Antitumor drugs that target the signaling of vascular endothelial growth factor and its receptors have attracted increasing attention with the development of antiangiogenic targeted therapy. Apatinib is a second-generation vascular endothelial growth factor receptor-2 inhibitor and a potent antiangiogenic agent. Apatinib is one of the recent oral molecular targeted anti tumor drugs. Clinical studies have indicated that apatinib exhibits high bioavailability and a tolerable safety profile. A series of large-scale randomized and controlled clinical trials before and after the release of the drug in the market have demonstrated encouraging objective response rate and survival benefit across a broad range of malignancies, including non-small cell lung cancer, breast cancer, and gastric cancer. Apa-tinib was approved and launched in China in 2014 as a subsequent-line treatment for patients with advanced gastric cancer. Apatinib is currently undergoing phase II/III clinical trials for the treatment of numerous cancer types, such as gastric carcinoma, lung cancer, he-patocellular carcinoma, esophageal cancer, and colorectal cancer. These clinical trials are conducted to determine the antitumor activi-ty of apatinib when administrated alone or in combination with other therapies. This review summarizes the latest research progress of apatinib, including antitumor mechanisms, clinical effects on different tumor types, safety profile and adverse effects, drug interac-tions, as well as drug resistance and biomarkers. This article presents a deeper understanding of the clinical application of apatinib in anti tumor treatment, and provides reference for future clinical practice in therapeutic options for cancer patients.

Various column chromatography, such as silica gel, Sephadex LH-20, ODS, and semi-preparative HPLC was used to isolate and purify the chemical constituents from Cinnamomum cassia. The structures were determined on the basis of NMR and MS spectral data analysis, together with the comparison with literature data. Fifteen compounds were isolated from the 85% aqueous ethanol extract of C. cassia, and their structures were identified as (2R, 3R)-5,7,3',4'-tetramethoxyflavan-3-ol( 1), (2R, 3R)-5,7-dimethoxy-3',4'-methylenedioxyflavan-3-ol (2), coumarin (3), cinnamic acid (4), (E)-2-hydroxy-phenylpropionic acid cinnamoyl ester (5), 3, 3', 4, 4'-tetrahydroxy biphenyl (6), methylstictic acid (7), epi-boscialin (8), (1R,2S,3S,4S)-2,3-epoxy-1, 4-dihydroxy-5-methyl-5-cyelohexene (9), 4,5-dihydroxy-3-methyl cyclohex-2-enone (10), cis-4-hydroxymellein (11), and 2-hydroxy-4-methoxyl-cinnamaldehyde (12). Compounds 5-11 were obtained from this genus plants for the first time.
Cinnamomum aromaticum ; chemistry ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Mass Spectrometry ; Molecular Structure

Objective To discuss Extracorporeal Membrane Oxygenation(ECMO) management method and effect during inter-hospital transport of potential cardiac death donors after cardiac death (DCD).Methods 8 potential donors after cardiac death with brain injury were supported by ECMO for inter-hospital transport.All donors were inserted Medtronic overall cannula into one side femoral artery and venous.The position of catheters were guided by ultrasound.The front-end of venous catheter located in the junction of atrium and inferior vena cava,meanwhile the front-end of artery catheter was below renal artery.100 IU/kg heparin was injected before inserting cannulas.Flow of ECMO maintained at 2.0～3.0 L/min,and oxygen flow was 2～3 L/min during ECMO supporting.When hemodynamics of potential donors were stable,patients were moved into ambulance with ECMO for inter-hospital transport.Results A total of 8 ECMO transports were performed for central circulatory collapse caused brain injury.Patients were previously cannulated and on ECMO prior to transport and transported a distance of more than 100 kilometer from our institution by ambulance.ECMO running times were 120 min,and operation process circulatory stable.Conclusion ECMO can ensure inter-hospital transport of potential donors after cardiac death safety.

Objective:To explore the protective effect of ischemic postconditioning on myocardium during emergency percutaneous coronary intervention (PCI) in patients with ST segment elevation myocardial infarction (STEMI) . Methods:According to different treatment method ,a total of 82 STEMI patients ,who hospitalized in the depart-ment of Cardiology of Affiliated Hospital of Guangxi Medical University from Jan 2011 to Dec 2012 and received PCI within 12h ,were divided into ischemic postconditioning group (n= 42) and pure reperfusion group (n= 40) . Heart function etc .were evaluated in both groups .Results:Compared with pure reperfusion group ,there were sig-nificant rise in complete ST segment resolution rate (55.0% vs .81.0% ) and left ventricular ejection fraction [ (0.5 ± 0.1) vs .(0.7 ± 0.1)] ,significant reductions in arrhythmia rate (60.0% vs .21.4% ) ,wall motion score index [WMSI ,(2.0 ± 0.7) scores vs .(1.3 ± 0.6) scores] ,myocardial infarction size [MIS ,(15.1 ± 7.1)% vs .(9.9 ± 5.3)% ] ,radionuclide myocardial perfusion defect extent score [ES ,(0.4 ± 0.1)% vs .(0.2 ± 0.1)% ] and severity score [SS ,(2.3 ± 1.1)% vs .(1.8 ± 1.2)% ] in ischemic postconditioning group ,P<0.05~ <0.01 .Conclusion:Is-chemic postconditioning can significantly improve extent of myocardial ischemia reperfusion injury and protect myo-cardial tissues in STEMI patients .

Objective To investigate the changes and significance of serum nitric oxide levels in the early stage after rat liver transplantation.Methods Male Sprague Dawley rats were used as do- nors and recipients of orthotopic liver transplantation,and the time of cold preservation and anhepatic phase was 4 h and 25 min respectively.Forty-eight rats were randomly divided into groups A,B and C (n=16 each).The samples of blood were taken from vena cava and hepatic tissues from left lobe 2 h, 4 h,6 h in groups A,B and C respectively after liver graft reperfusion.ALT and NO levels in serum were detected,and the expression of NF-?B in hepatic tissue was examined by immunohistochemical technique.Amounts of bile flow in 5 min after liver graft reperfused initially were measured.The pathological changes in liver tissues were observed.Results Amounts of bile flow in 5 min in group A (3.73?1.11?l) were greater than those group B (2.35?0.92?l) and group C (2.23?0.81?l) (P

Objective: To analyze the metabolicomics pathway in the rats with chronic glomerulonephritis intervened by tannins from Pericarpium Granati.Methods: Signal pathway analysis was carried out using the KEGG database and molecular metabolite annotation was performed using HMDB database.The enzyme or transporter and its related properties were analyzed.The metabolite path visualization was carried out by using MetPA network software.Results: The analysis of biological metabolism pathway showed that 12 metabolites involved in 16 metabolic pathways.The pathway of tryptophan metabolism, citrate cycle, phenylalanine metabolism, cysteine and methionine metabolism showed notable changes (P<0.05).Conclusion: The changes of phenylalanine metabolism, citrate cycle, tryptophan metabolism, cysteine and methionine metabolism in the rats with chronic glomerulonephritis intervened by tannins from Pericarpium Granati participate the pathological process.

Referring to the rapid developed life science and the higher requirements for the approval of innovative Chinese drugs in recent years, this paper described systematically the discovery, research and development (R&D) approaches for the innovative Chinese drugs under the new situation from the following five aspects, i. e., active components discovered from TCMs, the discovery of effective fractions of TCMs and their formulae, the R&D of TCM innovative drugs based on famous classic prescriptions and famous Chinese patent drugs, and the transformation of clinical effective prescriptions, on the basis of analysing the advantages of innovative drugs derived from natural products based on TCM theories and the problems existed in current R&D of new TCM drugs. Moreover, five suggestions are also given for the rapid development of TCM innovative drugs in China. All these will provide reference for the R&D of TCM innovative drugs.
China ; Drug Discovery ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; pharmacology ; Humans ; Medicine, Chinese Traditional ; trends ; Research

This study is to develop a sensitive method by using reversed-phase high performance liquid chromatography coupled with UV detector (HPLC-UV) to simultaneously determine four bioactive compounds, iriflophenone 3-C-beta-D-glucoside, iriflophenone 3,5-C-beta-D-diglucoside, mangiferin, and iriflophenone 2-O-alpha-L-rhamnoside in the leaves of Aquilaria sinensis. An Agilent Zorbax SB-C, column (4, 6 mm x 250 mm, 5 microm) was used, and the gradient elution was performed with mobile phase of 0.1% aqueous phosphoric acid and acetonitrile at a flow rate of 1 mL x min(-1). The detection wavelength was 280 nm, and the column temperature was 25 degrees C. The four marker compounds were well separated with good linearity (R2 > 0.9990), precision, stability and repeatabili y. The-recovery rates were in the range of 98.80%-101.39%. For 15 branch of the leaves, the contents of iriflophenone 3-C-beta-D-gluoside, iriflophenone 3,5-C-beta-D-diglucoside, mangiferin, and iriflophenone 2-O-alpha-L-rhamnoside were between 0.41-14.48, 0.72-3.85, 4.30-29.07, 0.24-5.06 mg, respectivley. This method is precise, accurate and reliable, which provides an efficient way for the quality control of the leaves of A. sinensis. This will promote the comprehensive usage of this plant.
Benzophenones ; analysis ; Chromatography, High Pressure Liquid ; methods ; Drugs, Chinese Herbal ; analysis ; Plant Leaves ; chemistry ; Spectrophotometry, Ultraviolet ; methods ; Thymelaeaceae ; chemistry ; Xanthones ; analysis

Objective To investigate the value of high frequency color doppler ultrasound for screening thyroid diseases in physi-cal examination people .Methods The detectable information of thyroid diseases using high frequency color doppler ultrasound in 1 413 physical examination people was analyzed .Results A total of 588 cases of the 1 413 people were detected to have thyroid dis-eases with positive rate of 41 .61% ,and the detectable rate increased with aging .The positive rate of female (349 cases ,54 .96% ) was statistically higher than that of male(239 cases ,30 .72% ) .Within the 588 people ,111 cases were diagnosed as diffused thyroid diseases and 488 cases were diagnosed as thyroid nodules by high frequency color doppler ultrasound .Twenty cases were confirmed to have thyroid carcinoma by pathologic examination ,with 3 males and 17 females .Twelve lesions were less than 1 .0 cm in diameter and were diagnosed as microcarcinoma .The smallest lesion was 6 mm × 5 mm .Conclusion The high frequency color doppler ultra-sound was useful in screening for thyroid diseases ,especially for carcinoma ,and should be used as routine examination item .

With polyethylene glycol vitamin E succinate (TPGS) as the carrier materials, and berberine hydrochloride ( BER) as model drug, we formed berberine hydrochloride (BER) -loaded TPGS nanomicells (BER-PMs) using filming-rehydration method to improve its solubility and in vitro anti-tumor effect. The transmission electron microscope (TEM) was used to observe the particle appearance; particle detector was used to detect the diameter and Zeta potential; and ultracentrifugation was utilized to determine the encapsulation efficiency (EE) and drug-loading (DD); dynamic dialysis method was used to study the in vitro release behavior of BER-PMs, and the anti-tumor activity against MCF-7 cells was determined by MTT method. Results showed that the average particle size of BER-PMs was (12.45 ± 1.46) nm; particle size was uniform and spherical; drug loading and encapsulation efficiency were (5.7 ± 0.22)% and (95.67 ± 5.35)%, respectively. Zeta potential was (-1.12 ± 0.23) mV; release rate within 24 h was 37.20% and 41.14% respectively in pH 7.4 and pH 6.5 phosphate buffer in vitro; compared with BER, BER-PMs can significantly inhibit MCF-7 cell proliferation (P < 0.05), promote cell apoptosis and improve the anti-tumor activity of BER in vitro. Therefore, the formed berberine hydrochloride micelle can more effectively promote the apoptosis of MCF-7 cell, and improve the drug's in vitro anti-tumor effect.
Antineoplastic Agents ; chemistry ; pharmacology ; Berberine ; chemistry ; pharmacology ; Cell Death ; drug effects ; Cell Survival ; drug effects ; Drugs, Chinese Herbal ; chemistry ; pharmacology ; Humans ; MCF-7 Cells ; Particle Size ; Polymers ; chemistry ; pharmacology ; Solubility