treatment 4 (MCFE 7.5% + ABLE 2.5%), and (7) treatment 5 (MCFE 2.5% + ABLE 7.5%). Hair length measurements were taken on days 7, 14, 21, and 28, and the average daily growth rate was calculated by dividing the change in hair length by the number of days. Hair weight was measured on day 28. Data analysis was conducted using both two-way and one-way ANOVA, and statistical significance was determined at P < 0.05. The treatment group 4 (MCFE 7.5% + ABLE 2.5%) showed a significant difference in hair growth compared to the normal control, positive control, and other treatment groups (P < 0.05). The group exhibited a 19.69 ± 0.38 mm increase in hair length, with a daily growth rate of 0.88 mm/day, and an increase in hair weight of 0.33 ± 0.003 g. The combination of MCFE and ABLE demonstrated potential as an anti-hair loss agent, effectively enhancing both hair length and weight.

本试验研究了桑葚果提取物(MCFE)与阿佛拉叶提取物(ABLE)联合使用对家兔毛发生长的影响。研究共分为7个处理组:(1)对照组(蒸馏水),(2)阳性对照(米诺地尔5%),(3)处理1 (MCFE 10%),(4)处理2 (ABLE 10%),(5)处理3 (MCFE 5% + ABLE 5%),(6)处理4 (MCFE 7.5% + ABLE 2.5%),(7)处理5 (MCFE 2.5% + ABLE 7.5%)。在第7、14、21和28天测量头发长度,用头发长度变化除以天数计算平均每日生长率。第28天测定毛重。数据分析采用双因素和单因素方差分析,P < 0.05为差异有统计学意义。治疗4组(MCFE 7.5% + ABLE 2.5%)与正常对照组、阳性对照组及其他治疗组相比,毛发生长差异有统计学意义(P < 0.05)。毛发长度增加19.69±0.38 mm,日生长率为0.88 mm/d,毛重增加0.33±0.003 g。MCFE和ABLE的组合证明了作为抗脱发剂的潜力,有效地增加头发的长度和重量。
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引用次数: 0
Fractionation of an ethanolic extract of purple leaves (Graptophyllum pictum) with antioxidant and lipoxygenase activity inhibition assay. 紫叶乙醇提取物的分离与抗氧化及脂氧化酶活性抑制试验。
IF 1.4 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-01-01 Epub Date: 2025-02-14 DOI: 10.4103/JAPTR.JAPTR_182_24
Feda Anisah Makkiyah, Siti Amalina, Eldiza Puji Rahmi, Dhigna Luthfiyani Citra Pradana

Graptophyllum pictum offers therapeutic potential that has received attention from researchers around the world. The purple leaf is native to New Guinea and has been widely distributed, including Indonesia. This study aims to determine the antioxidant activity and potential inhibition of the lipoxygenase (LOX) enzyme in the hexane fraction, ethyl acetate fraction, and water fraction of purple leaf. Samples were extracted by maceration using 96% ethanol, followed by multilevel fractionation using ethyl acetate, hexane, and water solvents. The fractions were determined for their antioxidant activity using the 2,2-diphenyl-1-picrylhydrazyl method, and their potential in LOX enzyme inhibition was analyzed using an ultraviolet-vis spectrophotometer. The ethyl acetate fraction showed the highest antioxidant activity with inhibition concentration (IC50) of 17.23 µg/mL; LOX inhibition was also demonstrated by the highest ethyl acetate fraction with IC50 133.47 µg/mL, followed by the hexane fraction, and then the water fraction. These results suggest purple leaves with ethyl acetate fraction can be a new drug innovation with antioxidant and anti-inflammatory properties, and this study can be used as an evaluation material for further drug development.

Graptophyllum pictum具有治疗潜力,已受到世界各地研究人员的关注。紫叶原产于新几内亚,并已广泛分布,包括印度尼西亚。本研究旨在测定紫叶中己烷、乙酸乙酯和水三组分的抗氧化活性和对脂氧合酶(LOX)酶的抑制作用。样品用96%乙醇浸泡提取,然后用乙酸乙酯、己烷和水溶剂进行多级分馏。采用2,2-二苯基-1-苦味酰肼法测定各组分的抗氧化活性,并采用紫外-可见分光光度计分析其对LOX酶的抑制作用。乙酸乙酯部位抗氧化活性最高,IC50为17.23µg/mL;乙酸乙酯部位对LOX的抑制作用最强,IC50为133.47µg/mL,其次是己烷部位,最后是水部位。上述结果表明,紫叶乙酸乙酯部分具有抗氧化和抗炎的特性,可作为进一步药物开发的评价材料。
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引用次数: 0
The immunomodulatory activity of parijoto fruit (Medinilla speciosa) fraction against phagocytosis macrophages and lymphocyte proliferation. 刺槐果提取物对吞噬、巨噬细胞和淋巴细胞增殖的免疫调节作用。
IF 1.4 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-01-01 Epub Date: 2025-02-14 DOI: 10.4103/JAPTR.JAPTR_248_24
Aji Winanta, Haidar Bagir, Rifki Febriansah, Arde Toga Nugraha

The immune system's principal functions are to preserve health and defend against dangerous invaders (antigens). Parijoto fruit (Medinilla speciosa) is a plant that can potentially have immunomodulatory activity because it contains flavonoid and terpenoid compounds. The aim of this research is to ascertain the total flavonoid and phytochemical content of the parijoto fruit fraction, as well as its potential in vitro immunomodulatory activity. The extraction of powdered parijoto fruit was conducted using 70% ethanol, followed by the separation into n-hexane, ethyl acetate, and water fraction. The phytochemical content was analyzed with gas chromatography (GC)-mass spectrometry. The total flavonoid contents were determined by colorimetric analysis. In addition, the immunomodulatory activity assay was conducted in vitro to evaluate the phagocytic activity (phagocytic capacity [PC] and phagocytic index) of macrophages and the proliferation of lymphocytes (stimulation index [SI]). The GC results showed that parijoto fruit extract contains 9,12-Octadecadienoic acid-, and phthalic acid. The ethyl acetate fraction exhibited the greatest total flavonoid concentration at 7.4094 ± 0.49 mg QE/g sample. In vitro, immunomodulatory tests showed that all fractions could significantly increase macrophage phagocytic activity compared to control cells. The highest value of PC and phagocytic index was found in the n-hexane phase with a concentration of 750 g/mL of 82.75 ± 0.87 and a concentration of 500 g/mL of 6.62 ± 0.19, respectively. The ethyl acetate fraction exhibited the most significant SI for lymphocyte proliferation, recorded at a concentration of 750 g/mL with a value of 8.70 ± 1.01. The ethyl acetate fraction's SI >3 value in the lymphocyte proliferation test suggests that it exhibits lymphocyte proliferation activity. The parijoto fruit may enhance the phagocytic role of macrophages and promote lymphocyte proliferation, indicating its potential as an immunomodulatory therapy.

免疫系统的主要功能是保持健康和抵御危险的入侵者(抗原)。因其含有黄酮类化合物和萜类化合物,故被认为是一种具有潜在免疫调节活性的植物。本研究的目的是确定异香果提取物中总黄酮和植物化学成分的含量,以及其体外免疫调节活性。用70%乙醇提取香参果粉,分离成正己烷、乙酸乙酯和水馏分。采用气相色谱-质谱联用技术分析植物化学成分。用比色法测定其总黄酮含量。此外,通过体外免疫调节活性测定,评估巨噬细胞的吞噬活性(吞噬能力[PC]和吞噬指数)和淋巴细胞的增殖(刺激指数[SI])。气相色谱结果表明,香参果提取物中含有9,12-十八二烯酸-和邻苯二甲酸。乙酸乙酯部位总黄酮含量最高,为7.4094±0.49 mg QE/g。体外免疫调节实验表明,与对照细胞相比,各组分均能显著提高巨噬细胞的吞噬活性。PC和吞噬指数在正己烷相中最高,浓度为750 g/mL为82.75±0.87,浓度为500 g/mL为6.62±0.19。乙酸乙酯部分对淋巴细胞增殖的SI最显著,浓度为750 g/mL,值为8.70±1.01。在淋巴细胞增殖试验中,乙酸乙酯组分的SI >3值表明其具有淋巴细胞增殖活性。参果可能增强巨噬细胞的吞噬作用,促进淋巴细胞增殖,提示其作为免疫调节疗法的潜力。
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引用次数: 0
Analysis of Vitamin K1 levels in several types of vegetables consumed by warfarin-used patients. 华法林患者食用的几种蔬菜中维生素K1水平的分析。
IF 1.4 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-01-01 Epub Date: 2025-02-14 DOI: 10.4103/JAPTR.JAPTR_156_24
Norisca Aliza Putriana, Taofik Rusdiana, Gabriella Joan, Driyanti Rahayu, Febrina Amelia Saputri

Vitamin K consumption needs to be monitored in people taking warfarin since it can impact the anticoagulation response. Vegetables are the primary nutritional source of Vitamin K1, in the form of Vitamin K1. The aim of this study was to measure the level of Vitamin K1 in various vegetables that were commercially sold in three major Bandung markets and were ingested by patients using warfarin at Hasan Sadikin Central General Hospital Bandung. High-performance liquid chromatography with an ultraviolet detector set at 245 nm was the analytical technique. One hundred percent methanol was used as the mobile phase, and it was isocratically eluted at a flow rate of 0.6 mL/min with a T3 column maintained at 25°C. The results indicated that the following Vitamin K1 levels were found in lettuce: 38.4391 ± 15.2650-64.4419 ± 19.0315 µg/100 g, in napa cabbage: 56.7445 ± 0.1569-273.2828 ± 8.3061 µg/100 g, in cabbage: 27.9531 ± 1.7487-217.0457 ± 7.2201 µg/100 g, and in spinach: 305.2868 ± 3.3058-970.7098 ± 14.1167 µg/100 g. The highest Vitamin K1 level was in spinach and the lowest was in lettuce.

服用华法林的人需要监测维生素K的摄入量,因为它会影响抗凝反应。蔬菜是维生素K1的主要营养来源,以维生素K1的形式存在。本研究的目的是测量万隆三个主要市场上出售的各种蔬菜中维生素K1的水平,这些蔬菜是万隆哈桑萨迪金中央综合医院使用华法林的患者摄入的。分析技术为高效液相色谱法,紫外检测器为245 nm。以100%甲醇为流动相,流速为0.6 mL/min, T3柱保持在25℃,等压洗脱。结果表明,莴苣中维生素K1含量为:38.4391±15.2650-64.4419±19.0315µg/100 g,甘蓝为:56.7445±0.1569-273.2828±8.3061µg/100 g,白菜为:27.9531±1.7487-217.0457±7.2201µg/100 g,菠菜为:305.2868±3.3058-970.7098±14.1167µg/100 g。菠菜中维生素K1含量最高,生菜中最低。
{"title":"Analysis of Vitamin K1 levels in several types of vegetables consumed by warfarin-used patients.","authors":"Norisca Aliza Putriana, Taofik Rusdiana, Gabriella Joan, Driyanti Rahayu, Febrina Amelia Saputri","doi":"10.4103/JAPTR.JAPTR_156_24","DOIUrl":"10.4103/JAPTR.JAPTR_156_24","url":null,"abstract":"<p><p>Vitamin K consumption needs to be monitored in people taking warfarin since it can impact the anticoagulation response. Vegetables are the primary nutritional source of Vitamin K1, in the form of Vitamin K1. The aim of this study was to measure the level of Vitamin K1 in various vegetables that were commercially sold in three major Bandung markets and were ingested by patients using warfarin at Hasan Sadikin Central General Hospital Bandung. High-performance liquid chromatography with an ultraviolet detector set at 245 nm was the analytical technique. One hundred percent methanol was used as the mobile phase, and it was isocratically eluted at a flow rate of 0.6 mL/min with a T3 column maintained at 25°C. The results indicated that the following Vitamin K1 levels were found in lettuce: 38.4391 ± 15.2650-64.4419 ± 19.0315 µg/100 g, in napa cabbage: 56.7445 ± 0.1569-273.2828 ± 8.3061 µg/100 g, in cabbage: 27.9531 ± 1.7487-217.0457 ± 7.2201 µg/100 g, and in spinach: 305.2868 ± 3.3058-970.7098 ± 14.1167 µg/100 g. The highest Vitamin K1 level was in spinach and the lowest was in lettuce.</p>","PeriodicalId":14877,"journal":{"name":"Journal of Advanced Pharmaceutical Technology & Research","volume":"16 1","pages":"35-41"},"PeriodicalIF":1.4,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11960828/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143772582","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Cytotoxic activity of Cyrtostachys renda extracts and fractions against MCF-7 and HeLa cancer cells through cell cycle arrest and apoptosis induction mechanism. 石竹提取物及其组分通过细胞周期阻滞和诱导凋亡机制对MCF-7和HeLa癌细胞的细胞毒活性。
IF 1.4 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-01-01 Epub Date: 2025-02-14 DOI: 10.4103/JAPTR.JAPTR_222_24
Syamsurizal, Sutrisno, Diah Tri Utami

In traditional medicine, Cyrtostachys renda has been used for its many bioactive components that are good for people's health. This research assessed the cytotoxic effects of extracts and fractions against Michigan Cancer Foundation-7 (MCF-7) and Henrietta Lacks (HeLa) cell lines. The extracts and fractions of root and fruit assess cytotoxic activities and inhibitory mechanisms against the MCF-7 and HeLa cancer cell lines, respectively. The fruit and roots of C. renda were extracted using the liquid-liquid method. The sample concentrations evaluated included extracts 31.5-1000 μg/mL, fractions 15.625-500 μg/mL, and doxorubicin 2-0.0625 μg/mL. Cytotoxicity was evaluated on MCF-7 and HeLa cells using an MTT assay. Morphological alterations were subsequently discovered utilizing an inverted microscope. Flow cytometry was utilized to find out the cell cycle's distribution and the apoptosis characteristics. The different parts and extracts showed cytotoxic effects on HeLa and MCF-7 cells, with IC50 values ranging from 30.69 ± 0.47 to 787.89 ± 1.77 µg/mL. Cell cycle studies showed that fraction A4 inhibited the cell cycle in MCF-7 cells at the G1 phase followed by the G2/M and S phases, while fraction B5 inhibited the cell cycle in HeLa cells at the G2/M phase. Both fractions showed the ability to induce apoptosis against MCF-7 and HeLa cells. The results showed that the fractions A4 and B5 showed cytotoxic activity against MCF-7 and HeLa cells by cell cycle arrest and apoptosis induction.

在传统医学中,水仙花因其许多有益人体健康的生物活性成分而被广泛使用。本研究评估了提取物和馏分对密歇根癌症基金会-7 (MCF-7)和亨丽埃塔·拉克斯(HeLa)细胞系的细胞毒性作用。根和果的提取物和馏分分别评估了对MCF-7和HeLa癌细胞系的细胞毒活性和抑制机制。采用液液法提取莲果和莲根。评价的样品浓度包括提取物31.5 ~ 1000 μg/mL、馏分15.625 ~ 500 μg/mL和阿霉素2 ~ 0.0625 μg/mL。使用MTT法评估MCF-7和HeLa细胞的细胞毒性。随后利用倒置显微镜发现形态学改变。流式细胞术检测细胞周期分布及凋亡特征。不同部位及提取物对HeLa和MCF-7细胞均有细胞毒作用,IC50值为30.69±0.47 ~ 787.89±1.77µg/mL。细胞周期研究表明,A4组分抑制MCF-7细胞G1期、G2/M期和S期的细胞周期,B5组分抑制HeLa细胞G2/M期的细胞周期。两组均有诱导MCF-7和HeLa细胞凋亡的作用。结果表明,A4和B5组分通过细胞周期阻滞和诱导凋亡对MCF-7和HeLa细胞具有细胞毒活性。
{"title":"Cytotoxic activity of <i>Cyrtostachys renda</i> extracts and fractions against MCF-7 and HeLa cancer cells through cell cycle arrest and apoptosis induction mechanism.","authors":"Syamsurizal, Sutrisno, Diah Tri Utami","doi":"10.4103/JAPTR.JAPTR_222_24","DOIUrl":"10.4103/JAPTR.JAPTR_222_24","url":null,"abstract":"<p><p>In traditional medicine, <i>Cyrtostachys renda</i> has been used for its many bioactive components that are good for people's health. This research assessed the cytotoxic effects of extracts and fractions against Michigan Cancer Foundation-7 (MCF-7) and Henrietta Lacks (HeLa) cell lines. The extracts and fractions of root and fruit assess cytotoxic activities and inhibitory mechanisms against the MCF-7 and HeLa cancer cell lines, respectively. The fruit and roots of <i>C. renda</i> were extracted using the liquid-liquid method. The sample concentrations evaluated included extracts 31.5-1000 μg/mL, fractions 15.625-500 μg/mL, and doxorubicin 2-0.0625 μg/mL. Cytotoxicity was evaluated on MCF-7 and HeLa cells using an MTT assay. Morphological alterations were subsequently discovered utilizing an inverted microscope. Flow cytometry was utilized to find out the cell cycle's distribution and the apoptosis characteristics. The different parts and extracts showed cytotoxic effects on HeLa and MCF-7 cells, with IC<sub>50</sub> values ranging from 30.69 ± 0.47 to 787.89 ± 1.77 µg/mL. Cell cycle studies showed that fraction A4 inhibited the cell cycle in MCF-7 cells at the G1 phase followed by the G2/M and S phases, while fraction B5 inhibited the cell cycle in HeLa cells at the G2/M phase. Both fractions showed the ability to induce apoptosis against MCF-7 and HeLa cells. The results showed that the fractions A4 and B5 showed cytotoxic activity against MCF-7 and HeLa cells by cell cycle arrest and apoptosis induction.</p>","PeriodicalId":14877,"journal":{"name":"Journal of Advanced Pharmaceutical Technology & Research","volume":"16 1","pages":"18-23"},"PeriodicalIF":1.4,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11960827/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143772584","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Preparation and evaluation of topical span 60-based oleogel of voriconazole. 以 span 60 为基础的伏立康唑局部用油凝胶的制备和评估。
IF 1.4 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-01-01 Epub Date: 2025-02-14 DOI: 10.4103/JAPTR.JAPTR_211_24
Hiba Muneer Fysal, Hanan Jalal Kassab

Voriconazole (VOR) is a triazole antifungal agent; it blocks the synthesis of ergosterol, available in the market orally and intravenously, but, not without various side effects. The aim of this study is development and characterization of VOR oleogel for the topical treatment of skin fungal infection to avoid the drug's systemic side effects that are associated with oral and IV routes. The gelator Span 60 (S) was added at different concentrations to different oils (oleic OO, grapeseed GO, and sesame oil SO) to obtain the minimum gelation concentration, the prepared formulas were subjected to various evaluation tests, and the optimum formula was checked for antifungal effect, and subjected to viscosity, and texture analysis. The optimized formula, Span60 with SO 14SSO, showed 100% drug release, good antifungal activity, and acceptable transition temperature. The study of viscosity demonstrated the pseudo-plastic shear thinning behavior. A Fourier-transform infrared study showed that the drug and excipients did not significantly interact. 14SSO might be a promising topical treatment option for skin fungal infections.

伏立康唑(Voriconazole, VOR)是一种三唑类抗真菌药物;它阻断麦角甾醇的合成,市面上有口服和静脉注射的麦角甾醇,但是,并非没有各种副作用。本研究的目的是开发和表征用于局部治疗皮肤真菌感染的VOR油凝胶,以避免药物与口服和静脉注射途径相关的全身副作用。将胶凝剂Span 60 (S)以不同的浓度加入到不同的油脂(油酸OO、葡萄籽GO和芝麻油SO)中,以获得最小的胶凝浓度,并对所制备的配方进行了各种评价试验,对最佳配方进行了抗真菌效果检查,并进行了粘度和质地分析。优化后的配方为含so14sso的Span60,释药100%,抗真菌活性良好,转化温度适宜。对黏度的研究证实了其伪塑性剪切减薄行为。傅里叶变换红外研究表明,药物和辅料之间没有明显的相互作用。sso可能是一种很有前途的局部治疗皮肤真菌感染的选择。
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引用次数: 0
Cytotoxic effect and apoptotic induction of tricyclohexyltin p-methoxycinnamate on HT-29 colorectal cancer cells: Implications for anticancer therapeutics. 对甲氧基肉桂酸三环己基锡对HT-29结直肠癌细胞的细胞毒作用和凋亡诱导:抗癌治疗的意义。
IF 1.4 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-01-01 Epub Date: 2025-02-14 DOI: 10.4103/JAPTR.JAPTR_427_23
Abdah Md Akim, Gul-E-Saba Chaudhry, Zeenia, Tan Weay Ken, Yeong Yik Sung, Tengku Sifzizul Tengku Muhammad

Colorectal cancer's escalating prevalence in Malaysia prompts the exploration of innovative anticancer agents; amidst this backdrop, tricyclohexyltin p-methoxycinnamate emerges as a synthesized organotin complex with unique bioactive properties. Notably, the novelty of this research lies in its groundbreaking investigation into the hitherto unexplored anticancer potential and mode of cell death induced by tricyclohexyltin p-methoxycinnamate on colon cancer (human colorectal adenocarcinoma cell line (HT-29)) cell lines. This study pioneers the assessment of tricyclohexyltin p-methoxycinnamate's cytotoxic effects through the "(3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide) assay," revealing a dose- and time-dependent cytotoxicity with IC50 values of 1.2 × 10-6M for 24 h, 1.0 × 10-6M for 48 h, and 5.0 × 10-7M for 72 h. The mode of cell death through "AO/PI" staining alongside cell cycle analysis, highlighting apoptosis as the predominant mode of cell death in the HT-29 cell line, accompanied by substantial cell cycle arrest at the sub-"G0" phase. The tricyclohexyltin p-methoxycinnamate's shown potential antiproliferative properties, cell cycle arrest, and apoptosis in HT-29 cancer cells. This novel insight into the compound's mode of action positions it as a promising candidate for future anticancer therapeutics. The study underscores the urgency of investigating innovative approaches amidst the rising colorectal cancer rates, emphasizing the compound's potential through further in-depth studies and preclinical trials.

结直肠癌在马来西亚的发病率不断上升,促使创新抗癌药物的探索;在此背景下,对甲氧基肉桂酸三环己基锡作为一种具有独特生物活性的有机锡配合物而出现。值得注意的是,本研究的新颖之处在于它开创性地探索了迄今为止尚未探索的三环己基锡对甲氧基肉桂酸对结肠癌(人结直肠癌细胞系(HT-29))细胞系的抗癌潜力和细胞死亡模式。本研究通过“(3-[4,5-二甲基噻唑-2-基]-2,5-二苯基溴化四唑)测定法”首次评估了对甲氧基肉桂酸三环己基锡的细胞毒性作用。显示出剂量和时间依赖性的细胞毒性,IC50值分别为1.2 × 10-6M(24小时)、1.0 × 10-6M(48小时)和5.0 × 10-7M(72小时)。通过“AO/PI”染色和细胞周期分析,细胞死亡模式显示,细胞凋亡是HT-29细胞系中主要的细胞死亡模式,伴随着亚“G0”期的大量细胞周期停滞。对甲氧基肉桂酸三环己基锡在HT-29癌细胞中显示出潜在的抗增殖、细胞周期阻滞和细胞凋亡特性。这种对化合物作用方式的新见解使其成为未来抗癌治疗的有希望的候选者。该研究强调了在结直肠癌发病率不断上升的情况下研究创新方法的紧迫性,强调了该化合物通过进一步深入研究和临床前试验的潜力。
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引用次数: 0
Screening of the most common MEFV variants in 416 patients of familial mediterranean fever living in Northwest of Iran. 伊朗西北部416例家族性地中海热患者中最常见MEFV变异的筛查
IF 1.4 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-01-01 Epub Date: 2025-02-14 DOI: 10.4103/JAPTR.JAPTR_22_24
Armin Gharibi, Esmaeil Babaei, Ali Vahabi

Familial Mediterranean Fever (FMF) is an inherited disorder with an autosomal recessive pattern of inheritance. FMF is the most prevalent among ethnic populations originating from the Mediterranean region and results from pathogenic mutations in the Mediterranean fever (MEFV) gene. For the materials and methods employed in this study, a total of 416 patients from the northwestern region of Iran were screened for the presence of 18 commonly occurring variants in the MEFV gene. The screening process involved the use of multiplex amplification-ligation polymerase chain reaction coupled with fluorescently labeled DNA probes. This technique enabled the detection of single nucleotide polymorphisms, which are variations in a single nucleotide base within the MEFV gene sequence. The initial manifestation of symptoms occurred between the ages of 1 and 20 years in 63.46% of the cases studied. The four most commonly observed clinical manifestations among the patients were abdominal pain, fever, joint pain, and vomiting. Molecular analysis of 18 prevalent MEFV variants in 416 FMF patients revealed the underlying genetic causes in 242 individuals. Out of these 242 cases, 129 patients (53.3%) were heterozygous carriers of a single pathogenic variant, 19 patients (7.8%) were homozygous for a single variant, 48 patients (19.83%) were compound heterozygotes harboring two different pathogenic variants, and 46 patients (19%) exhibited multiple variants, which were classified as complex cases. The R202Q variation emerged as the most prevalent among the four genotypic groups and exhibited the highest allele frequency (39.94%), followed by E148Q (20.62%), M694V (15.14%), and V726A (15.14%). Genetic profiling of MEFV variations revealed a predominance of R202Q, with E148Q, M694V, and V726A occurring in descending order of frequency. The allele frequency of the R202Q variant exhibited a statistically significant difference when compared to other ethnic groups, with the exception of the Turkish population. Interestingly, while the M694V variant is reported as the most prevalent in several other populations and ethnic groups, in our study cohort, it emerged as the third most common variant. This finding suggests that the frequencies of specific alleles can vary substantially across different countries, populations, and ethnic groups.

家族性地中海热(FMF)是一种常染色体隐性遗传的遗传病。FMF在地中海地区的少数民族人群中最为普遍,由地中海热(MEFV)基因的致病性突变引起。本研究采用的材料和方法,对来自伊朗西北地区的416名患者进行了MEFV基因18种常见变异的筛查。筛选过程包括使用多重扩增-连接聚合酶链反应与荧光标记的DNA探针相结合。该技术能够检测单核苷酸多态性,即MEFV基因序列中单个核苷酸碱基的变异。63.46%的病例最初症状表现在1 - 20岁之间。患者最常见的4种临床表现为腹痛、发热、关节痛和呕吐。对416例FMF患者18种流行MEFV变异的分子分析揭示了242例患者的潜在遗传原因。242例病例中,单一致病变异杂合携带者129例(53.3%),单一致病变异纯合携带者19例(7.8%),两种不同致病变异复合杂合携带者48例(19.83%),多致病变异46例(19%),属于复杂病例。4个基因型组中,R202Q变异最为普遍,等位基因频率最高(39.94%),其次是E148Q(20.62%)、M694V(15.14%)和V726A(15.14%)。MEFV变异的遗传分析显示,R202Q占优势,E148Q、M694V和V726A的出现频率由高到低。除土耳其人外,R202Q变异的等位基因频率与其他种族相比具有统计学上的显著差异。有趣的是,虽然M694V变异在其他几个人群和种族群体中最为普遍,但在我们的研究队列中,它是第三个最常见的变异。这一发现表明,特定等位基因的频率在不同的国家、人群和种族群体中可能存在很大差异。
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引用次数: 0
Mycochemical analysis and antibacterial activities of aqueous Kulat Pelawan (Heimioporus spp.) mushroom extracts. 白桦栗(Kulat Pelawan, Heimioporus spp.)菌液的真菌化学分析及抑菌活性。
IF 1.4 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-01-01 Epub Date: 2025-02-14 DOI: 10.4103/JAPTR.JAPTR_152_24
Sari Darmasiwi, Lucia Dhiantika Witasari, Alivia Nur Maysaroh, Arfista Deska Khairunnisa

The bioprospection of Heimioporus spp. has not been extensively explored because of its limited distribution and cultivation. This investigation aims to examine the proximate, mycochemicals, and antibacterial properties of aqueous Heimioporus spp. extracts. The dried mushroom was analyzed for nutritional content quantitatively, and mycochemicals were identified quantitatively. Antimicrobial activities were studied using disc diffusion assays and minimum inhibitory and bactericidal concentrations. Mushroom extracts were produced by maceration at 25°C ± 2°C for 48 h and boiled at 100°C for 30 min to yield cold aqueous extract (CAE) and hot aqueous extract (HAE), respectively, which were then tested against Escherichia coli, Staphylococcus aureus, and Propionibacterium acnes. The mycochemicals were analyzed for their alkaloids, flavonoids, terpenoids, and saponins. The study utilized ANOVA and DMRT statistical analysis software, with P < 0.05, to analyze the results. Results showed high protein (30.88%), carbohydrate (47.57%), and fat content (0.61%). The CAE showed higher antibacterial activity than the HAE against E. coli (9.67 ± 0.58 mm) and S. aureus (10.00 ± 0.00 mm) but no antibacterial activity against P. acnes (P < 0.05). The CAE had more mycochemicals than HAE. Results suggested that Heimioporus spp. is a potential functional food with health benefiits, which has high lipid, carbohydrate, and protein content. Its extracts revealed strong antibacterial properties against E. coli and S. aureus but no inhibition against P. acnes.

由于黑孔菌属的分布和栽培范围有限,其生物前景尚未得到广泛探讨。本研究的目的是研究海蚤水提取物的近似值、霉菌化学物质和抗菌性能。对其营养成分进行了定量分析,并对真菌化学物质进行了定量鉴定。采用圆盘扩散法和最低抑菌浓度和杀菌浓度研究其抑菌活性。在25°C±2°C条件下浸泡48 h,在100°C条件下煮沸30 min,分别得到冷水浸提物(CAE)和热水浸提物(HAE),然后对大肠杆菌、金黄色葡萄球菌和痤疮丙酸杆菌进行抑菌试验。分析真菌化学物质的生物碱、黄酮类、萜类和皂苷。采用方差分析和DMRT统计分析软件对结果进行分析,P < 0.05。结果:蛋白质(30.88%)、碳水化合物(47.57%)、脂肪(0.61%)含量高。CAE对大肠杆菌(9.67±0.58 mm)和金黄色葡萄球菌(10.00±0.00 mm)的抑菌活性高于HAE,但对痤疮链球菌(P < 0.05)没有抑菌活性。CAE比HAE有更多的真菌化学物质。研究结果表明,海螺具有较高的脂质、碳水化合物和蛋白质含量,是一种具有潜在保健价值的功能性食品。其提取物对大肠杆菌和金黄色葡萄球菌有较强的抑菌作用,但对痤疮杆菌无抑制作用。
{"title":"Mycochemical analysis and antibacterial activities of aqueous Kulat Pelawan (<i>Heimioporus</i> spp.) mushroom extracts.","authors":"Sari Darmasiwi, Lucia Dhiantika Witasari, Alivia Nur Maysaroh, Arfista Deska Khairunnisa","doi":"10.4103/JAPTR.JAPTR_152_24","DOIUrl":"10.4103/JAPTR.JAPTR_152_24","url":null,"abstract":"<p><p>The bioprospection of <i>Heimioporus</i> spp. has not been extensively explored because of its limited distribution and cultivation. This investigation aims to examine the proximate, mycochemicals, and antibacterial properties of aqueous <i>Heimioporus</i> spp. extracts. The dried mushroom was analyzed for nutritional content quantitatively, and mycochemicals were identified quantitatively. Antimicrobial activities were studied using disc diffusion assays and minimum inhibitory and bactericidal concentrations. Mushroom extracts were produced by maceration at 25°C ± 2°C for 48 h and boiled at 100°C for 30 min to yield cold aqueous extract (CAE) and hot aqueous extract (HAE), respectively, which were then tested against <i>Escherichia coli</i>, <i>Staphylococcus</i> <i>aureus,</i> and <i>Propionibacterium acnes.</i> The mycochemicals were analyzed for their alkaloids, flavonoids, terpenoids, and saponins. The study utilized ANOVA and DMRT statistical analysis software, with <i>P</i> < 0.05, to analyze the results. Results showed high protein (30.88%), carbohydrate (47.57%), and fat content (0.61%). The CAE showed higher antibacterial activity than the HAE against <i>E. coli</i> (9.67 ± 0.58 mm) and <i>S. aureus</i> (10.00 ± 0.00 mm) but no antibacterial activity against <i>P. acnes</i> (<i>P</i> < 0.05). The CAE had more mycochemicals than HAE. Results suggested that <i>Heimioporus</i> spp. is a potential functional food with health benefiits, which has high lipid, carbohydrate, and protein content. Its extracts revealed strong antibacterial properties against <i>E. coli</i> and <i>S. aureus</i> but no inhibition against <i>P. acnes.</i></p>","PeriodicalId":14877,"journal":{"name":"Journal of Advanced Pharmaceutical Technology & Research","volume":"16 1","pages":"42-46"},"PeriodicalIF":1.4,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11960825/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143772703","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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Journal of Advanced Pharmaceutical Technology & Research
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