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61.
Seung Young Lee Eunjung Moon Sun Yeou Kim Kang Ro Lee 《Bioorganic & medicinal chemistry letters》2013,23(7):2140-2144
Five new quinic acid derivatives (1–5), together with 10 known quinic acid derivatives (6–15), were isolated from the MeOH extract of Pimpinella brachycarpa (Umbelliferae). Their structures were established on the basis of spectroscopic analyses including extensive 2D NMR studies (COSY, HMQC and HMBC). Isolated compounds 1–15 were evaluated for their inhibitory activities on nitric oxide (NO) production in an activated murine microglial cell line. Compounds 2, 3, 8 and 11 significantly inhibited NO production without high cell toxicity in lipopolysaccharide (LPS)-activated BV-2 cells, a microglia cell line (IC50 = 4.66, 12.52, 9.04 and 12.11 μM, respectively). 相似文献
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Jung-eun Park Chiman Song Keehyun Choi Taebo Sim Bongjin Moon Eun Joo Roh 《Bioorganic & medicinal chemistry letters》2013,23(20):5515-5518
A series of 3,4-diarylpyrrolidin-2-one was designed, prepared and evaluated as triple reuptake inhibitors for antidepressant. Most compounds exhibited comparable in vitro efficacy as norepinephrine and dopamine transporter reuptake inhibitors. Especially, 2i showed better potency than GBR-12909 (IC50 = 14 nM) which was used as reference compound for dopamine transporter. In addition, 2a and 2b showed inhibition (5.17 μM–85.6 nM) for three transporters. 相似文献
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Minsoo Koh Jong-Cheol Lee Changhee Min Aree Moon 《Bioorganic & medicinal chemistry》2013,21(8):2305-2313
Mounting evidence suggests that metformin (N,N-dimethylbiguanide), a widely prescribed drug for the treatment of type II diabetes, exerts an anti-tumor effect on several cancers including breast cancer. Breast cancer has been estimated as one of the most commonly diagnosed types of cancer among women. In particular, triple-negative breast cancers are associated with poor prognosis and metastatic growth. In the present study, we synthesized a novel metformin derivative 5 (HL010183) and metformin salts, 9a, 9b, and 9c (metformin gamma-aminobutyric acid (GABA) salt, metformin pregabalin salt and metformin gabapentin salt), which exerted more potent inhibitory effects on the proliferation and invasiveness of Hs578T triple-negative breast carcinoma cells than metformin. Importantly, 5 showed approximately 100-fold more potent effects compared to metformin. In a triple-negative breast cancer xenograft model, 5 showed a comparable degree of inhibitory effect on in vivo tumor growth at the 100 mg/kg dose to that of metformin at 500 mg/kg. Our results clearly demonstrate that 5 exerts a potent anti-tumor effect both in vitro and in vivo, paving the way for a strategy for treatment of triple-negative breast cancer. 相似文献
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Hye Ran Park Jae Meen Lee Jin Wook Kim Jung-Ho Han Hyun-Tai Chung Moon Hee Han Dong Gyu Kim Sun Ha Paek 《PloS one》2016,11(11)
ObjectiveWe retrospectively analyzed our experience with time-staged gamma knife stereotactic radiosurgery (GKS) in treating large arteriovenous malformation(AVM)s;≥ 10 cm3).MethodsForty-five patients who underwent time-staged GKS (2-stage, n = 37;3-stage,n = 8) between March 1998 and December 2011 were included. The mean volume treated was 20.42±6.29 cm3 (range, 10.20–38.50 cm3). Obliteration rates of AVMs and the associated complications after GKS were evaluated.ResultsMean AVM volume (and median marginal dose) at each GKS session in the 37 patients who underwent 2-stage GKS was 19.67±6.08 cm3 (13 Gy) at session 1 and 6.97±6.92 cm3 (17 Gy) at session 2. The median interval period was 39 months. After follow-up period of 37 months, the complete obliteration rate was 64.9%. The mean AVM volume (and median marginal dose) at each GKS session in the 8 patients who underwent 3-stage GKS was 23.90±6.50 cm3 (12.25 Gy), 19.43±7.46 cm3 (13.5 Gy), 7.48±6.86 cm3 (15.5 Gy) at session 1, 2, and 3, respectively. The median interval duration between each GKS session was 37.5 and 38 months, respectively. After a median follow-up period of 47.5 months, 5 patients (62.5%) achieved complete obliteration. Postradiosurgical hemorrhage developed in 5 patients (11.1%) including one case of major bleeding and 4 cases of minor bleeding. No patient suffered from clinically symptomatic radiation necrosis following radiation.ConclusionTime-staged GKS could be an effective and safe treatment option in the management of large AVMs. 相似文献
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Daniel C. Ilut Alexander E. Lipka Namhee Jeong Dong Nyuk Bae Dong Hyun Kim Ji Hong Kim Neelam Redekar Kiwoung Yang Won Park Sung-Taeg Kang Namshin Kim Jung-Kyung Moon M. A. Saghai Maroof Michael A. Gore Soon-Chun Jeong 《TAG. Theoretical and applied genetics. Theoretische und angewandte Genetik》2016,129(3):453-468