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Journal of Ocean University of China 2022年第3期21卷 782-788页

作者： ZHANG Pengpeng ZHANG Miaomiao DONG Kaiyu ZHANG Yicong YANG Shuang WANG Yuanhong JIANG Tingfu YU Mingming LV Zhihua School of Medicine and Pharmacy Ocean University of ChinaQingdao266003China Laboratory for Marine Drugs and Bioproducts of Qingdao National Laboratory for Marine Science and Technology Qingdao266003China Key Laboratory of Glycoscience&Glycotechnology of Shandong Province Qingdao266003China Key Laboratory of Marine Drugs Ministry of Education of ChinaQingdao266003China

Chito-oligosaccharide(COS)had shown a variety of biological activities and potential biomedical implications.The present study investigated the pharmacokinetics,bioavailability,and in vitro absorption of COS with degrees of polymerization(DPs)2-7 and explored the influence of DPs on them.From Caco-2 cell permeation studies,COS were low permeability compounds with no directional effects,suggesting a low in vivo absorption mediated by facilitation diffusion and paracellular absorption.After an intragastrical administration to rats,COS2 showed the highest systemic exposure in six oligosaccharides.The bioavailability of COS2-7 was 7.33%,6.11%,4.67%,4.13%,4.02%,0.99%,respectively.Differences in bioavailability for each COS correlated to structural variations,with high DPs contributing to a decrease in bioavailability.In conclusion,COS could be absorbed by the intestinal tract both in vitro and in vivo.The very low oral bioavailability of COS could be due to low permeability.DPs can affect absorption and bioavailability of COS2-7.This study provided evidence for the absorption characteristics of COS2-7 to help us better understanding the pharmacological actions.

关键词： chito-oligosaccharide(COS) Caco-2 transport pharmacokinetics bioavailability

Nutritional properties of Europen eel(Anguilla anguilla)bone peptide-calcium and its apoptosis effect on Caco-2 cells

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Food Science and Human Wellness 2022年第6期11卷 1482-1490页

作者： Hui Teng Yuewei Qian Xiaoyun Fan Hui Cao Yuting Tian Lei Chen Guangdong Provincial Key Laboratory of Aquatic Product Processing and Safety Guangdong Province Engineering Laboratory for Marine Biological ProductsGuangdong Provincial Engineering Technology Research Center of SeafoodKey Laboratory of Advanced Processing of Aquatic Product of Guangdong Higher Education InstitutionCollege of Food Science and TechnologyGuangdong Ocean UniversityZhanjiang 524088China College of Food Science Fujian Agriculture and Forestry UniversityFuzhou 350002China

The present study aimed at making a rational usage for European eel bone by-products by preparing Europen eel bone peptide chelated calcium(EBPC-Ca).Nutritional properties and bioactivity of EBPC-Ca were evaluated.Results showed that nutritional properties of calcium ions will cause intra-and inter-molecular folding and aggregation of peptide to uniformly form EBPC-Ca chelate.The chelated compound of EBPC and calcium ion triggered a strong apoptosis in heterogeneous human epithelial colorectal adenocarcinoma(Caco-2)in concentration-and time-dependent manners.Western blot analysis revealed that the EBPC-Ca induced apoptosis may be the result of a blocked autophagy flux through mitochondrial-dependent pathway.Additionally,the increase in FGF-23 protein expression inhibited the absorption of calcium ions and alleviated cell apoptosis.It was also found that the cell apoptosis occurs with significant increases in the levels of reactive oxygen species(ROS)and Ca^(2+)in the cells,indicating the anti-tumor potential of EBPC-Ca may involve multiple channels.

关键词： Europen eel bone Peptide Calcium Nutritional properties Caco-2 Apoptosis

Mechanistic studies of the transport of peimine in the Caco-2 cell model

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Acta Pharmaceutica Sinica B 2016年第2期6卷 125-131页

作者： Lihua Chen Xueping Lu Xinli Liang Dandan Hong Zhiyu Guan Yongmei Guan Weifeng Zhu Key Laboratory of Modern Preparation of TCM of Ministry of Education Jiangxi University of TCM

Fritillaria thunbergii Miq. has been widely used in traditional Chinese medicine for its expectorant, antitussive, antiinflammatory and analgesic properties. Moreover, modern pharmacological studies have demonstrated that F. thunbergii Miq. has efficacy in the treatment of leukemia and cancers of the liver and cervix. Although the alkaloid, peimine, is largely responsible for these pharmacological effects, it has very low oral bioavailability. The aim of this study was to investigate the intestinal absorption of peimine in Caco-2 cell monolayers. Having demonstrated that peimine is non-toxic to Caco-2 cells at concentrations o200 μmol/L, the effect of peimine concentration, p H, temperature, efflux transport protein inhibitors and EDTA-Na_2 on peimine transport were studied. The results show that peimine transport is concentration-dependent; that at p H 6.0 and 7.4, the P_(app(AP-BL))of peimine is not significantly different but the Papp(BL-AP)) is; that both Papp(AP-BL)and P_(app(BL-AP))at 4 1C are significantly higher than their corresponding values at 37 1C; that the P-glycoprotein(P-gp) inhibitors, verapamil and cyclosporin A, increase absorption of peimine; and that EDTA-Na2 has no discernible effect. In summary,the results demonstrate that the intestinal absorption of peimine across Caco-2 cell monolayers involves active transport and that peimine is a substrate of P-gp.

关键词： Peimine Intestinal absorption Caco-2 cell monolayer P-glycoprotein Transport mechanism

Novel C-17 spirost protostane-type triterpenoids from Alisma plantago-aquatica with antiinflammatory activity in Caco-2 cells

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Acta Pharmaceutica Sinica B 2019年第4期9卷 809-818页

作者： Qinghao Jin Jianqing Zhang Jinjun Hou Min Lei Chen Liu Xia Wang Yong Huang Shuai Yao Bang Yeon Hwang Wanying Wu Dean Guo Shanghai Institute of Materia Medica Chinese Academy of SciencesShanghai 201203China School of Pharmacy Shenyang Pharmaceutical UniversityShenyang 110016China University of Chinese Academy of Sciences Beijing 100049China College of Pharmacy Chungbuk National UniversityCheongju 2816South Korea

Twenty-one protostane-type triterpenoids with diverse structures, including nine new compounds(1 e9), were isolated from the of Alisma plantago-aquatica Linn. Structurally, alisolides A-F(1 e6), composed of an oxole group coupled to a five-membered ring, represent unusual C-17 spirost protostane-type triterpenoids. Alisolide H(8) is a novel triterpenoid with an unreported endoperoxide bridge. Alisolide I(9) represents the first example of 23,24-acetal triterpenoid. Their structures were elucidated based on spectroscopic analysis, wherein the absolute configurations of 4-6, 8 were further confirmed by the Mo2(OAc)4-induced ECD method. Furthermore, all isolates were evaluated for their inhibitory effects on LPS-induced NO production in Caco-2 cells, and all the compounds showed remarkable inhibitory activities, with IC50 values in the range of 0.76 e38.20 mmol/L.

关键词： Alisma plantago-aquatica Linn. Protostane-type triterpenoids Caco-2 cells LPS-induced NO production

靛玉红固体脂质纳米粒的制备及Caco-2单层细胞转运研究

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中国药学杂志 2023年第22期58卷 2085-2091页

作者：舒婷常艳波杨蓉郭嘉斌任静成都大学药学院四川省药物制剂及装备工程技术研究中心成都610106 四川省药品检验研究院成都610045

目的制备靛玉红(indirubin,IND)固体脂质纳米粒(IND-SLN),并通过Caco-2单层细胞转运实验评价其渗透性。方法采用溶剂注入法制备IND-SLN,以包封率和粒径为考察指标,进行单因素筛选,用Box-Behnken响应面优化处方,采用透析法评价IND-SLN的... 详细信息

目的制备靛玉红(indirubin,IND)固体脂质纳米粒(IND-SLN),并通过Caco-2单层细胞转运实验评价其渗透性。方法采用溶剂注入法制备IND-SLN,以包封率和粒径为考察指标,进行单因素筛选,用Box-Behnken响应面优化处方,采用透析法评价IND-SLN的体外释放,通过Caco-2单层细胞转运实验比较了IND原料药与IND-SLN的渗透性。结果经优化得到IND-SLN最优处方:药物与载体脂质比例1∶15;载体脂质与磷脂比例1∶1。透射电镜下IND-SLN呈球状分布,无聚集;IND-SLN粒径为(189.93±7.23)nm;Zeta电位为(-31.67±0.60)mV;差示扫描量热法(DSC)测定显示,IND-SLN中的药物吸热峰消失;体外释放实验中,IND-SLN累积释放度较原料药明显增加;Caco-2细胞实验测得IND-SLN表观渗透系数为(5.19±2.18)×10^(-10)cm^(2)·s^(-1),远高于原料药。结论将IND制备成IND-SLN可显著提高药物渗透性。

关键词：靛玉红固体脂质纳米粒响应面法体外释放 Caco-2 渗透性

The Absorption and Transport of Magnolol in Caco-2 Cell Model

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Chinese Journal of Integrative Medicine 2013年第3期19卷 206-211页

作者：吴安国曾宝黄孟秋李生梅陈建南赖小平 Research Center of New Drug Development Guangzhou University of Chinese Medicine Research Institute of Mathematical Engineering of Guangzhou University of Chinese Medicine in Dongguan

Objective： To investigate the absorption and transport mechanism of magnolol in Caco-2 cell model. Methods： A human intestinal epithelial cell model Caco-2 cell in vitro cultured was applied to study the absorption and transport of magnolol, the effects of time, donor concentration, P-gp inhibitor verapamil, pH and temperature on the absorption and transport of magnolol were investigated. The determination of magnolol was performed by high performance liquid chromatography, then the values of apparent permeability coefficient （Papp） and Pratio Basolateral-to-Apical （BL-to-AP）/Apical-to-Basolateral （AP-to-BL） were calculated. Results： In Caco-2 cell model, comparing the amounts of transport of AP-to-BL and BL-to-AP, the latter was larger. At the same donor concentration, either the amounts of transport of AP-to-BL or BL-to-AP increased with increase in donor concentration and incubation time. Verapamil could significantly improve the amounts of transport of AP- to-BL. The transport of AP-to-BL and BL-to-AP depended on temperature, and there was no significant effect of pH on the transport of AP-to-BL. Conclusion： Magnolol could be transported through the intestinal mucosa via a passive diffusion mechanism primarily, coexisting with a carrier-mediated transport, at the same time, the efflux mechanism could be involved.

关键词： magnolol Caco-2 inhibitor the apparent permeability coefficient P-gp passive transport

Transcellular transport characteristics of huperzine alone or in combination with ginkgolide B across Caco-2 and Madin-Darby canine kidney cell monolayer

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Asian Pacific Journal of Tropical Medicine 2014年第11期7卷 889-894页

作者： Wen-Cui Zhao Zhi-Hong Hou Qi Zhang Wei Zheng Pharmacy Department 208th Hospital of PLA. Hospital Office 208th Hospital of PLA. Infirmary 208th Hospital of PLA.

Objective:To study the various processes involved in transcellular transport(TT) of huperzine A alone or in combination with ginkgolide B in Caco-2 and Madin-Darby canine renal(MDCK)cell monolayer.Methods:The transepithelial passage was assayed in the apical-to-basolateral(AP to BL) direction and opposite direction(BL to AP) in both cell lines.The determination of huperzine A and ginkgolide B were performed by high performance liquid chromatography(HPLC).The passage rates of huperzine A and ginkgolide B were calculated.Bi-directional TT(absorption and secretion) were taken in huperzine A and ginkgolide B in Caco-2 and MDCK cell monolayer.Results:TT absorption and secretion kinetics of huperzine A and ginkgolide B across two cells existed at the same time.The passage rates of huperzine A were increased significantly with adding different concentrations of ginkgolide B.Conclusions:The compound preparations of HA in combination with CB for dementia caused by cerebral ischemic have synergistic effects on the pharmacodynamics,and improve the bioavailability through BBB.

关键词： Caco-2 Huperzine A Ginkgolide B Madin-Darby canine renal Transcellular Transport

坤复康片中芍药内酯苷在Caco-2细胞模型中的吸收特征研究

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中国现代应用药学 2022年第1期39卷 20-26页

作者：王爱萍周萍张涛潘海滔钦博徐人杰绍兴市妇幼保健院妇科二病区浙江绍兴312000 绍兴市妇幼保健院临床药学室浙江绍兴312000 绍兴市妇幼保健院遗传实验室浙江绍兴312000 绍兴市妇幼保健院检验科浙江绍兴312000

目的研究坤复康片中的芍药内酯苷在Caco-2细胞模型中的跨膜吸收特征,探讨人小肠对芍药内酯苷的吸收和转运。方法研究了不同药物浓度、pH值、温度和抑制剂对芍药内酯苷在Transwell细胞培养板中从顶膜(apical,AP)到基底(basolateral,BL)... 详细信息

目的研究坤复康片中的芍药内酯苷在Caco-2细胞模型中的跨膜吸收特征,探讨人小肠对芍药内酯苷的吸收和转运。方法研究了不同药物浓度、pH值、温度和抑制剂对芍药内酯苷在Transwell细胞培养板中从顶膜(apical,AP)到基底(basolateral,BL)的双向渗透吸收的影响。结果芍药内酯苷以3种测试浓度给药时(5,20和100μmol·L^(−1)),从AP到BL方向的表观渗透系数(P_(app))值范围为(3.27~5.37)×10^(–7) cm·s^(–1)。相反,从BL到AP,P_(app)值范围为(6.64~9.63)×10^(–7) cm·s^(–1)。数据表明,芍药内酯苷转运具有pH和温度依赖性。芍药内酯苷的细胞通透性受多种抑制剂影响,包含Na^(+)/K^(+)离子通道抑制剂钒酸钠,多耐药蛋白抑制剂MK571和吲哚美辛及乳腺癌耐药蛋白抑制剂芹菜素。当坤复康溶液加入后,芍药内酯苷从AP到BL方向的P_(app)值显著增加。结论芍药内酯苷在Caco-2细胞模型中的肠道吸收较差,其吸收机制可能涉及多种蛋白介导的主动转运。

关键词：芍药内酯苷 Caco-2 口服给药吸收机制

Intestinal Absorption of Ergostane and Lanostane Triterpenoids from Antrodia cinnamomea Using Caco-2 Cell Monolayer Model

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Natural Products and Bioprospecting 2015年第5期5卷 237-246页

作者： Qi Wang Xue Qiao Yi Qian Zi-wei Li Yew-min Tzeng De-min Zhou De-an Guo Min Ye State Key Laboratory of Natural and Biomimetic Drugs School of Pharmaceutical Sciences Peking University38 Xueyuan RoadBeijing 100191China Institute of Biochemical Sciences and Technology Chaoyang University of TechnologyTaichung 41349Taiwan

Antrodia cinnamomea is a precious medicinal mushroom.It exhibits promising therapeutic effects on cancer,intoxication,hypertension,hepatitis,and inflammation.Its major bioactive constituents are ergostane and lanostane triterpenoids.In this study,we used intestinal Caco-2 cell monolayer model to reveal the intestinal absorption property of 14 representative triterpenoids from A.cinnamomea.The bidirectional transport through the monolayer at different time points was monitored by a fully validated LC/MS/MS method.In the case of pure compounds,ergostanes 5(25R-antcin H),6(25Santcin H)and 10(25R-antcin B)could readily pass through the Caco-2 cell layer,whereas lanostanes 13(dehydroeburicoic acid)and 14(eburicoic acid)could hardly pass through.When the cells were treated with A.cinnamomea extract,antcins A,B,C,H and K(1–6 and 9–11)were absorbed via passive transcellular diffusion,and showed high PAB and PBA values(>2.5×10^(-5) cm/s).Meanwhile,the lanostanes dehydrosulphurenic acid(8),15a-acetyldehydrosulphurenic acid(12),13 and 14 exhibited poor permeability.Transport features of these compounds were consistent with their pharmacokinetic behaviors in rats.This study could also be helpful in predicting the intestinal absorption of A.cinnamomea in human.

关键词： Antrodia cinnamomea Ergostane Lanostane Triterpenoids Caco-2

Comparison of intestinal absorption of two insulin-mimic vanadyl complexes using Caco-2 monolayers as model system

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Chinese Science Bulletin 2003年第9期48卷 876-881页

作者： YANGXiaogai YUANLan WANGKui YANGXiaoda DepartmentofChemicalBiology SchoolofPharmaceuticalSciencesPekingUniversityBeijing100083China AnalyticalCenterofPekingUniversity Beijing100083China NationalResearchLaboratoriesofNaturalandBiomimeticDrugs SchoolofPharmaceuticalSciencesPekingUniversityBeijing100083China LaboratoriesofPreventiveDrugs SchoolofPharmaceuticalSciencesPekingUniversityBeijing100083China

Intestinal absorption of two oxovanadium complexes, vanadyl acetylacetonate (VO(acac)2) and bis (maltolato)-oxovanadium (VO(ma)2), has been compared using Caco-2 monolayers as a model system. The two compounds are similar in chemical structures but different in glucose-lowering effects. Our experimental results show that they are both transported via passive diffusion with apparent permeabilty coefficients (apical→basolateral) of (82.0 ± 6.7)× 10-7 and (14.6 ± 0.7)× 10-7 cm· s-1, respec-tively. This suggests that absorptivity of VO(acac)2 is much higher than that of VO(ma)2. This difference may be related to the metabolism of either compound, or its ligand, or both in the course of the transport. However, This difference in absorption will cause the great difference in bioavailability,which might account for better efficacy of VO(acac)2 than VO(ma)2 as the insulin-mimic agent.

关键词：氧矾根络合物 Caco-2 肠内吸收模型系统胰岛素模拟物 ADME