JOURNAL OF CHEMICAL AND ENGINEERING DATA
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2022
·
IF 3.119
Zhengxu Li,Hao Wu,Baifeng Hu,Jin Guo,Yuxiang Liu,Han Yue,Hongkang Zhao,Qunsheng Li
The solubility of 2′,4′-dihydroxyacetophenone (2′,4′-DHAP) in 10 monosolvents (methanol, ethanol, n-propanol, isopropanol, n-butanol, isobutanol, methyl acetate, ethyl acetate, propyl acetate, and benzene) and two binary solvents (ethanol + ethyl acetate and n-propanol + ethyl acetate) was determined using a gravimetric method at 101.3 kPa from 293.15 to 333.15 K. The experimental solubility was demonstrated to increase with the increasing temperature. The solubility of 2′,4′-DHAP is the highest in pure isopropanol, and the two binary solvents present a solubilizing effect on the solute. Furthermore, six thermodynamic models were employed to fit the solid–liquid equilibrium data, and the correlation results manifested that the modified Apelblat model had minimum ARD values of less than 1%. Finally, the KAT-LSER model was employed to analyze the solvent effect at 298.15 K. The results show that the contribution of the four interaction types α, β, π*, and δH account for 15.84%, 15.30%, 18.33%, and 50.53% of the total interaction force, respectively, and the solvent–solvent interaction represented by δH is the dominant factor affecting the solubility of 2′,4′-DHAP.
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FUNDAMENTAL & CLINICAL PHARMACOLOGY
·
2023
·
IF 2.9
Yanting Li,Zhenwei Xie,Liming Chen,Xiangxing Liu,Shuang Li,Shichun Ye,Hongyan Tang,Chongyou Lee,Qun Gu,Fang Men,Jiaojiao Zhang,Dingyuan Hu,Yuanli Jiang,Xiaochun Wang,Qian Wang,Yufei Feng,Suping Niu,Yan Liu,Yi Fang
Background It was evidenced that cetylpyridinium-chloride (CPC) mouthwash could inhibit SARS-COV-2 activity and reduce salivary viral load, thus reducing SARS-CoV-2 transmission. However, due to insufficient residence time in the oral cavity, CPC-containing mouthwashes have no prolonged antiviral effect. The duration of action of the CPC buccal tablet is expected to be longer than that of the mouthwash. However, there are currently no reports on the salivary drug concentration of CPC buccal tablets. Objective The study aimed to investigate the salivary drug concentration of CPC buccal tablets and the antiviral effect of CPC on SARS-CoV-2 in vitro. Trial design This is a single-dose, single-arm clinical trial, involving 10 Chinese healthy subjects who received 2-mg CPC buccal tablet to collect saliva samples and to detect saliva concentration at different timepoints within 2 h (Clinical Trial Registration Number: NCT05802628, Registration Date: April 6, 2023). Materials and methods CPC concentration in saliva was detected by liquid chromatography tandem mass spectrometry (LC–MS/MS), and pharmacokinetic parameters were calculated based on the non-compartmental model. With an in vitro antiviral experiment, the activity of CPC buccal tablets against SARS-CoV-2 and its cellular toxicity was tested. Results Drug concentrations in saliva at 15 min, 30 min, 1 h, 1.5 h, and 2 h after administration were 8008.33 (1042.25, 41081.11), 2093.34 (373.15, 5759.83), 1016.58 (378.66, 3480.68), 891.77 (375.66, 6322.07), and 717.43 (197.87, 2152.71) ng/mL. PK parameters of saliva concentration: C max = 8008.33 (1042.25, 41081.11) ng/mL, AUC 0-t = 4172.37 (904.42, 13912.61) ng/mL * h, AUC 0-∞ = 6712.85 (1856.77, 19971.12) ng/mL * h, T 1/2 = 1.22 (0.59, 2.83) h, T max = 0.25 (0.25, 0.25) h. As determined in in vitro experiment, CPC was active on SARS-CoV-2 with cytotoxic and inhibitory activity of CC50 = 35.75 μM (≈12155 ng/mL) and EC50 = 7.39 μM (≈2512.6 ng/mL). Conclusions The comparison between the salivary CPC concentration and EC50/CC50 values from in vitro antiviral experiments suggests that CPC buccal tablets may inhibit SARS-CoV-2 activity, and the inhibition may last for approximately 30 min without cytotoxicity.
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COLLOIDS AND SURFACES B-BIOINTERFACES
·
2023
·
IF 5.8
Jie Huang,Xiao Tang,Ziqiong Yang,Jianqiu Chen,Kun Wang,Chengnan Shi,Zihan Liu,Ming Wu,Qian Du
Irinotecan (CPT-11) is used as a first or second-line chemotherapy drug for the treatment and management of colorectal cancers. In vitro studies have shown that 7-ethyl-10-hydroxycamptothecin (SN38), the active metabolite of CPT-11, displays promising anticancer efficacy. However, its poor aqueous solubility and hydrolytic degradation result in its lower oral bioavailability and impracticable clinical application. To overcome these limitations, a novel amphiphilic chitosan derivative, deoxycholic acid decorated N’-nonyl-trimethyl chitosan, was synthesized. Nano-micelles loaded with SN38 were subsequently prepared to enhance the bioavailability and anti-tumor efficacy of the drug through oral administration. The nano-micelles demonstrated improved dilution stability, enhanced greater mucosal adherence, significant P-gp efflux inhibition, and increased drug transport in the intestine by paracellular and transcellular pathways. Consequently, both the in vivo pharmacokinetic profile and therapeutic efficacy of SN38 against cancer were substantially improved via the micellar system . Thus, the developed polymeric micelles can potentially enhance the SN38 oral absorption for cancer therapy, offering prospective avenues for further exploration.
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FOOD CHEMISTRY
·
2021
·
IF 7.514
Li Zhong,Rui Wang,Qin-Hui Wen,Jian Li,Jia-Wei Lin,Xin-An Zeng
In this study, the binding mechanism between bovine serum albumin (BSA) and three gingerols ([6]-, [8]- and [10]-gingerol) was evaluated to explore an effective strategy for improving solubility and stability of gingerols. The fluorescence analysis suggested gingerols could bind with BSA to form a stable BSA/gingerols complex and [10]-gingerol had the strongest binding affinity ( K a = 4.016 × 10 4 L/mol) at 298 K. Thermodynamic parameters and molecular modeling validated that hydrophobic interaction and hydrogen bonds were the main driving force for the interaction of BSA/gingerols. Gingerols bound to BSA at site I (subdomain IIA) resulted in a conformational change of BSA with a structure shrinkage, which was responsible for the decrease of surface hydrophobicity. The formation of BSA/gingerols complexes promoted the solubility of [6]-, [8]- and [10]-gingerol increasing by 1.50, 6.04 and 23.50 times, respectively. In addition, the stability and antioxidant capacity of gingerols was significantly improved after binding with BSA.
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JOURNAL OF SEPARATION SCIENCE
·
2019
·Vol. 43
·期 3
·569-576
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IF 2.516
Ruonan Shuang,Mengdi Wang,Juanling Mao,Jiamei Zou,Yuhui Ping
10-Hydroxycamptothecin is a drug to cure various cancers. However, the 10-hydroxycamptothecin cannot be widely applied in clinics due to fast elimination and resistance of various cancers to the drug. Nevertheless, co-treatment with tetrandine is known to reverse the resistance of multi-drug resistant cancers, and may present an effective strategy to improve the efficacy of 10-hydroxycamptothecin. In order to improve the bioavailability and prolong the treatment time of the 10-hydroxycamptothecin in vivo, we prepared 10-hydroxycamptothecin-tetrandrine liposome complexes with 10-hydroxycamptothecin as the basic anticancer drug, tetrandrine and liposomes as carriers. In this article, an ultra-high performance liquid chromatography tandem mass spectrometry method for the analysis of 10-hydroxycamptothecin and tetrandrine in plasma has been developed, validated, and utilized to compare the pharmacokinetics of both drugs in the original dosage form and administered as liposome complexes. According to the pharmacokinetic parameters of mean residence time, half-life period and clearance rate, the 10-hydroxycamptothecin-tetrandrine liposome complexes prolongs the retention and circulation time of 10-hydroxycamptothecin in vivo, achieving a good sustained release effect. To the best of our current knowledge, the pharmacokinetic properties of 10-hydroxycamptothecin-tetrandrine liposome complexes in rats have not been reported yet. Our study can provide a helpful reference for further related study.
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RSC Advances
·
2018
·Vol. 8
·期 72
·41368-41375
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IF 2.936
Liangliang He,Jinjin Xu,Qi Wang,Yezi Zhang,Zifei Qin,Yang Yu,Zhengming Qian,Zhihong Yao,Xinsheng Yao
Shogaols, mainly [6]-shogaol (6S), [8]-shogaol (8S) and [10]-shogaol (10S), the predominant and characteristic pungent phytochemicals in ginger, are responsible for most of its beneficial effects. However, poor oral bioavailability owing to extensive glucuronidation limits their application. The present study aimed to characterize the glucuronidation pathways of 6S, 8S and 10S by using pooled human liver microsomes (HLM), human intestine microsomes (HIM) and recombinant human UDP-glucosyltransferases (UGTs). The rates of glucuronidation were determined by incubating shogaols with uridine diphosphate glucuronic acid-supplemented microsomes. Kinetic parameters were derived by appropriate model fitting. Reaction phenotyping assays, activity correlation analyses and relative activity factors were performed to identify the main UGT isoforms. As a result, one mono-4′-O-glucuronide was detected after incubating each shogaol with HLM and HIM. Enzymes kinetic analysis demonstrated that glucuronidation of shogaols consistently displayed the substrate inhibition profile, and the liver showed higher metabolic activity for shogaols (CLint = 1.37–2.87 mL min−1 mg−1) than the intestine (CLint = 0.67–0.85 mL min−1 mg−1). Besides, reaction phenotyping assays revealed that UGT2B7 displayed the highest catalytic ability (CLint = 0.47–1.17 mL min−1 mg−1) among all tested UGTs. In addition, glucuronidation of shogaols was strongly correlated with AZT glucuronidation (r = 0.886, 0.803 and 0.871 for glucuronidation of 6S, 8S and 10S, respectively; p < 0.01) in a bank of individual HLMs (n = 9). Furthermore, UGT2B7 contributed to 40.8%, 34.2% and 36.0% for the glucuronidation of 6S, 8S and 10S in HLM, respectively. Taken altogether, shogaols were efficiently metabolized through the glucuronidation pathway, and UGT2B7 was the main contributor to their glucuronidation.
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JOURNAL OF HETEROCYCLIC CHEMISTRY
·
2014
·Vol. 51
·期 4
·1094-1099
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IF 0.873
Guangfan Han,Jiawei Du,Lizhuang Chen,Lijun Zhao
A series of 2-amino-7-methoxy-4-aryl-4 H -chromene-3-carbonitrile compounds 2 were obtained by condensation of 3-methoxyphenol with β-dicyanostyrenes 1 in absolute ethanol containing piperidine. The intermediate enamines 3 were prepared by compounds 2 with 5-substituted-1,3-cyclohexanedione using p -toluenesuflonic acid (TsOH) as catalyst. The title compounds 11-amino-3-methoxy-8-substituted-12-aryl-8,9-dihydro-7 H -chromeno[2,3- b ]quinolin-10(12 H )-one 4 were synthesized by cyclization of the intermediate enamines 3 in THF with K 2 CO 3 /Cu 2 Cl 2 as catalyst. The structures of all compounds were characterized by elemental analysis, IR, MS, and 1 H NMR spectra. The crystal structure of compound 4i was determined by single-crystal X-ray diffraction analysis.
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INDUSTRIAL & ENGINEERING CHEMISTRY RESEARCH
·
2013
·
IF 2.206
Jiangfeng Yang,Junmin Li,Wei Wang,Libo Li,Jinping Li
Three hydrophobic microporous high-silica zeolites, DDR (with an 8-membered ring), silicalite-1 (a 10-membered ring), and beta (a 12-membered ring) were synthesized. The Si/Al ratios were 230, 1350, and 35, respectively. The samples were characterized by X-ray diffraction, scanning electron microscopy, thermal gravimetric analysis, water vapor adsorption, and volumetric nitrogen adsorption. They were tested for their CO2, CH4, and N2 adsorption properties at pressures of up to 10 bar at 288–313 K after activation, and the results were correlated with the Langmuir model. The heat of adsorption was calculated using the Clausius–Clapeyron equation based on the adsorption isotherms. These data were used to estimate the separation selectivities for CO2/CH4 and CH4/N2 binary mixtures at 298 K, using the ideal adsorbed solution theory (IAST) model. Experimental results showed that DDR and beta have good selectivities for CO2/CH4, because they have narrow pores (DDR) or more balance metal ions (relatively low Si/Al ratios beta) effect separately. The synthesized silicalite-1 has the lowest SCO2/CH4 but has the most suitable orifices for methane adsorption and the highest SCH4/N2. In addition, the breakthrough data for CH4/N2 mixtures further indicates that silicalite-1 is more suitable for the CH4 enrichment than the commercially used sorbents zeolite-5A and 13X. From the reproducibility of CH4 and N2 adsorption isotherms on silicalite-1, we can infer that which has the potential to be a commercial sorbent by the stable adsorption properties.
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PLANTA MEDICA
·
2016
·Vol. 82
·期 03
·230-237
·
IF 1.99
Xueli Zhang,Jiajia Lv,Liling Wang,Hua Shao
Taxanes are a class of bioactive compounds isolated from the Taxus species. 10-Deacetylbaccatin III is one of the popular taxane compounds with antitumor activity, but the pharmacokinetic profile of this compound remains elusive. Previously, we prepared the taxane fractions from the twigs and leaves of Taxus chinensis var. mairei containing 20.4 % 10-deacetylbaccatin III. This study aimed to investigate the pharmacokinetics of 10-deacetylbaccatin III and biodistribution, and explore the potential changes when it was administered in the form of taxane extracts. A simple, sensitive, and reliable liquid chromatography-tandem mass spectrometry method was developed and validated for the quantitative determination of 10-deacetylbaccatin III in biosamples. The results showed that 10-deacetylbaccatin III, after oral dosing, displayed a quick absorption into the blood and distribution into major organs. Oral administration of 10-deacetylbaccatin III in the form of taxane mixtures led to a 16-fold increase in the systemic exposure of pure 10-deacetylbaccatin III, with the AUC0-U in the plasma increasing from 25.75 ± 11.34 to 231.36 ± 70.12 µg h/L (p T. chinensis var. mairei, which contributed to an enhanced systemic exposure of pharmacologically active taxanes.
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JOURNAL OF MATERIALS CHEMISTRY
·
2011
·Vol. 22
·期 6
·2632-2640
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IF 5.101
Daqin Chen,Yunlong Yu,Feng Huang,Hang Lin,Ping Huang,Anping Yang,Zhaoxing Wang,Yuansheng Wang
We present a novel strategy involving the lanthanide dopant-induced formation of ultrasmall (sub-10 nm) uniform Ln3+:BaF2/Ln3+:SrF2 active-core/active-shell architectures. The lanthanide ions doped in the shell are demonstrated to play a key role to retard the growth of the core/shell nanocrystals. Particularly, adopting ∼3 nm Tm3+,Yb3+:BaF2 nanocrystals as cores prepared by a solvothermal reaction, growth of Gd3+,Nd3+:SrF2 shells is successfully induced on the surfaces of these cores through a thermal decomposition process, forming ∼7 nm highly uniform and monodisperse Tm3+,Yb3+:BaF2/Gd3+,Nd3+:SrF2 active-core/active-shell nanocubes. In this architecture, the Gd3+,Nd3+:SrF2 shell not only benefits the enhancement of the near-infrared to near-infrared upconversion luminescence of the Tm3+,Yb3+:BaF2 core, but also acts as the host to realize the near-infrared to near-infrared downconversion luminescence of Nd3+ dopants and the paramagnetism of Gd3+ ones. Importantly, the doping of Tm3+/Yb3+ and Nd3+ into the core and shell respectively effectively suppresses the adverse energy transfer from Tm3+ to Nd3+ as well as from Nd3+ to Yb3+, resulting in lessening of the quenching for both Tm3+ upconversion and Nd3+,Yb3+ downconversion emissions. These hydrophobic core/shell nanocrystals are further converted into hydrophilic ones using thioglycolic acid as the surface ligand. The sub-10 nm water-soluble active-core/active-shell architectures with near-infrared to near-infrared dual-modal luminescence and proper paramagnetism may find potential applications in biomedical imaging and detection.
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MOLECULAR NUTRITION & FOOD RESEARCH
·
2024
·Vol. 68
·期 19
·2400098
·
IF 4.5
Xinqi Huang,Lu Xiu,Yumei An,Yuan Gong,Sunao Li,Xueshi Chen,Chao Liu,Jianghuiwen Lu,Haiyan Shan,Jie Chang,Mingyang Zhang
The objective of this study is to elucidate how Royal jelly (RJ) and 10-hydroxy-2-decanoic acid (10-HDA) prevents diabetic skin dysfunction by modulating the pyroptosis pathway. Type 2 diabetes models are induced by fat diet consumption and low dose of streptozotocin (STZ) in C57BL/6J mice and treated with RJ (100 mg kg –1 day –1 ) and 10-HDA, the major lipid component of royal jelly (100 mg kg −1 day −1 ) for 28 weeks. The results show that serum concentrations of glucose and triglyceride are significantly lower in the RJ group or 10-HDA than diabetes mellitus (DM) group. Compared to the control group, pyroptosis proteins, GSDMD, ASC, Caspase-1, and IL-1β are increased in the skin of the diabetic model, accompanied by the activation of the Wnt/β-catenin signal pathway. Further evaluations by RJ exhibit superior improvement of skin damage, repress activation of the Wnt/β-catenin pathway, and attenuate keratinocyte pyroptosis, but 10-HDA cannot completely suppress the activation of Wnt/β-catenin pathway and pyroptosis, which shows a relatively weak protective effect on skin damage which shows that RJ is a better effect on skin injury after DM.
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HYDROMETALLURGY
·
2025
·
IF 5.3
Haokai Peng,Zuoying Cao,Shengxi Wu,Qinggang Li,Mingyu Wang,Xinsheng Wu,Wenjuan Guan,Guiqing Zhang
As the demand for Ni continues to rise, the recovery of Ni from electroplating sludge leachate has become an effective approach to alleviate supply constraints. However, the presence of impurities such as Cu, Zn, and Ca in the leachate complicates the Ni recovery process. To address these challenges, a novel pyridine group extractant, 2-((dodecylthio) methyl) pyridine (DMPY), was designed, synthesized, and evaluated for its synergistic performance with Versatic 10 (C 10 H 20 O 2 ) in selectively extracting Ni. Under optimal conditions, Ni was selectively recovered from electroplating sludge leachate including Cu, Zn, and Ca through three steps of the extraction processes. Mechanistic studies revealed that both DMPY and Versatic 10 anion coordinated with Ni 2+ , providing charge balance, forming the complex [Ni 2+ (DMPY) 2 (C₁₀H 19 O₂ − ) 2 ]. This synergistic solvent system significantly improved Ni extraction efficiency while minimizing reagent consumption. In conclusion, The DMPY-Versatic 10 system offers a sustainable and environmentally friendly solution, enhancing the hydrometallurgical treatment of polymetallic electroplating sludge and contributing to resource recovery and environmental protection.
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