Anticancer properties of novel pyrazole‐containing biguanide derivatives with activating the adenosine monophosphate‐activated protein kinase signaling pathway

Biguanides, including metformin and phenformin, have emerged as promising anticancer agents. However, the high dose needed for their efficient anticancer properties restricts their clinical application. In an attempt to obtain higher active compounds than these parent compounds, pyrazole‐containing biguanide derivatives were synthesized and screened for in vitro cytotoxicity against human cancer cell lines. Clonogenic assays and scratch wound healing assays demonstrated that these new derivatives profoundly inhibit cell proliferation and migration. Compounds 10b and 10d exhibited strong potency with low IC₅₀ values in the range of 6.9‐28.3 μM, far superior to phenformin and metformin. Moreover, 20 μM 10b and 10d resulted in 72.3‐88.2% (p < 0.001) inhibition of colony formation and 29.3‐60.7% (p < 0.05) inhibition of cell migration. Mechanistically, 10b and 10d activated adenosine monophosphate‐activated protein kinase, leading to inactivation of the mammalian target of rapamycin (mTOR) signaling pathway with the regulation of 4EBP1 and p70S6K. These results suggest the value of these novel biguanide derivatives as candidates with therapeutic potential for the treatment of bladder and ovarian cancer.     

Systematic review and meta-analysis assessing the knowledge and use of the female condom among Nigerians

BackgroundThe female condom (FC) is a critical component in a comprehensive and sustainable approach to prevent HIV, other sexually transmitted infections and unintended pregnancies.ObjectivesThis review provides comprehensive information about Nigerian''s knowledge and use of FC.MethodsWe screened search output, evaluated study eligibility, and extracted data in duplicate. Data from similar studies were combined in a meta-analysis.ResultsThere was a significantly (p < 0.0001) high-level of awareness amongst the respondents. However, the use of the FC was very low at 5.5% among female respondents. There was a significant (p < 0.0001) difference between FC awareness and use. The main reasons for FC use were prevention of unintended pregnancy (55%) and STIs/HIV (31%). We observed a significant difference between reasons of non-use of the FC [F (5, 13) = 5.195, P = 0.0077]. Furthermore, there were significant differences between the sources of information on FC [F (3, 8) = 32.89, P < 0.0001].ConclusionDespite the high levels of awareness, especially among the female respondents, the use of the FC has remained extremely low even among the young, educated undergraduate students. There is aneed for robust and consistent advocacy to make the FC available and affordable.     

Effect of Huangqin decoction on regulating intestinal flora in colitis mice characterized as inhibition of the NOD2-dependent pathway

ContextChinese herb Huangqin decoction (HQD) can regulate intestinal flora in ulcerative colitis (UC) mice.ObjectiveOur study clarifies the mechanism of HQD in regulating the intestinal flora of UC mice.Materials and methodsMale C57BL/6 mice were randomly divided into six groups: Control, Model (3% DSS), Sulfasalazine (500 mg/kg), HQD-L (250 mg/kg), HQD-M (500 mg/kg), and HQD-H (1000 mg/kg) groups. Measurement of body weight, colon length, DAI, and haematoxylin–eosin staining were conducted. FISH and 16S rDNA detected colonic bacterial infiltration and intestinal flora changes. The expression of RegIIIγ and PRRs (NOD2, TLR5, TLR4) were detected by FCM and WB, respectively. In addition, WB, qPCR, or IHC were used to detect the expression of NOD2, MyD88, RIP2, and NF-κB p65 in the colon. ELISA was used to determine cytokines.ResultsCompared with the model group (DAI score, 2.38 ± 0.05; histological score, 4.08 ± 0.54), HQD treatment significantly reduced the DAI score (L, 2.16 ± 0.09; M, 1.45 ± 0.05; H, 1.18 ± 0.05) and histological score (L, 3.16 ± 0.82; M, 2.50 ± 0.81; H, 1.51 ± 0.76); restored the weight, the colonic length (p < 0.05). 16S rDNA identification showed HQD regulated the balance of intestinal flora. Moreover, HQD suppressed the expression of RegIIIγ (p < 0.05) and prevented colonic bacterial infiltration. Furthermore, WB results showed NOD2, and TLR4 were inhibited by HQD, especially NOD2 (p < 0.01). The data of WB, qPCR, and IHC demonstrated that the NOD2-dependent pathway was inhibited by HQD (p < 0.01).Discussion and conclusionsHQD (1000 mg/kg) regulates the intestinal flora of colitis mice, mainly characterized as inhibition of the NOD2-dependent pathway. These results indicate that HQD has potential.     

New insights into roles of basophils in initiating T helper type 2 immunity

Allergic diseases, mainly mediated by T helper type 2 (Th2) immunity, have become a worldwide public health problem. Traditional Chinese medicine (TCM) has long been used in treating and preventing allergic symptoms. As the new target of anti-allergy TCM, basophils, after approximately 140 years since their discovery, are just now gaining respect as important contributors in the pathogenesis underlying allergic inflammation and disease. In addition to their role as effector cells, basophils can release early IL-4, migrate from circulatory system into draining lymph nodes, present antigen to naive CD4+ T cells, and promote the differentiation of Th2 cells. Herein, we briefly summarized the recent research advances of the essential contributions of basophils in the initiation of Th2 immune responses.     

健肝散颗粒冲剂合阿德福韦酯片治疗慢性乙型病毒性肝炎疗效观察

目的观察健肝散颗粒冲剂合阿德福韦酯片治疗慢性乙型病毒性肝炎(CHB)的临床疗效。方法治疗组58例予自拟中药健肝散颗粒冲剂,并联合抗乙肝病毒药物阿德福韦酯片治疗;对照组52例只服用阿德福韦酯片治疗。结果治疗组总有效率为93%,对照组总有效率为85%,2组比较有显著性差异(P<0.05);同时肝功能(ALT、AST)和症状体征积分变化亦优于对照组。结论健肝散颗粒冲剂合阿德福韦酯片治疗CHB疗效显著。     

How to improve CHMs quality: enlighten from CHMs ecological cultivation

Chinese herbal medicines (CHMs) are one of the important bioresources of medicine, which works by unlocking nature''s ability to prevent diseases and recover from illnesses. Recently, it has ascended to the world stage and become a global icon. Nowadays, a considerable of researches have focused on the quality evaluation of CHMs. However, it is difficult to meet the reasonable needs of human beings for safe drug use to evaluate the quality of a huge number of inferior goods for the CHMs contaminated by pesticides and heavy metals. Hence to explore an eligible medicinal plant cultivation pattern, which can provide high quality CHMs sustainably, is most promising. This review analyzed the situation and characteristics of medicinal plant resources in different periods, including wild-harvested resources and domestic cultivation during different stages, putting forward that ecological cultivation must be the way to develop medicinal plant cultivation and to obtain high quality CHMs.     

An improved autoradiographic technique for the detection of antibody-forming cells

An autoradiographic technique for the detection of antibody-forming cells has been developed for the assay of anti-DNP responses. The lymphoid cells suspension to be assayed was allowed to sediment on to a glass slide coated with DNP-conjugated gelatin to which the secreted antibody bound during subsequent incubation. The bound antibody and its Ig class was revealed by a second incubation using ¹²⁵I-anti-immunoglobulin reagents followed by autoradiography. Studies on the sensitivity and specificity of the method are presented and its advantages over other techniques described. The technique should be readily applicable to other haptens.     

中医药治疗输卵管性不孕的研究进展

输卵管性不孕是导致不孕症的一个重要因素。其发病率有逐年升高的趋势,给患者带来了经济和心理的负担,因此引起广大医务工作者的重视。西医治疗输卵管性不孕,存在着费用昂贵、粘连反复出现等问题。在临床实践中,中医药治疗输卵管性不孕有明显的疗效,优势凸显。因此本研究对输卵管性不孕的病因、治法进行综述,以期在临床治疗中提供经验和范例。     

地奈德乳膏联合透明质酸修护生物膜治疗成人面部湿疹疗效观察

目的观察地奈德乳膏联合透明质酸修护生物膜治疗成人面部湿疹的近期疗效。方法将入选的116例患者随机分为两组,试验组(61例)予透明质酸修护生物膜联合地奈德乳膏外用治疗,对照组(55例)单纯外用地奈德乳膏治疗,两组患者疗程均为2周。结果治疗第1周后,试验组和对照组的疗效总积分较治疗前显著降低(P均0.05),试验组的总积分与对照组相比,差异有统计学意义(P0.05);试验组疗效(有效率为83.61%)和对照组(有效率为60%)相比差异有统计学意义(P0.05)。治疗第2周后,试验组和对照组的总积分均较治疗前显著下降(P均0.05);试验组的总积分与对照组相比差异无统计学意义(P0.05);试验组疗效(有效率为86.89%)和对照组(有效率为85.45%)差异无统计学意义(P0.05)。第4周试验组复发率为5.67%,低于对照组(19.15%)(P0.05)。结论地奈德乳膏联合透明质酸修护生物膜治疗面部湿疹疗效较好,复发率低。