Experimental and Therapeutic Medicine
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2019
·Vol. 17
·期 5
·3501-3508
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IF 1.448
Jing Jin,Qiao‑Yun Hu,Wen‑Wen Xu,Wen‑Jia Zhu,Bei Liu,Jing Liu,Wei Wang,Hui‑Fang Zhou
Tanshinone IIA (TSIIA) is a major component of Salvia miltiorrhiza, a Chinese herb that exhibits a therapeutic effect on polycystic ovary syndrome (PCOS). The present study replicated PCOS via the neonatal treatment of estradiol in mice. Estrous cycles, body and ovarian weight, serum levels of testosterone and estradiol were determined. Histological examination of ovaries was performed. The mRNA and protein levels of aromatase luteinizing hormone receptor and follicle‑stimulating hormone (FSHR) in ovaries and granule cells were assayed by reverse transcription‑quantitative polymerase chain reaction and western blotting, respectively. TSIIA was revealed to reverse all disorders induced by estradiol treatment, including prolonged estrous cycles, increased body and ovarian weight, increased atretic cyst‑like follicles and decreased corpus luteum, large antral follicles and preovulatory follicles. These improvements in PCOS as a result of TSIIA treatment are likely due to the revised testosterone/estradiol balance, as TSIIA reversed the decrease in aromatase mRNA, the enzyme that converts androgen to estrogen. As the expression of aromatase is regulated by the FSH pathway, TSIIA‑mediated elevation in FSHR expression may lead to the upregulation of aromatase. Therefore, TSIIA revises the balance of androgen and estrogen by rescuing the reduced expression of FSHR and aromatase, thus attenuating murine PCOS. The current study aimed to further the application of natural drugs in the treatment of PCOS to confront the side effects of hormone drugs and expand the use of TSIIA.
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ANALYTICA CHIMICA ACTA
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2019
·
IF 5.256
Lingzhong Wan,Guanda Gong,Hao Liang,Guangming Huang
In situ identification and quantification of unsaturated fatty acid (FA) C=C positional isomers in human serum is herein performed by negative-ion paper spray (PS) mass spectrometry. Typically, by direct application of an alternating current (AC) voltage to the wet paper, the PS ionization could perform stably in the negative-ion mode without severe discharge. We suppose epoxidation reaction between unsaturated C=C bonds and reactive oxidative species might be initiated by a mild electrical discharge, which could be rapidly and controllably produced via a low amplitude AC voltage. Upon collision-induce dissociation (CID), the epoxide was fragmented to generate diagnostic ions indicating the C=C location. The intensity of the characteristic product ions could also be used for absolute quantification of the FA C=C positional isomers. The limits of detection (LODs) and limits of quantification (LOQs) were roughly in the range of 0.0178–0.0506 μ M and 0.0218–0.3634 μ M for standard FAs. Without the additional sample preparations or reactive chemical reagents , epoxidation of unsaturated FAs and ionization of the epoxide could be achieved in one-step by negative-ion mode PS, which enable a promising methodology for on-site clinical diagnosis.
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Acta Pharmaceutica Sinica B
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2019
·
IF 5.808
Fangfang Li,Zongliang Liu,Heyuan Sun,Chunmei Li,Wenyan Wang,Liang Ye,Chunhong Yan,Jingwei Tian,Hongbo Wang
Gliomas are the most common primary intracranial neoplasms among all brain malignancies, and the microtubule affinity regulating kinases (MARKs) have become potential drug targets for glioma. Here, we report a novel dual small-molecule inhibitor of MARK3 and MARK4, designated as PCC0208017. In vitro, PCC0208017 strongly inhibited kinase activity against MARK3 and MARK4, and strongly reduced proliferation in three glioma cell lines. This compound attenuated glioma cell migration, glioma cell invasion, and angiogenesis. Molecular mechanism studies revealed that PCC0208017 decreased the phosphorylation of Tau, disrupted microtubule dynamics, and induced a G2/M phase cell cycle arrest. In an in vivo glioma model, PCC0208017 showed robust anti-tumor activity, blood–brain barrier permeability, and a good oral pharmacokinetic profile. Molecular docking studies showed that PCC0208017 exhibited high binding affinity to MARK3 and MARK4. Taken together, our study describes for the first time that PCC0208017, a novel MARK3/MARK4 inhibitor, might be a promising lead compound for treatment of glioma.
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NEW JOURNAL OF CHEMISTRY
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2019
·Vol. 43
·期 34
·13363-13370
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IF 3.069
Weifen Niu,Juan Jia,Junkai Li,Chao Zhang,Keming Yun
The lysosome is known to be an acidic organelle that is ubiquitous in cells. Acidic pH is a characteristic feature of lysosomes, and aberrant lysosomal pH values have been manifested to be associated with diverse diseases. In order to monitor the lysosomal pH changes, we developed a ratiometric emission NIR-fluorescent probe (CzQl) for the quantitative analysis of the lysosomal pH in living cells and in vivo. CzQl was constructed via the ethylene bridging of carbazole derivatives and quinoline. The protonation of the probe resulted in a marked green-to-red emission color change. The probe exhibited an ideal pKa value of 4.60 with a linear relationship in the pH range of 3.9–5.3, which covered most of the pH ranges of lysosomes, and was useful for the quantitative detection and imaging of lysosomal pH changes. Moreover, CzQl exhibited easy loading capability, high selectivity, a large Stokes shift, specific lysosome-targeting ability and low cytotoxicity; thereby, it was successfully used for monitoring the lysosomal pH changes at a cellular level as well as the LPS-mediated inflammation in vivo.
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ANALYTICA CHIMICA ACTA
·
2019
·
IF 5.256
Pei Dai,Dajiao Hou,Shun Guo,Lihua Zhu,Ming Lei,Heqing Tang
A new determination method for total bromine in electronic devices was developed by using ultrasound assisted extraction , copper-catalyzed reductive debromination and ion chromatography (UAE-RD-IC). It was found that all the added brominated flame retardants (polybrominateddiphenyl ethers, polybrominated biphenyls , tetrabromobisphenol A, and hexabromocyclododecane) could be completely debrominated by using copper-based catalysts and reducing agent N 2 H 4 •H 2 O. The complete debromination of brominated flame retardants released all of their bromine in the form of bromide ions, which could be determined by ion chromatography. After the extraction parameters were optimized by achieving the maximum IC signal in the certified reference material GBW(E) 082725, the UAE-RD-IC method was established for the determination of total bromine in solid samples. By analyzing the certified reference material, the Br content was obtained as 695.3 ± 16.0 mg kg −1 , being well consistent with its standard value (694.54 ± 30.63 mg kg −1 ). The relative standard deviation (RSD) of five parallel determinations was 1.7%, indicating the good repeatability of the developed method. The proposed method was further applied to analyze the samples of cables and computer mouse shells. For all these practical samples, the Br contents obtained by the UAE-RD-IC method were in good agreement with that obtained by the standard oxygen bomb combustion-IC method. It was noted that the new method has a detection limit of Br of about 20 mg kg −1 , being much lower than that (75 mg kg −1 ) of the traditional oxygen bomb combustion-IC method for total bromine detection. Therefore, the proposed method was qualified as a practical method to measure total bromine content in actual electronic devices with good analytical performances of accuracy, precision and sensitivity.
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International Journal of Oral Science
·
2019
·Vol. 11
·期 1
·1-12
·
IF 2.75
Jiang Yuanjing,Zhang Shixian,Mao Chuanqing,Lai Yongzhen,Wu Di,Zhao Hu,Liao Caiyu,Chen Weihui
The Hedgehog (Hh) signalling pathway is essential for cellular proliferation and differentiation during embryonic development. Gain and loss of function of Hh signalling are known to result in an array of craniofacial malformations. To determine the critical period for Hh pathway antagonist-induced frontal bone hypoplasia, we examined patterns of dysmorphology caused by Hh signalling inhibition. Pregnant mice received a single oral administration of Hh signalling inhibitor GDC-0449 at 100 mg•kg − 1 or 150 mg•kg − 1 body weight at preselected time points between embryonic days (E)8.5 and 12.5. The optimal teratogenic concentration of GDC-0449 was determined to be 150 mg•kg − 1 . Exposure between E9.5 and E10.5 induced frontal bone dysplasia, micrognathia and limb defects, with administration at E10.5 producing the most pronounced effects. This model showed decreased ossification of the frontal bone with downregulation of Hh signalling. The osteoid thickness of the frontal bone was significantly reduced. The amount of neural crest-derived frontal bone primordium was reduced after GDC-0449 exposure owing to a decreased rate of cell proliferation and increased cell death.
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JOURNAL OF MICROENCAPSULATION
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2019
·
IF 2.04
Ran Li,Rui Bao,Qiu-Xuan Yang,Qi-Long Wang,Michael Adu-Frimpong,Qiu-Yu Wei,Toreniyazov Elmurat,Hao Ji,Jiang-Nan Yu,Xi-Ming Xu
Aims: The aim was to improve the absorption and bioavailability of [6]-shogaol with β-cyclodextrin (β-CD) prior to in vitro and in vivo evaluation.Methods: [6]-Shogaol/β-CDs inclusion complexes (6-S-β-CDs) were developed using saturated aqueous solution method and characterised with appropriate techniques. The absorption and bioavailability potential of [6]-shogaol was evaluated via in vivo pharmacokinetics and in situ intestinal perfusion.Results: The results of characterisation showed that 6-S-β-CDs (drug loading, 7.15%) were successfully formulated. In vitro release study indicated significantly improved [6]-shogaol release. Pharmacokinetic parameters such as Cmax, AUC0–36 h, and oral relative bioavailability (about 685.36%) were substantially enhanced. The in situ intestinal perfusion study revealed that [6]-shogaol was markedly absorbed via passive diffusion in the intestinal segments, and duodenum followed by ileum and jejunum.Conclusions: Cyclodextrin inclusion technology could enhance the intestinal absorption and oral bioavailability of hydrophobic drugs like [6]-shogaol.
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HIGH PERFORMANCE POLYMERS
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2019
·
IF 1.584
Yiyi Li,Yiting Xu,Shicheng Wang,Hongchao Wang,Meng Li,Lizong Dai
This study reports a strategy for further simplifying the synthesis process of polyaniline-modified graphene (An/G) nanocomposite. For this purpose, the An/G nanocomposite was prepared by expanded graphite (EG) and aniline (An) via in situ polymerization. The structures and morphologies of the An/G nanocomposite were examined by Fourier transform infrared spectroscopy, X-ray diffraction, scanning electron microscopy, transmission electron microscopy, Raman spectroscopy, ultraviolet–visible spectroscopy and atomic force microscopy. The results show that the An/G nanocomposite was synthesized successfully. The coatings were prepared using polyaniline (PANI) and An/G as the fillers and epoxy resin as the matrix. The anti-corrosion performance was evaluated by electrochemical impedance spectroscopy, Tafel polarization curve and salt immersion test. When An/G100 nanocomposite with a mass ratio of An to EG of 100:1 as a filler is used, the coating on the steel exhibited superior anti-corrosion effect. In particular, the impedance at 0.01 Hz of the coating with the An/G100 nanocomposite at a low loading of 2 wt% (An/G100-2) remained constant above 1 × 1010 Ω·cm2 for up to 35 days in 3.5 wt% sodium chloride solution. The Tafel plots reveal that the undamaged zone of the An/G100-2 coating possessed a high corrosion potential of −0.16 V, and the corrosion current density was only 1.5 × 10−11 A cm−2. The protective mechanism of graphene and PANI is discussed.
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BIOSYSTEMS ENGINEERING
·
2019
·
IF 2.983
Chengpeng Xu,Shengying Ye,Xiaolei Cui,Xianliang Song,Xueting Xie
Aflatoxin B1 (AFB1) is the most common and toxic among the aflatoxin group. Improper storage of both raw and processed peanut oil makes it susceptible to AFB1 production. Here, a closed-loop photocatalytic reactor consisting of a glass tube coated with TiO 2 as a catalyst has been developed to study the photocatalytic detoxification of AFB1 in peanut oil. The removal rates of AFB1 in the photocatalytic process were apparently higher than that of the photolysis process. It is inappropriate to approximate Langmuir–Hinshelwood kinetics by a first-order kinetic expression based on the experimental kinetic data for the photocatalytic process. The newly proposed Weibull distribution model provides a good description of the kinetics of the photocatalytic process over the ranges of initial AFB1 concentrations and light intensities studied. The key parameters affecting the detoxification efficiency in terms of the reliable life of this model are described.
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OncoTargets and Therapy
·
2019
·
IF 3.046
Yubin Ji,Yichen Liu,Nina Xue,Tingting Du,Liyuan Wang,Rui Huang,Ling Li,Chunhong Yan,Xiaoguang Chen
Purpose Esophageal squamous-cell carcinoma (ESCC) is the most common subtype of esophageal cancer, with a poor clinical outcome. Cryptotanshinone (CTS) is the main bioactive compound from the root of Salvia miltiorrhiza Bunge. Our study aimed to investigate the anti-cancer effects and molecular mechanisms of CTS on ESCC. Materials and methods We investigated the anti-tumor activity of CTS on ESCC in vitro and in vivo. Activation of the STAT3 signaling pathway was evaluated in ESCC and HEK-Blue™ IL-6 cells. Cell viability was assessed by the MTT assay. Apoptosis and cell cycle arrest were assessed using flow cytometry. Cell migration was detected by a scratch wound assay. Results CTS inhibited STAT3 expression and IL-6-mediated STAT3 activation in esophageal cancer cells. Subsequently, CTS dose-dependently inhibited the proliferation of esophageal cancer cells via induction of cell apoptosis. Furthermore, CTS suppressed the migration of esophageal cancer cells. In vivo, CTS inhibited tumor growth of EC109 cell in xenograft mice without any obvious effect on body weight. Conclusion Our results indicated that STAT3 inhibition may be a therapeutic target for esophageal cancer. CTS could provide a potential approach for esophageal cancer therapy by influencing the janus kinase-2/STAT3 signaling pathway.
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ANALYTICAL CHEMISTRY
·
2019
·
IF 6.35
Lin Zhou,Hanfeng Hou,Huan Wei,Lina Yao,Lei Sun,Ping Yu,Bin Su,Lanqun Mao
Oxygen (O2) is involved in many life activities, and its in vivo monitoring is of vital importance. In vivo electrochemistry with carbon fiber microelectrode (CFME) has been proven to be a suitable technique, but the surface fouling propensity poses a great challenge to its current stability and reliability. Herein we electro-grafted silica nanoporous membrane (SNM) consisting of uniform, closely packed, and vertically aligned nanochannels on the CFME surface, which was capable of protecting the surface effectively from biofouling and, meanwhile, preserving the permeability to O2. In comparison with a bare CFME, the SNM/CFME after implantation in the brain of a live rat maintained its analytical sensitivity to O2. Moreover, the implanted electrode could monitor O2 continuously under the in vivo condition, exhibiting an excellent current stability, as well as a fast response, up to 2 h. Further considering the high permeability, selectivity, and biocompatibility of SNM, we believe the modified CFME is a highly reliable sensor for long-term in vivo monitoring of O2, as well as other neurochemicals, with promise in physiological, ethological, and neurological studies.
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Artificial Cells Nanomedicine and Biotechnology
·
2018
·
IF 3.026
Kaili Wang,Chunjing Guo,Shaohua Zou,Yueming Yu,Xinxin Fan,Bingjie Wang,Mengna Liu,Lei Fang,Daquan Chen
To remedy the problems resulting from the usage of anti-cancer drugs in cancer chemotherapy, such as deficient drug concentration in tumour cells, low water-solubility and non-specific distribution of antitumour drugs, a kind of reduction-sensitive polymer prodrug of curcumin (Cur) containing in the nano-echinus was synthesized and designed. The nano-echinus-like nanomedicine presented synergistic effect with glycyrrhetic acid (GA) and oligomeric hyaluronic (HA) for targeting and combating HepG2 human liver cancer cell. Firstly, a kind of small molecular prodrug of Cur, dithiodipropionic acid-Cur (-SS-Cur), was chemically conjugated onto the side chain of the conjugated glycyrrhetic acid- oligomeric hyaluronic (GA-HA) to generate an amphiphilic polymeric prodrug of Cur, GA-HA-SS-Cur. The obtained GA-HA-SS-Cur prodrug and subsidiary material mPEG-DSPE could self-assemble into a sea urchin-like micelles in aqueous media and release Cur rapidly in response to glutathion (GSH). Then, Cur was loaded into the nano-echinus with a particle size of (118.1 ± 0.2 nm) and drug-loading efficiency of (8.03 ± 2.1%). The structure of GA-HA-SS-Cur was characterized by 1H-NMR in this report. The morphology of micelles was observed with a transmission electron microscope (TEM). Subsequently, the reduction-sensitivity of the nano-echinus was confirmed by the changes in in-vitro drug release after different concentrations of GSH treatment. Besides, the cellular uptake behaviour and MTT assays of the nano-echinus were investigated, suggesting that the nano-echinus was of desirable safety and could be taken into HepG2 cells in a time-dependent manner. Later, anti-tumour efficacy in vivo revealed the effective inhibition of tumour growth.
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