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Six Phthalides as Potent Modulators of the Blood Tumor Barrier Increase the Transmembrane Transport of Compatible Compounds Via Transcellular and Paracellular Pathways 作为血液肿瘤屏障强效调节剂的六种邻苯二甲酸酯类化合物可通过跨细胞和细胞外途径增加兼容化合物的跨膜转运
IF 0.9 4区 医学 Q4 CHEMISTRY, MEDICINAL Pub Date : 2024-04-17 DOI: 10.1007/s11094-024-03103-3
Xiao-jin Liu, Shu-yuan Shuai, Guo-song Zhang, Qin Zheng, Peng-yi Hu, Zi-qi Li, Ri-qun Liu, Shu-hua Xiao

The treatment of brain tumors is greatly limited due to the presence of the blood tumor barrier (BTB). Our previous research has shown that the essential oil of chuanxiong promoted temozolomide entry into glioma cells and enhanced temozolomide-induced anticancer efficiency in vivo. Phthalides account for the largest proportion of essential oil and, therefore, this study was conducted to investigate the effects of six phthalides on the transmembrane transport of compatible compounds across the BTB and the mechanism. The results showed that different concentrations of senkyunolide H (SH), senkyunolide A (SA), ligustilide (LIG), butylidenephthalide (BP), n-butylphthalide (NBP) and neocnidilide (NOL) significantly increase the permeability from A (apical side) to B (basolateral side) (Papp(AB)) of fluorescein isothiocyanate 4000 (FITC4000), while NBP, NOL and SA could also significantly increase Papp(B→A). Western blot analysis indicated that these phthalides down-regulated expressions of claudin-5, occludin and ZO-1 to increase the permeability of BTB. LIG, SA, SH, NBP and NOL significantly increased Papp(AB) and the efflux ratio of the P-gp substrate rhodamine 123 attribute to down-regulate the expressions of P-gp. The expression of caveolin-1 was also down-regulated by the six phthalides. LIG, SA, SH, NBP and NOL acted as effective absorption enhancers in BTB via both the transcellular route and the paracellular route.

由于血肿瘤屏障(BTB)的存在,脑肿瘤的治疗受到很大限制。我们之前的研究表明,川芎精油能促进替莫唑胺进入胶质瘤细胞,提高替莫唑胺诱导的体内抗癌效率。邻苯二甲酸酯类化合物在精油中所占比例最大,因此,本研究对六种邻苯二甲酸酯类化合物对相容化合物跨 BTB 跨膜转运的影响及其机制进行了研究。结果表明,不同浓度的番木鳖内酯 H(SH)、番木鳖内酯 A(SA)、藁本内酯(LIG)、亚丁基邻苯二甲酸丁酯(BP)n-butylphthalide (NBP) 和 neocnidilide (NOL) 能显著提高异硫氰酸荧光素 4000(FITC4000)从 A(顶端)到 B(基底侧)的通透性(Papp(AB)),而 NBP、NOL 和 SA 也能显著提高 Papp(B→A)。Western 印迹分析表明,这些酞类化合物下调了 claudin-5、occludin 和 ZO-1 的表达,从而增加了 BTB 的通透性。LIG、SA、SH、NBP 和 NOL 能显著增加 P-gp底物罗丹明 123 属性的 Papp(AB)和外流比,从而下调 P-gp 的表达。六种邻苯二甲酸盐还下调了洞穴素-1的表达。LIG、SA、SH、NBP和NOL通过跨细胞途径和旁细胞途径在BTB中起到了有效的吸收促进作用。
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引用次数: 0
Study of the Pressing Process of N-Butyl-N-Methyl-1-Phenylpyrrolo-[1,2-a]Pyrazine-3-Carboxamide (GML-3) Tablets Using Mathematical Modeling Techniques 利用数学建模技术研究 N-丁基-N-甲基-1-苯基吡咯并[1,2-a]吡嗪-3-甲酰胺(GML-3)片剂的压片工艺
IF 0.9 4区 医学 Q4 CHEMISTRY, MEDICINAL Pub Date : 2024-04-17 DOI: 10.1007/s11094-024-03107-z
V. B. Markeev, S. V. Tishkov, E. V. Blynskaya, K. V. Alekseev

N-Butyl-N-methyl-1-phenylpyrrolo[1,2-a]pyrazine-3-carboxamide (GML-3) is an original molecule developed at the Research Zakusov Institute of Pharmacology. GML-3 has both anxiolytic and antidepressant activity, which makes the development of tablets based on it a promising task. Optimization of the pressing process is currently an urgent task of the pharmaceutical industry because this technological stage has a significant impact on the disintegration of tablets and the release of the active pharmaceutical ingredient. The Heckel and Kuenz–Leuenberger models were used to study the pressing process of GML-3 tablets. These models were compared to select the most reliable description of pressing GML-3 tablets from granules. Granules with polyvinylpyrrolidone (PVP) and hydroxypropylmethylcellulose (HPMC) as a binder were used.

N-丁基-N-甲基-1-苯基吡咯并[1,2-a]吡嗪-3-甲酰胺(GML-3)是扎库索夫药理学研究所开发的一种原创分子。GML-3 同时具有抗焦虑和抗抑郁活性,因此开发以其为基础的片剂前景广阔。压片工艺的优化是制药业当前的一项紧迫任务,因为这一技术阶段对片剂的崩解和活性药物成分的释放有重大影响。Heckel 模型和 Kuenz-Leuenberger 模型被用来研究 GML-3 片剂的压片工艺。通过对这些模型进行比较,选出了最能可靠描述从颗粒压制 GML-3 片剂的模型。使用聚乙烯吡咯烷酮(PVP)和羟丙基甲基纤维素(HPMC)作为粘合剂的颗粒。
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引用次数: 0
Chemical Composition and Antioxidant Activity of Petroleum Ether Extract from Kaempferia galanga L. 山奈石油醚提取物的化学成分和抗氧化活性
IF 0.9 4区 医学 Q4 CHEMISTRY, MEDICINAL Pub Date : 2024-04-17 DOI: 10.1007/s11094-024-03101-5
Zhaobao Xiang, Xueli Ping, Pengfei Chen, Linfeng You, Bin Zhou

Kaempferia galanga L. (KGL) from Hainan, China was extracted by ultrasonic-assisted extraction with 90% ethanol solution, and then extracted with petroleum ether after the ethanol extract was recovered to be alcohol free. The antioxidant activity of the petroleum ether fraction of KGL was first tested using the ABTS method. GC-MS was used to analyze the chemical constituents of the petroleum ether fraction. The scavenging effect on ABTS free radicals of the petroleum ether fraction was weak, indicating that the antioxidant activity of the petroleum ether fraction was moderate. A total of 25 chemical components were identified by GC-MS analysis. The main components with higher content were 2,6,11-trimethyl dodecane, ethyl p-methoxy cinnamate, and ethyl cinnamate, which accounted for 81.64%. Furthermore, 11 kinds of constituents of the petroleum ether extract were obtained from KGL for the first time. This experiment clarifies firstly the main chemical composition of petroleum ether fraction from KGL, which provides some scientific basis for the further exploration and use of petroleum ether fraction from KGL and the comparative analysis of the chemical composition of KGL in different regions.

用 90% 的乙醇溶液超声辅助提取中国海南的山奈(KGL),乙醇提取液回收至无醇后再用石油醚提取。首先用 ABTS 法检测了 KGL 石油醚馏分的抗氧化活性。采用 GC-MS 分析石油醚馏分的化学成分。石油醚馏分对 ABTS 自由基的清除作用较弱,表明石油醚馏分的抗氧化活性适中。通过气相色谱-质谱分析,共鉴定出 25 种化学成分。含量较高的主要成分是 2,6,11-三甲基十二烷、对甲氧基肉桂酸乙酯和肉桂酸乙酯,占 81.64%。此外,还首次从 KGL 中获得了 11 种石油醚提取物成分。该实验首次明确了KGL石油醚馏分的主要化学成分,为KGL石油醚馏分的进一步开发利用和不同地区KGL石油醚馏分化学成分的对比分析提供了一定的科学依据。
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引用次数: 0
Utilization of Phytochemicals as Nutraceutical in the Prophylaxis of Dengue 利用植物化学物质作为预防登革热的保健品
IF 0.9 4区 医学 Q4 CHEMISTRY, MEDICINAL Pub Date : 2024-04-17 DOI: 10.1007/s11094-024-03105-1
Jyoti Baranwal, Swastika Singh, Smriti Kushwaha, Archana Jyoti

Every year, during the monsoon season, dengue, an infectious disease transmitted by the Aedes aegypti mosquito and caused by the dengue virus, occurs. The frequency and prevalence of dengue fever, as well as deaths from its consequences, have increased dramatically in recent years. Despite the fact that the infection has affected a large number of people worldwide, no specific and efficient drug treatment is known. Researchers are working tirelessly to find a cure, focusing their efforts on developing therapeutic treatments that block or inhibit the activity of specific Dengue virus (DENV) proteins. This review focuses on the phytochemical constituents present in traditionally used natural remedies for the treatment of dengue such as papaya leaf extract, goat milk, kiwi fruit, dragon fruit, and coconut water. Undoubtedly, the contents of this review will motivate researchers to do more novel work in this area which will accelerate the journey towards the exploration of the pharmacological activity of natural compounds.

每年的季风季节都会发生登革热,这是一种由登革热病毒引起、由埃及伊蚊传播的传染病。近年来,登革热的发病率和流行率以及因登革热导致的死亡人数急剧上升。尽管感染登革热的人数在全球范围内居高不下,但目前尚无有效的特效药物。研究人员正孜孜不倦地寻找治疗方法,致力于开发能阻断或抑制特定登革热病毒(DENV)蛋白活性的治疗方法。这篇综述的重点是木瓜叶提取物、羊奶、奇异果、火龙果和椰子汁等传统用于治疗登革热的天然疗法中的植物化学成分。毫无疑问,这篇综述的内容将激励研究人员在这一领域开展更多新颖的工作,从而加快探索天然化合物药理活性的进程。
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引用次数: 0
Prospects of Creating Collagen Substances Based on a Study of the Physical and Chemical Characteristics of Proteins of Hydrobiont Dermal Emulsions 根据对 Hydrobiont 皮肤乳液蛋白质的物理和化学特性的研究创建胶原蛋白物质的前景
IF 0.9 4区 医学 Q4 CHEMISTRY, MEDICINAL Pub Date : 2024-04-17 DOI: 10.1007/s11094-024-03108-y
S. S. Antipov, D. V. Tarasova, M. M. Borodina, M. V. Likhodzievskaya, D. A. Cherenkov, T. N. Khmelevskaya, L. V. Antipova, V. G. Artyukhov

Proteins of the collagen family were identified in the dermal emulsion of a freshwater fish, the African clary catfish (Clarias gariepinus). Acumulative assessment of their physicochemical properties gave reason to consider the emulsion obtained using the developed method as a source of functional biopolymers, particularly collagen proteins. The fractional composition, charge state, molecular mass, and the ability for hydrolysis by Clostridium histolytica collagenase were experimentally determined. Evaluation of the amino-acid composition allowed the analogy and features of collagen proteins of animal and fish origin to be identified. The studied emulsions were shown to contain negatively charged proteins with molecular masses >100 kDa, the fractions of which contained predominantly collagen. The results supported the assumption that a significant part of the hydrobiont collagen was type I collagen, which made it possible to consider them in the future as a basis for various substances and served as a starting point for understanding the physicochemical functioning essentials and assessing the possibility of using them in pharmaceutical technologies.

在淡水鱼非洲鲶鱼(Claras gariepinus)的真皮乳液中发现了胶原蛋白家族的蛋白质。对其理化性质的累积评估表明,有理由将使用所开发方法获得的乳液视为功能性生物聚合物(尤其是胶原蛋白)的来源。实验测定了胶原蛋白的部分组成、电荷状态、分子质量以及组织溶解梭菌胶原酶的水解能力。通过对氨基酸组成的评估,确定了动物和鱼类胶原蛋白的类比和特征。研究表明,所研究的乳液中含有分子质量为 100 kDa 的带负电荷的蛋白质,其中的馏分主要含有胶原蛋白。研究结果支持这样的假设,即水生生物胶原蛋白的很大一部分是 I 型胶原蛋白,这使得将来有可能将其视为各种物质的基础,并作为了解其物理化学功能本质和评估将其用于制药技术的可能性的起点。
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引用次数: 0
In-Vitro Effect of Ammodaucus Leucotrichus Flower and Fruit Essential Oils on Nitric Oxide Production and Arginase Activity in Human Peripheral Blood Mononuclear Cells (PBMC) from Patients with Behçet Disease Ammodaucus Leucotrichus 花和果精油对白塞氏病患者外周血单核细胞(PBMC)一氧化氮生成和精氨酸酶活性的体外效应
IF 0.9 4区 医学 Q4 CHEMISTRY, MEDICINAL Pub Date : 2024-04-17 DOI: 10.1007/s11094-024-03104-2
Djamel Messaoudene, Nourelhouda Ghozali, Hayet Neghliz, Tarek Benabdelkader, Houda Belguendouz, Malika Terahi, Fifi Otmani, Chafia Touil-Boukoffa

Ammodaucus leucotrichus is an Algerian aromatic medicinal plant, widely known as “Oum-draiga or Kamoune-l’ibel”. In folk medicine, the flower and fruit of this plant are widely used for the treatment of cough, fever, diarrhea, colic, and cold. In this study, we describe for the first time the modulatory effects of flower and fruit essential oils (EOs) of A. leucotrichus subsp. leucotrichus on NOS and Arginase activities and their regulation during Behçet disease, an auto-inflammatory vasculitis of unknown etiology. The EOs were obtained by Clevenger-hydrodistillation and their chemical composition was analyzed by gas chromatography-mass spectrometry (GC-MS). The peripheral blood mononuclear cells of 20 patients and 15 control samples (PBMC) were cultured in RPMI-1640 and incubated with or without seeds and the flowers’ essential oil from A. leucotrichus was dissolved in DMSO (0.01%). Culture supernatants were harvested after 24 h of incubation. NO and urea measurements were, respectively, performed by modified Griess and Berthelot methods. Our results show that essential oils for both fruits and flowers significantly reduce the production of NO production in a concentration-dependent manner. In contrast, significantly increased urea was noted in treated PBMC of BD patients. Our study suggests that EOs extracted from the flower and fruit of A. leucotrichus could have potential immuno-modulatory effects characterized by a down-regulation and up-regulation of NO and urea, respectively, probably by NOS/Arginase balance regulation.

Ammodaucus leucotrichus 是阿尔及利亚的一种芳香药用植物,被广泛称为 "Oum-draiga 或 Kamoune-l'ibel"。在民间医学中,这种植物的花和果实被广泛用于治疗咳嗽、发烧、腹泻、腹绞痛和感冒。在这项研究中,我们首次描述了白千层子花和果实精油(EOs)对 NOS 和精氨酸酶活性的调节作用,以及它们在白塞病(一种病因不明的自身炎症性血管炎)中的调节作用。这些环氧乙烷是通过克莱文格尔蒸馏法获得的,其化学成分通过气相色谱-质谱法(GC-MS)进行了分析。将 20 例患者和 15 例对照样本的外周血单核细胞(PBMC)在 RPMI-1640 中培养,并与或不与种子一起培养。培养 24 小时后收获培养上清。分别采用改良的格里斯法和贝特洛法测定氮氧化物和尿素。我们的结果表明,果实和花的精油都能以浓度依赖的方式显著降低 NO 的产生。与此相反,经处理的 BD 患者血浆细胞中尿素明显增加。我们的研究表明,从白花蛇舌草的花和果实中提取的环氧乙烷可能具有潜在的免疫调节作用,其特点是分别下调和上调 NO 和尿素,可能是通过 NOS/Arginase 平衡调节。
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引用次数: 0
Synthesis, Characterization and Biological Evaluation of Novel Benzimidazole Derivatives against Candida albicans 新型苯并咪唑衍生物对白色念珠菌的合成、表征和生物学评价
IF 0.9 4区 医学 Q4 CHEMISTRY, MEDICINAL Pub Date : 2024-04-17 DOI: 10.1007/s11094-024-03099-w
Monika Chauhan, Shivani Gupta, Sarvesh Paliwal, Sumitra Nain

In heterocyclic chemistry, benzimidazole is recognized as a “privileged structure” due to its association with a wide range of biological activities. In this present research work, we included the synthesis, characterization and biological evaluation of substituted derivatives. The designated derivatives were synthesized by the condensation method. ortho-Phenylenediamine was used as the starting material. The designated benzimidazole derivatives were synthesized using different acids and aldehydes. Further, the in-vitro antifungal-activity-synthesized compounds were evaluated against Candida albicans using the agar well diffusion method and the culture tube method. It was concluded that all the designated derivatives of benzimidazole exhibited prominent antifungal activity and can be considered as potent leads in future antifungal research.

在杂环化学中,苯并咪唑是公认的 "特权结构",因为它具有广泛的生物活性。在本研究工作中,我们对取代衍生物进行了合成、表征和生物学评价。这些指定的衍生物是通过缩合法合成的,起始原料为邻苯二胺。使用不同的酸和醛合成了指定的苯并咪唑衍生物。此外,还采用琼脂井扩散法和培养管法对合成的化合物对白色念珠菌的体外抗真菌活性进行了评估。结果表明,所有指定的苯并咪唑衍生物都具有突出的抗真菌活性,可作为未来抗真菌研究的有效线索。
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引用次数: 0
Development of a Quantitative Determination Method for Polysorbate 80 in Biologicals by Size-Exclusion High-Performance Liquid Chromatography 利用尺寸排阻高效液相色谱法开发生物制品中聚山梨醇酯 80 的定量检测方法
IF 0.9 4区 医学 Q4 CHEMISTRY, MEDICINAL Pub Date : 2024-04-17 DOI: 10.1007/s11094-024-03110-4
O. B. Rounova, M. G. Korotkov, O. B. Ustinnikova

Aquantitative determination method for polysorbate 80 in biological medicinal preparations using size-exclusion chromatography with UV detection was developed. OASIS HLB solid-phase extraction cartridges were used to extract polysorbate 80 from formulations with high protein concentrations. The HPLC separation was performed using a TSKgel G2000SWX column in isocratic mode. The mobile phase was phosphate buffer (0.1 M) containing sodium sulfate (0.1 M) and sodium dodecyl sulfate (0.1%). The developed method could be used for quantitative determination of polysorbate 80 in biological medicinal products.

采用尺寸排阻色谱-紫外检测法,建立了生物药剂中聚山梨酯 80 的定量测定方法。使用 OASIS HLB 固相萃取柱从蛋白质浓度较高的制剂中萃取聚山梨醇酯 80。在等度模式下,使用 TSKgel G2000SWX 色谱柱进行高效液相色谱分离。流动相为含硫酸钠(0.1 M)和十二烷基硫酸钠(0.1%)的磷酸盐缓冲液(0.1 M)。所建立的方法可用于生物药品中聚山梨酯80的定量检测。
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引用次数: 0
Synthesis of 5,5′-(Disulfanediyl)bis[3-phenyl-1,3,4-thiadiazole-2(3H)-thione] and Study of Its Anti-Inflammatory Activity 5,5′-(二硫二基)双[3-苯基-1,3,4-噻二唑-2(3H)-硫酮]的合成及其抗炎活性研究
IF 0.9 4区 医学 Q4 CHEMISTRY, MEDICINAL Pub Date : 2024-04-16 DOI: 10.1007/s11094-024-03094-1
G. S. Shakirzyanova, L. Yu. Izotova, O. Kh. Kholbekov, F. Yu. Zhaloliddinov, G. G. Rakhmonova, B. N. Babaev

5,5′-(Disulfanediyl)bis[3-phenyl-1,3,4-thiadiazole-2(3H)-thione] was synthesized by oxidative condensation in the presence of chloride ions. The structure of the resulting compound was identified by an x-ray crystal structure analysis, for which the crystallographic data were obtained. The anti-inflammatory activity of the synthesized disulfide was studied for the first time in a carrageenan edema model. 5,5′-(Disulfanediyl)bis[3-phenyl-1,3,4-diazole-2(3H)-thione] was shown to have anti-inflammatory and antiexudative activity at doses of 10 and 20 mg/kg. Its effect was close to that of the drug Nimesil.

在氯离子存在下,通过氧化缩合合成了 5,5′-(二磺酰基)双[3-苯基-1,3,4-噻二唑-2(3H)-硫酮]。通过 X 射线晶体结构分析确定了所得化合物的结构,并获得了晶体学数据。首次在角叉菜胶水肿模型中研究了合成二硫化物的抗炎活性。结果表明,5,5′-(二硫化二基)双[3-苯基-1,3,4-二唑-2(3H)-硫酮]在剂量为 10 和 20 毫克/千克时具有抗炎和抗渗出活性。其效果接近于药物 Nimesil。
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引用次数: 0
Acetaminophen and Thiosalicylic Acid Sensor Based on Carbon Paste Electrode Modified with Multi-Walled Carbon Nanotubes and Natural Deep Eutectic Solvent 基于多壁碳纳米管和天然深共晶溶剂修饰的碳浆电极的对乙酰氨基酚和硫代水杨酸传感器
IF 0.9 4区 医学 Q4 CHEMISTRY, MEDICINAL Pub Date : 2024-04-16 DOI: 10.1007/s11094-024-03090-5
Ebrahim Zarei, Maryam Vafadar, Alireza Asghari

A carbon paste electrode (CPE) modified with multi-walled carbon nanotubes (MWCNTs) and natural deep eutectic solvent (NADES) was prepared and applied for the simultaneous voltammetric determination of acetaminophen (ACP) and thiosalicylic acid (TSA) in real samples. Electrochemical impedance spectroscopy (EIS) was applied for investigation of electron transfer rate of [Fe(CN)6]3-/4- as a redox couple probe on the MWCNTs/NADES/CPE surface. The modified electrode preserved and combined the properties of individual modifiers synergistically. Significant enhancement in the peak current responses of ACP and TSA were observed at the modified electrode compared to the bare electrode. Under the optimal conditions, a linear dynamic range of 5–2900 μM for ACP and 5–2250 μM for TSA was obtained. The limit of detection (LOD) for ACP and TSA were 4.71 μM and 4.35 μM, respectively. Finally, this method was successfully employed for the determination of ACP and TSA in real samples.

制备了用多壁碳纳米管(MWCNTs)和天然深共晶溶剂(NADES)修饰的碳浆电极(CPE),并将其用于同时伏安法测定实际样品中的对乙酰氨基酚(ACP)和硫代水杨酸(TSA)。电化学阻抗光谱(EIS)被用于研究 MWCNTs/NADES/CPE 表面作为氧化还原偶探针的[Fe(CN)6]3-/4-的电子转移率。改性电极保留并协同结合了单个改性剂的特性。与裸电极相比,修饰电极上 ACP 和 TSA 的峰值电流响应显著增强。在最佳条件下,ACP 和 TSA 的线性动态范围分别为 5-2900 μM 和 5-2250 μM。ACP 和 TSA 的检出限(LOD)分别为 4.71 μM 和 4.35 μM。最后,该方法被成功地应用于实际样品中 ACP 和 TSA 的测定。
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引用次数: 0
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Pharmaceutical Chemistry Journal
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