• Title/Summary/Keyword: 501

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Curcumin Analogue A501 induces G2/M Arrest and Apoptosis in Non-small Cell Lung Cancer Cells

  • Xia, Yi-Qun;Wei, Xiao-Yan;Li, Wu-Lan;Kanchana, Karvannan;Xu, Chao-Chao;Chen, Da-Hui;Chou, Pei-Hong;Jin, Rong;Wu, Jian-Zhang;Liang, Guang
    • Asian Pacific Journal of Cancer Prevention
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    • v.15 no.16
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    • pp.6893-6898
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    • 2014
  • Curcumin and its analogues have been reported to exert anti-cancer activity against a variety of tumors. Here, we reported A501, a new curcumin analogue. The effect of A501 on cell viability was detected by MTT assay, the result showed that A501 had a better inhibiting effect on the four non-small cell lung cancer (NSCLC) cells than that of curcumin. Moreover, Colony forming experiment showed A501 significant restrained cell proliferation. Flow cytometry displayed A501 can cause G2/M arrest and induce apoptosis. Western blotting showed that A501 decreased the expression of cyclinB1, cdc-2, bcl-2, while increased the expression of p53, cleaved caspase-3 and bax. In conclusion, curcumin analogues A501 played antitumor activity by inhibiting cell proliferation and inducing apoptosis of NSCLC cells. And it was likely to be a promising starting point for the development of curcumin-based anticancer drugs.

Increased Expression of a Chemically Synthesized Human Lysozyme Gene in Saccharomyces cerevisiae (Saccharomyces cerevisiae에서 합성된 Human Lysozyme 유전자의 발현증대)

  • 김기운;최선욱;이승철;백현동;황용일
    • Microbiology and Biotechnology Letters
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    • v.26 no.1
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    • pp.34-39
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    • 1998
  • We have already prepared a human lysozyme (HLY) structural gene from chemically synthesized 38 oligomers with high codon usage in Saccharomyces cerevisiae. For directing the synthesis and secretion of HLY in S. cerevisiae, two types of expression vectors, a YCp centromere-based vector, pHK101 and a YEp 2-$\mu\textrm{m}$ circle-based vector, pHK501 were constructed. With the resulting plasmids, we have confirmed that yeast transformant harboring pHK501 has more secreted HLY than pHK101-transformant by using a lysoplate and a turbidimetric assay. In flask cultivation, pHK501-transformant produced active HLY about 8 times (55 units/$m\ell$) higher than pHK101-transformant. From batch cultivation, the HLY productivity was obtained with 1.12 units/$m\ell$/h, corresponding to a 1.8-fold increase compared with flask fermentation. These results indicate that yeast transformant with pHK501 vector overexpressed and secreted HLY than that of YCp type vector.

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Histopathological Evaluation of Heart Toxicity of a Novel Selective PPAR-γ Agonists CKD-501 in db/db Mice

  • Yang, Hyun-Il;Kim, Woo Sik;Kim, Dal-Hyun;Kang, Jin Seok
    • Biomolecules & Therapeutics
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    • v.21 no.1
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    • pp.84-88
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    • 2013
  • High risk of cardiovascular diseases caused by existing PPAR-${\gamma}$ agonists such as rosiglitazone and pioglitazone has been recently reported. CKD-501 is a novel selective PPAR-${\gamma}$ agonist as a potential target to reduce cardiovascular risk in non-insulin dependent diabetes mellitus (NIDDM). In this study, We investigated potential cardiotoxicity of CKD-501 and compared its toxicity with that of rosiglitazone or pioglitazone using db/db mice. After 12-week repeated administration of CKD-501 at doses of 3, 10 and 30 mg/kg/day or rosiglitazone at doses of 10 and 30 mg/kg/day or pioglitazone at doses of 200 and 540 mg/kg/day, animals were sacrificed for investigation of potential toxicities. Diameters of left ventricles and areas of cardiomyocytes were measured. And lipid accumulation and apoptosis in heart muscle were examined by oil red O staining and TUNEL staining, respectively. Diameters of left ventricles were significantly increased in high dose treatment group of pioglitazone compared to control (p<0.05), while other groups showed a tendency for an increase. All test articles induced significantly the increase of area of cardiomyocytes in heart compared to control (p<0.01), in regular order as pioglitazone > CKD-501 ${\geq}$ rosiglitazone. However, lipid accumulation and apoptotic changes in heart were not observed in all dosing groups. Taken together, the myocardial cell hypertrophy of CKD-501 are relatively lower than that of pioglitazone and similar to rosiglitazone. And it is suggested that the myocardial cell hypertrophy of CKD-501 are less adverse in clinical use for the management of the NIDDM.

Quantitative and Comparative Analysis of Urinary Steroid Levels upon Treatment of an Anti-Diabetic Drug, CKD-501 using Gas Chromatography-Mass Spectrometry

  • Sadanala, Krishna Chaitanya;Jung, Byung-Hwa;Jang, In-Jin;Chung, Bong-Chul
    • Journal of Pharmaceutical Investigation
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    • v.41 no.1
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    • pp.37-43
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    • 2011
  • Urinary steroid levels were investigated in the treatment of CKD-501, a new anti-diabetic drug candidate. CKD-501 was administered orally at the dosage of 1, 2, 4 mg/day for 7 days to normal men (n=18). Urine was collected before, during and after stopping the drug administration and the urinary level of androgen, estrogen, progestin and corticoids were quantified using GC-MS (gas chromatography-mass spectrometry). Only urinary corticosteroid and an androgen, DHEA levels among all the analyzed steroids, have been found to increase progressively, reaching significant levels on the last day of drug treatment and later declined after the drug treatment is withdrawn. Therefore, it was thought that an increase in the urinary corticoid and DHEA levels could be a characteristic of CKD-501, since it prominently acts on the glucose sensitivity and suppresses the triglyceride levels. In conclusion, it was found that CKD-501, an anti-diabetic drug candidate, affects the glucocorticoid and DHEA levels and it plays a crucial role in glucose homeostasis.

DENTAL NEWS

  • The Korean Dental Association
    • The Journal of the Korean dental association
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    • v.27 no.6 s.241
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    • pp.501-501
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    • 1989
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Control of Ginseng Damping-off by Streptomyces sp. A75 and A501 (Streptomyces sp. A75와 A501 균주의 인삼 잘록병에 대한 방제효과)

  • Lee, Sang Yeob;Song, Jaekyeong;Yun, Bong-Sik;Park, Kyeong hun;Kim, Jeong Jun;Han, Ji Hee
    • The Korean Journal of Mycology
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    • v.44 no.4
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    • pp.330-337
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    • 2016
  • Streptomyces sp. A75 and A501 inhibited the mycelial growth of pathogenic Rhizoctonia solani and Pythium sp., which cause the ginseng disease known as damping-off. Three methods were evaluated for the control of these pathogens, using a mixture of the culture broths from Streptomyces sp. A75 and A501. The methods tested were seed dipping with 50-fold diluted broth, drenching of soil with 100-fold diluted broth after sowing, and combined seed dipping and drenching. These methods reduced the incidence of ginseng damping-off caused by R. solani by 81.3%, 84.8%, and 32.2% and that caused by Pythium sp. by 51.0%, 52.1%, and 75.3%, respectively. Based on these results, the combination of seed dipping and soil drenching after sowing using a mixture of the culture broths from Streptomyces sp. A75 and A501 effectively reduced the incidence of damping-off in ginseng.

Branch-and-Bound Algorithm for Division of Perfect Nine Dart Combinations (퍼펙트 9 다트 조합의 나눗셈 분기한정 알고리즘)

  • Lee, Sang-Un
    • The Journal of the Institute of Internet, Broadcasting and Communication
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    • v.22 no.4
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    • pp.87-94
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    • 2022
  • This paper researched a study to find a combination of acquisition scores for 9 dart throws, which is the minimum number of dart tactile throws in 501 point dart games. The maximum score that can be obtained by throwing once in a dart game is 60 points, which can end the perfect dart game with 60 points eight times according to 60×8+21×1=501, and if you earn 21 points once, you can finish the game with 9 throws. This is called 9-dart finish. As such, only 18 and 14 studies on the combination of scores that can obtain 501 points with 9 throws are known, and no studies have been conducted applying the exhaustive search algorithm. This paper proposed a division branch-and-bound algorithm as a method of simplifying the O(2n) exponential time performance complexity of the typical branch-and-bound method of a exhaustive search method, to polynomial time complexity. The proposed method limited the level to 8, jumped to a quotient level of 501/60, and backtracked to explore only possible score combinations in the previous level. The possible score combinations of the nine perfect games found with the proposed algorithm were 90(101 cases).