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Impact of radish seeds (Semen Raphani) on the absorption and transportation of ginsenosides in the Caco-2 cell model: a UPLC-ESI-MS analysis. 萝卜籽(Semen Raphani)对人参皂苷在 Caco-2 细胞模型中的吸收和运输的影响:UPLC-ESI-MS 分析。
IF 1.7 3区 医学 Q2 Medicine Pub Date : 2024-06-13 DOI: 10.1080/10286020.2024.2366008
Hui Li, Wen-Shuo Zhang, Rui Liu, Wei Wang, Li-Li Jiao, Zhi Liu, Wei Wu

This study examined the impact of Semen raphani on the absorption of ginsenosides from Panax ginseng C.A. Meyer (ginseng) using a Caco-2 cell model and Ultra-High-Performance Liquid Chromatography-Electrospray Ionization-Tandem Mass Spectrometry (UPLC-ESI-MS). Six primary ginsenosides (Rg1, Re, Rb1, Rb2, Rc, Rd) were quantified. Results showed that Semen Raphani increased the efflux rate of ginsenosides, particularly at higher concentrations, suggesting it inhibits their absorption. The research elucidates the intestinal absorption process of ginsenosides and the antagonistic mechanism of Semen Raphani against ginseng.

本研究利用 Caco-2 细胞模型和超高效液相色谱-电喷雾离子化-串联质谱法(UPLC-ESI-MS)研究了 Semen raphani 对人参中人参皂苷吸收的影响。对六种主要人参皂甙(Rg1、Re、Rb1、Rb2、Rc、Rd)进行了定量分析。结果表明,人参皂苷的外流率增加,尤其是在浓度较高的情况下,这表明它抑制了人参皂苷的吸收。该研究阐明了人参皂苷的肠道吸收过程以及半枝莲对人参的拮抗机制。
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引用次数: 0
Three new flavonoids from the roots of Sophora tonkinensis. 从越南槐根中提取的三种新黄酮类化合物。
IF 1.7 3区 医学 Q2 Medicine Pub Date : 2024-06-11 DOI: 10.1080/10286020.2024.2364909
Xiao-Yun Yan, Rui Zhang, Ya-Nan Yang, Zi-Ming Feng, Jian-Shuang Jiang, Xiang Yuan, Dong-Mei Wang, Guo-Cheng Wang, Xu Zhang, Pei-Cheng Zhang

Three new flavonoids including two isoflavanones sophortones A and B (1 and 2), and one chalcone sophortone C (3) were isolated from the roots of Sophora tonkinensis. Their structures were established by UV, IR, HRESIMS, and NMR data. The absolute configurations of 1 and 2 were determined by electronic circular dichroism (ECD) calculations.

从根国槐中分离出了三种新的黄酮类化合物,包括两种异黄烷酮类植物黄酮 A 和 B(1 和 2),以及一种查尔酮类植物黄酮 C(3)。通过紫外、红外、HRESIMS 和核磁共振数据确定了它们的结构。通过电子圆二色性(ECD)计算确定了 1 和 2 的绝对构型。
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引用次数: 0
Modeling and biological evaluation of pegmolesatide, a novel and potent erythropoiesis-stimulating agent. 一种新型强效红细胞生成刺激剂 pegmolesatide 的建模和生物学评估。
IF 1.7 3区 医学 Q2 Medicine Pub Date : 2024-06-11 DOI: 10.1080/10286020.2024.2362376
En-Jia Zhou, Xu-Li Lang, Min-Jian Yang, Han-Yu Sun, Meng-Yao Hao, Jing Jin, Bao-Lian Wang, Ai-Jun Li, Xiao-Jian Wang

Pegmolesatide, a synthetic, polyethylene-glycolylated, peptide-based erythropoiesis-stimulating agent (ESA), has been recently approved in China. Pegmolesatide is derived from the structure of endogenous erythropoietin (EPO), a natural product in mammals. This study compared the in vitro effects and selectivity of pegmolesatide to those of recombinant EPO and carbamylated EPO (CEPO) through computer-aided analyses and biological tests. The findings indicate that pegmolesatide exhibited the same stimulating effect on erythropoiesis as EPO with fewer side effects than EPO and CEPO.

聚乙二醇化肽基合成红细胞生成刺激剂(ESA)--聚乙二醇化肽(Pegmolesatide)最近在中国获得批准。Pegmolesatide是从哺乳动物体内的天然产物--内源性促红细胞生成素(EPO)的结构中提取出来的。本研究通过计算机辅助分析和生物试验,比较了培高乐塞与重组 EPO 和氨甲酰化 EPO(CEPO)的体外效应和选择性。研究结果表明,与 EPO 和 CEPO 相比,pegmolesatide 对红细胞生成的刺激作用与 EPO 相同,但副作用较小。
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引用次数: 0
Lycium barbarum polysaccharides regulate the gut microbiota to modulate metabolites in high-fat diet-induced obese rats 枸杞多糖调节肠道微生物群,从而调节高脂饮食诱导的肥胖大鼠体内的代谢物。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2024-06-10 DOI: 10.1080/10286020.2024.2355130

Lycium Barbarum Polysaccharides (LBP) can benefit lipid parameters such as total cholesterol, triglyceride, and high-density lipoprotein levels and upregulate the level of Firmicutes, increase the diversity of gut microbiota and reduce metabolic disorders, finally relieving weight gain of obese rats. But it cannot reverse the outcome of obesity. Over 30 differential metabolites and four pathways are altered by LBP.

枸杞多糖对总胆固醇、甘油三酯和高密度脂蛋白等血脂指标有益处,并能提高固醇菌的水平,增加肠道微生物群的多样性,减少代谢紊乱,最终缓解肥胖大鼠的体重增加。但它无法逆转肥胖的结果。枸杞多糖改变了 30 多种不同的代谢物和四种途径。
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引用次数: 0
Possible mechanism for the protective effect of active ingredients of astragalus membranaceus on diabetes nephropathy. 黄芪有效成分对糖尿病肾病的保护作用的可能机制。
IF 1.7 3区 医学 Q2 Medicine Pub Date : 2024-06-10 DOI: 10.1080/10286020.2024.2364350
Yu Li, Jing Wang

Astragali Radix (AR), a common traditional Chinese medicinal herb, exhibits protective effects on diabetic nephropathy (DN) in extensive researches. Aticles focusing on AR in PubMed were collected and reviewed in order to summarize the latest pharmacological effects on DN. The action mechanisms for protectiving effects of AR were associated with regulation of anti-fibrosis, anti-inflammation, anti-oxidative stress, anti-podocyte apoptosis, restoration of mitochondrial function, restoration of endothelial function in diabetes nephropathy experimental models. Consequently, AR hold promise as potential novel therapeutics for the treatment of DN.

黄芪(Aragali Radix,AR)是一种常见的中药材,大量研究表明其对糖尿病肾病(DN)具有保护作用。为了总结黄芪对糖尿病肾病的最新药理作用,我们收集并查阅了 PubMed 上有关黄芪的文章。AR 保护作用的作用机制与糖尿病肾病实验模型中的抗纤维化、抗炎、抗氧化应激、抗结节细胞凋亡、线粒体功能恢复、内皮功能恢复有关。因此,AR有望成为治疗糖尿病肾病的潜在新型疗法。
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引用次数: 0
Design, synthesis, and anti-oomycete activity of 3-acyloxymaltol/ethyl maltol derivatives 3-acyloxymaltol/ethyl maltol 衍生物的设计、合成和抗霉菌活性。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2024-06-10 DOI: 10.1080/10286020.2024.2355144

Twenty 3-acyloxymaltol/ethyl maltol derivatives (7a-j and 8a-j) were synthesized and evaluated in vitro for their anti-oomycete activity against Phytophthora capsici, respectively. Among all of twenty derivatives, more than half of the compounds 7f, 7h, 8a-h and 8j had anti-oomycete activity higher than the positive control zoxamide (EC50 = 22.23 mg/L), and the EC50 values of 18.66, 20.32, 12.80, 16.18, 10.59, 14.98, 16.80, 10.36, 15.32, 12.64, and 13.59 mg/L, respectively. Especially, compounds 8c and 8f exhibited the best anti-oomycete activity against P. capsici with EC50 values of 10.59 and 10.36 mg/L, respectively. Overall, hydroxyl group of maltol/ethyl maltol is important active modification site.

合成了 20 种 3-乙酰氧基麦芽酚/乙基麦芽酚衍生物(7a-j 和 8a-j),并分别在体外评估了它们对蝙蝠蛾属真菌的抗真菌活性。在所有 20 个衍生物中,超过半数的化合物 7f、7h、8a-h 和 8j 的抗真菌活性高于阳性对照佐酰胺(EC50 = 22.23 mg/L),EC50 值分别为 18.66、20.32、12.80、16.18、10.59、14.98、16.80、10.36、15.32、12.64 和 13.59 mg/L。特别是化合物 8c 和 8f 对荚膜蘑菇菌的抗真菌活性最好,EC50 值分别为 10.59 和 10.36 毫克/升。总之,麦芽酚/乙基麦芽酚的羟基是重要的活性修饰位点。
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引用次数: 0
Three new antinociceptive diterpenoids from the fruits of Rhododendron molle 杜鹃花果实中的三种新的抗痛觉二萜类化合物。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2024-06-08 DOI: 10.1080/10286020.2024.2345826

Investigation of the fruits of Rhododendron molle G. Don led to the isolation of three new grayanane-type diterpenoids, rhodomolleins LIV-LVI (1-3). The structures and absolute configurations of new compounds were fully elucidated by spectroscopic analysis and single-crystal X-ray diffraction, including HRESIMS, 1 D and 2 D NMR data. Compounds 1-3 were evaluated for analgesic activities utilizing an acetic acid-induced writhing test in mice. Compound 1 showed a significant antinociceptive effect with writhe inhibition rates of 72.9% and 100% at doses of 6 mg/kg and 20 mg/kg in mice, respectively. The binding mode of 1 to N-ethylmaleimide-sensitive factor (NSF, PDB: 6IP2) was explored by molecular docking, indicating the presence of hydrogen bond interactions which account for its analgesic activity.

通过对杜鹃花果实(Rhododendron molle G. Don)的研究,我们分离出了三种新的灰岩型二萜类化合物,即杜鹃花苷 LIV-LVI(1-3)。通过光谱分析和单晶 X 射线衍射,包括 HRESIMS、1 D 和 2 D NMR 数据,完全阐明了新化合物的结构和绝对构型。利用醋酸诱导的小鼠蠕动试验评估了化合物 1-3 的镇痛活性。化合物 1 显示出了明显的镇痛效果,在剂量为 6 毫克/千克和 20 毫克/千克时,对小鼠的蠕动抑制率分别为 72.9% 和 100%。通过分子对接研究了化合物 1 与 N-乙基马来酰亚胺敏感因子(NSF,PDB:6IP2)的结合模式,结果表明氢键相互作用是其镇痛活性的原因。
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引用次数: 0
Enantioselective formal total synthesis of dihydrospirotryprostatin B 二氢螺前列素 B 的对映体选择性正式全合成。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2024-06-01 DOI: 10.1080/10286020.2024.2355504

Spirotryprostatins are representative members of medicinally interesting bioactive molecules of the spirooxindole natural products. In this communication, we present a novel enantioselective total synthesis of the spirooxindole alkaloid dihydrospirotryprostatin B. The synthesis takes advantage of copper-catalyzed tandem reaction of o-iodoanilide chiral sulfinamide derivatives with alkynone to rapidly construct the key quaternary carbon stereocenter of the natural product dihydrospirotryprostatin B.

螺旋前列腺素是螺旋吲哚类天然产物中具有药用价值的生物活性分子的代表成员。该合成利用铜催化的邻碘苯胺手性亚磺酰胺衍生物与炔酮的串联反应,快速构建了天然产物二氢螺螺昔他丁 B 的关键季碳立体中心。
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引用次数: 0
Ionones from cigar tobacco leaves 雪茄烟叶中的酮类化合物
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2024-05-30 DOI: 10.1080/10286020.2024.2342509

Phytochemical studies on cigar tobacco leaves led to the isolation of 18 ionone-type compounds, including previously undescribed cigatobanes E (1) and F (2). Additionally, compounds vomifoliol acetate (3), dehydrovomifoliol (4), 8,9-dihydromegastigmane-4,6-diene-3-one (5), 7α,8α-epoxyblumenol B (6), 3-oxoactinidol (12), and loliolide acetate (15), 4β-hydroxy-dihydroactinidiolide (17), were found in tobacco leaves for the first time. The structural elucidation of all compounds was accomplished through rigorous spectral analysis.

通过对雪茄烟叶进行植物化学研究,分离出了 18 种离子酮类化合物,其中包括以前未曾描述过的雪茄烟烷 E(1)和 F(2)。此外,还在烟叶中首次发现了醋酸 vomifoliol(3)、脱氢 vomifoliol(4)、8,9-二氢化雌甾-4,6-二烯-3-酮(5)、7α,8α-环氧布卢门醇 B(6)、3-oxoactinidol(12)和醋酸 loliolide(15)、4β-羟基二氢内酯(17)等化合物。通过严格的光谱分析,所有化合物的结构都得到了阐明。
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引用次数: 0
Biotransformation and metabolite activity analysis of flavonoids from propolis in vivo 蜂胶中黄酮类化合物在体内的生物转化和代谢活性分析。
IF 1.3 3区 医学 Q3 CHEMISTRY, APPLIED Pub Date : 2024-05-24 DOI: 10.1080/10286020.2024.2355142

Propolis is a natural resinous compound produced by bees, mixed with their saliva and wax, and has a range of biological benefits, including antioxidant and anti-inflammatory effects. This article reviews the in vivo transformation of propolis flavonoids and their potential influence on drug efficacy. Despite propolis is widely used, there is little research on how the active ingredients of propolis change in the body and how they interact with drugs. Future research will focus on these interactions and the metabolic fate of propolis in vivo.

蜂胶是一种由蜜蜂产生的天然树脂化合物,与蜜蜂的唾液和蜡混合在一起,具有一系列生物功效,包括抗氧化和消炎作用。本文回顾了蜂胶类黄酮的体内转化及其对药物疗效的潜在影响。尽管蜂胶被广泛使用,但有关蜂胶活性成分在体内如何变化以及如何与药物相互作用的研究却很少。未来的研究将重点关注这些相互作用以及蜂胶在体内的代谢命运。
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引用次数: 0
期刊
Journal of Asian Natural Products Research
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