TOXICOLOGY AND APPLIED PHARMACOLOGY
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2012
·
IF 4.447
Juan Li,Cai-Xia Dai,Hua Sun,Lu Jin,Chong-Yi Guo,Wei Cao,Jie Wu,Hai-Yan Tian,Cheng Luo,Wen-Cai Ye,Ren-Wang Jiang
Podophyllotoxin (POD) is a naturally occurring lignan with pronounced antineoplastic and antiviral properties. POD binds to tubulin and prevents the formation of mitotic spindle . Although cases of overdose or accidental ingestion are quite often, no specific therapy is currently available to treat the POD intoxication. In the current investigation, the protective effects and mechanisms of curcumin (CUR) on podophyllotoxin toxicity were evaluated in vitro and in vivo . The results showed that CUR could protect POD-induced cytotoxicity by recovering the G2/M arrest and decrease the changes of membrane potential and microtubule structure in Vero cells. A significant decrease of mortality rates was observed in Swiss mice treated by intragastrical administration of POD + CUR as compared with POD alone. The POD + CUR group also exhibited decreases in plasma transaminases , alkaline phosphatase , lactate dehydrogenase , plasma urea , creatinine and malondialdehyde level but elevated superoxide dismutase and glutathione levels as compared to the POD group. Histological examination of the liver and kidney demonstrated less morphological changes in the treatment of POD + CUR as compared with POD alone. The mechanism of the protective effects might be due to the competitive binding of CUR with POD in the same colchicines binding site as revealed by the tubulin polymerization assay and the molecular docking analysis, and the antioxidant activity against the oxidative stress induced by POD. In summary, both in vitro and in vivo data indicated the promising role of CUR as a protective agent against the POD poisoning.
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RSC Advances
·
2015
·Vol. 5
·期 47
·37697-37702
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IF 3.84
Liuyi Yin,Yufeng Hu,Xianming Zhang,Jianguang Qi,Weiting Ma
Batch reaction experiments were performed to investigate the salt effect on the yield of trioxane in the reaction solution. The salts considered include NaHSO4, Na2SO4, NaH2PO4, Na2HPO4, KCl, NaCl, LiCl, ZnCl2, MgCl2, and FeCl3. The effects of the anionic structure and the cation charge density on the yield of trioxane in the reaction solution were elucidated and the mechanisms that govern such effects were established. It is shown that the first four salts exerted a negative effect on the yield of trioxane in the reaction solution and such an effect increased progressively from left to right. This trend is due to the formation of NaHSO4, H3PO4, or (H3PO4 and NaH2PO4), which decreased the concentration of H+ in the solution. The latter six salts showed a positive effect on the yield of trioxane in the reaction solution. The salt effect paralleled the ability of the salt to decrease the water activity of the reaction solution and followed the order KCl < NaCl < LiCl < ZnCl2 < MgCl2 < FeCl3. Continuous production experiments were performed to investigate the salt effect on the concentration of trioxane in the distillate. The salts considered were KCl, NaCl, LiCl, ZnCl2, MgCl2, and FeCl3, and the salt effect increased progressively from left to right. Such an effect was shown to be determined by the ability of the salt to increase the yield of trioxane in the reaction solution and to increase the relative volatilities of trioxane and water and of trioxane and oligomers.
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JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
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2014
·
IF 3.107
Guang Yang,Tan Yang,Wendian Zhang,Miao Lu,Xiang Ma,Guangya Xiang
The antitumor efficacy of ursolic acid (UA) was limited by poor hydrophilicity and low bioavailability. To overcome this issue, UA was encapsulated in liposomes modified with folate conjugates for better solubility and bioavailability. This novel agent was prepared by a thin-film dispersion method and characterized by mean diameter, zeta potential, and entrapment efficiency (160.1 nm, −21.2 mV, and 88.9%, respectively). In vitro, cellular uptake efficiency, cytotoxicity, apoptosis, and cell cycle analyses were performed to show that folate-receptor (FR) positive cells endocytose more FR-targeted liposome (FTL-UA) than nontargeted PEGylated liposome (PL-UA) and that FTL-UA induced more cytotoxicity and higher apoptosis than PL-UA. Pharmacokinetic assessments showed advantages of systemic bioavailability of FTL-UA (AUC = 218.32 mg/L·h, t1/2 = 7.61 h) over free UA (AUC = 36.88 mg/L·h, t1/2 = 0.78 h). In vivo, FTL-UA showed significantly higher human epidermoid carcinoma (KB) inhibition in Balb/c nu/nu mice compared to PL-UA or free UA. The results indicate the great potential of FTL-UA against KB tumor.
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FLUID PHASE EQUILIBRIA
·
2014
·
IF 2.241
Ye Yuan,Yixin Leng,Hui Shao,Chunxiang Huang,Kai Shan
The solubility of dl -malic acid in water, ethanol and ethanol + water mixtures was investigated by a static analytical technique using the acid–base titration method at temperatures ranging from 298.15 to 333.15 K. The experimental results indicated that the solubility of dl -malic acid in the binary solvent mixtures increases with increasing temperature and decreases with increasing mass fraction of ethanol. The measured solid–liquid equilibrium (SLE) data were correlated by the modified Apelblat, λh and van’t Hoff equations. The calculated solubility demonstrated good agreement with the experimental data. It was found that the modified Apelblat equation could give the best correlation results, and subsequently used to derive the standard enthalpy, entropy and Gibbs energy change of solution of dl -malic acid in ethanol + water binary mixtures.
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PHOTOCHEMISTRY AND PHOTOBIOLOGY
·
2014
·Vol. 90
·期 5
·1144-1149
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IF 2.684
Zhi Li,Li-Li Pan,Fei-Long Zhang,Xia-Li Zhu,Yang Liu,Zhen-Zhong Zhang
This report explores some properties of 80–200 nm nanoparticles containing 5-aminolevulinic acid (ALA) and fullerene (C60) for photodynamic therapy (PDT). Compared with ALA, the nanoparticles yielded more protoporphyrin IX (PpIX) formation in cells and tissues and to a significant improvement in antitumor efficacy in tumor-bearing mice. Maximum levels of PpIX were obtained 4 h after administration and selective PpIX formation in tumor was observed. These nanoparticles appear to be a useful vehicle for drug delivery purposes. In this study, a procedure for preparing fullerene nanoparticles containing ALA was developed. The product alone exhibited no detectable toxicity in the dark and was superior to ALA alone in promoting PpIX biosynthesis and PDT efficacy both in culture and in a murine tumor model. These results suggest that this procedure could be the basis for an improved PDT protocol for cancer control.
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GREEN CHEMISTRY
·
2014
·Vol. 16
·期 8
·3881-3889
·
IF 6.852
Chenhua Shu,Tonghua Sun,Qingbin Guo,Jinping Jia,Ziyang Lou
In order to improve the desulfurization efficiency, an ionic liquid (IL) was used as the solvent for the desulfurization of diesel fuel with nickel boride. The nickel boride prepared in IL–H2O showed high specific surface area. The desulfurization efficiency of model organosulfur compounds in this work was higher than that in the previous studies. The desulfurization reactivity of model organosulfur compounds followed the order of BT (DBT) > 3-MBT > 4,6-DMDBT. Furthermore, the products of model organosulfur compounds after desulfurization were analyzed by GC/MS and their corresponding reaction routes were proposed. The effectiveness of nickel salts followed the order of NiCl2 (Ni(OAc)2) > NiSO4 > Ni(NO3)2. The desulfurization efficiency of model diesel fuels reached 90.6% under the conditions of B/S molar ratio = 9, Ni(OAc)2/S molar ratio = 3, oil/IL volume ratio = 3, water content in IL = 5%, and reaction time = 50 min. ILs maintained their original structures after regeneration. Finally, the desulfurization of real diesel fuel was carried out and a desulfurization efficiency of 88.6% was obtained in 50 min.
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JOURNAL OF HAZARDOUS MATERIALS
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2014
·
IF 4.331
Yan-Qing Wang,Chun-Yun Tan,Shu-Lin Zhuang,Peng-Zhan Zhai,Yun Cui,Qiu-Hua Zhou,Hong-Mei Zhang,Zhenghao Fei
Being the first-degree toxic pollutants, chlorophenols (CP) have potential carcinogenic and mutagenic activity and toxicity. Since there still lacks studies on molecular interactions of chlorophenols with trypsin, one major binding target of many exogenous environmental pollutants, the binding interactions between five chlorophenols, 2-CP, 2,6-DCP, 2,4,6-TCP, 2,4,6-TCP, 2,3,4,6-TCP and PCP and trypsin were characterized by the combination of multispectroscopic techniques and molecular modeling. The chlorophenols bind at the one main site of trypsin and the binding induces the changes of microenvironment and global conformations of trypsin. Different number of chloride atoms significantly affects the binding and the binding constants K A ranks as K A (2-CP) < K A (2,6-DCP) ≈ K A (2,4,6-TCP) < K A (2,3,4,6-TCP) < K A (PCP). These chlorophenols interacts with trypsin mainly through hydrophobic interactions and via hydrogen bonding interactions and aromatic–aromatic π–π stacking interaction. Our results offer insights into the binding mechanism of chlorophenols with trypsin and provide important information for possible toxicity risk of chlorophenols to human health.
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Artificial Cells Nanomedicine and Biotechnology
·
2014
·
IF 0
Meihao Liang,Xiaoliang Zheng,Linglan Tu,Zhen Ma,Zunyuan Wang,Dongmei Yan,Zhengrong Shen
In order to study the liver targeting of the N-galactosylated chitosan (GC) polymer in liver, we first conjugated the lactobionic acid with chitosan (CS) to obtain the carrier of GC with different degree of substitution of lactosyl group. Western blot was performed to detect the expression levels of the asialoglycoprotein receptors (ASGPR) in the cell lines of HepG2, SMMC-7721, and HL-7702. The protein level of ASGPR was lower in HepG2 compared to HL-7702 and SMMC-7721. Although all treated by CS, viabilities of HL-7702 and HepG2 did not experience any significant drop, while viability of SMMC-7721 decreased 15% on average from control. It was the first data about the inhibitory effect of GC on the liver cells. Fluorescein isothiocyanate (FITC) labeled GC (GC-FITC) was injected intravenously into mice at a dose of 0.02 μmol/mouse. GC-FITC showed maximum liver localization at 5 min and even detectable at 48 h after injection. Further, the accumulation of GC in liver was about 5.4-fold higher than that of CS. In conclusion, GC demonstrated its higher efficacy in drug liver targeting and thus could be a more promising drug or gene carrier in future therapies.
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PHARMAZIE
·
2014
·Vol. 69
·期 12
·898-903
·
IF 1.003
Xia Meng-Ming,Wang Li,Pan Pei-Pei,Wang Hai-Yun,Chen Meng-Chun,Chen Yi,Dai Da-Peng,Cai Jian-Ping,Hu Guo-Xin
CYP2C9 is one of four known members of the human cytochrome P450 CYP2C superfamily, with at least 57 CYP2C9 alleles being previously identified. Genetic polymorphisms of CYP2C9 significantly influence the efficacy and safety of some drugs, which might cause adverse effects and therapeutic
failure. The purpose of the present study was to clarify the role of 36 CYP2C9 alleles, 21 novel alleles (*36-*56) found in the Chinese population, in the oxidative metabolism of diclofenac in vitro. Insect microsomes expressing the 36 human CYP2C9 alleles were incubated with 2-100
μM diclofenac for 30 min at 37°C and terminated by the addition of 30 μL 0.1 M HCl. Diclofenac and 4'-hydroxyl (OH)-diclofenac, the major diclofenac metabolite, were analyzed by high-performance liquid chromatography (HPLC). Compared with wild-type CYP2C9*1, most variants
showed significantly altered values in Vmax, Km and intrinsic clearance (Vmax/Km). Only one variant exhibited markedly increased intrinsic clearance value, whereas 31 variants exhibited significantly decreased values. Thus, this study demonstrated
that more attention should be given to subjects carrying these CYP2C9 alleles when administering diclofena.
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Frontiers in Immunology
·
2026
·
IF 7
Yulin Wen,Shuangye Li,Jincan Jian,Jiahui Liu,Shuai Wang,Haomeng Wu
Background5-Aminosalicylic acid (5-ASA) is a first-line therapy for ulcerative colitis, but whether dosing timing influences its therapeutic efficacy remains unclear. This study aims to investigate the chronopharmacological effects of 5-ASA in experimental colitis.MethodsA dextran sulfate sodium (DSS)-induced colitis model was used to compare the therapeutic effects of 5-ASA administered at different Zeitgeber times. Colonic proteomic profiling was performed to identify circadian-responsive proteins associated with differential drug efficacy. Intestinal epithelial-specific Bmal1 knockout mice were used to determine whether the circadian clock regulates the chronopharmacological response to 5-ASA.Results5-ASA showed marked time-dependent efficacy in DSS-induced colitis, with greater protection at ZT14 than at ZT2. Proteomic analysis identified ferritin heavy chain 1 (FTH1) as a circadian-responsive protein associated with differential treatment outcomes. 5-ASA suppressed FTH1 expression, whereas FTH1 overexpression attenuated anti-inflammatory effects of 5-ASA. Moreover, intestinal epithelial-specific deletion of Bmal1 largely abolished diurnal variation in both FTH1 expression and 5-ASA efficacy, indicating that the intestinal clock coordinates the time-dependent response to 5-ASA.ConclusionThese findings identify FTH1 as a circadian-responsive factor linked to the time-dependent efficacy of 5-ASA and support circadian-guided optimization of 5-ASA administration as a potential strategy for improving UC treatment.
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ACS Sustainable Chemistry & Engineering
·
2025
·
IF 7.3
Jinglun Du,Huiling You,Changyan Zhu,Changhua Wang,Xintong Zhang,Yichun Liu
Sustainable nitrogen fixation is essential for advancing agriculture and chemical production. However, existing methods face trade-offs between energy intensity and efficiency. Low-activation-energy approaches fail to dissociate nitrogen effectively due to the strong N2 bond, while energy-intensive methods face energy loss from product decomposition. Here, we present an in-water plasma-based nitrogen fixation system that integrates metal electrodes (W, Al, and Fe) to achieve in situ activation of pulsed discharging plasma. This design enables efficient nitrogen dissociation and selective product formation of soluble nitrogen species (nitrate, nitrite, and ammonia), while minimizing decomposition through optimized product diffusion. This system achieves an energy consumption of 1.14 MJ mol–1 and a production rate of 12.9 mmol h–1 cm–2 for total soluble nitrogen species, surpassing other water-assisted methods and rivaling the Haber–Bosch process. Operating under ambient conditions, this electricity-driven, carbon-neutral approach offers a sustainable and efficient solution for decentralized application in agriculture and chemical production.
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ACS Applied Materials & Interfaces
·
2025
·
IF 8.2
Yandai Lin,Xinru Kong,Zhe Liu
Nitric oxide (NO)-based gas therapy has attracted increasing attention as a promising approach for tumor treatment, but elevated levels of glutathione (GSH) in the tumor microenvironment significantly limit their therapeutic effectiveness. In this study, a type of engineered photoactivatable nanomicelles Ce6/NI@PEP@HA (CNPH) were developed for combinational photodynamic and NO gas therapy. CNPH was capable of targeted accumulation to tumors, where it depleted GSH and released NO to effectively produce reactive oxygen species (ROS) with oxidative damage under laser irradiation at 660 nm. The GSH consumption induced the deactivation of glutathione peroxidase activity, leading to enhanced accumulation of toxic lipid peroxide and enabled a ferroptosis-like therapeutic outcome. Additionally, the effective production of NO and ROS resulted in mitochondrial dysfunction, characterized by the disruption of mitochondrial membrane potential and decreased adenosine triphosphate concentration. The in vivo animal experiments indicated that the combinational photodynamic and NO gas therapy achieved a tumor inhibition of 89.1%, and it has proven to be a more effective tumor therapy strategy in contrast to any single modality. In consequence, ferroptosis-like combinational tumor therapy has opened up a new horizon to a cutting-edge and noninvasive paradigm for advanced tumor treatments.
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