Tumor cells can metabolize glucose through glycolysis to intermediates for biomacromolecule synthesis by inhibiting the activity of the pyruvate dehydrogenase complex (PDC) in mitochondria. In this process, pyruvate dehydrogenase kinases (PDKs) play a key role. The inhibition of the activity of PDKs can effectively block this metabolic pathway, activate mitochondrial oxidative metabolism, and induce tumor cell apoptosis. PDK inhibitors have become a research hotspot in medicinal chemistry, and novel structures targeting classical binding sites have been synthesized. In this paper, recent research progress on PDK inhibitors is reviewed to provide information on these latest entities and to explore their clinical applicability.

Objective To explore the effect of interferon-?(IFN-?)on phenotypic transition of human Tenon’s conjunctival capsular fibroblast(HTCF). Methods Cultured HTCF derived from 4 operated human cataracts was induced for 48 hours in absence or presence of IFN-? and/or transforming growth factor-?1(TGF-?1). Then immunocytochemistry and Western blot technology were used to detect the ?-smooth muscle actin(?-SMA)expression and identificate the cell phenotype. Results In contrast to normal HTCF, IFN-?(10 ng/mL) inhibited the expression of ?-SMA(P

Objective To observe the protective effect of Erigeron Breviscapus(Vant.)Hand-Mazz(EBHM) on retinal ganglion cells(RGCs) and optic nerve in rabbits with elevated intraocular pressure(IOP). Methods Twenty rabbits with chronic elevated IOP were divided into two groups randomly: EBHM treated group(the ocular hypertension with EBHM treated subgroup and the normal IOP with EBHM treated subgroup) and untreated group(the simple ocular hypertension subgroup and the simple normal IOP subgroup). EBHM was irrigated into the stomachs to the treated group after IOP elevated continuously for 7 d.For light and electron microscopy studies,the rabbits' eyes were made into eyeball samples and optic nerve samples after 60 d.The density of RGCs,thickness of retinal nerve fiber layer(RNFL),and optic nerve axons were observed and quantitated by computer image analysis system.The ultra-microstructure changes of RGCs and optic nerve axons were observed by electron microscope.Results(①The RNFL) thickness,RGCs density and number of axons of the two ocular hypertension subgroups were decreased,compared with those of the two normal IOP subgroups(P

Objective To study the clinical value of capsule endoscopy for small bowel diseases in pediatric and adolescent patients.Methods Clinical data of 61 pediatric and adolescent patients who underwent capsule endoscopy from February 2007 to April 2014 was respectively analyzed.The positive diagnostic results and safety were observed.Results Of 61 patients,the CE procedures were completed successfully in 58 patients,and failed in 3 patients because of the gastric stasis.Forty-one positive lesions were found in small intestine,and the detection rate was 70.69％.Positive findings included angiodysplasias,Crohn' s disease,Meckel diverticula,ulcer,P-J syndrome,protrusion lesion and enteritis,etc.Finally,29 patients were confirmed (50％),3 (5.17％) were misdiagnosed and 1 (1.72％) was missed.Twenty-two patients underwent other small bowel examinations besides the capsule endoscopy.And the accuracy of capsule endoscopy was 81.82％.All capsules were successfully swallowed by the patients and evacuated within two weeks.No complications such as capsule retention or intestinal obstruction occurred.Conclusion Capsule endoscopy is a safe and well tolerated procedure with high diagnostic rate,which has a prospective clinical value in small bowel diseases in pediatric and adolescent patients.

Objective:To analyze the usage of anti-hypertensive drugs in our hospital,and provide a reference for clinical rational drug use.Method:With the consumption sort and DDDs analysis,the consumption of anti-hypertensive drugs used in 2006-2008 was analyzed.Result:The consumption of anti-hypertensive drugs in our hospital increased every year,and the consumption of the angiotensinⅡreceptor blockers(ARB),calcium channel blockers(CCB),angiotensin-converting enzyme inhibitor(ACEI) in three years were the top three of the total drug consumptions.Conclusion:The use of anti-hypertensive drugs was basically rational in our hospital and matched the domestic usage of anti-hypertensive drugs.

Animals ; Antioxidants ; metabolism ; Fatigue ; blood ; Female ; Hypericum ; chemistry ; Male ; Mice ; Mice, Inbred ICR ; Physical Conditioning, Animal ; Plant Extracts ; pharmacology

Objective To investigate the effect of angiotensinⅡ(AngⅡ) type 1 receptor blocker losartan on the cyclooxygenase 2 (COX-2) expression in metabolic syndrome (MS)kidney. Methods Seven-week-old male obese Zucker rats,a model of MS,were randomly divided into losartan treated and untreated group,and lean Zucker rats were used as controls.The obese Zucker rata of treated group received losartan for 4 months continuously.COX-2 expression was examined for all rats after 4 months.AngⅡ-stimulated mesangial cells and cortical tissue from AngⅡ-infused C57BL/6 mouse kidney by osmotic minipumps were used in this study.RNA and protein were obtained from renal cortical tissue or mesangial cells for RT-PCR and Western blot.Results Compared to the lean controls,obese Zucker rats showed a significant increase of COX-2 expression in the renal cortical tissue and these abnormalities were prevented by administration of losartan. Furthermore,the direct stimulation of AngⅡincreased COX-2 expression in mesangial cells in vitro and renal cortical tissue in vivo.Conclusions MS-induced COX-2 expression in the kidney is regulated by AngⅡ.Losartan as a non COX-2 inhibitor can protect MS kidney,at least in part,by inhibition of COX-2 activation.

AIM:To investigate NO-donor sodium nitroprusside(SNP)-induced apoptosis of human airway smooth muscle cells(HASMCs) of passive sensitization by serum from allergic asthmatic patients.METHODS: The technique of human airway smooth muscle(HASMCs) passively sensitized with serum from allergic asthmatic patients was adopted.The effect of SNP on the survival rate of passively sensitized HASMCs was detected by MTT method.Apoptosis of cells was detected by TUNEL and flow cytometry.RESULTS:(1) Compared to sensitized group,the survival rate of passively sensitized HASMCs decreased in SNP+sensitized group(n=5,P

Death ; Hematoma, Subdural/etiology* ; Humans ; Syphilis, Congenital/complications*

OBJECTIVETo evaluate the clinical efficacy and efficacy sustainable time of acupuncture in knee osteoarthritis (KOA).

METHODSThe non-randomized concurrent control trial was adopted. One hundred and ninety-three cases of KOA were divided into an immediate acupuncture group (group A, 97 cases) and a delayed acupunc-weeks at the end of treatment. In group B, the same acupuncture therapy was applied after waiting 4 weeks. The acupoints in the two groups were Liangqiu (ST 34), Dubi (ST 35), Zusanli (ST 36), Yanglingquan (GB 34), Yinlingquan (SP 9), Xuehai (SP 10), Xiyan (EX-LE 4), Xiyangguan (GB 33). WOMAC (Western Ontario and McMasters Universities Osteoarthritis) was used for the assessment of the primary index and VAS (visual analogue scale) was for the secondary index. The evaluation was accomplished by the patients at the beginning of trial, on the 4th and 8th weeks. In each group, 72 patients finished the trial and the data of the lost cases were included in the final data analysis.

RESULTSIn the 4th week of trial, WOMAC score was (25. 8+/-22.0) in group A difference (P<0. 001). VAS scorewas (31. 8+/-24. and was (43.8+/-22.2) in group B, indicating the significant 6) in group A and was (56. 6 +/-25. 8) in group B, indicating very significant difference (P<0. 001). In the 8th week, the efficacy was reduced slightly in the follow-up of group A, but it was improved apparently as compared Acupuncture relieves joint pain and improves joint function obviously.by th patiĩeffr,a Mtaetfti-?an tf ri-with that before treatment.

CONCLUSIONAcupuncture relieves joint pain and improves joint function obviously.The effect of acupuncture is still sustainable in 4 weeks after terminating the treatment.

Acupuncture Points ; Acupuncture Therapy ; Adult ; Aged ; Arthralgia ; therapy ; Female ; Humans ; Male ; Middle Aged ; Osteoarthritis, Knee ; therapy ; Treatment Outcome