Currently, the resistance of first-line anti-tuberculosis drugs has made the prevention and treatment of tuberculosis increasingly difficult, posing a serious threat to global public health. Several studies have shown that efflux pumps are one of the important causes for bacteria to develop multi-drug resistance and extremely-drug resistance, and efflux pump inhibitors can inhibit the efflux of antibacterial drugs, thereby reducing bacterial drug resistance. Numerous natural products and synthetic compounds have been reported to possess efflux pump inhibitory activity, but they have not been applied in clinical settings because of their toxicity, pharmacokinetic properties, etc. Therefore, we summarized the efflux pump inhibitory activity, antimicrobial activity, and structure-activity relationships of reported efflux pump inhibitors against Mycobacterium tuberculosis in recent years, providing references for the development of new efflux pump inhibitors with better activity and lower toxicity.

To study the protective effect of Danshen Tongluo capsule on rat hearts in the myocardial infarction (MI) model. After being fed with high fat diets for one month, the SD rats were randomly divided into the sham group and the model group according to the left ventricular ejection fraction (EF). The MI model group was duplicated by ligating coronary artery and then divided into five groups: the model group, the positive control group (model + captopril), the small dose group (model + Danshen Tongluo), the medium dose group (model + Danshen Tongluo) and the high dose group (model + Danshen Tongluo). Four weeks later, changes in myocardium ultra-structure were observed by hemodynamics, cardiac ultrasound and electron microscope. The results showed: (1) All doses of Danshen Tongluo capsule could significantly reduce the left ventricular end diastolic pressure (LVEDP) (P <0.01), increase the maximum internal pressure of the left ventricle (+ dp/dtmax), and lower the drop rate of left ventricular pressure (- dp/dtmax), with statistical significances in medium and high dose groups; (2) The B ultrasound results showed increase in EF and left ventricular shortening fraction (FS) in all dose groups of Danshen Tongluo capsule; (3) The medium dose group showed significant decrease in myocardial infarction index (P <0.01) and injured and fractured myofilament and sarcomere of ischemic myocardium in myocardial ultra-structure; All of Danshen Tongluo capsule-treated groups revealed reduction in myocardial injury and myocardial infraction area. The study preliminarily proves that Danshen Tongluo capsule can improve hemodynamic function, and has a protective effect on myocardial ischemia.
Animals ; Capsules ; Drugs, Chinese Herbal ; therapeutic use ; Hemodynamics ; drug effects ; Male ; Myocardial Infarction ; drug therapy ; pathology ; physiopathology ; Myocytes, Cardiac ; ultrastructure ; Rats ; Rats, Sprague-Dawley ; Ventricular Function, Left ; drug effects

Coronary artery disease (CAD) is one of the leading causes of death. Safflower attracts great attention owing to its anti-ischemia/reperfusion injury effect. Ninety-three patients with CAD were included and randomized into safflower treatment group, PCI group and control group. Low-dose dobutamine stress echocardiography (DSE) was performed to measure end-systolic volume (ESV), end-diastolic volume (EDV), left ventricular ejection fraction (LVEF) and wall motion score index (WMSI) to determine the recovery of hibernating myocardium and cardiac function in all patients before treatment and after 3-month follow-up. The study was to investigate the effects of safflower on hibernating myocardial revascularization and cardiac function. It was found that LVEF was significantly improved, while the ESV and WMSI were significantly reduced after 2-week treatment in safflower and PCI treatment groups. No significant differences were found between safflower and PCI treatment groups in ESV, EDV, WMSI and LVEF after treatment Safflower injection effectively improved hibernating myocardial function.
Aged ; Carthamus tinctorius ; chemistry ; Coronary Artery Disease ; drug therapy ; physiopathology ; Drugs, Chinese Herbal ; administration & dosage ; Female ; Heart ; drug effects ; physiopathology ; Humans ; Male ; Middle Aged ; Myocardial Revascularization ; Myocardial Stunning ; drug therapy ; physiopathology ; surgery ; Recovery of Function

OBJECTIVETo observe the effect of Feiyanning Granule (FYN) on tumor growth and cell cycle distribution in mice with Lewis lung cancer, as well as its influence on G1/S cell cycle checkpoint dominating signaling RB-E2F1 bio-axis.

METHODSModeled C57BL/6 mice were randomly divided into 6 groups: the model group (A), the DDP treated group (B) peritoneally injected with cisplatin 0.1 mg on d1, d3 and d5 after modeling, and the 4 FYN treated groups (C-F), administered via gastrogavage with FYN Decoction, and FYN Granule in small-, median- and high- dose respectively for 14 days. The tumour inhibiting rate, tumour weight, and body weight of mice were observed after treatment; cell cycle distribution was detected by flow cytometry (FCM), RB-E2F1mRNA expressions in tumour tissue were analyzed by RT-PCR, and their protein expressions by Western blot.

RESULTSTumour weight in the 5 treated groups was lower than that in the model group (P < 0.05, P < 0.01). Body weight in group E was significantly higher than that in group A and B (P < 0.05, P < 0.01). FCM analysis showed the proportion of G0/G1 phase was higher in group E than in group A, B and C (P < 0.01), and cancer cell proliferation index (PI) in group E was lower than in group B (P < 0.05, P < 0.01). RT-PCR showed mRNA level of E2F1 was lower, but that of RB was significantly higher in group E than those in group A, B and C respectively (P < 0.01). Westem blot analysis showed the protein expression of E2F1 was lower in group E and B than that in group A (P < 0.05), while the protein expression of Rb in group E was higher than that in group A, B and C (P < 0.05).

CONCLUSIONThe effect of FYN in inhibiting Lewis lung cancer growth was related to its intervention on cancer cell cycle distribution which blocks most tumor cells in G0/G1 phase. Moreover, FYN can reduce MDM2 expression, enhance P53 expression to influence cell cycle G1/S checkpoint dominating signaling, so as to achieve the effect of antagonizing lung cancer cell proliferation.

Animals ; Carcinoma, Lewis Lung ; metabolism ; pathology ; Cell Cycle Checkpoints ; drug effects ; Cell Line, Tumor ; Cell Proliferation ; drug effects ; Drugs, Chinese Herbal ; pharmacology ; Male ; Mice ; Mice, Inbred C57BL ; Signal Transduction ; drug effects

The pathogenesis of acquired immune deficiency syndrome-associated recurrent oral ulcerations (AIDS-ROU) remained obscure and these was no specific treatment for it. Syndrome differentiation in traditional Chinese medicine (TCM) focus on integral regulation and has an advantage of the disease that etiology and pathogenesis remain obscure. A draft of Chinese medicine diagnosis and treatment standard procedure for AIDS-ROU was established by literature retrieval and peer review. Two questionnaires were carried out to investigate the confirmation and advice of in-group specialist to key points of the draft including diagnosis, treatment and nursing. Then the procedures were revised accordingly. The preliminary results showed the recovery rate of complete questionnaires in the 1st survey was 96%. Specialists confirmed more on outline, case history and physical examinations, syndrome differentiation of hyperactivity of fire due to Yin deficiency syndrome (HFYDS), treatment of heat accumulated in heart and spleen syndrome (HAHSS) and HFYDS, treatment of western medicine and nursing. They held different opinions on incidence, treatment of deficiency of spleen-QI and stomach-QI syndrome (DSSS) and criterion of therapeutical evaluation. Cronbach coefficient alpha (CCA) was 0.998 and split-half reliability R was 0.91. Recovery rate of complete questionnaires in 2nd survey was 100%. Specialists confirmed more on outline, etiology and pathogenesis, case history and physical examination, auxiliary examination, diagnostic criteria, syndrome differentiation and treatment of HAHSS and HFYDS. They held different opinions on syndrome differentiation and treatment of intermingled cold and heat syndrome and DSSS, nursing and the other therapies. CCA was 0.428 and split-half reliability R was 0.96. Coefficient of variations of the 2nd survey were less than those of the 1st survey, which mean coordination was improved. Each single item in two surveys contributed less difference in overall results according to weight coefficients. A new revision of the procedure was preliminarily established according to results of two surveys. Experts'activeness, concentration and coordination were good in two surveys. They had reached consensus in key points of the draft including diagnosis, treatment and nursing on the whole.
Acquired Immunodeficiency Syndrome ; complications ; Consensus ; Female ; Humans ; Male ; Medicine, Chinese Traditional ; methods ; standards ; Oral Ulcer ; complications ; diagnosis ; therapy ; Recurrence ; Reference Standards ; Surveys and Questionnaires

OBJECTIVETo study the risk factors in high prevalence district of birth defects (BD) to provide evidence for intervention development.

METHODSQuantitative analysis had been carried out based on the investigation at three counties in Shanxi province. 491 useable questionnaires had been collected with a response rate as 94.6%. Binary logistic regression was performed to analyze the risk factors of BD.

RESULTSData from logistic regression analyses revealed that factors as: the status of family income, knowledge on healthy birth and rearing, behavior and illness during pregnancy were influencing the occurrence of BD, with OR values as 0.535, 3.265, 0.403 and 1.379 respectively. Better family income and knowledge on BD were negatively (P values are 0.000 and 0.001 respectively), while illness during pregnancy and alcohol intake of the husbands were positively correlated (P values are 0.005 and 0.012 respectively) to the occurrence of BD.

CONCLUSIONMeasures as accelerating the development of local economy, providing education on BD knowledge to the couples, changing negative life style and improving the health status would reduce the risk of BD. Preconceptional-periconceptional care seemed to be the new idea for healthy pregnancy and healthy baby.

China ; epidemiology ; Congenital Abnormalities ; economics ; epidemiology ; Female ; Health Behavior ; Humans ; Income ; Male ; Pregnancy ; Pregnancy Complications ; epidemiology ; Risk Factors ; Social Class

Acute Disease ; Adult ; Chemical and Drug Induced Liver Injury ; etiology ; Female ; Humans ; Male ; Occupational Exposure ; Trichloroethanes ; poisoning

AIMTo investigate the chemical constituents of the bulbs of Fritillaria wabuensia.

METHODSChromatography techniques were used to isolate the chemical constituents. EI-MS, 1HNMR, 13 CNMR and DEPT were used to determine the structures of the isolated constituents.

RESULTSThree alkaloids were isolated from the bulbs of Fritillaria wabuensia, and were identified as imperialine (I), imperialine-beta-N-oxside (II), isoverticine-beta-N-oxide (III).

CONCLUSIONIsoverticine-beta-N-oxide was isolated from the bulbs of Fritillaria wabuensia for the first time. Isoverticine-beta-N-oxide is a new alkaloid.

Cevanes ; chemistry ; isolation & purification ; Cyclic N-Oxides ; chemistry ; isolation & purification ; Fritillaria ; chemistry ; Molecular Structure ; Plants, Medicinal ; chemistry ; Triterpenes ; chemistry ; isolation & purification

OBJECTIVETo observe the effect of electroacupuncture at Zusanli (ST 36) on phosphorylated extracellular signal-regulated kinase 1/2 (pERK1/2) in the dorsal horn of spinal cord induced by plantar inflammation in the rat.

METHODSAll the rats were randomly divided into 5 groups: normal control group, simple electroacupuncture group, formalin group, formalin plus ipsilateral electroacupuncture group and formalin plus contralateral electroacupuncture group. The acute inflammation animal model was made by injection of 100 microL of 4% formalin into the right posterior foot pad. Electroacupuncture was given at "Zusanli" (ST 36) for 30 min, with sparse-dense waves, frequency 2-15 Hz, and intensity 2-3 mA. One and a half hours latter, the rats were killed under anesthesia, and pERK1/2 expression in the lumbar dorsal horn were investigated with immunohistochemical method.

RESULTSThe positive cells were rarely seen (6.45 +/- 1.05) in the superficial spinal cord in the control group; a few cells (14.07 +/- 3.19) in ipsilateral superficial spinal cord were found in the electroacupuncture group. The number of pERK1/2-positive neurons (26.57 +/- 4.93) in lamina I - II0 of the ipsilateral dorsal horn in the formalin group increased significantly. After electroacupuncture at ipsilateral Zusanli (ST 36), the number of positive cells (20.79 +/- 5.21) had a tendency to decrease, but with no statistically significant difference. However, after electroacupuncture at contralateral Zusanli (ST 36), the number of positive cells (14.75 +/- 3.03) significantly decreased as compared with the non-acupuncture group (P < 0.05).

CONCLUSIONThe inhibition of ERK1/2 phosphorylation in the spinal cord dorsal horn by electroacupuncture is possibly involved in acupuncture analgesic effect.

Acupuncture Analgesia ; Acupuncture Points ; Animals ; Electroacupuncture ; Male ; Mitogen-Activated Protein Kinase 1 ; metabolism ; Mitogen-Activated Protein Kinase 3 ; metabolism ; Phosphorylation ; Posterior Horn Cells ; enzymology ; Rats ; Rats, Sprague-Dawley

OBJECTIVETo investigate the ultrasonographic features of epididymides in congenital obstructive azoospermia (COA) and acquired obstructive azoospermia (AOA).

METHODSA total of 211 infertile men with obstructive azoospermia were observed by scrotal ultrasonography, and the features of the epididymal ultrasonograms were compared between COA and AOA.

RESULTSCOA exhibited significantly higher rates of ectasia in the epididymal head, cord-like changes, abrupt tapering and absence of the epididymal body and tail than AOA (P < 0.05), while AOA showed markedly higher rates of epididymal body and tail duct ectasia and epididymal inflammatory mass than COA (P < 0.01). Tubular ectasia of the epididymal duct in the head, body and tail were markedly higher in the COA (14 [5.9%], 41 [17.2%] and 20 [8.4%] cases in 236 epididymides) than in the AOA (P < 0.05). Retiform ectasia were markedly higher in the AOA (119 [64.0%], 142 [76.3%] and 109 [58.6%] cases in 186 epididymides) than in the COA (P < 0.05), with statistically significant differences between the two groups (P < 0.05). Ultrasonographically, the epididymides of the COA patients were characterized by irregular ectasia of the epididymal tube with decreased and unclear wall echoes (P < 0.05), and those of the AOA patients by regular ectasia with enhanced wall echoes (P < 0.01).

CONCLUSIONThe ultrasonographic epididymal features of COA are obviously different from those of AOA, which is of important clinical application value for distinguishing the two conditions from each other.

Adult ; Azoospermia ; congenital ; diagnostic imaging ; Epididymis ; diagnostic imaging ; Humans ; Male ; Middle Aged ; Ultrasonography