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#32791578   2020/08/14 To Up

Beneficial effect of anti-diabetic drugs for nonalcoholic fatty liver disease.

Nonalcoholic fatty liver disease (NAFLD) is the most common liver disorder and is associated with various metabolic diseases, including type 2 diabetes mellitus. There are no approved drugs for NAFLD, and the only approved treatment option is weight reduction. As insulin resistance plays an important role in the development of NAFLD, many anti-diabetic drugs have been evaluated for the treatment of NAFLD. Improvement of liver enzymes has been demonstrated by many anti-diabetic drugs, but histological assessment still remains insufficient. Pioglitazone could become the first-line therapy for T2DM patients with NAFLD, based on evidence of histological improvement in patients with biopsy-proven nonalcoholic steatohepatitis (NASH). Liraglutide, another promising alternative, is not yet recommended in patients with NAFLD/NASH due to limited evidence. Therefore, well-designed randomized controlled trials should be performed in the near future to demonstrate if and how anti-diabetic drugs can play a role in the treatment of NAFLD.
Kyung-Soo Kim, Byung-Wan Lee

1771 related Products with: Beneficial effect of anti-diabetic drugs for nonalcoholic fatty liver disease.

1 mg100 TESTS1 mg100ug1 mg0.1 mg200

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#32791549   2020/08/13 To Up

[Current diagnosis and treatment of chronic lymphocytic leukaemia].

Two major advances were made in the treatment of chronic lymphocytic leukaemia (CLL): the addition of the antibody rituximab to chemotherapy two decades ago and the introduction of the targeted agents during the last few years. Four targeted drugs with different mechanisms of action were added to the armamentarium of CLL treatment: the anti-CD20 antibody obinutuzumab, the two kinase inhibitors ibrutinib and idelalisib, which target the Bruton tyrosine kinase (BTK) and Phosphatidylinositiol-3-Kinase (PI3K) respectively in the B-cell receptor signalling pathway, as well as the Bcl2-antagonist venetoclax.Recently, the combination of venetoclax/obinutuzumab was approved for the first-line treatment of all CLL patients based on a phase-III trial in elderly unfit patients. This combination was shown to be clearly superior to chlorambucil/obinutuzumab and should become the preferred first-line treatment for the so called "slow-go" patients. Other options for these elderly, unfit patients are continuous ibrutinib or chlorambucil/obinutuzumab. Although data from phase-III studies are not yet available, venetoclax/obintuzumab may also be offered to younger, fit patients. Established therapeutic options for these so called "go go" patients are ibrutinib, fludarabin/cyclophosphamide/rituximab or bendemustine/rituximab (if > 65 years). Patients with the high-risk parameters deletion 17p or TP53mutation are known to poorly respond to chemo(immuno)therapy and should receive either ibrutinib or venetoclax/obinutuzumab.Thus, a choice has to be made between a continuous monotherapy with ibrutinib or a time-limited combination with either venetoclax/obinutuzumab (12 months) or chemoimmunotherapy (usually 6 months). In addition to disease-related factors (e. g. presence of deletion 17p/TP53 mutation, IgHV mutational status, prior therapies), comorbidities, co-medication and the specific side effects of the CLL therapies (myelosuppression, infections and secondary malignancies for chemoimmunotherapy; cardiac toxicity, bleeding and autoimmune disease for ibrutinib; tumour-lysis syndromes and infections for venetoclax) the patient's expectations need to be considered.
Paula Cramer, Julia von Tresckow, Barbara Eichhorst, Michael Hallek

1540 related Products with: [Current diagnosis and treatment of chronic lymphocytic leukaemia].

25 mg 50 UG1000 tests100ul100ug10 mg 5 G200 2.5 mg100ug1 mg

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#32791522   // To Up

Epitope Analysis and Efficacy Evaluation of Phosphatase 2C (PP2C) DNA Vaccine Against Toxoplasma gondii Infection.

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P X Song, S H Yao, Y Yao, J Zhou, Q F Li, Y H Cao, S Y He

2938 related Products with: Epitope Analysis and Efficacy Evaluation of Phosphatase 2C (PP2C) DNA Vaccine Against Toxoplasma gondii Infection.

1000 100 100 µg500 100 100 µg100 100ug/vialML100 100

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#32791403   2020/07/28 To Up

Semisynthesis of novel magnolol-based Mannich base derivatives that suppress cancer cells via inducing autophagy.

Magnolol, a natural bioactive neolignan, was found in the bark of a traditional Chinese medicine Magnoliae officinalis ("Hou Po" in Chinese). In this study, thrity-two magnolol-based Mannich base derivatives 3a-p and 4a-p were synthesized, and evaluated for their anti-proliferative activities against a panel of human tumor cell lines (T47D, MCF-7, Hela and A549). Among all derivatives, compound 3p displayed the most potent antiproliferative activity against T47D, MCF-7 and Hela cell lines with IC values of 0.91, 3.32 and 1.71 μM, respectively. Compared with the parental magnolol and the positive drug cisplatin, 3p exhibited up to 76.1-fold and 10.3-fold enhancement of cytotoxic effect on T47D cancer cells, respectively. Mechanism study revealed that the most potent derivative 3p suppressed cancer cells via inducing autophagy. Moreover, 3p also possessed suppressive effects on migration of T47D and Hela cancer cells. In addition, some interesting structure-activity relationships (SARs) were also summarized.
Ting Xu, Zhiyuan Zheng, Yong Guo, Li-Ping Bai

1273 related Products with: Semisynthesis of novel magnolol-based Mannich base derivatives that suppress cancer cells via inducing autophagy.

Two 96-Well Microplate Ki50.00 mlOne 96-Well Microplate Ki100|uI x 10 vials100tests96 testsOne 96-Well Microplate KiOne 96-Well Microplate Ki100ìl x 10 vialsOne 96-Well Microplate Ki1 vialOne 96-Well Microplate Ki

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#32791401   2020/07/26 To Up

Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer.

The dysfunction of histone deacetylase (HDACs) is closely related to tumorigenesis and development, which has been emerged as an attractive drug design target for cancer therapy. In the present study, we designed and synthesized a series of novel HDAC inhibitors using a substituted quinazoline as the capping group and attaching 3, 5-dimethylbenyl as a potential metabolic site protector. 23g and 23h were demonstrated potent HDAC inhibitory activities and anti-proliferative effects against MDA-MB-231 cells. In addition, 23g and 23h both could significantly increase the acetylation level of intracellular proteins, especially in α-Tubulin and HSP90. 23g and 23h displayed a slight different anti-tumor mechanism, 23g mainly induced apoptosis while 23h induced obviously ER-Stress. Furthermore, 23g and 23h both induced autophagy and migration inhibition. In pharmacokinetics assay, 23g showed a significant improvement of pharmacokinetic profile for oral administration. Additionally, 23g presented more potent anti-proliferation and anti-migration activity than SAHA in zebrafish MDA-MB-231 cell line-derived xenograft model. Together, these results demonstrate that 23g is a novel oral HDAC inhibitor with a potential capacity of treating breast cancer.
Dahong Yao, Chenyang Li, Jin Jiang, Jian Huang, Jinhui Wang, Zhendan He, Jin Zhang

2983 related Products with: Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer.



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#32791400   2020/07/24 To Up

Bicyclic polyprenylated acylphloroglucinols and their derivatives: structural modification, structure-activity relationship, biological activity and mechanism of action.

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Yeelin Phang, Xueying Wang, Yue Lu, Wenwei Fu, Changwu Zheng, Hongxi Xu

2009 related Products with: Bicyclic polyprenylated acylphloroglucinols and their derivatives: structural modification, structure-activity relationship, biological activity and mechanism of action.

50 ug5mg10 ug1000 10 mg100 assays 96 Tests 400Tests100 mg100ug100 assays

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#32791397   2020/07/13 To Up

Discovery of novel quinazolinone derivatives as potential anti-HBV and anti-HCC agents.

As a continuation of earlier works, a series of novel quinazolinone derivatives (5a-s) were synthesized and evaluated for their in vitro anti-HBV and anti-hepatocellular carcinoma cell (HCC) activities. Among them, compounds 5j and 5k exhibited most potent inhibitory effect on HBV DNA replication in both drug sensitive and resistant (lamivudine and entecavir) HBV strains. Interestingly, besides the anti-HBV effect, compound 5k could significantly inhibit the proliferation of HepG2, HUH7 and SK- cells, with IC values of 5.44, 6.42 and 6.75 μM, respectively, indicating its potential anti-HCC activity. Notably, the in vitro anti-HCC activity of 5k were more potent than that of positive control 5-fluorouracil and sorafenib. Further studies revealed that compound 5k could induce HepG2 cells apoptosis by dose-dependently upregulating Bad and Bax expression and decreasing Bcl-2 and Bcl-xl protein level. Considering the potent anti-HBV and anti-HCC effect, compound 5k might be a promising lead to develop novel therapeutic agents towards HBV infection and HBV-induced HCC.
Jingying Qiu, Qingqing Zhou, Yinpeng Zhang, Mingyu Guan, Xin Li, Yueting Zou, Xuan Huang, Yali Zhao, Wang Chen, Xiaoke Gu

1106 related Products with: Discovery of novel quinazolinone derivatives as potential anti-HBV and anti-HCC agents.

100μl100ug100μl100μl100ug Lyophilized100μl100ug Lyophilized100μl20 mg

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#32791353   2020/06/18 To Up

Evaluation of novobiocin and telmisartan for anti-CHIKV activity.

Chikungunya has re-emerged as an epidemic with global distribution and high morbidity, necessitating the need for effective therapeutics. We utilized already approved drugs with a good safety profile used in other diseases for their new property of anti-chikungunya activity. It provides a base for a fast and efficient approach to bring a novel therapy from bench to bedside by the process of drug-repositioning. We utilized an in-silico drug screening with FDA approved molecule library to identify inhibitors of the chikungunya nsP2 protease, a multifunctional and essential non-structural protein required for virus replication. Telmisartan, an anti-hypertension drug, and the antibiotic novobiocin emerged among top hits on the screen. Further, SPR experiments revealed strong in-vitro binding of telmisartan and novobiocin to nsP2 protein. Additionally, small angle x-ray scattering suggested binding of molecules to nsP2 and post-binding compaction and retention of monomeric state in the protein-inhibitor complex. Protease activity measurement revealed that both compounds inhibited nsP2 protease activity with IC values in the low micromolar range. More importantly, plaque formation assays could show the effectiveness of these drugs in suppressing virus propagation in host cells. We propose novobiocin and telmisartan as potential inhibitors of chikungunya replication. Further research is required to establish the molecules as antivirals of clinical relevance against chikungunya.
Praveen Kumar Tripathi, Anjali Soni, Shiv Pratap Singh Yadav, Ankit Kumar, Nitika Gaurav, Siva Raghavendhar, Pradeep Sharma, Sujatha Sunil, Ashish, Bhyravabhotla Jayaram, Ashok Kumar Patel

1891 related Products with: Evaluation of novobiocin and telmisartan for anti-CHIKV activity.

0.1ml (1mg/ml)1000 0.1 ml100μg0.1 mg25 µg0.2 mg25 µg100μg100.00 ul1 ml

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#32791348   2020/08/10 To Up

A triple-coated ligament graft to facilitate ligament-bone healing by inhibiting fibrogenesis and promoting osteogenesis.

Absence of ligament-bone healing due to poor bioactivity and hyperplasia of fibrous tissue caused by immune response severely impairs ligament grafts' functional duration in anterior cruciate ligament (ACL) reconstruction. While osteogenic modification is a popular technique for promoting ligament-bone integration, inadequate osseointegration remains a common experience, due to occupying fibrous hyperplasia and impaired osteogenesis potential. In the present study, a triple-nano-coating polyethylene terephthalate (PET) graft was developed by polydopamine self-assembly, chondroitin sulfate (CS) chemical-grafting and BMP-2 physical-immobilization to facilitate robust ligament-bone healing, The CS/polydopamine-modified PET (C-pPET) graft was demonstrated to inhibit fibrogenesis by regulating polarization of macrophages and promoting the secretion of anti-inflammatory factors. Moreover, the immunoregulatory function of CS cooperated with BMP-2 to facilitate osteogenic differentiation of stem cells, promoting the expression of ALP, Runx2, OCN and COL I. Bone regeneration was significantly enhanced at early-middle stage in the BMP-loaded pPET (B/pPET) group, while occurring at middle-late stage in the C-pPET group. Continuous new bone formation and optimal ligament-bone healing were observed in the B/C-pPET group via sequential and synergistic immune osteogenesis by CS and cytokine osteogenesis by BMP-2. Thus, the present study revealed a practical avenue for the promotion of ligament-bone healing through the development of a triple-nano-coating engineered ligament combining immunoregulatory anti-fibrogenesis and sequential-synergistic osteogenesis, which holds a great potential for improving the clinical efficacy of ligament graft in ACL reconstruction.
Yamin Li, Ximeng Guo, Shikui Dong, Tonghe Zhu, Yunsu Chen, Song Zhao, Guoming Xie, Jia Jiang, Hongyan He, Changsheng Liu, Jinzhong Zhao

2119 related Products with: A triple-coated ligament graft to facilitate ligament-bone healing by inhibiting fibrogenesis and promoting osteogenesis.

100 100ug Lyophilized1 module100ul200 100ul100 assays10 mg1 g1 mL20 1 module

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#32791325   2020/08/10 To Up

Very important dark sky areas in Europe and the Caucasus region.

ALAN (artificial light at night) can give, if done adequately, a lot of benefits for human society, but it affects reproduction, navigation, foraging, habitat selection, communication, trophic and social interactions of the biota in the same time. Taking into account dramatic increase in light pollution of the night sky and night environment during the past decades, the creation of refugia where natural habitats are not influenced by ALAN is very important. We selected promising territories without, or with a low impact of, ALAN for the development of a VIDA (Very Important Dark Area) Network in Europe and the Caucasus region. 54 VIDAs within the borders of 30 countries were chosen, located in different biogeographic regions, at different altitudes, and in juxtaposition with protected areas. Special attention has been paid to sea and ocean islands, non-polluted by ALAN, as well as to large parts of European Russia and Kazakhstan where there is still a low level of light pollution. These places might be a basis for the protection of biodiversity from the consequences of ALAN, and they can also serve as key education centers for increasing the awareness of the problem of light pollution of the sky at night. Due to the fact that light propagates far away in the atmosphere, the protection of VIDAs can be obtained only if a strong anti-light pollution action is enforced also in the surrounding areas, at least 100 km from the borders of the VIDAs.
Mykyta Peregrym, Erika Pénzesné Kónya, Fabio Falchi

2511 related Products with: Very important dark sky areas in Europe and the Caucasus region.

100 μg100 μg100 μg100 μg100 μg100 μg100 μg100 μg100 μg100 μg100 μg100 μg

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