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Journal of Biosciences and Medicines 2024年第2期12卷 282-293页

作者： Muhammed Majeed Kalyanam Nagabhushanam Sarang Bani Anjali Pandey Smitha Thazhathidath Sami-Sabinsa Group Limited Bengaluru India Sabinsa Corporation New Jersey USA

In recent years, metabolic syndrome has been a growing health concern across the world. The role of nutraceuticals and functional foods in this area has a significant place due to the adverse effects of contemporary modes of treatment. CurCousin® is a nutritional ingredient containing bioactive Calebin A, (analog of Curcumin) with self-affirmed GRAS status. CurCousin® has been a clinically studied dietary supplement ingredient with a positive impact on body weight, lipid levels and metabolic health. Bioenhancers play an important role in increasing the bioavailability of the active in turn enhancing efficacy as well as reducing the dosage required to achieve the therapeutic effect. This study investigated the possible pharmacokinetic interaction between CurCousin® at two different doses (2.25 and 4.5 mg/kg) in the presence and absence of BioPerine® (0.27 mg/kg), a natural bioenhancer in Sprague-Dawley rats. The results revealed that the addition of BioPerine® into CurCousin® (2.25 mg/kg) half the dose when administered enhances the bioavailability and was equipotent to CurCousin® (4.5 mg/kg) double the dose without BioPerine®. Thus, leading to future clinical studies to evaluate its improved pharmacological efficacy as well as reduced therapeutic dosage.

关键词： Metabolic Health bioavailability Pharmacokinetics CurCousin® BioPerine® Calebin A

Boswellic acids: a review on its pharmacological properties, molecular mechanism and bioavailability

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Traditional Medicine Research 2024年第10期9卷 64-74页

作者： Na Cui Ming-Jie Li Yi-Wen Wang Qian Meng Ya-Jun Shi Yi Ding Department of Pharmacy 3201 HospitalHanzhong 723000China Department of Pharmacy Xijing HospitalFourth Military Medical UniversityXi’an 710032China School of Pharmacy Shaanxi University of Traditional Chinese medicineXianyang 712046China

Boswellic acids is a general term for a series of pentacyclic triterpenoid compounds that are isolated from the oleogin resin of the Boswellia genus and serve as the main active *** exhibits a wide range of biological activities,such as anti-inflammatory,anti-cancer,antibacterial,antiviral,hepatoprotective,neuroprotective,anti-diabetic,and anti-thrombotic *** a result,it has gained significant recognition among practitioners of traditional Chinese and Indian *** biological effects may be associated with multiple molecular targets and signal transduction ***,the poor pharmacokinetic properties of the substance lead to lower bioavailability,which affects its *** address this issue,scientists have proposed a number of strategies,such as solid dispersions,phytosome®technologies,and novel drug delivery *** article aims to provide a comprehensive overview for boswellic acids on the phytochemistry,molecular mechanisms,potential therapeutic applications,and strategies to improve bioavailability.

关键词： boswellic acids molecular mechanism pharmacological properties bioavailability

Fabrication of taxifolin loaded zein-caseinate nanoparticles and its bioavailability in rats

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Food Science and Human Wellness 2023年第6期12卷 2306-2313页

作者： Ying Li Hang Su Wenjun Wang Zhongping Yin Jing’en Li En Yuan Qingfeng Zhang Jiangxi Key Laboratory of Natural Product and Functional Food College of Food Science and EngineeringJiangxi Agricultural UniversityNanchang 330045China College of Pharmacy Jiangxi University of Traditional Chinese MedicineNanchang 330006China

Taxifolin loaded zein-caseinate nanoparticles(TZP)were fabricated by the anti-solvent method and were used as an oral delivery vehicle to improve their bioavailability in the *** formulations of TZP were *** mass ratio of 1:1:2 between taxifolin,zein and sodium caseinate,the particle size andζpotential of TZP were(168.74±0.35)nm and−(57.67±0.25)mV,while the encapsulation and loading efficiency of taxifolin were(85.83±0.89)%and(17.11±0.88)%,*** freeze-drying,TZP exhibited excellent redispersibility in water without *** characterization showed that taxifolin existed in amorphous form in TZP and its interaction with the protein was *** encapsulating in TZP,the excellent dispersion of taxifolin in water signifi cantly improve its diffusion velocity through a semipermeable *** oral administration,taxifolin and its 5 metabolites were identifi ed in rat plasma by ultra high performance liquid chromatography(UPLC)with quadrupole time-of-flight mass spectrometry(UPLC-QTOF-MS).The dynamic variation of taxifolin and its metabolites in plasma were then quantifi ed by UPLC with a triple-quadrupole typemass spectroscopy(UPLC-QqQ-MS/MS).A pharmacokinetic study showed that the bioavailability of taxifolin increased from 0.35%to 0.52%through TZP *** plasma concentration of taxifolin glucuronide and methylated taxifolin glucuronide was much higher than *** was the dominating metabolism pathway of taxifolin in vivo.

关键词： Taxifolin Zein nanoparticles Characterization bioavailability

Absolute bioavailability,dose proportionality,and tissue distribution of rotundic acid in rats based on validated LC-QqQ-MS/MS method

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Journal of Pharmaceutical Analysis 2022年第2期12卷 278-286页

作者： Haihua Shang Xiaohan Dai Mi Li Yueyi Kai Zerong Liu Min Wang Quansheng Li Yuan Gu Changxiao Liu Duanyun Si School of Pharmacy Shenyang Pharmaceutical UniversityShenyang110016China State Key Laboratory of Drug Delivery and Pharmacokinetics Tianjin Institute of Pharmaceutical ResearchTianjin300301China Research Unit for Drug Metabolism Chinese Academy of Medical SciencesTianjin300301China

Rotundic acid(RA),an ursane-type pentacyclic triterpene acid isolated from the dried barks of Ilex rotunda Thunb.(Aquifoliaceae),possesses diverse *** further study its pharmacokinetics,a simple and sensitive liquid chromatography with triple quadrupole mass spectrometry(LC-QqQ-MS/MS)method was developed and validated to quantify RA concentration in rat plasma and tissue using etofesalamide as an internal standard(IS).Plasma and tissue samples were subjected to one-step protein *** separation was achieved on a ZORBAX Eclipse XDB-C_(18) column(4.6mm×50mm,5μm)under gradient conditions with eluents of methanol:acetonitrile(1:1,V/V)and 5mM ammonium formate:methanol(9:1,V/V)at 0.5mL/*** reaction monitoring transitions were performed at m/z 487.30→437.30 for RA and m/z 256.10→227.10 for IS in the negative *** developed LC-QqQ-MS/MS method exhibited good linearity(2-500 ng/mL)and was fully validated in accordance with *** and Drug Administration bioanalytical *** proportionality and bioavailability in rats were determined by comparing pharmacokinetic data after single oral(10,20,and 40mg/kg)and intravenous(10mg/kg)administration of *** distribution was studied following oral administration at 20mg/*** results showed that the absolute bioavailability of RA after administration at different doses ranged from 16.1%to 19.4%.RA showed good dose proportionality over a dose range of 10-40 mg/*** was rapidly absorbed in a dose-dependent manner and highly distributed in the *** conclusion,this study is the first to systematically elucidate the absorption and distribution characteristics of RA in rats,which can provide additional information for further development and evaluation of RA in drug metabolism and pharmacokinetic studies.

关键词： Rotundic acid LC-QqQ-MS/MS bioavailability Tissue distribution Pharmacokinetics Dose proportionality

Evaluation of the bioavailability of Metals in Sediment from the Southern Coastal Wetland of the Qiantang Estuary by Using Diffusive Gradients in Thin Films Technique

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Journal of Ocean University of China 2022年第2期21卷 375-387页

作者： FENG Weihua WANG Zhifu ZHU Wenzhuo ZHENG Fangqin ZHANG Dongrong XU Hengtao Key Laboratory of Engineering Oceanography Second Institute of OceanographyMNRHangzhou 310012China College of Marine Science&Technology Zhejiang Ocean UniversityZhoushan 316022China

Metal pollution has become an major issue governing the wetland ecosystem *** southern coastal wetland of the Qiangtang Estuary are facing unusual perturbation due to rapid development along the embayment in recent *** study evaluated the bioavailability of metals(Cu,Pb,Cd,Cr and Zn)in the sediment of the southern coastal wetland of the Qiangtang Es-tuary using diffusive gradients in thin films(DGT)techniques and compared with several methods based on total metal *** results showed that the contents of Cr,Pb,Cd and Cu in sediment,as detected using DGT,were considerably correlated with the exchangeable fraction and the content in Phragmites australis roots,while a weak correlation was observed for ***,DGT analysis could be used to evaluate the bioavailability and potential risk of Cr,Cd,Pb and Cu for *** indices,such as DGT concentration,bioaccumulation in ***,geoaccumulation index(Igeo)and potential ecological risk index(RI),revealed that Cd was a major potential ecological risk factor along the southern coast wetland of the Qiantang Estuary,especially in the upstream region,which is potentially more vulnerable to the anthropogenic pollution.

关键词： diffusive gradients in thin films estuarine wetland metal bioavailability

Abductive statistical methods improve the results of calibration curve bioassays:An example of determining zinc bioavailability in broiler chickens

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Animal Nutrition 2022年第3期10卷 294-304页

作者： Gene M.Pesti Lynne Billard Shu-Biao Wu Robert A.Swick Thi Thanh Hoai Nguyen Natalie Morgan The University of New England ArmidaleNSW2351Australia The University of Georgia AthensGA30602USA

In this paper,we discuss the theory behind calibration curve experiments and their application to a zinc(Zn)bioavailability study with broiler *** replicates of 16 male commercial broiler chicks were fed starter diets for 14 *** diets had different levels of a potential Zn source and one was a positive control with standard industry levels of Zn for *** commonly used methods of calculating bioavailability means and confidence intervals(CI)from a calibration curve(standard curve)experiment to estimate the bioavailability of a new zinc source in broiler chickens were *** methods compared were the following:1)the Counter-Intuitive Method uses a multiple-range test to compare unknown test and standard samples;2)the Intuitive Method uses standard linear regression and inverts the equation to predict Zn bioavailability for each replicate of test samples;3)the Abductive Method uses Graybill's Equation,based on theory and observation,to estimate CI's;and 4)the Sophistic Method uses reverse regression,and calculates Zn bioavailability values directly from the *** Counter-Intuitive Method only gives information about which standards the test samples are,or are not,significantly different from respectively(average available Zn not predicted).The Intuitive Method ignores error about the standard curve and theoretically cannot estimate the CI directly(X±SEM=107.5±15.8 mg Zn/kg).The Sophistic Method underestimates and overestimates the test sample mean values above and below the mean of the standards,respectively(X=96.6 mg Zn/kg).The Abductive Method has an advantage over the other methods:The mean prediction estimation is consistent with theory(107.5±6.1 mg Zn/kg;X±SEM).When test or“unknown”samples are near the mean of the standard samples,the CI is smaller than when near the extremes of the calibration *** calibration curve error is small(R^(2)>approximately 0.95),there is little advantage to using the Abductive Method,but wh

关键词： Calibration curve Standard curve Confidence interval bioavailability

Effect of processing on bioaccessibility and bioavailability of bioactive compounds in coffee beans

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Food Bioscience 2022年第2期46卷 1-13页

作者： Hanjing Wu Jingyu Gu Amrit BK Malik A.Nawaz Colin J.Barrow Frank R.Dunshea Hafiz A.R.Suleria School of Agriculture and Food Faculty of Veterinary and Agricultural SciencesThe University of MelbourneParkville3010VICAustralia Commonwealth Scientific and Industrial Research Organisation(CSIRO) Agriculture and Food671 Sneydes RoadPrivate Bag 16WerribeeVictoria3030Australia Centre for Chemistry and Biotechnology School of Life and Environmental SciencesDeakin UniversityWaurn PondsVIC3217Australia Faculty of Biological Sciences The University of LeedsLeedsLS29JTUK

Coffee is one of the most prevalent and functional beverages around world owing to its rich content of bioactive *** compounds and alkaloids are two primary groups of bioactive compounds in coffee beans,which have been proven healthy benefits in regular and suitable daily *** have been recognized as protective factors,especially phenolic compounds,to perform high antioxidant capacities and potential to relieve the occurrence of chronic diseases and partial *** content and composition of bioactive and anti-nutritional compounds in coffee beans can be mainly influenced by variety,processing and storage *** cultivar of Arabica coffee beans(***)exhibits lower content of phenolic compounds but similar anti-nutritional substances with the comparison to Robusta(***).Comparing to green coffee beans,reasonable roasting contributes to the improvement of phenolic content and its total antioxidant activity because of the liberation of bound phenolic compounds and the generation of novel compounds with antioxidant *** intensive roasting will not only decrease the number of bioactive compounds within the coffee beans but also stimulate the generation of endogenous anti-nutritional compounds,which consequently reduce the coffee nutritional *** fluctuations of moisture content during storage would be the primary reason of the changes in the content of bioactive *** compounds in coffee beans perform outstanding bioaccessibility but relatively lower absorption efficiency because of the combination with other *** roasting would improve the bioavailability of bioactive *** interaction between phenolic compounds and proteins would also influence the bioavailability and bioactivity of bioactive compounds and final nutritional value after consumption.

关键词： Coffee beans Phenolic compounds Alkaloids Anti-nutritional compounds Roasting bioavailability

Improving the stability and bioavailability of tea polyphenols by encapsulations:a review

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Food Science and Human Wellness 2022年第3期11卷 537-556页

作者： Zhiya Yin Ting Zheng Chi-Tang Ho Qingrong Huang Qingli Wu Man Zhang Department of Food Science Rutgers UniversityNJ 08901USA New Use Agriculture and Natural Plant Products Program epartment of Plant BiologyRutgers UniversityNJ 08901USA Department of Medicinal Chemistry Rutgers UniversityNJ 08854USA Center for Agricultural Food Ecosystems The New Jersey Institute for FoodNutrition and HealthRutgers UniversityNJ 08901USA

Tea polyphenols(TPPs)have attracted significant research interest due to their health ***,TPPs are sensitive to certain environmental and gastrointestinal conditions and their oral bioavailability was found to be very *** systems made of food-grade materials have been reported to improve the shelf-life,bioavailability and bioefficacy of *** review discusses the chemistry of TPPs;the setbacks of TPPs for application;and the strategies to counteract application limitations by rationally designing delivery *** overview of different formulations used to encapsulate TPPs is provided in this study,such as emulsion-based systems(liposome,nanoemulsion,double emulsion,and Pickering emulsion)and nano/microparticles-based systems(protein-based,carbohydrate-based,and bi-polymer based).In addition,the stability,bioavailability and bioactivities of encapsulated TPPs are evaluated by various in vitro and in vivo *** current findings provide scientific insights in encapsulation approaches for the delivery of TPPs,which can be of great value to TPPs-fortified food *** explorations are needed for the encapsulated TPPs in terms of their applications in the real food industry as well as their biological fate and functional pathways in vivo.

关键词： Tea polyphenols Encapsulation Stability bioavailability Bioefficacy

Roles of effective stabilizers in improving oral bioavailability of naringenin nanocrystals:Maintenance of supersaturation generated upon dissolution by inhibition of drug dimerization

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Asian Journal of Pharmaceutical Sciences 2022年第5期17卷 741-750页

作者： Guangshuai Zhang Haishan Guan Jianfeng Li Mo Li Xiaofan Sui Baocheng Tian Huiming Dong Bingyang Liu Zhonggui He Ning Li Mingming Zhao Qiang Fu Wuya College of Innovation Shenyang Pharmaceutical UniversityShenyang 110016China Department of Pharmacy Shengjing Hospital of China Medical UniversityShenyang 110004China School of Pharmacy Shenyang Pharmaceutical UniversityShenyang 110016China Liaoning Institute for Drug Control Shenyang 110016China School of Pharmacy Binzhou Medical UniversityYantai 264003China Liaoning Inspection Examination and Certification Centre Shenyang 110016China

Nanocrystals(NCs),a colloidal dispersion system formulated with stabilizers,have attracted widespread interest due to their ability to effectively improve the oral bioavailability of poorly water-soluble *** stabilizer plays a key role because it can affect the physical stability and even the oral bioavailability of ***,how stabilizers affect the bioavailability of NCs remains *** this study,F68,F127,HPMC,and PVP were each used as a stabilizer to formulate naringenin *** NCs formulated with PVP exhibited excellent release behaviors,cellular uptake,permeability,oral bioavailability,and anti-inflammatory *** underlying mechanism is that PVP effectively inhibits the formation of naringenin dimer,which in turn improves the physical stability of the supersaturated solution generated when NC is *** finding provides insights into the effects of stabilizers on the in vivo performances of NCs and supplies valuable knowledge for the development of poorly water-soluble drugs.

关键词： Nanocrystals Stabilizers bioavailability Supersaturation maintenance Dimer

Effect of digestive enzymes and pH on variation of bioavailability of green tea during simulated in vitro gastrointestinal digestion

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Food Science and Human Wellness 2022年第3期11卷 669-675页

作者： Wei Qin Sunantha Ketnawa Yukiharu Ogawa Graduate School of Horticulture Chiba University648MatsudoMatsudo 271-8510Japan

To exam ine the effect of digestive attributes such as digestive enzymes and pH on changes in phenolic compound content and antioxidant activity during digestion,the bioavailability of green tea infusion was investigated using a simulated in vitro gastrointestinal digestion *** total polyphenol content(TPC)decreased to 65%–70%throughout the mimicked normal digestion(MD)compared to the initial *** total flavonoid content(TFC)decreased to approximately 25%after starting the gastric stage(pH 1.2);however,it regained to approximately 60%in the intestinal stage(pH 6.8).The mimicked digestive condition without digestive enzymes(WOE),which followed only the pH conditions of MD,showed significantly lower TPC and TFC values than *** percentage of antioxidant activity based on the initial values indexed by DPPH,ABTS,and FRAP gradually declined from approximately 60%at the gastric stage to approximately 40%at the final digestion ***,the percentage of residual MIC was around 50%at the gastric ***,it gradually increased at the intestinal *** significantly lower antioxidant activity showed for WOE than MD throughout the simulated *** study demonstrated that digestive enzymes and pH play a crucial role in the bioavailability of green tea infusion.

关键词： Green tea Polyphenols Antioxidant activity Digestive enzyme bioavailability