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RISS 인기검색어
- 검색키워드
- 저자 : 문형룡(Hyung Ryong Moon) (검색결과 5 건)
- 무료
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- 유료
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Acyclonucleoside 류의 합성(3) -Ribavirin 유도체의 합성-
문형룡(Hyung Ryong Moon),양재욱(Jae Wook Yang),김문환(Moon Hwan Kim),천문우(Moon Woo Chun),정원근(Won Keun Chung) 대한약학회 1989 약학회지 Vol.33 No.6
The Synthesis of acyclic derivatives of ribavirin (2''-azido and halo seco derivatives) for the development of new antiviral agents is described. These acyclic nucleosides are synthesized from ribavirin by the method of ring opening reaction of sugar moietry.
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새로운 사이클로프로필 뉴크레오사이드 유도체의 합성과 생리활성
강진아(Jin-Ah Kang),천부순(Pusoon Chun),문형룡(Hyung Ryong Moon) 대한약학회 2012 약학회지 Vol.56 No.4
Synthesis of novel cyclopropyl pyrimidine and purine nucleoside derivatives 2~8 with α-configuration was successfully accomplished using an epoxide-ring opening reaction, lactonization, a hydroboration-oxidation reaction and a Mitsunobu reaction as the key steps. Antiviral activities against HSV-1 and -2, HIV-1 and -2, coxsackie B1and B3 viruses and poliovirus were assayed. Three compounds 4, 7 and 8 exhibit cytotoxicity-derived antiviral activity only in HIV-1 and -2.
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벤조[b][1,4]옥사진-3(4H)-치온 유도체의 합성과 이들의 타이로시네이즈 저해 활성
김도현(Do Hyun Kim),천부순(Pu soon Chun),정해영(Hae Young Chung),문형룡(Hyung Ryong Moon) 대한약학회 2017 약학회지 Vol.61 No.1
To investigate whether a “β-phenyl-α,β-unsaturated thiocarbonyl” scaffold can play a key role in tyrosinase inhibition, benzo[b][1,4]oxazine-3(4H)-thione derivatives bearing the scaffold were synthesized through a three-step reaction including Knoevenagel condensation. Four compounds showed not only high binding affinity with tyrosinase on docking simulation but also greater inhibitory activity against mushroom tyrosinase than arbutin. These results indicate that a “β- phenyl-α,β-unsaturated thiocarbonyl” may serve as an important chemical scaffold for potent tyrosinase inhibitors.
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이은경(Eun Kyeong Lee),김주현(Ju Hyun Kim),문경미(Kyoung Mi Moon),하수경(Sugyeong Ha),노상균(Sang-Gyun Noh),김대현(Dae Hyun Kim),이봉기(Bonggi Lee),김도현(Do Hyun Kim),김수정(Su Jeong Kim),울라술탄(Sultan Ullah),문형룡(Hyung Ryong Moo 한국생명과학회 2017 생명과학회지 Vol.27 No.2
본 연구에서는 (E)-2-(substituted benzylidene)-2,3-dihydro-1H-cyclopenta[a]naphthalen-1-one 유도체들을 합성했으며, 합성된 유도체들이 멜라닌 생성과정의 주요 효소인 tyrosinase 활성을 저해할 수 있는지에 대하여 확인하였다. 19종류의 유도체들의 tyrosinase 저해활성을 측정해본 결과, MHY3655 (IC50 = 0.1456 μM)가 가장 큰 저해활성을 나타냈으며 이는 대조군인 코직산(IC50 = 17.2 μM) 보다 큰 효능을 보였다. 게다가, Lineweaver-Burk 분석법을 이용하여 MHY3655가 경쟁적 저해 기전으로 tyrosinase 활성을 저해하였고, docking simulation으로 MHY3655가 tyrosinase에 직접 결합함을 재확인하였다. 마지막으로, B16F10 melanoma 세포에서 MHY3655의 세포독성을 평가한 결과 1-20 μM 사이의 MHY3655는 세포독성을 나타내지 않았다. 이상의 결과에서, 신물질 MHY3655은 우수한 tyrosinase 저해활성을 나타내며, 이는 미백 화장품 소재로서 활용할 가치가 있으리라 사료된다. The inhibition of tyrosinase, a key enzyme in mammalian melanin synthesis, plays an important role in preventing skin pigmentation and melanoma. Therefore, tyrosinase inhibitors are very important in the fields of medicine and cosmetics. However, only a few tyrosinase inhibitors are currently available because of their toxic effects on skin or lack of selectivity and stability. Therefore, we synthesized a novel series of (E)-2-(substituted benzylidene)-2,3-dihydro-1H-cyclopenta[a]naphthalen-1-one derivatives and evaluated their inhibitory effects on mushroom tyrosinase, with the aim of discovering a novel tyrosinase inhibitor. Among 19 derivatives, MHY3655 (IC50 = 0.1456 μM) showed the strongest inhibitory effect on tyrosinase activity compared to kojic acid (IC50 = 17.2 μM), a well-known tyrosinase inhibitor. In addition, MHY3655 showed competitive inhibition on Lineweaver-Burk plots. We confirmed that MHY3655 strongly interacts with mushroom tyrosinase residues through the docking simulation. Substitutions with a hydroxy group at both R2 and R4 in the phenyl ring indicated that these groups play a major role in the high binding affinity to tyrosinase. Further, MHY3655 did not show cytotoxicity at the concentrations tested in B16F10 melanoma cells. In conclusion, the novel compound MHY3655 potentially shows tyrosinase inhibitory activity, and it could be used as an ingredient in whitening cosmetics.
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Hyeyoung Jeon(전혜영),Seulah Lee(이슬아),Seonguk Yang(양성욱),EunJin Bang(방은진),Il Young Ryu(유일영),Yujin Park(박유진),Hee Jin Jung(정희진),Hae Young Chung(정해영),Hyung Ryong Moon(문형룡),Jaewon Lee(이재원) 한국생명과학회 2021 생명과학회지 Vol.31 No.8
멜라닌 색소는 포유동물의 피부, 머리카락, 눈, 신경계에 풍부하게 존재한다. 멜라닌은 다양한 환경적 스트레스로부터 피부를 보호하며, 생리학적 산화-환원 완충 작용을 통해 항상성을 유지한다. 그러나, 과도한 멜라닌 축적은 간반, 주근깨, 노인성 흑자, 염증성 색소침착을 일으킬 수 있다. 티로시나아제는 멜라닌의 생합성 경로 조절에 아주 중요한 역할을 하는 것으로 알려져 있다. 티로시나아제의 활성을 저해하는 다양한 미백제가 개발되었지만 알러지, DNA손상, 세포독성, 돌연변이 유발 등을 야기하는 부작용으로 인해 임상적 적용이 제한되었다. 본 논문에서 여러 4-크로마논 유도체를 합성하여 티로시나아제 억제 활성을 조사하였다. 이들 화합물 중 MHY1294는 IC50가 5.1±0.86 μM으로 양성 대조군인 코직산(14.3±1.43 μM) 보다 나은 티로시나아제 효소 억제 활성을 나타냈다. 또한 MHY1294는 티로시나아제의 촉매 부위에서 경쟁적인 억제 작용을 보였으며 코직산보다 더 큰 기질 결합 친화성을 가지는 것으로 확인되었다. 뿐만 아니라, MHY1294는 B16F10 흑색종 세포에서 멜라닌 세포 자극 호르몬(α-MSH)에 의해 유도되는 멜라닌 합성과 세포 내 티로시나아제 활성을 유의적으로 억제하였다. 결론적으로 본 연구는 MHY1294가 과도한 멜라닌 축적에 대한 약물 제제 및 미백제로서의 개발 가능성이 있음을 시사한다. Melanin pigments are abundantly distributed in mammalian skin, hair, eyes, and nervous system. Under normal physiological conditions, melanin protects the skin against various environmental stresses and acts as a physiological redox buffer to maintain homeostasis. However, abnormal melanin accumulation results in various hyperpigmentation conditions, such as chloasma, freckles, senile lentigo, and inflammatory pigmentation. Tyrosinase, a copper-containing enzyme, plays an important role in the regulation of the melanin pigment biosynthetic pathway. Although several whitening agents based on tyrosinase inhibition have been developed, their side effects, such as allergies, DNA damage, mutagenesis, and cytotoxicity of melanocytes, limit their applications. In this study, we synthesized 4-chromanone derivatives (MHY compounds) and investigated their ability to inhibit tyrosinase activity. Of these compounds, (E)-3-(4-hydroxybenzylidene)chroman-4-one (MHY1294) more potently inhibited the enzymatic activity of tyrosinase (IC50 = 5.1±0.86 μM) than kojic acid (14.3±1.43 μM), a representative tyrosinase inhibitor. In addition, MHY1294 showed competitive inhibitory action at the catalytic site of tyrosinase and had greater binding affinity at this site than kojic acid. Furthermore, MHY1294 effectively inhibited α-melanocyte stimulating hormone (α-MSH)-induced melanin synthesis and intracellular tyrosinase activity in B16F10 melanoma cells. The results of the present study indicate that MHY1294 may be considered as a candidate pharmacological agent and cosmetic whitening ingredient.
ScienceON
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