Targeting colorectal cancer with Herba Patriniae and Coix seed:Network pharmacology,molecular docking,and in vitro validation

BACKGROUND Herba Patriniae and Coix seed(HC)constitute a widely utilized drug combination in the clinical management of colorectal cancer(CRC)that is known for its diuretic,anti-inflammatory,and swelling-reducing properties.Although its efficacy has been demonstrated in a clinical setting,the active compounds and their mechanisms of action in CRC treatment remain to be fully elucidated.AIM To identify the active,CRC-targeting components of HC and to elucidate the mechanisms of action involved.METHODS Active HC components were identified and screened using databases.Targets for each component were predicted.CRC-related targets were obtained from human gene databases.Interaction targets between HC and CRC were identified.A“drug-ingredient-target”network was created to identify the core components and targets involved.Gene Ontology(GO)and Kyoto Encyclopedia of Genes and Genomes(KEGG)analyses were conducted to elucidate the key pathways involved.Molecular docking between core targets and key components was executed.In vitro experiments validated core monomers.RESULTS Nineteen active components of HC were identified,with acacetin as the primary active compound.The predictive analysis identified 454 targets of the active compounds in HC.Intersection mapping with 2685 CRC-related targets yielded 171 intervention targets,including 30 core targets.GO and KEGG analyses indicated that HC may influence the phosphoinositide 3-kinase(PI3K)/Akt signaling pathway.Molecular docking showed that acacetin exhibited an optimal interaction with AKT1,identifying PI3K,AKT,and P53 as key genes likely targeted by HC during CRC treatment.Acacetin inhibited HT-29 cell proliferation and migration,as well as promoted apoptosis,in vitro.Western blotting analysis revealed increased p53 and cleaved caspase-3 expression and decreased levels of p-PI3K,p-Akt,and survivin,which likely contributed to CRC apoptosis.CONCLUSION Acacetin,the principal active compound in the HC pair,inhibited the proliferation and migration of HT-29 cells and promoted apoptosis through the PI3K/Akt/p53 signaling pathway.

Anti-lipid-oxidation effects and edible safety evaluation of the oil extracted by a supercritical CO_(2) process from coix seed fermented by Monascus purpureus

The physicochemical properties and composition of coix seed oil produced by Monascus purpureus fermentation and supercritical CO_(2)extraction were determined.Anti-lipid-oxidation and edible safety were evaluated using a cholesterol-fish oil model,acute oral toxicity assay,and genetic toxicity assay in vitro and in vivo,respectively.The results show that the extraction oil from fermented coix seed(FCS-O)had good physicochemical quality and abundant active components with physiological function.In particular,γ-tocotrienol,γ-oryzanol,coixenolide and oleic acid concentrations reached 72.83μg/g,745.96μg/g,9.65 mg/g and 316.58 mg/100 g DW,respectively.The FCS-O exhibited higher antioxidant capability in inhibiting lipid oxidation and peroxidation.Compared to the blank control,the concentrations of 7-ketocholestreol and peroxide only were 8.42μg/mL and 16.16 mmol/kg at 168 h of oxidation(P<0.01).In addition,the FCS-O has been confirmed to be a very safe edible oil,with no acute toxicity(LD50>10 g/kg bw,considered actually non-toxic)and no induced mutagenicity,cytotoxicity or genotoxicity.These results serve as a good safety reference for future application of the oil from fermented coix seed.The development and utilization of this kind of oil will be beneficial as a food,food ingredient,nutritional supplement,or natural food antioxidant to promote good health function.

Anti-tumor effect of coix seed based on the theory of medicinal and food homology

Coix seed is a dry and mature seed of Coix lacryma-jobi L.var.ma-yuen(Roman.)Stapf in the Gramineae family.Coix seed has a sweet,light taste,and a cool nature.Coix seed enters the spleen,stomach,and lung meridians.It has the effects of promoting diuresis and dampness,strengthening the spleen to prevent diarrhea,removing arthralgia,expelling pus,and detoxifying and dispersing nodules.It is used for the treatment of edema,athlete's foot,poor urination,spleen deficiency and diarrhea,dampness and obstruction,lung carbuncle,intestinal carbuncle,verruca,and cancer.The medicinal and health value is high,and it has been included in the list of medicinal and food sources in China,which has a large development and application space.This article reviews the current research achievements in the processing methods and anti-tumor activities of Coix seed and provides examples of its clinical application in ancient and modern times,aiming to provide reference for further research on Coix seed and contribute to its clinical application and development.Through the analysis of the traditional Chinese patent medicines,and simple preparations and related health food of Coix seed queried by Yaozhi.com,the source,function,and dosage form of Coix seed were comprehensively analyzed,with a view of providing a reference for the development of Coix seed medicine and food.

Study on the mechanism of Coix seed in the treatment of colon cancer Based on network pharmacology

Objective:Study on the mechanism of Coix seed in the treatment of colon cancer based on network pharmacology.Methods:The main chemical components of Coix seed were identified by TCMP,and the target sites of drug components were screened.The target of the protein was mapped to the corresponding gene target through the Uniprot database.Genecards database was used to find the target gene of human colon cancer disease,and then the disease gene target was combined with the drug gene target to screen the common target of disease-drug composition,and the STRING platform was used to construct the drug component-disease target protein interaction.(PPI)network model.The Bioconductor database was used to analyze the potential targets,related molecular functions and signaling pathways of cocoon in the treatment of colon cancer by GO and KEGG enrichment.The disease-drug component-target-signal pathway network was established by Cytoscape software.Results:It was found that there are 9 pharmacodynamics and 28 targets related to colon cancer treatment,and GO functional enrichment analysis is based on correction.P<0.05 screened 346 molecular functional related items,including 256 biological processes,48 molecular functions,and 42 cell components.KEGG functional enrichment analysis screened 24 related pathways according to the adjusted P<0.05.Conclusion:PTGS2,AR,ESR1,PGR,ADH1C,AKR1B1,LTA4H,NCOA1,NCOA2 and other related targets may be potential targets for the treatment of colon cancer.

Insights into a novel chrysanthemum-coix seed beverage prepared by enzymatic hydrolysis: Chemical profile, sensory quality, and functional property

Yin-deficiency-heat(YDH)syndrome characterized by inflammatory lesions is a common sub-health state in human body.Chrysanthemum and coix seed are commonly used to improve YDH syndrome.The chemical,volatile,and phenolic profiles and sensory and functional properties of five plant-based solid beverages(PSB)prepared by hydrothermal treatment coupling with enzymatic hydrolysis by amylase and protease using chrysanthemum and coix seed as materials were determined.Chrysanthemum-coix seed beverage had wonderful water solubility,reduced bitter and sour taste,sweet taste,and harmonious aroma.Chrysanthemum phenolics extracted by enzymatic hydrolysis might impact multiple metabolic pathways and biological processes to intervene in inflammation and most of them had high bioaccessibility.PSB promoted the production of beneficial gut microbiota metabolites.Chrysanthemum-coix seed beverages exerted more positive effects on YDH syndrome due to anti-inflammatory phenolics from chrysanthemum and resistant starch/dextrin from coix seed facilitating short-chain fatty acids production.This study provided new sight for developing plant-based beverages with anti-YDH syndrome potential.

Identification of anti-hyperuricemic components from Coix seed

Coix seed is a nutritious food with the effect of reducing uric acid.Few studies have been performed on the relevant active compounds.In this study,uric-acid-lowering active compounds were isolated and screened from Coix seed,and their structures were identified using NMR and mass spectrometry.The study showed that Coix seed effectively reduced serum uric acid and creatinine levels,suppressed liver xanthine oxidase activity,and improved kidney damage in mice due to hyperuricemia.Two major anti-hyperuricemic compounds were identified,namely,1-phenyl-1,3,3-propanetriamine(compound 1)and dihydroferulic acid(compound 2),among which compound 1 was a new compound,and compound 2 was separated from Coix seed for the first time.Two compounds showed potent inhibitory activity in vitro against xanthine oxidase,with IC_(50) values of 230.48 and 373.09μM,respectively.Furthermore,the molecular docking results indicated that the compounds could inhibit enzyme activity by interacting with residues within the active pocket of xanthine oxidase.This study provided a new alternative for the development of uric acid-lowering medications by identifying an anti-hyperuricemic alkaloid from Coix seed.

Analysis of metabolites of coix seed fermented by Monascus purpureus

In this study,an untargeted metabolomics method based on LC-MS was used to investigate the differential metabolites of coix seed after fermentation by Monascus purpureus.The compounds with highly correlated variable importance in projection(VIP)values of orthogonal partial least squares discriminant analysis(OPLS-DA)were selected as the important metabolites of coix seed samples.Coix seed was fermented by M.purpureus for 9 d.The color value units(CVU)of pigment in fermented coix seed reached 157.47 CVU/g,and the contents of total phenols and total flavonoids were 0.32 mg/g and 1.2 mg/g,respectively.A total of 270 differential metabolites were detected,including amino acids,peptides,fatty acids,phenols,steroids,and their derivatives,of which the relative contents of 187 metabolites showed a significant upward trend(p<0.05).Amino acids,peptides and analogues accounted for the largest proportion at 26%,among which most metabolites were enriched.For example,N-alpha-acetyllysine,l-tryptophan and l-arginine exhibited a fold change(FC)of 6200.87,330.29,and 35.59,respectively.In particular,the detected steroid metabolites accounted for 3%of the total metabolites,and they all participated in the same pathway,in which androsterone,2-methoxyestrone and etiocholanolone were upregulated.The synthesis of these steroids was related to the precursors and enzymes in the pathway,such as dehydroepiandrosterone,androstenedione,and 3beta-hydroxy-delta5-steroid dehydrogenase(HSD3B).The results of this study reveal M.purpureus fermentation can successfully transform coix seed,improving the functional activities of metabolites.Thus,this process has high development value with important applications in the food industry.

非酿酒酵母与酿酒酵母混合发酵对薏米酒醪色泽及风味的影响

该研究分别考察了商业酿酒酵母(Saccharomyces cerevisiae)(SC)单菌发酵,商业酿酒酵母(SC)分别与非酿酒酵母德尔布有孢圆酵母(Torulaspora delbrueckii)(TD)、东方伊萨酵母(Issatchenkia orientalis)(IO)、粟酒裂殖酵母(Schizosaccharomyces pombe)(SP)混合发酵对薏米酒醪基础理化特性、颜色和挥发性风味物质的影响。结果表明,与SC组发酵相比,混合发酵降低了薏米酒醪的酒精度、pH和还原糖含量,可增加酒醪的亮度;混合发酵增加挥发性风味物质的种类,SC组、TD+SC组、IO+SC组和SP+SC组分别检出43种、49种、48种和48种挥发性风味物质,可显著增加酯类化合物含量(P<0.05),其中,SP+SC组显著增加了苯乙醛、壬醛和3-羟基-2-丁酮的含量(P<0.05),SC组的标志性化合物为正戊醇、2,3-丁二醇、苯乙醇等;TD+SC组为正癸醇、2-甲基丁醇、丁二酸二乙酯等;IO+SC组为异戊酸、苯甲酸乙酯、苯乙酸乙酯等;SP+SC组为乙酸异丁酯、丁酸乙酯、苯乙醛等。综上,非酿酒酵母和商业酿酒酵母混合发酵有助于提高薏米酒醪的色泽及风味品质。

薏苡仁油联合5-FU对结肠癌HCT-116细胞株增殖、凋亡的影响

目的:分析薏苡仁油联合5-氟尿嘧啶(5-fluorouracil,5-FU)对结肠癌HCT-116细胞株增殖、凋亡的影响及其作用机制。方法:采用四甲基偶氮唑盐(methyl thiazolyl tetrazdium,MTT)法测定不同浓度薏苡仁油、5-FU以及薏苡仁油+5-FU对人结肠癌HCT-116细胞株的生长抑制效应;采用流式细胞术检测细胞凋亡情况;采用逆转录聚合酶链反应(RT-PCR)检测生存蛋白(Survivin)mRNA表达水平。结果:薏苡仁油、5-FU、5-FU+薏苡仁油均对人结肠癌HCT-116细胞增殖产生一定抑制作用,且薏苡仁油浓度越高,作用时间越长,细胞增殖抑制率越高,3组比较差异有统计学意义(P<0.05);与薏苡仁油组及5-FU组相比,5-FU+薏苡仁油组细胞增殖抑制率更高,差异有统计学意义(P<0.05)。薏苡仁油组、5-FU组、5-FU+薏苡仁油组的细胞凋亡率均高于空白对照组,差异有统计学意义(P<0.05);薏苡仁油浓度越高,细胞凋亡率也越高,差异有统计学意义(P<0.05);5-FU+薏苡仁油组细胞凋亡率高于5-FU组及薏苡仁油组,差异有统计学意义(P<0.05)。与空白对照组相比,不同浓度薏苡仁油组Survivin mRNA表达降低,差异有统计学意义(P<0.05);5-FU组Survivin mRNA表达升高,差异有统计学意义(P<0.05);5-FU+薏苡仁油组Survivin mRNA表达较5-FU组降低,差异有统计学意义(P<0.05)。结论:薏苡仁油能抑制结肠癌HCT-116细胞增殖,诱导细胞凋亡,与5-FU联合应用能发挥药物协同作用,其作用机制可能与调控Survivin mRNA表达有关。

抹茶对贮藏期间薏仁米脂质氧化的影响

目的:利用天然物质抹茶延长薏仁米货架期。方法:以新鲜薏仁米为原料,经过不同剂量抹茶茶粉处理,测定贮藏期间薏仁米的水分含量、脂肪酸值、过氧化值、丙二醛含量等各项指标及菌落总数和脂质氧化关键酶的变化。结果:经不同剂量抹茶茶粉处理均会抑制薏仁米贮藏期间脂肪酸值、过氧化值、丙二醛含量以及脂肪酶和脂肪氧化酶活性的上升,减少水分的消耗及微生物的生长繁殖。抹茶对薏仁米的保藏效果存在一定程度的剂量依赖性,但添加质量分数为0.05%和0.08%的抹茶茶粉处理的保藏效果差异较小。贮藏4个月后,与自封袋组相比,添加质量分数为0.05%的抹茶茶粉处理组中薏仁米的脂肪酸值、过氧化值和丙二醛含量分别降低了31.60%,30.77%,44.83%,脂肪酶和脂肪氧化酶活性分别降低了23.05%,28.74%,且游离脂肪酸组成和含量与新鲜薏仁米更相似。结论:抹茶能有效抑制薏仁米贮藏期间脂质氧化,延长其货架期。

抗性早熟汤剂治疗中枢性性早熟女童的疗效与安全性

目的探讨抗性早熟中药汤剂对中枢性性早熟女童的疗效及安全性。方法搜集2021—2023年于江西省儿童医院内分泌遗传代谢科就诊的中枢性性早熟女童共127例为研究对象,根据是否接受抗性早熟中药汤剂治疗分为治疗组73例与对照组54例。对照组予健康宣教及饮食调整;治疗组在对照组治疗基础上加用抗性早熟中药汤剂(1袋·次^(-1),2次·d^(-1)),根据服药后情况,随证另加炒薏苡仁(5 g)口服。治疗6个月后,比较2组治疗有效率及治疗前后骨龄、骨龄/年龄、身高、体重指数(BMI)、子宫长径、卵巢容积、促黄体生成素(LH)基础值、LH峰值、LH/促卵泡刺激素(FSH)峰值、乳房Tanner分期,并监测观察组不良反应以评估其安全性。结果治疗组治疗有效率(84.9%)明显高于对照组(11.1%)(P<0.05)。治疗前,2组各观察指标水平比较差异均无统计学意义(P<0.05);治疗后2组乳房Tanner分期分布差异有统计学意义(P<0.05),治疗组的骨龄、骨龄/年龄、卵巢容积、基础LH值、LH峰值、LH/FSH峰值均低于对照组(P<0.05)。治疗组治疗后BMI低于治疗前(P<0.05),治疗前后骨龄/年龄、子宫长径比较差异无统计学意义(P>0.05);对照组治疗后骨龄/年龄、子宫长径较治疗前升高(P<0.05)。2组治疗前后身高比较差异均无统计学意义(P>0.05)。治疗组治疗过程中有13例患儿腹泻,另加炒薏苡仁口服后症状缓解,无其他不良反应事件发生。结论抗性早熟中药汤剂治疗中枢性性早熟女童疗效肯定,安全性良好,且不会影响患儿的生长速度和增加体重。

薏苡附子败酱散通过抗三结构域蛋白21-Toll样受体4-t-核因子-κB信号通路对类风湿关节炎MH7A细胞的影响

目的观察不同浓度薏苡附子败酱散对肿瘤坏死因子-α(TNF-α)诱导的类风湿关节炎成纤维细胞(MH7A)增殖、凋亡及炎症反应的影响,探究其作用机制。方法2022年2―8月,大鼠用不同浓度薏苡附子败酱散及蒸馏水灌胃制备含药血清;20μg/L的TNF-α处理的MH7A细胞记为TNF-α组,TNF-α+含药血清处理的MH7A细胞记为薏苡附子败酱散低浓度组、薏苡附子败酱散中浓度组、薏苡附子败酱散高浓度组,正常培养的MH7A细胞标记为对照组。细胞计数试剂盒(CCK8)、流式细胞术、酶联免疫吸附测定(ELISA)检测细胞的存活、凋亡及白细胞介素(IL)-1β、干扰素(IFN)-γ;蛋白质印迹法(WB)检测基质金属蛋白酶(MMP)-3、MMP-9、抗三结构域蛋白21(TRIM21)、Toll样受体4(TLR4)、t-核因子(NF)-κB p65、磷酸化(p)-NF-κB p65、p-NF-κB抑制因子(IκB)-α和t-IκB-α蛋白表达。pcDNA 3.1组(转染空载体)、pcDNA+TRIM21组(转染pcDNA 3.1+TRIM21)、薏苡附子败酱散中浓度+si-con组(转染si-con+4.70 g/kg含药血清)、薏苡附子败酱散中浓度+si-TRIM21组(转染si-TRIM21+4.70 g/kg含药血清)。结果与对照组相比,TNF-α组细胞存活率(105.07±1.90比185.67±3.06)、TRIM21(0.56±0.02比0.68±0.04)、MMP-3(0.18±0.00比0.63±0.02)、MMP-9(0.39±0.01比0.82±0.01)、TLR4(0.25±0.02比0.68±0.07)、p-NF-κB p65(0.24±0.01比0.68±0.06)、p-IκB-α(0.22±0.01比0.55±0.04)蛋白表达和IL-1β(31.65±0.66比101.93±0.60)、IFN-γ(8.53±0.16比63.76±1.35)含量均显著升高,凋亡率(6.54±0.06比1.17±0.08)均显著降低;与TNF-α组相比,薏苡附子败酱散低浓度组(185.67±3.06比153.77±3.09;0.68±0.04比0.37±0.02;0.63±0.02比0.47±0.02;0.82±0.01比0.73±0.01;103.2±0.7比92.93±0.85;66.3±1.45比54.47±1.46;0.68±0.07比0.53±0.05;0.68±0.06比0.53±0.06;0.55±0.04比0.47±0.01;1.84±0.07比6.67±0.28)、薏苡附子败酱散中浓度组(185.67±3.06比136.23±1.57;0.68±0.04比0.57±0.02;0.63±0.02比0.37±0.02;0.82±0.01比0.57±0.00;103.2±0.7比86.4±0.75;66.3±1.45比38.1±0.92;0.68±0.07比0.43±0.07;0.68±0.06比0.59±0.01;0.55±0.04比0.40±0.03;1.84±0.07比9.59±0.29)、薏苡附子败酱散高浓度组(185.67±3.06比143.47±1.50;0.68±0.04比0.47±0.02;0.63±0.02比0.41±0.05;0.82±0.01比0.62±0.00;103.2±0.7比89.63±0.42;66.3±1.45比40.17±0.90;0.68±0.07比0.51±0.06;0.68±0.06比0.69±0.07;0.55±0.04比0.41±0.02;1.84±0.07比8.89±0.08)细胞存活率、TRIM21、MMP-3、MMP-9蛋白和IL-1β、IFN-γ含量及TLR4、p-NF-κB p65、p-IκB-α蛋白表达均显著降低,凋亡率均显著升高(P<0.05);与pcDNA组相比,pcDNA+TRIM21组细胞TRIM21蛋白表达(0.24±0.03比0.51±0.04)、细胞凋亡率(1.61±0.11比12.43±0.61)均显著升高,MMP-3(0.64±0.02比0.41±0.04)、MMP-9(0.82±0.03比0.45±0.02)、IL-1β(110.63±0.55比90.93±0.60)、IFN-γ(64.5±0.82比48.1±1.25)及细胞存活率(179.03±0.74比120.07±0.60)均显著降低;敲减TRIM21显著抑制薏苡附子败酱散中浓度对损伤细胞的治疗作用且显著升高TLR4(0.45±0.06比0.61±0.02)、p-NF-κB p65(0.49±0.02比0.56±0.02)、p-IκB-α(0.38±0.01比0.62±0.01)的蛋白表达。结论薏苡附子败酱散增强TNF-α诱导的MH7A细胞的生存能力,其作用机制与上调TRIM21抑制TLR4-NF-κB信号通路活性有关。

薏米对果蝇生长发育的影响

以黑腹果蝇为试验材料,设置不同浓度的薏米培养基(0%、10%、15%、20%),探究薏米培养基对果蝇繁殖力、雌雄比例、体重、寿命及过氧化氢酶(CAT)活性的影响,以期为薏米的合理使用提供理论依据.结果显示:随着薏米浓度的逐渐提高,果蝇的成蛹数、羽化数、寿命和体重均呈现先升高后降低的趋势.当薏米浓度在0%~15%区间时,果蝇的成蛹数、羽化数、寿命和体重均呈现为逐渐提高,15%时各项所测指标最高:成蛹数、羽化数分别为64.33只和60.00只,雌、雄果蝇的寿命分别为65 d和62 d,雌、雄果蝇的体重分别达1.382 g和1.180 g.果蝇的过氧化氢酶(CAT)活性也随薏米浓度的增加而增加,当浓度为20%时,过氧化氢酶活性最高,雌、雄果蝇分别达15.77 U/mg和14.96 U/mg.可见,15%的薏米培养基最适宜果蝇的生长发育,20%的薏米培养基对果蝇CAT活性的提高最显著,但薏米浓度对果蝇的雌雄比例影响不明显.

薏米联合低渣肠内营养治疗炎症性肠病相关研究

目的探讨在原有肠内营养支持方案的基础上,加上薏米对于炎症性肠病的治疗效果的提升。方法通过随机分组,将62例IBD疾病患者随机分为低渣肠内营养组(对照组)和薏米联合低渣肠内营养组(干预组),分别测量干预前后的相关指标来进行统计分析。结果干预组(薏米联合低渣肠内营养)的患者在体重,总蛋白,白蛋白,及血红蛋白等方面的提升均优于对照组(低渣肠内营养)。结论薏米联合低渣肠内营养支持有利于炎症性肠病患者的肠道功能恢复以及改善患者的多项营养相关指标。

电子束辐照对薏苡仁中5种真菌毒素降解率以及甘油三油酸酯含量的影响

为了科学利用电子束辐照技术有效降解薏苡仁中的5种真菌毒素[黄曲霉毒素4种:AFB_(1)、AFB_(2)、AFG_(1)和AFG_(2);玉米赤霉烯酮(ZEA)],利用高效液相色谱法,测定了不同剂量[0(未辐照)、2、4、6、8、10 kGy)的电子束辐照处理以及适宜剂量电子束辐照结合不同的水分、pH值、双氧水(H_(2)O_(2))处理后薏苡仁中5种真菌毒素降解率以及甘油三油酸酯含量的变化。结果表明:薏苡仁中5种毒素的降解率均随辐照剂量的增大而逐渐提高,其中8 kGy剂量处理的5种毒素降解率与10 kGy剂量处理差异均不显著,因此确定电子束辐照降解薏苡仁中5种毒素的适宜剂量为8 kGy。8 kGy剂量的电子束辐照时,控制薏苡仁水分含量为10%~12%,pH值为8~9,添加1.0%浓度的H_(2)O_(2),薏苡仁中5种真菌毒素的降解率高,且甘油三油酸酯含量仍能达到《中国药典》(2020版)标准。研究结果可为利用电子束辐照降解薏苡仁中5种毒素提供技术支持。

薏苡仁化学成分及抗肿瘤作用研究进展

薏苡仁是临床应用极为广泛的中药,具有健脾止泻、利水消肿、渗湿除痹、清热排脓、解毒散结等功效。现代药理学研究表明脂肪酸及其酯类、内酰胺类、三萜类、酚类、甾醇类、多糖类为薏苡仁中主要的抗肿瘤成分,可通过抑制肿瘤细胞增殖、诱导细胞凋亡、抑制细胞迁移和侵袭、抗肿瘤血管生成、逆转多药耐药、放化疗增敏、免疫调节、抑制癌前病变等多个途径达到抗肿瘤的作用,其中薏苡仁油是最主要的抗肿瘤成分,由薏苡仁油制成的中成药康莱特注射液在临床上应用广泛,效果显著。薏苡仁可用于多种肿瘤的辅助治疗,对于临床常见肿瘤如肺癌、口腔癌、鼻咽癌等头颈部肿瘤,肝癌、胃癌、结直肠癌、胰腺癌等消化道肿瘤,乳腺癌、前列腺癌、卵巢癌、子宫颈癌等生殖及泌尿系肿瘤均有明显的治疗作用,具有防止术后肿瘤复发转移、减轻放化疗的不良反应、提高患者生存质量、增强患者免疫力等方面的优势。论述薏苡仁及其提取物主要抗肿瘤成分及对多种恶性肿瘤及其并发症的作用效果及机制,为薏苡仁临床应用及未来发展方向提供依据。

薏米多肽-钙、锌螯合物制备及结构表征

目的:制备1种薏米多肽-钙、锌螯合物并研究其结构。方法:利用枯草芽孢杆菌和嗜热链球菌混合发酵薏米,采用葡聚糖凝胶Sephadex G-15、反相高效液相色谱(RP-HPLC)分离纯化薏米发酵液得到薏米多肽(CSP),Tricine-十二烷基硫酸钠-聚丙烯酰胺凝胶(Tricine-SDS-PAGE)电泳检测其分子质量。以锌螯合率和钙螯合率为指标,在单因素实验的基础上,采用响应面试验优化薏米多肽-钙、锌螯合物(CSP-Ca-Zn)的制备工艺,采用紫外光谱、红外光谱和荧光光谱表征其结构。结果:薏米发酵液经Sephadex G-15分离得到4个峰,其中A3的钙、锌螯合率最高。RP-HPLC分离A3得到的CSP纯度达93.91%,其分子质量约7.8 ku。CSP与Ca-Zn螯合的最佳制备工艺为:CSP与钙、锌质量比4.4∶1,钙、锌质量比1∶1,pH 3.7,在此条件下,锌螯合率、钙螯合率分别达到52.63%和63.79%。CSP与钙、锌螯合的主要位点是氨基氮、羧酸基,其空间结构也发生改变。结论:所确定的螯合工艺条件使CSP同时螯合钙、锌两种金属,为薏米多肽新产品的开发提供了技术参考,为制作食源性有机钙、锌补充剂提供了新思路。

基于糖脂代谢调控的薏苡仁提取物生物学活性作用机制探讨

糖脂代谢是人体生命活动的一项基础能量代谢,有助于人体正常生长发育、维持细胞组织营养和调节机体的动态平衡。薏苡仁是中药的利水渗湿药之一,其主要有效单体成分包括多糖类、酯类、脂肪酸类等,其中具有多种与糖脂代谢相关的生物活性,由于其生物学上的积极治疗作用,故在糖脂代谢紊乱相关疾病中具有治疗潜力。因此,回顾有关薏苡仁提取物对糖脂代谢失调相关疾病影响的文献,对相关机制进行整理、分析、总结,从而得出薏苡仁提取物可以通过调控糖脂代谢,在调节肠道菌群、抗炎、镇痛、抗癌等方面发挥多组分、多靶点、多途径以及相互协调的干预效应,使薏苡仁调控糖脂代谢成为疾病治疗的新策略。

软骨及姜黄联合葛根薏仁提取物对膝骨关节炎大鼠软骨损伤的改善作用

系统研究了姜黄提取物、软骨提取物、葛根薏仁提取物单独及联合使用对膝骨关节炎大鼠软骨损伤的改善作用,主要从减少膝关节肿胀(炎症)、促进软骨细胞修复和关节基质修复方面,研究了3种提取物在大鼠膝骨关节炎中的协同效应。结果显示:姜黄提取物在抑制关节肿胀、改善软骨损伤方面有较明显的作用,具体表现在能较好地改善Ⅱ型胶原蛋白(CollagenⅡ)、基质金属蛋白酶3(MMP3)、软骨寡聚基质蛋白(COMP)、肿瘤坏死因子-α(TNF-α)及超氧化物歧化酶(SOD)的水平;软骨提取物主要通过改善MMP3、COMP、TNF-α、前列腺素E2(PGE2)及SOD水平起到明显改善关节炎病变的效果;葛根薏仁提取物能够提高CollagenⅡ及SOD水平,抑制MMP3、COMP、TNF-α和白细胞介素1β(IL-1β)的升高,从而改善大鼠膝关节病变程度;3种提取物的复合使用对大鼠膝关节软骨的修复作用最为突出,且对各生化指标的异常改变均有更佳的改善效果。由此可见,通过对姜黄提取物、软骨提取物及葛根薏仁提取物的比例优化,可开发出具有显著抗炎和修复软骨作用的功能性食品,为实现“健康中国2030”添砖加瓦。

间接竞争酶联免疫分析用于薏苡仁中杂色曲霉毒素的快速检测研究

杂色曲霉毒素(Sterigmatocystin,ST)是一种主要由杂色曲霉和构巢曲霉等真菌产生的次级代谢产物,其结构与黄曲霉毒素相似,具有潜在的致癌性和毒性,严重危害人类生命健康。研究发现部分中药易ST污染,但目前针对中药中ST的快速检测研究相对较少。通过系统优化样品前处理条件及影响检测灵敏度的关键参数,建立了简便的间接竞争酶联免疫分析法(ic-ELISA),用于消费量较大的药食同源薏苡仁中ST的快速筛查。所建立ic-ELISA的半数抑制浓度(Half-Maximal Inhibitory Concentration,IC 50)为0.11 ng/mL,线性范围为6.25~100μg/kg,加标回收率在79.27%~99.95%之间,相对标准偏差(RSD)<12%。此外,该方法可抗基质干扰,只需利用溶剂标准曲线即可进行定量。用所建立的ic-ELISA对96批薏苡仁样品进行了检测,并用液相色谱-串联质谱(LC-MS/MS)对阳性样品进行了确证。该ic-ELISA快速、准确、经济,可作为薏苡仁中ST高通量快筛的技术手段,同时为其他中药中ST的快速检测提供参考。