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

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 ingredient.It exhibits a wide range of biological activities,such as anti-inflammatory,anti-cancer,antibacterial,antiviral,hepatoprotective,neuroprotective,anti-diabetic,and anti-thrombotic properties.As a result,it has gained significant recognition among practitioners of traditional Chinese and Indian medicine.These biological effects may be associated with multiple molecular targets and signal transduction pathways.However,the poor pharmacokinetic properties of the substance lead to lower bioavailability,which affects its effectiveness.To address this issue,scientists have proposed a number of strategies,such as solid dispersions,phytosome®technologies,and novel drug delivery systems.This article aims to provide a comprehensive overview for boswellic acids on the phytochemistry,molecular mechanisms,potential therapeutic applications,and strategies to improve bioavailability.

Enhancement in Bioavailability of CurCousin®, A Minor Metabolite from Curcuma longa by Addition of BioPerine® —A Pharmacokinetic Study

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.

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

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 rat.The formulations of TZP were optimized.With 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)%,respectively.After freeze-drying,TZP exhibited excellent redispersibility in water without aggregation.Physicochemical characterization showed that taxifolin existed in amorphous form in TZP and its interaction with the protein was observed.After encapsulating in TZP,the excellent dispersion of taxifolin in water signifi cantly improve its diffusion velocity through a semipermeable membrane.After 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 fabrication.The plasma concentration of taxifolin glucuronide and methylated taxifolin glucuronide was much higher than taxifolin.Glucuronidation was the dominating metabolism pathway of taxifolin in vivo.

Effect of Glycosylation on the Physicochemical Properties,Structure and Iron Bioavailability of Ferritin Extracted from Tegillarca granosa

Iron deficiency anemia(IDA)is a major global health problem.Tegillarca granosa has been considered as an excellent source of iron given its high content of iron-binding protein,ferritin.The aim of the present study was to determine the physicochemical properties,protein structures,and iron uptake of ferritin extracted from T.granosa,and to evaluate the potential impacts of chitosan glycosylation on these characteristics.Based on Box-Behnken design and response surface methodology,the optimal conditions for glycosylation included a ferritin/chitosan mass ratio of 4:1,a pH of 5.5,a reaction time of 10 min,and a reaction temperature of 50℃.Glycosylation caused decreased surface hydrophobicity and elevated water-holding capacity of ferritin due to the introduction of hydrophilic groups.Additionally,glycosylation improved antioxidant capacity of ferritin by 20.69%–189.66%,likely owing to the protons donated by saccharide moiety to terminate free radical chain reaction.The in vitro digestibility of ferritin was elevated by 22.56%–104.85%after glycosylation,which could be associated with lessβ-sheet content in secondary structure that made the glycosylated protein less resistant to enzymatic digestion.The results of the iron bioavailability in Caco-2 cells revealed that ferritin(78.85–231.77 ngmg^(−1))exhibited better iron bioavailability than FeSO4(51.48–114.37 ngmg^(−1))and the values were further elevated by glycosylation with chitosan(296.23–358.20 ngmg^(−1)),which may be related to the physicochemical properties of ferritin via glycosylation modification.These results provide a basis for the development of T.granosa derived ferritin and its glycosylated products,and can promote the utilization of aquatic resources.

Optimized solubility and bioavailability of genistein based on cocrystal engineering

With various potential health-promoting bioactivities,genistein has great prospects in treatment of a series of complex diseases and metabolic syndromes such as cancer,diabetes,cardiovascular diseases,menopausal symptoms and so on.However,poor solubility and unsatisfactory bioavailability seriously limits its clinical application and market development.To optimize the solubility and bioavailability of genistein,the cocrystal of genistein and piperazine was prepared by grinding assisted with solvent based on the concept of cocrystal engineering.Using a series of analytical techniques including single-crystal X-ray diffraction,powder X-ray diffraction,Fourier transform infrared spectroscopy,differential scanning calorimetry and thermogravimetric analysis,the cocrystal was characterized and confirmed.Then,structure analysis on the basis of theoretical calculation and a series of evaluation on the stability,dissolution and bioavailability were carried out.The results indicated that the cocrystal of genistein and piperazine improved the solubility and bioavailability of genistein.Compared with the previous studies on the cocrystal of genistein,this is a systematic and comprehensive investigation from the aspects of preparation,characterization,structural analysis,stability,solubility and bioavailability evaluation.As a simple,efficient and green approach,cocrystal engineering can pave a new path to optimize the pharmaceutical properties of natural products for successful drug formulation and delivery.

Preparation and bioavailability in healthy volunteers of cefaclor modified-release capsules

Aim To investigate whether modified-release cefaclor capsules could lead to a more suitable pharmacokinetic profile in the plasma. Methods Cefaclor pellets were prepared by extrusion/spheronization and coated by Eudragit L30D-55 or Eudragit NE30D, then the two sorts of pellets were filled to capsules in a 35：65 ratio to made a modified-release （MR） capsules. The bioavailability of the MR capsules was studied in 24 healthy volunteers after oral administration in a fast state using a commercially available immediate release （IR） capsule as a reference. Results The results showed that the MR formulation had a relatively good bioavailability compared with the commercial capsules, as well as a longer time keeping drug level above MIC than immediate release capsule. The relative bioavailability of the MR capsules was 97.4- 12.1%. Conclusion The data of the present study indicate that time of cefaclor plasma concentration above MIC can be substantially prolonged if cefaclor is administered as a modified- release product.

新烟碱类杀虫剂哌虫啶在3种典型土壤中的生物有效性

为探究新烟碱类杀虫剂哌虫啶在3种典型土壤中的降解及其生物有效性,本研究在室内模拟土壤生境,以赤子爱胜蚯蚓和哌虫啶分别作为受试模式生物和目标污染物,采用蚯蚓生物富集量和间接生物测量法,研究哌虫啶在不同类型土壤中的生物有效性。研究结果表明:哌虫啶在棕壤、红壤和黑土中的降解半衰期分别为11.45~12.62、12.42~14.38 d和5.19~10.21 d,在3种典型土壤中的降解速度为黑土>棕壤>红壤。哌虫啶在蚯蚓体内的生物累积量随其在土壤中含量的增加而增大,在10 mg·kg^(-1)哌虫啶处理下,棕壤、红壤和黑土中蚯蚓体内哌虫啶的含量分别为190、210 ng·g^(-1)和160 ng·g^(-1),生物富集法研究表明,哌虫啶在黑土中的生物有效性较低,在红壤和棕壤中的生物有效性相对较高。不同处理的蚯蚓受到哌虫啶的氧化胁迫,其蛋白质含量、抗氧化酶活性、谷胱甘肽巯基转移酶活性和丙二醛含量具有显著的差异性(P<0.05),各指标在黑土中受到的影响较小,在棕壤和红壤中受到的影响较大,哌虫啶在有机质含量丰富的黑土中生物有效性较弱,而在棕壤和红壤中生物有效性较强。

大麻二酚递送体系的研究进展

大麻二酚因其在治疗疼痛、焦虑、神经及运动障碍等方面的作用而备受关注。但大麻二酚存在水溶性低、首过代谢效应及全身生物利用度较低的缺点,极大限制了它的应用。构建递送体系可改善大麻二酚的药代动力学特征和生物利用度。综述了近年来用于提高大麻二酚溶解性及生物利用度的递送体系,分析了聚合物颗粒、脂质体、醇质体及环糊精递送体系的优势与局限性,展望了大麻二酚递送载体的发展方向,为开发新的大麻二酚纳米制剂提供参考。

某废弃煤矿区土壤重金属污染风险评价

煤矿在开采过程中产生大量煤矸石、洗煤水等废弃物,其中的重金属污染物经沉降、径流、淋滤等作用迁移、扩散至周边水土环境中,对生态环境构成威胁。为研究某废弃煤矿区土壤重金属污染状况,评价重金属污染生态风险,检测了该矿区煤矸石、水、土壤样品中Cu、Pb、Zn、As、Cr、Ni、Hg、Cd元素质量分数,利用单因子指数法和潜在生态危害指数法分别分析了土壤重金属污染状况和潜在生态风险;重点分析了矿区洗煤厂下游土壤重金属污染特征,并采用改进BCR连续提取法分析了洗煤厂下游土壤样品重金属元素(Cu、Zn、Cd)形态,借鉴风险评价编码法评价了重金属元素的生物有效性和环境风险。结果表明:①以平均值计,废弃煤矿区煤矸石中重金属质量分数较低,仅Cr元素质量分数稍高于土壤中的质量分数,且煤矸石中重金属元素质量分数均未超过相应的农用地土壤风险筛选值,对矿区土壤重金属污染影响小。②废弃煤矿区土壤重金属超标元素为Cu、Zn、Cd、Ni、As,Cu、Zn、Ni和As元素污染较轻微,Cd元素污染较严重;Cu、Zn、Ni元素污染区主要集中在矸石山西部和东南部地块,在空间分布上有一定重合;As元素污染分布在矸石山东北部地块,Cd元素污染在矿区广泛分布,以中度–重度污染为主。③Cd、Hg元素存在潜在生态危害风险,Cd元素潜在生态危害风险程度高,重金属元素综合潜在生态危害风险等级较高,主要为中等-强风险。④洗煤厂下游区域沿水流方向土壤重金属元素总体呈递减趋势,Cd元素污染较严重,Cu、Zn、Ni、As元素污染集中在洗煤厂下游200 m内,剖面样品中垂向方向上重金属元素质量分数呈递减趋势,在垂向上没有累积。⑤矿区地下水水质较好,矿井排水重金属元素质量分数及pH满足Ⅲ类地表水水质标准限值,矿井水外排对周边土壤重金属污染影响小。⑥Cu和Zn元素酸可提取态占比低,生物有效性低,Cd元素酸可提取态占比高,呈高度风险–极高风险,生物有效性强,环境风险高。基于矿区重金属污染现状,建议进一步加强土壤重金属污染防治工作,加强源头治理、农产品食品安全监测和Cd元素污染调查研究工作。

包封类胡萝卜素运载体系研究进展

类胡萝卜素主要存在于深色的水果蔬菜中,具有抗炎和抗氧化等生物活性功能,可以增强人体免疫系统,帮助抵御各种病毒,包括SARS-CoV2和其它病毒。类胡萝卜素也是天然的抗氧化剂和着色剂,在保护人体健康和工业发展方面起着重要的作用。然而,类胡萝卜素稳定性差和生物利用度低等缺陷使其不能充分发挥生物活性,这限制了类胡萝卜素在食品领域的应用。针对这些问题,可以利用食品级包封材料对类胡萝卜素进行包封处理来解决。本文简述类胡萝卜素的代谢过程和影响其生物利用度的因素,重点介绍包封类胡萝卜素递送系统的研究现状,旨在为类胡萝卜素在食品中的应用提供参考。

鄱阳湖流域赣江(南昌段)沉积物磷赋存形态特征及释放风险分析

本研究采用化学连续提取法,分析赣江南昌段表层沉积物磷赋存形态特征及其生物有效性,并通过等温吸附实验探讨了沉积物磷释放风险。结果显示:赣江南昌段表层沉积物总磷(TP)含量范围为235.21~702.24 mg/kg,均值为522.93 mg/kg,具有较高的空间异质性。所有采样点位中无机磷(IP)均以闭蓄态磷(Oc-P)为主要赋存形态,各形态无机磷含量特征表现为:Oc-P>铁结合态磷(Fe-P)>碎屑钙磷(De-P)>自生钙磷(ACa-P)>可交换态磷(Ex-P)>铝结合态磷(Al-P);有机磷(OP)以残渣态有机磷(Res-P_(o))为主要赋存形态,按活性划分表现为:非活性有机磷(NOP)>中活性有机磷(MLOP)>活性有机磷(LOP)。生物有效磷(BAP)含量范围为61.59~218.27 mg/kg,占TP含量的比例为27.07%。BAP总量及占TP的比例均处于较低水平,沉积物内源磷释放风险较低。BAP中Fe-P平均占比为56.72%,表明沉积物磷潜在释放风险主要来源于Fe-P。TP、Fe-P和De-P之间均存在显著相关关系,表明外源输入可能是赣江沉积物磷的主要来源。采样期间赣江南昌段沉积物磷平衡浓度(EPC 0)高于上覆水溶解性活性磷(SRP)浓度,磷吸附饱和度(DPS)均低于沉积物磷大量流失的临界值25%,表明此阶段沉积物磷虽作为上覆水的“磷源”,但出现大量释磷的可能性不高。因此,沉积物内源磷释放引起赣江水体富营养化的风险不高,这意味着赣江水体应更多关注外源输入问题。本研究结果为赣江南昌段水环境的科学管理提供了数据支撑和科学依据。

FeSO_(4)对水稻根表铁膜及污染稻田土中镉迁移转运影响研究

选取湖南某污染稻田耕作层土壤,通过盆栽实验外源施加硫酸亚铁(FeSO_(4)),研究FeSO_(4)对水稻根表铁膜及污染稻田土中镉(Cd)迁移转运的影响。结果表明,随着FeSO_(4)施加量增加(0~320 mg/kg),水稻根际土壤pH值呈下降趋势,最高下降了0.70;水稻盆栽土壤TCLP-Cd含量与对照组相比出现一定程度上升;施加FeSO_(4),降低了水稻茎叶、谷壳、糙米中Cd含量,增加了水稻植株根表铁膜的数量,一定程度上控制了水稻对土壤中Cd的吸收。但施加外源铁影响了土壤pH值及Cd的生物有效性,在实际稻田施加FeSO_(4)时建议与石灰等其他碱性修复材料进行组配,以获得更好的阻控效果。

中国优控多环芳烃土壤污染特征及国内外生物可给性研究进展

多环芳烃(PolycyclicAromaticHydrocarbons,PAHs)是一类持久性有机污染物,容易在土壤中累积并且毒性显著,但PAHs在土壤固相上的吸附性较强,基于土壤污染总量暴露会导致高估人群健康风险。本研究基于2000―2020年间发表的123篇文献,总结了我国土壤中16种优先控制多环芳烃(∑_(16)PAHs)的污染浓度分布和组成特征,介绍了11种常见的模拟PAHs生物可给性测试方法和主要影响因素,并总结了PAHs的生物可给性系数范围。调研表明土壤∑_(16)PAHs最高与平均浓度分别为23250和1314.7μg·kg^(–1),污染较为严重;近年来PAHs生物可给性测试方法主要基于生理原理提取法(PBET),在模拟消化过程和吸附剂等方面不断完善和改进,并且消化条件、土壤性质等因素对生物可给性结果影响较大。16种PAHs的生物可给性平均值范围为13.2%~72.4%,其中■和苯并[b]荧蒽的生物可给性较高,对∑_(16)PAHs暴露产生贡献较高。本调研结果为开展土壤PAHs污染精细化风险评估研究提供重要理论参考依据。

纳米石杉碱甲脂质体的热稳定性及分配系数

采用薄膜旋蒸-超声法制备了纳米石杉碱甲脂质体(Hup-A-Lip),并对其微观形貌、包封率、相变温度、分配系数及生物利用度等进行了研究.结果表明:Hup-A-Lip呈粒径约40 nm的球形结构;包封率为(82.74±2.68)%;相变温度为67℃,在25~60℃具有较好的热力学稳定性;Hup-A-Lip中药物与脂质体膜之间的作用力以静电相互作用和氢键为主;石杉碱甲(Hup-A)经脂质体包封后,明显提高了游离药物的生物利用度.

食品中自微乳体系的组成、制备及促进生物活性物质生物利用的研究进展

随着人们健康膳食意识的增强,开发食品功能作用引起了人们的广泛关注。自微乳体系是一种由油相、表面活性剂、助表面活性剂和生物活性物质以一定比例混合后形成的无水预浓缩体系。通过自微乳体系荷载食品生物活性物质可改善其生物利用度,并充分发挥其生理及药理活性。本文系统综述了自微乳的基本性质、组分及制备方法,整理了近年来自微乳体系在食品领域促进生物活性物质生物利用的应用实例,为自微乳体系在食品领域的推广应用提供了参考。

Determination of Loratadine in Human Plasma by High Performance Liquid Chromatography-Electrospray Mass Spectrometry and Studies on Its Pharmacokinetics and Relative Bioavailability

A new HPLC MS method to determine loratadine in human plasma was established. The method involved extracting drug with organic solvent under basic conditions. The samples were seperated by ODS column and determined by mass detector. The calibration curve of loratadine was linear within the range of 0.4～100 ng·mL -1 with r=0.9995 . The recovery of this method was within 95%～104%, within day and between day RSD were less than 12%. To study the pharmacokinetics and relative bioavailability of loratadine tablets, two formulations of loratadine tablets were given to 18 healthy male volunteers according to a randomized 2 way cross over design. The C max , AUC 0 t and T max values of the two formulations were 51.89±20.18 ng·mL -1 and 52.48±22.35 ng·mL -1 ; 140.75±88.42 ng·h·mL -1 and 147.24±92.33 ng·h·mL -1 ; 0.81±0.35 h and 0.81±0.27 h respectively. Results from statistic analysis showed that there were no significant difference between the C max , AUC 0-t and T max values of the two formulations. The relative bioavailability of tablets I with respect to tablets II was 97%±13% from the AUC 0 t measurement. Bioequivalance was observed between the two tablets.

果胶与多酚相互作用机制及其对食品加工特性影响的研究进展

果胶和多酚共存于植物性食品体系中。除天然存在的果胶-多酚复合物外,在受到加热、高压、干燥等外力作用的食品加工过程中,两者会快速且自发地进行相互作用。果胶与多酚之间的相互作用会影响食品的理化性质和功能特性。本文总结了果胶与多酚相互作用的机制、内部和外部多重影响因素、主要的研究方法并结合Langmuir和Freundlich常见的等温吸附模型对果胶与多酚之间的吸附行为进行描述和定量表征。此外还探讨了两者相互作用对食品加工特性及多酚生物可利用性的影响,分析了该领域的研究方向和发展趋势。

葛根素-猴头菇不溶性膳食纤维复合微胶囊的制备及理化性质的研究

目的:旨在制备葛根素-猴头菇不溶性膳食纤维复合微胶囊,通过提高其包埋率、抗氧化特性和生物可及性,进而促进葛根素相关产品的研发。方法:采用2.0%卡拉胶、3.0%海藻酸钠、0.5 g猴头菇不溶性膳食纤维、10.0 mg葛根素、5.0%的CaCl2溶液制得葛根素微胶囊(以不添加不溶性膳食纤维作为对照组),计算其包埋率、抗氧化特性、模拟体内消化释放率、生物可及性,并通过扫描电子显微镜(SEM)、X射线衍射(XRD)、傅里叶变换红外光谱(FT-IR)观察其微观结构。结果:猴头菇不溶性膳食纤维能够作为葛根素微胶囊的壁材,且包埋率均高于75.8%,最高可达94.66%,葛根素的承载量由空白组的0.60%增加到添加膳食纤维最高可达1.37%;消化前后DPPH、ABTS+两种自由基的清除能力显著低于未添加猴头菇不溶性膳食纤维的葛根素微胶囊(P<0.05),能够达到延缓抗氧化特性的作用;模拟体内消化的研究发现猴头菇不溶性膳食纤维包埋的葛根素(最低为9.46%)相对于游离的葛根素(17.46%)在胃中能够缓慢的释放,在进入肠道后迅速释放出来并大量溶于模拟肠道液中,使得葛根素肠道中的释放率从游离的22.93%增加到添加不溶性膳食纤维的最高可达92.59%,实现肠道的精准释放,显著提高了葛根素的生物可及性,是游离葛根素的2.9~3.9倍;SEM、FT-IR、XRD从微观层面证实超声辅助提取法所得猴头菇不溶性膳食纤维作为葛根素微胶囊的壁材,能够改善对照组微胶囊将葛根素裸露的缺点,使得微胶囊质地更紧密,也证实猴头菇不溶性膳食纤维的包埋使得葛根素的结晶度降低或消失以及葛根素的特征衍射峰发生偏移或减弱,达到良好的包埋效果。结论:添加猴头菇不溶性膳食纤维能够提高葛根素的溶出速率,延缓葛根素抗氧化的时长,实现其在肠道中的定点释放,提高葛根素的生物可及性和生物利用率,可以作为葛根素微胶囊的壁材。

Pharmacokinetics and Absolute Bioavailability of the Sublingual Naloxone Hydrochloride Tablet in Dogs

The pharmacokinetics and absolute bioavailability of the sublingual naloxone tablet were studied with HPLC-electrochemical detection. Eight male dogs received single 5 mg dose of naloxone intravenously, the plasma concentration-time curves could be fitted to two-compartment open model, with 12.0 min of t1/2( , 143.4 min of t1/2( and 7.92 mg(min/L of AUC. The same eight dogs received 5 mg dose of the sublingual naloxone tablet after an interval of a week. The main pharmacokinetic parameters were: t1/2ka = 11.0 min, t1/2( = 15.4 min, t1/2( = 164.1 min, Tmax = 27.7 min, Cmax = 34.2 ng / ml, and AUC = 6.79 mg(min / L, respectively. The plasma concentration-time curves were fitted to the first order absorption two-compartment open model also. The mean absolute bioavailability of the sublingual naloxone tablet was 86.8 ( 10.9%. No statistically significant differences were found with t1/2(, t1/2(, ( and ( between the two routes of administration. These results indicated that the course of disposition for naloxone in dogs was similar for the two routes of administration, and the absolute bioavailability of the sublingual naloxone tablet was high. Thus satisfactory clinical effects could be expected.

柚皮素及其纳米递送体系研究进展

柚皮素是广泛存在于柑橘类水果中一种黄酮类化合物,具有多种生理功效,如抗肿瘤、抗氧化和抗炎活性等。然而,由于柚皮素的疏水性,导致其生物利用度较差,应用潜力受到阻碍。为了提高柚皮素的生物利用度,研究人员开发了包括聚合物纳米颗粒、脂质体、纳米乳液、纳米混悬液在内的纳米递送系统。在此,该文对柚皮素的生理功能、体内代谢及其纳米递送体系进行了介绍,针对目前研究中存在的问题对未来柚皮素纳米递送体系的研究方向和应用前景进行了展望。