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Sesamin is an effective spleen tyrosine kinase inhibitor against IgE-mediated food allergy in computational,cell-based and animal studies
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作者 Yu Li Xuerui Chen +4 位作者 Longhua Xu Xintong Tan Dapeng Li Dongxiao Sun-Waterhouse Feng Li 《Food Science and Human Wellness》 2025年第2期469-483,共15页
Food allergy has become a global concern.Spleen tyrosine kinase(SYK)inhibitors are promising therapeutics against allergic disorders.In this study,a total of 300 natural phenolic compounds were firstly subjected to vi... Food allergy has become a global concern.Spleen tyrosine kinase(SYK)inhibitors are promising therapeutics against allergic disorders.In this study,a total of 300 natural phenolic compounds were firstly subjected to virtual screening.Sesamin and its metabolites,sesamin monocatechol(SC-1)and sesamin dicatechol(SC-2),were identified as potential SYK inhibitors,showing high binding affinity and inhibition efficiency towards SYK.Compared with R406(a traditional SYK inhibitor),sesamin,SC-1,and SC-2 had lower binding energy and inhibition constant(Ki)during molecular docking,exhibited higher bioavailability,safety,metabolism/clearance rate,and distribution uniformity ADMET predictions,and showed high stability in occupying the ATP-binding pocket of SYK during molecular dynamics simulations.In anti-dinitrophenyl-immunoglobulin E(Anti-DNP-Ig E)/dinitrophenyl-human serum albumin(DNP-HSA)-stimulated rat basophilic leukemia(RBL-2H3)cells,sesamin in the concentration range of 5-80μmol/L influenced significantly the degranulation and cytokine release,with 54.00%inhibition againstβ-hexosaminidase release and 58.45%decrease in histamine.In BALB/c mice,sesamin could ameliorate Anti-DNP-Ig E/DNP-HSA-induced passive cutaneous anaphylaxis(PCA)and ovalbumin(OVA)-induced active systemic anaphylaxis(ASA)reactions,reduce the levels of allergic mediators(immunoglobulins and pro-inflammatory cytokines),partially correct the imbalance of T helper(Th)cells differentiation in the spleen,and inhibit the phosphorylation of SYK and its downstream signaling proteins,including p38 mitogen-activated protein kinases(p38 MAPK),extracellular signalregulated kinases(ERK),and p65 nuclear factor-κB(p65 NF-κB)in the spleen.Thus,sesamin may be a safe and versatile SYK inhibitor that can alleviate Ig E-mediated food allergies. 展开更多
关键词 Food allergy Spleen tyrosine kinase sesamin Computational tools RBL-2H3 cells BALB/c mice
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Optimal Conditions for the Purification of Sesamin by Recrystallization 被引量:4
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作者 刘末 周仁杰 +1 位作者 吴静 雷红 《Agricultural Science & Technology》 CAS 2017年第7期1202-1204,1364,共4页
[Objective] Sesamin has been widely used in healthy food and medicines in recent years due to its prominent biological functions. This study was aimed to determine the optimal parameters for sesamin recrystallization,... [Objective] Sesamin has been widely used in healthy food and medicines in recent years due to its prominent biological functions. This study was aimed to determine the optimal parameters for sesamin recrystallization, to obtain high-quality and high-purity sesamin. [Method] The effects of solid-liquid ratio, heating tempera- ture and cooling temperature on sesamin recrystallization were investigated by sin- gle-factor experiments and orthogonal array testing (ORT). The purity of resulting sesamJn was investigated by HPLC, [Result] The optimal conditions for the purifica- tion of sesamin were solid-liquid ratio of 1:10, heating temperature of 45 ℃ and cooling temperature of 25 ℃. Under these conditions, the purity of sesamin reached 95.26%. [Conclusion] Recrystallization is an effective technique to purify sesamin from sesame meal. Moreover, HPLC is also an ideal method for analyzing the purity of sesamin. 展开更多
关键词 sesamin RECRYSTALLIZATION Orthogonal array testing HPLC
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Antioxidant lignans sesamin and sesamolin in sesame(Sesamum indicum L.):a comprehensive review and future prospects 被引量:3
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作者 Senouwa Segla Koffi DOSSOU XU Fang-tao +3 位作者 Komivi DOSSA ZHOU Rong ZHAO Ying-zhong WANG Lin-hai 《Journal of Integrative Agriculture》 SCIE CAS CSCD 2023年第1期14-30,共17页
Sesame(Sesamum indicum L.)is a significantly lucrative cash crop for millions of small-holder farmers.Its seeds are an important source of a highly appreciated vegetable oil globally and two clinically essential antio... Sesame(Sesamum indicum L.)is a significantly lucrative cash crop for millions of small-holder farmers.Its seeds are an important source of a highly appreciated vegetable oil globally and two clinically essential antioxidant lignans,sesamin and sesamolin.Accordingly,many countries import millions of tons of sesame seed every year.The demand for lignan-rich sesame seeds has been increasing in recent years due to the continuous discovery of several pharmacological attributes of sesamin and sesamolin.To meet this demand,the sesame breeder’s primary objective is to release sesame cultivars that are enriched in oil and lignans.Thus,it is necessary to summarize the information related to the sesamin and sesamolin contents in sesame in order to promote the joint efforts of specialized research teams on this important oilseed crop.In this article,we present the current knowledge on the sesamin and sesamolin contents in S.indicum L.with respect to the updated biosynthesis pathway,associated markers,governing loci,available variability in sesame germplasm,the in planta potential roles of these compounds in sesame,and the newly discovered pharmacological attributes.In addition,we propose and discuss some required studies that might facilitate genomics-assisted breeding of high lignan content sesame varieties. 展开更多
关键词 Sesamum indicum lignan biosynthesis ANTIOXIDANTS molecular breeding sesamin and sesamolin
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Inhibition of two stages of melanin synthesis by sesamol,sesamin and sesamolin 被引量:1
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作者 Montra Srisayam Natthida Weerapreeyakul Kwanjai Kanokmedhakul 《Asian Pacific Journal of Tropical Biomedicine》 SCIE CAS 2017年第10期886-895,共10页
Objective: To investigate the antimelanogenesis properties of three sesame compoundssesamol, sesamin and sesamolin via two stages of melanin synthesis vis-à-vis sunscreen function and enzyme inhibition in melanom... Objective: To investigate the antimelanogenesis properties of three sesame compoundssesamol, sesamin and sesamolin via two stages of melanin synthesis vis-à-vis sunscreen function and enzyme inhibition in melanoma cell line in order to search for alternative depigmenting agents.Methods: Antimelanogenic effects of sesame lignans were assessed in SK-MEL2 compared with the reference depigmenting agents, kojic acid and b-arbutin, in order to evaluate:(a) the sunscreen function of sesamol, sesamin and sesamolin by measurement of UV absorbtion property;(b) the inhibition of tyrosinase activity through mushroom and cellular tyrosinase; and(c) the effect on melanin content and melanogenic protein expression(tyrosinase, TRP-1 and TRP-2) by Western blot analysis; and(d) the toxicity of sesamol, sesamin and sesamolin to cells using cell cytotoxicity assay.Results: The results showed that sesamin, sesamolin and sesamol exerted satisfiable sunscreen function by absorbed UVB at 290 nm. Sesamol exhibited the highest inhibition of mushroom tyrosinase activity, but lipophilic sesamolin exhibited the highest cellular tyrosinase inhibition(IC_(50) of 1.6 μM) followed by sesamin, sesamol, and kojic acid,respectively. The order from high to low inhibition of melanin pigment was detected in the SK-MEL2 treated with sesamolin, sesamin, sesamol, kojic acid, and b-arbutin,respectively. Sesamolin and sesamin successfully inhibited cellular tyrosinase activity and respectively decreased TRP-1/TRP-2(36%/15%) and TRP-1 levels(16%), thereby inhibiting melanogenesis via antityrosinase activity. No cytotoxicity to SK-MEL2 or Vero(normal) cell lines was observed at the lignan concentrations that exerted an antimelanogenic effect.Conclusions: Three sesame lignans prevent melanin synthesis through 2 stages:(a) by blocking melanin-induction and(b) by interrupting melanogenic enzyme production. This study provides evidence that sesamol, sesamin and sesamolin are potential for antimelanogenesis agents. 展开更多
关键词 SESAMOL sesamin SESAMOLIN TYROSINASE TRP-1/TRP-2 Antimelanogenesis
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Sesamin enhances nitric oxide bioactivity in aortas of spontaneously hypertensive rats 被引量:1
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作者 Jie-renYANG XiangKONG WeiLI 《中国药理学与毒理学杂志》 CAS CSCD 北大核心 2015年第S1期38-38,共1页
OBJECTIVE To explore the underlying mechanisms involved in the effect of sesamin on aortic NO bioactivity in spontaneously hypertensive rat(SHR).METHODS Sesamin was orally administered for consecutive 8 weeks in SHR.S... OBJECTIVE To explore the underlying mechanisms involved in the effect of sesamin on aortic NO bioactivity in spontaneously hypertensive rat(SHR).METHODS Sesamin was orally administered for consecutive 8 weeks in SHR.Systolic blood pressure(SBP)was measured using the tail-cuff method.The aortas were isolated and in vitro vascular reactivity studies were performed.Superoxide anion production in carotid arteries was assessed by dihydroethidium fluorescence staining.The protein expression of endothelial nitric oxide synthase(eNOS),phosphorylated eNOS(P-eNOS),dihydrofolate reductase(DHFR),nicotinamide adenine dinucleotide phosphate(NADPH)oxidase subunit p47 phox and copper,zinc-superoxide dismutase(Cu/Zn-SOD)in aortas was detected by Western blotting.The dimeric form of eNOS in aortas was determined by low-temperature SDS-PAGE.Aortic level of nitrotyrosine and activities of antioxidant enzymes,namely,total SOD(T-SOD),glutathione peroxidase(GPx)and catalase were also detected.RESULTS In SHR,sesamin treatment reduced SBP,improved vascular relaxation induced by acetylcholine and enhanced aortic NO bioactivity.Sesamin treatment enhanced NO biosynthesis in SHR aortas was due to upregulated P-eNOS and suppressed eNOS uncoupling,and the latter effect might be attributed to decreased nitrotyrosine and upregulated DHFR.Sesamin also reducd the NO oxidative inactivation and decreased the superoxide anion production through downregulation of p47 phox and amelioration of eNOS uncoupling.In addition,sesamin treatment did not alter the levels of GPx and catalase activity but obviously reduced the compensatory elevated T-SOD activity and Cu/Zn-SOD protein expression.CONCLUSION Chronic treatment with sesamin could reduce hypertension and improve endothelial dysfunction through enhancement of NO bioactivity in SHRs aortas. 展开更多
关键词 sesamin spontaneously HYPERTENSIVE RAT ENDOTHELIAL
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Separation of Sesamin and Sesamolin by a Supercritical Fluid-Simulated Moving Bed 被引量:2
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作者 Ming-Tsai Liang Ru-Chien Liang +3 位作者 Li-Rong Huang Ping-Hsuan Hsu Yu-Hsuan Wu Hung-En Yen 《American Journal of Analytical Chemistry》 2012年第12期931-938,共8页
This work shows how the sesamin and sesamolin in sesame seed can be extracted, enriched and purified by the related technologies of supercritical carbon dioxide. Sesame oil is first obtained from the sesame seeds by s... This work shows how the sesamin and sesamolin in sesame seed can be extracted, enriched and purified by the related technologies of supercritical carbon dioxide. Sesame oil is first obtained from the sesame seeds by supercritical carbon dioxide extraction (SFE);lignans in the oil are enriched and precipitated as the top product by supercritical fluid fractionation technology (SFF);the crude lignans are then separated by supercritical fluid-simulated moving bed chromatography (SF-SMB) to obtain pure sesamin and sesamolin. The simulated moving bed is a continuous chromatography;the use of supercritical carbon dioxide as the desorbent simplifies the downstream treatment. By experimental validation, this work also shows that replacing liquid by SF as the desorbent for the SMB automatically creates a gradient operation for the SMB and enlarges the separable range of the operating conditions. Both the design and operation of the SF-SMB are introduced in this paper. The application of SF-SMB to the separation of sesamin and sesamolin provides a novel example for demonstrating the diversity of SF and the potential applications for the production of natural products and the development of botanical drugs. 展开更多
关键词 SUPERCRITICAL FLUID Simulated-Moving BED sesamin SESAMOLIN SUPERCRITICAL FLUID Extraction SUPERCRITICAL FLUID FRACTIONATION
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Identification and determination of (+)-sesamin in Semen Cuscutae by capillary GC and GC-MS 被引量:1
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作者 Yan LI Min YE +2 位作者 Hu Wei LIU Xiu Hong JI Yu Ning YAN 《Chinese Chemical Letters》 SCIE CAS CSCD 2000年第12期1073-1076,共4页
(+)-Sesamin was found in Semen Cuscutae for the first time. A rapid and simple approach for the analysis of(+)-sesamin in different sources of Semen Cuscutae is proposed, which used GC-FID for the determination of(+)-... (+)-Sesamin was found in Semen Cuscutae for the first time. A rapid and simple approach for the analysis of(+)-sesamin in different sources of Semen Cuscutae is proposed, which used GC-FID for the determination of(+)-sesamin and CC-MS for its identification. The result suggested that this approach could be used to identify Semen Cuscutae from various sources based on the different content of(+)-sesamin in them. 展开更多
关键词 gas chromatography gas chromatography-mass spectrometry (+)-sesamin Semen Cuscutae
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Effect of Temperature Variation on the Separation of Sesamin and Sesamolin by Simulated Moving Bed 被引量:1
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作者 Ming-Tsai Llang Ru-Chien Liang +2 位作者 Ling-Ya Wang Hung-En Yen Kuo-Tong Lee 《Journal of Chemistry and Chemical Engineering》 2011年第6期479-486,共8页
In this work, sesamin and sesamolin is separated and purified by SMB (simulated moving bed) chromatography. Purity of sesamin and sesamolin can reach 99.2% and 99.9 %, and they can be recovered by 99.9% and 99.4%, r... In this work, sesamin and sesamolin is separated and purified by SMB (simulated moving bed) chromatography. Purity of sesamin and sesamolin can reach 99.2% and 99.9 %, and they can be recovered by 99.9% and 99.4%, respectively. Concentrations of the extract and raffinate was monitored and periodical change of the concentration was observed on experiment. Effects of non-linear adsorption, dead volume, and temperature on the separation are reviewed by the triangle theory to explain the periodical change of concentration. It is found that dead volume has little effect, and temperature fluctuation significantly affects thc separation by SMB. The temperature seriously affects the robust operation of SMB due to the change of Henry's constant, which will change the selectivity and restrain the productivity. Although the productivity in this study is only 0.0416 g/L-hr, the cost of the stationary phase used in this study is much lower than that of packed in analytical column. By using this stationary phase, the authors are still able to separate the mixture of sesamin and sesmolin. This will economically attract attention for the application of SMB to purify bioactive compounds on developing botanical drugs. 展开更多
关键词 Simulated moving bed sesamin SESAMOLIN chromatography.
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Effect of Arbuscular Mycorrhizal Fungi and Their Partner Bacteria on the Growth of Sesame Plants and the Concentration of Sesamin in the Seeds
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作者 Sachie Horii Takaaki Ishii 《American Journal of Plant Sciences》 2014年第20期3066-3072,共7页
Arbuscular mycorrhizal fungi (AMF) can stimulate the plant growth. Pseudomonas sp. (KCIGC01) NBRC109613 isolated from the spores of Glomus clarum IK97, an AMF, is reported to support the plant growth and development a... Arbuscular mycorrhizal fungi (AMF) can stimulate the plant growth. Pseudomonas sp. (KCIGC01) NBRC109613 isolated from the spores of Glomus clarum IK97, an AMF, is reported to support the plant growth and development as partner bacteria (PB) for AMF REF _Ref399417929 \r \h \* MERGEFORMAT [1]. In order to investigate the effect of G. clarum IK97 and Pseudomonas sp. (KCIGC01) NBRC109613 on the secondary metabolites, these microorganisms were inoculated to sesame plants. The inoculation of these microorganisms stimulated the growth of sesame. The rate of sesame root colonization in G. clarum IK97 + Pseudomonas sp. (KCIGC01) NBRC109613 inoculated plants (66.4% ± 4.4%) was higher than that in G. clarum IK97 alone inoculated plants (39.2% ± 5.8%). Furthermore, the content of sesamin in sesame seeds was increased by the inoculation of these microorganisms. In particular, the content of sesamin in the treatment inoculated with G. clarum IK97 and Pseudomonas sp. (KCIGC01) NBRC-109613 was 11.4 ± 1.5 mg/g seed. The results suggest that AMF and their partner bacteria can stimulate the growth and development of sesame plants and increase the content of sesamin in the seeds. 展开更多
关键词 ARBUSCULAR Mycorrhizal Fungi PARTNER BACTERIA sesamin SESAMOLIN
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Potential immunomodulatory role of sesamin in combating immune dysregulation associated with COVID-19
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作者 Amin F.Majdalawieh Sarah M.Yousef Imad A.Abu-Yousef 《Asian Pacific Journal of Tropical Biomedicine》 SCIE CAS 2021年第10期421-428,共8页
The ongoing outbreak of novel coronavirus disease 2019(COVID-19),caused by severe acute respiratory syndrome coronavirus 2(SARS-CoV-2),has caused an unprecedented global health crisis.Development of a cure for this de... The ongoing outbreak of novel coronavirus disease 2019(COVID-19),caused by severe acute respiratory syndrome coronavirus 2(SARS-CoV-2),has caused an unprecedented global health crisis.Development of a cure for this devastating disease is currently at full speed,with several vaccines against COVID-19 already authorized and administered.Currently,demand for these vaccines far exceeds supply.As such,boosting immunity represents a viable route to halt the rapid spread of SARS-CoV-2 and limit fatalities until vaccines become more readily and widely available.The use of phytochemicals appears to be a promising panacea.Sesamin,a lignan isolated from Sesamum indicum seeds,is known for its potent pharmacological properties,and is therefore hypothesized as a potential candidate in the therapeutic regimen against COVID-19.Herein,we highlight the confirmed therapeutic anti-inflammatory and immune-modulatory potential of sesamin against myriads of respiratory disorders,and tentatively suggest that sesamin may exert similar potent effects against COVID-19.Precisely,we speculate that sesamin may help alleviate COVID-19 via restoring Th1/Th2 balance and preventing inflammation and cytokine storm development.Additionally,we further support the promising role of sesamin against COVID-19 by underscoring the direct evidence,which suggests that sesamin may demonstrate promising inhibitory potential against three important SARS-CoV-2 targets,namely main protease,spike protein,and angiotensin-converting enzyme 2 receptor.Although preliminary,there is ample evidence to propose sesamin as a potential phytotherapeutic and prophylactic candidate against COVID-19.Further in vitro,in vivo,and preclinical studies are required to further substantiate the role of sesamin in the prevention and/or treatment of COVID-19. 展开更多
关键词 sesamin SARS-CoV-2 COVID-19 IMMUNOMODULATION ANTI-INFLAMMATORY Cytokine storm Th1/Th2 balance
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Beneficial Regulatory Effects of Sesamin on Intestinal Flora of Mice
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作者 Yu DENG Mengxi WANG +2 位作者 Xiaogeng LIU Pan LIU Hong LEI 《Agricultural Biotechnology》 CAS 2022年第6期84-88,共5页
The effects of sesamin on intestinal microflora of mice with normal diet were studied by in vitro animal feces anaerobic culture system.The results showed that treatment with sesamin could significantly change the int... The effects of sesamin on intestinal microflora of mice with normal diet were studied by in vitro animal feces anaerobic culture system.The results showed that treatment with sesamin could significantly change the intestinal flora structure of mice,increasing the abundance of probiotics Lactobacillus and Bifidobacterium and inhibiting the growth of harmful bacteria Enterococcus.High-throughput sequencing analysis showed that sesamin could affect the structure and composition of fecal microflora of mice,and the abundance of probiotics such as Bacillus and Bifidobacterium increased.Sesamin also could increase the expression of tight contiguous protein Occludin and Claudin-1 in colonic tissue of mice,which was benefit to the adhesion of probiotics.In conclusion,sesamin intervention could improve the composition and abundance of intestinal microorganisms in mice with normal diet,which had a beneficial regulatory effect on the intestinal health. 展开更多
关键词 sesamin Intestinal flora Beneficial regulatory effect Abundance of probiotics
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芝麻素通过p38 MAPK/Nrf2/HO-1信号通路缓解大鼠急性肺损伤的作用研究 被引量:1
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作者 刘金华 赵田甜 胡根 《实用中西医结合临床》 2025年第6期1-4,12,共5页
目的探讨芝麻素对脂多糖(LPS)诱导大鼠急性肺损伤的保护作用及其作用机制。方法采用随机数字表法将大鼠分为空白对照组(Control组)、模型组(LPS组)及芝麻素干预组(LPS+SSM组),每组6只。Control组不做任何处理,LPS+SSM组按320 mg/kg灌胃... 目的探讨芝麻素对脂多糖(LPS)诱导大鼠急性肺损伤的保护作用及其作用机制。方法采用随机数字表法将大鼠分为空白对照组(Control组)、模型组(LPS组)及芝麻素干预组(LPS+SSM组),每组6只。Control组不做任何处理,LPS+SSM组按320 mg/kg灌胃芝麻素,LPS组按10 mL/kg灌浓度为0.5%的羧甲基纤维素钠,1次/d,连续喂养1周(造模前干预处理)。LPS组和LPS+SSM组采用气管注射LPS(5 mg/kg)建立急性肺损伤模型,造模成功6 h后取样。观察三组肺组织病理变化、炎症细胞因子、p38 MAPK磷酸化水平、核转录因子红系2相关因子2(Nrf2)及血红素加氧酶-1(HO-1)蛋白表达。结果HE染色显示,与Control组相比,LPS组大鼠肺泡结构受到破坏,肺泡间隙明显增厚,肺泡壁、肺泡腔或间质可见炎症细胞大量浸润;LPS+SSM组肺间质仅有轻微渗出,部分肺泡壁增厚,无透明膜形成,病理学损伤较LPS组减轻。大鼠肺组织湿/干重比(W/D)显示,Control组、LPS+SSM组W/D值均低于LPS组(P<0.05)。Control组、LPS+SSM组血清白细胞介素-1β(IL-1β)、肿瘤坏死因子-α(TNF-α)水平均低于LPS组,Control组血清IL-1β、TNF-α水平均低于LPS+SSM组(P<0.05)。Western blot显示,Control组、LPS+SSM组大鼠肺组织p38 MAPK磷酸化水平低于LPS组,而Control组低于LPS+SSM组(P<0.05);Control组、LPS组Nrf2、HO-1均低于LPS+SSM组,而Control组低于LPS组(P<0.05)。结论芝麻素对LPS诱导的大鼠急性肺损伤发挥了显著的保护作用,其潜在机制可能与p38 MAPK/Nrf2/HO-1信号通路的激活有关。 展开更多
关键词 急性肺损伤 芝麻素 脂多糖 p38 MAPK Nrf2/HO-1
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Mechanisms of sesamol and sesamin inhibitingα-glucosidase activity by spectroscopy and molecular docking 被引量:1
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作者 Shijia Zhang Yiren Zhang +4 位作者 Emad Karrar Qingzhe Jin Hui Zhang Gangcheng Wu Xingguo Wang 《Food Bioscience》 SCIE 2023年第3期1641-1648,共8页
Sesamol and sesamin inhibitα-glucosidase activity and may therefore be effective in treating type 2 diabetes,but their mechanisms remain unknown.Therefore,the inhibitory effects of sesamol and sesamin onα-glucosidas... Sesamol and sesamin inhibitα-glucosidase activity and may therefore be effective in treating type 2 diabetes,but their mechanisms remain unknown.Therefore,the inhibitory effects of sesamol and sesamin onα-glucosidase activity were analyzed by multispectral technique and molecular docking.Our findings indicated that the sesamol and sesamin had a significant influence onα-glucosidase activity,with IC_(50) values of 0.96 mM and 0.33 mM,respectively,and their inhibition types were non-competitive.Both sesamol and sesamin quenched the fluorescence by a static quenching mechanism.The results of three-dimensional(3D)fluorescence,circular dichroism(CD)spectroscopy and Fourier transform infrared spectrometer(FT-IR)showed that both sesamol and sesamin had certain effects on the conformation ofα-glucosidase.Molecular docking results revealed that both sesamol and sesamin could spontaneously bind toα-glucosidase and form hydrogen bonds with some of the amino acid residues of the enzyme.As a result,this study sheds new light on sesamol/sesamin as a potentialα-glucosidase inhibitor. 展开更多
关键词 SESAMOL sesamin Α-GLUCOSIDASE Inhibition mechanism SPECTROSCOPY Molecular docking
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基于Pickering乳液模板法的芝麻素结肠靶向微胶囊的制备
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作者 刘金金 雷红 +2 位作者 邓瑜 孔令艳 薛梅 《中国食品学报》 北大核心 2025年第3期265-274,共10页
以酸改性凹凸棒颗粒稳定的O/W型Pickering乳液为模板,以芝麻素为芯材、大豆分离蛋白和壳聚糖盐酸盐为壁材,通过单因素实验和响应面试验优化芝麻素结肠靶向微胶囊的制备工艺,并研究其性能。通过体外模拟消化试验研究微胶囊的结肠靶向作... 以酸改性凹凸棒颗粒稳定的O/W型Pickering乳液为模板,以芝麻素为芯材、大豆分离蛋白和壳聚糖盐酸盐为壁材,通过单因素实验和响应面试验优化芝麻素结肠靶向微胶囊的制备工艺,并研究其性能。通过体外模拟消化试验研究微胶囊的结肠靶向作用及缓释性能。结果表明,Pickering乳液的最优制备工艺为pH 6.0、颗粒质量分数1.5%、油相体积分数2.0%。芝麻素微胶囊的最优制备工艺为pH 5.0、芯壁比1∶2.0、壁材比1∶1.0、水浴温度55℃、水浴时间3 h。微胶囊中芝麻素的包埋率为(71.36±0.61)%,具有显著的结肠靶向作用和缓释性能。本研究为芝麻素微胶囊作为改善肠道菌群的功能食品的研发提供试验依据。 展开更多
关键词 芝麻素 凹凸棒 Pickering乳液 微胶囊 结肠靶向
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基于mRNA-seq研究芝麻素对高血压合并血脂异常大鼠脂肪性肝病的防治作用机制
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作者 王运东 李雪宁 +10 位作者 李墨萱 曹文静 戎浩 杨晨 朱雪睿 许欣雨 王烨 张雅 金欢欢 洪宗元 张俊秀 《中国临床药理学与治疗学》 北大核心 2025年第7期876-888,共13页
目的:观察芝麻素(SES)对高血压合并血脂异常大鼠脂肪性肝病的防治作用,并基于mRNAseq探讨其可能机制。方法:利用高脂高胆固醇饮食喂养自发性高血压大鼠(SHR),建立高血压合并血脂异常大鼠模型,给予SES连续治疗16周。实验分为WKY、SHR、Mo... 目的:观察芝麻素(SES)对高血压合并血脂异常大鼠脂肪性肝病的防治作用,并基于mRNAseq探讨其可能机制。方法:利用高脂高胆固醇饮食喂养自发性高血压大鼠(SHR),建立高血压合并血脂异常大鼠模型,给予SES连续治疗16周。实验分为WKY、SHR、Model和Model+SES组(160 mg·kg^(-1)·d^(-1))。采用尾袖法检测大鼠的血压;监测体质量并计算体质量指数;超声检测肝脏形态并测量肝脏厚度;称量肝脏湿重并计算肝脏指数;水位上升法检测肝脏体积,ELISA法检测血清甘油三酯(TG)、总胆固醇(TC)、低密度脂蛋白胆固醇(LDL-C)、高密度脂蛋白胆固醇(HDL-C)、丙氨酸氨基转移酶(ALT)、天门冬氨酸氨基转移酶(AST)和总胆汁酸(TBA);mRNA-seq对肝脏进行测序分析;HE染色观察肝脏的组织形态学变化;油红O染色观察肝脏的脂肪变性程度;MASSON染色观察肝脏的纤维化程度;q-PCR检测Aldh1a7、Nnmt、Irs2、Pltp和Scd mRNA的表达;Western blotting检测Scd、Nnmt、AMPK、p-AMPK、PPARα和PPARγ蛋白的表达。结果:SES连续给药高血压合并血脂异常大鼠16周后,血压降低(P<0.01)和体质量减轻,血清的TG、TC和LDL-C降低、HDL-C升高,血清的ALT和AST降低(P<0.01),肝脏重量减轻和脏器指数减小、肝脏厚度减小和肝脏体积减小,肝脏脂肪变性和肝脏纤维化程度改善(P<0.05)。各组大鼠肝脏共有545个差异mRNA,其中278个上调,267个下调,在27个共同差异表达mRNA中,筛选出与脂质代谢相关的5个mRNA,分别为Aldh1a7、Nnmt、Irs2、Pltp和Scd。KEGG富集分析富集通路为AMPK和PPAR。进一步验证,SES给药组肝脏的Scd mRNA表达减少,Nnmt mRNA表达增加,Scd蛋白表达下降,Nnmt、AMPK、p-AMPK、PPARα和PPARγ蛋白表达上升(P<0.05)。结论:SES具有防治高血压合并血脂异常大鼠的脂肪性肝病的作用,其作用机制可能与降低肝脏中Scd表达水平,升高Nnmt、AMPK、p-AMPK、PPARα和PPARγ表达有关。 展开更多
关键词 高血压 血脂异常 脂肪性肝病 转录组测序 芝麻素
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芝麻素对调和油煎炸稳定性的影响
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作者 张天宇 魏学鼎 +3 位作者 王澍 何东平 雷芬芬 周力 《中国油脂》 北大核心 2025年第7期21-26,共6页
为促进芝麻素作为天然抗氧化剂在煎炸油中的应用,考察了芝麻素对调和油煎炸稳定性的影响。将未添加抗氧化剂的大豆油、棕榈油、葵花籽油、菜籽油按照一定比例调配制得调和油,并以其中的大豆油为对照分别添加0.02%的芝麻素、0.05%的天然... 为促进芝麻素作为天然抗氧化剂在煎炸油中的应用,考察了芝麻素对调和油煎炸稳定性的影响。将未添加抗氧化剂的大豆油、棕榈油、葵花籽油、菜籽油按照一定比例调配制得调和油,并以其中的大豆油为对照分别添加0.02%的芝麻素、0.05%的天然维生素E(V_(E))和0.02%的特丁基对苯二酚(TBHQ),进行32 h的连续煎炸试验,分析煎炸过程中油样酸值、极性组分含量、碘值、过氧化值和脂肪酸组成的变化。结果表明:随着煎炸时间的延长,所有煎炸油的酸值、极性组分含量均增加,碘值均降低,未添加抗氧化剂的空白油样的过氧化值增加,添加抗氧化剂油样的过氧化值则呈先升高后降低再升高趋势;添加抗氧化剂可有效抑制油样酸值和过氧化值的升高和碘值的降低,总体来看TBHQ的效果最好,芝麻素次之,V_(E)效果较差;随着煎炸时间的延长,煎炸油的不饱和脂肪酸含量降低,饱和脂肪酸含量升高,不饱和脂肪酸含量变化幅度大小顺序为空白油样>添加V_(E)油样>添加芝麻素油样>添加TBHQ油样,相对于大豆油,调和油的不饱和脂肪酸含量变化较小;总体来看,调和油的反式脂肪酸含量低于大豆油。综上,芝麻素可以提高煎炸油的氧化稳定性,其效果介于TBHQ和V_(E)之间。 展开更多
关键词 芝麻素 大豆油 调和油 煎炸稳定性
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基于转录组学和网络药理学探讨芝麻素减轻肝缺血再灌注损伤的作用机制
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作者 张亚东 杨微杰 +3 位作者 朱思琪 李晟赫 孙小雅 马玉霞 《河北医科大学学报》 2025年第9期1046-1052,共7页
目的基于转录组学数据和网络药理学分析探讨芝麻素减轻肝缺血再灌注损伤的作用机制。方法对高通量基因表达数据库(Gene Expression Omnibus,GEO)中肝缺血再灌注损伤相关数据集进行分析得到差异表达基因(differentially expressed genes,... 目的基于转录组学数据和网络药理学分析探讨芝麻素减轻肝缺血再灌注损伤的作用机制。方法对高通量基因表达数据库(Gene Expression Omnibus,GEO)中肝缺血再灌注损伤相关数据集进行分析得到差异表达基因(differentially expressed genes,DEGs)并筛选出核心基因,对DEGs进行京都基因与基因组百科全书(Kyoto Encyclopedia of Genes and Genomes,KEGG)富集分析。通过对芝麻素靶点与肝缺血再灌注损伤相关靶点进行交集分析,明确芝麻素减轻肝缺血再灌注损伤的潜在作用靶点,利用这些靶点进行蛋白质-蛋白质相互作用(protein-protein interaction,PPI)网络构建,并基于多算法联合获取核心靶点。随后,对潜在靶点进行KEGG富集分析。使用AutodockTools软件对芝麻素和核心靶点进行分子对接。结果分析GSE15480数据集共获得DEGs 318个,经过筛选得到8个核心基因。KEGG富集分析主要涉及白细胞介素(interleukin,IL)-17信号通路等相关通路。通过作用靶点交集得到芝麻素减轻肝缺血再灌注损伤潜在靶点108个,拓扑分析后得到核心靶点9个。KEGG富集分析主要集中在IL-17信号通路等相关通路。结果提示,芝麻素可能通过靶向IL-17信号通路中的前列腺素内过氧化物合酶(prostaglandin-edoperoxide synthase,PTGS2)、IL-6和IL-1β发挥保护作用。分子对接结果显示,芝麻素与核心靶点PTGS2、IL-6、IL-1β的结合能分别为-8.08 kcal/mol、-6.37 kcal/mol和-7.75 kcal/mol,均显示出了良好的结合性。结论芝麻素可能通过靶向IL-17信号通路中的PTGS2、IL-6和IL-1β减轻肝缺血再灌注损伤。 展开更多
关键词 再灌注损伤 转录组学 网络药理学 芝麻素
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芝麻素对长春瑞滨诱导人肺腺癌A549细胞凋亡的影响
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作者 金永彪 杨哲智 +2 位作者 姜云峰 林星 车成日 《延边大学医学学报》 CAS 2024年第2期85-89,共5页
[目的]探讨芝麻素对长春瑞滨诱导人肺腺癌A549细胞株凋亡的影响.[方法]选择人肺腺癌A549细胞株进行体外传代培养,制备成浓度为1.0×105个/mL的细胞悬浮液并接种于96孔板中.实验设空白组(加入DMEM培养液)、对照组(加入DMEM培养液及... [目的]探讨芝麻素对长春瑞滨诱导人肺腺癌A549细胞株凋亡的影响.[方法]选择人肺腺癌A549细胞株进行体外传代培养,制备成浓度为1.0×105个/mL的细胞悬浮液并接种于96孔板中.实验设空白组(加入DMEM培养液)、对照组(加入DMEM培养液及人肺腺癌A549细胞株)、芝麻素组(芝麻素10、20、30、40、50、60、70、80、90、100μg/mL)、长春瑞滨组(长春瑞滨5、10、15、20、25、30、35μg/mL)及联合用药组(加入IC50浓度的芝麻素和长春瑞滨,IC50为后续联合用药组实验药物浓度).空白组加入160μL的DMEM培养液,对照组及实验组各加入160μL已制备好的人肺腺癌A549细胞株悬浮液,待细胞株贴壁后,空白组、对照组及实验组分别加入20μL的生理盐水和20μL各相关浓度的药物.采用MTT法检测细胞增殖能力,利用倒置显微镜及HE染色法观察细胞形态学变化,采用流式细胞仪检测细胞凋亡情况.[结果]在10~100μg/mL质量浓度范围内,低质量浓度的芝麻素具有抑制A549细胞株增殖的作用,IC50质量浓度为40μg/mL;在5~35μg/mL质量浓度范围内,长春瑞滨具有抑制A549细胞株增殖的作用,且随着药物质量浓度升高细胞抑制率升高,IC50质量浓度为20μg/mL;芝麻素与长春瑞滨联合用药对A549细胞株的抑制率明显高于单药用药(P<0.01).倒置显微镜及HE染色法观察结果显示,与对照组比较,芝麻素(40μg/mL)、长春瑞滨(20μg/mL)及联合用药(芝麻素40μg/mL+长春瑞滨20μg/mL)作用于A549细胞株48 h后贴壁细胞数量均明显减少,细胞间连接疏松,贴壁能力减弱,部分细胞体积变小、变圆或呈不规则形,核染色质凝集,细胞膜起泡形成凋亡小体,失去原有肿瘤细胞多角形或梭形形态,且联合用药组较单药组上述变化更为明显.流式细胞仪检测结果显示,药物作用48 h后,芝麻素组(40μg/mL)、长春瑞滨组(20μg/mL)及联合用药组(芝麻素40μg/mL+长春瑞滨20μg/mL)细胞凋亡率均明显高于对照组(P<0.01),且联合用药组早期凋亡率明显高于单独用药组(P<0.01).[结论]芝麻素可增强长春瑞滨诱导人肺腺癌A549细胞凋亡的作用. 展开更多
关键词 芝麻素 长春瑞滨 人肺腺癌A549细胞株 凋亡
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菟丝子化学成分、药理作用研究进展及其质量标志物(Q-Marker)预测 被引量:35
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作者 陈鲁宁 胡扬 +9 位作者 辛国松 陈鹰翔 宗政 宋辉 孙向明 徐蓓蕾 张文君 王昊 杨智惠 李文兰 《中草药》 CAS CSCD 北大核心 2024年第15期5298-5314,共17页
菟丝子Cuscutae Semen始载于《神农本草经》,具有补益肝肾、固精缩尿、明目安胎的功效,主要含有黄酮类、木脂素类、多糖等化学成分。现代研究表明,菟丝子具有保护生殖系统、免疫调节、抗肿瘤等药理作用。《中国药典》2020年版仅将金丝... 菟丝子Cuscutae Semen始载于《神农本草经》,具有补益肝肾、固精缩尿、明目安胎的功效,主要含有黄酮类、木脂素类、多糖等化学成分。现代研究表明,菟丝子具有保护生殖系统、免疫调节、抗肿瘤等药理作用。《中国药典》2020年版仅将金丝桃苷作为菟丝子质量控制标准,对菟丝子质量整体评价较为单一且专属性差。通过对菟丝子的本草考证、化学成分、药理作用和临床应用进行综述,并基于质量标志物(quality marker,Q-Marker)的概念,从植物亲缘性、化学成分可测性、入血成分、药对配伍等进行Q-Marker预测。初步推测金丝桃苷、紫云英苷、异鼠李素、山柰酚、异槲皮苷、槲皮素、绿原酸、阿魏酸、芝麻素等成分为菟丝子主要的Q-Marker,为建立和完善菟丝子质量评价体系提供参考。 展开更多
关键词 菟丝子 质量标志物 质量标准 金丝桃苷 紫云英苷 山柰酚 绿原酸 芝麻素
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菟丝子治疗骨关节炎:网络药理学分析及实验验证 被引量:13
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作者 张天栋 彭青平 +3 位作者 刘欢 冯建国 易茜 黄文华 《中国组织工程研究》 CAS 北大核心 2024年第28期4516-4521,共6页
背景:菟丝子具有补肝肾、益精髓的功效,而骨关节炎的主要病机为肝肾亏虚,推测菟丝子与骨关节炎之间有一定的联系。目的:基于网络药理学和分子对接的分析手段挖掘骨关节炎和菟丝子之间的潜在联系,对中药本草菟丝子的作用机制进行合理的... 背景:菟丝子具有补肝肾、益精髓的功效,而骨关节炎的主要病机为肝肾亏虚,推测菟丝子与骨关节炎之间有一定的联系。目的:基于网络药理学和分子对接的分析手段挖掘骨关节炎和菟丝子之间的潜在联系,对中药本草菟丝子的作用机制进行合理的推测与验证。方法:先在中草药数据库TCMSP中筛选菟丝子的有效活性成分和作用靶点,另在疾病数据库GeneCards、OMIM、TTD中收集骨关节炎的相关基因;取交集后进行一系列分析,并筛选出核心基因;通过对核心基因的富集分析选择菟丝子作用于骨关节炎的通路,通过分子对接验证核心基因的作用,并依此选择合适的有效活性成分进行实验验证。结果与结论:①筛选出11种菟丝子的有效活性成分,菟丝子和骨关节炎有66个交集靶点基因,后续筛选出12个核心基因,包括肿瘤坏死因子、白细胞介素1B、TP53、RACα丝氨酸/苏氨酸蛋白激酶(AKT1)、血管内皮生长因子A、基质金属蛋白酶9、前列腺素过氧合酶2、胱天蛋白酶3、表皮生长因子、过氧化物酶体增生激活受体γ、白细胞介素10、血管细胞黏附因子1;②对核心基因进行富集分析后,选择经典炎症通路核因子κB信号通路进行后续菟丝子缓解骨关节炎炎症的分析验证;根据各活性成分和通路核心基因前列腺素过氧合酶2进行分子对接后得到的结果,选择亲和力最高的芝麻素进行后续细胞实验验证,结果证实了菟丝子的有效成分芝麻素可以通过抑制白细胞介素1β诱导的核因子κB信号通路降低环氧合酶2的表达;③结果表明,菟丝子的活性有效成分芝麻素通过抑制白细胞介素1β诱导的核因子κB信号通路降低环氧合酶2的表达,达到改善骨关节炎炎症的作用,证实了菟丝子在骨关节炎方面的治疗效果。 展开更多
关键词 菟丝子 骨关节炎 芝麻素 核因子ΚB信号通路 环氧合酶2 网络药理学 分子对接 炎症反应
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