Article
Immunology
Wonki Kim, Jeong-Hoon Jang, Xiancai Zhong, Hyungseok Seo, Young-Joon Surh
Summary: 15d-PGJ(2) promotes the resolution of intestinal colitis by reducing neutrophils and M1 macrophages, increasing M2 macrophage proportion, and decreasing the expression of pro-inflammatory cytokine IL-6 in macrophages.
FRONTIERS IN IMMUNOLOGY
(2021)
Article
Cell Biology
Eun-Hee Kim, Su-Jung Kim, Hye-Kyung Na, Wonshik Han, Nam-Jung Kim, Young-Ger Suh, Young-Joon Surh
Summary: The study found that 15d-PGJ2 activates VEGF expression through NRF2-driven induction of HO-1 in human breast cancer cells, suggesting a novel oncogenic mechanism. Elevated levels of 15d-PGJ2 during the inflammatory response were linked to poor clinical outcomes in breast cancer patients. Levels of 15d-PGJ2, COX-2, NRF2, and HO-1 were found to be increased in human breast cancer tissues.
Article
Chemistry, Multidisciplinary
Airat M. Gimazetdinov, Aidar Z. Al'mukhametov, Mansur S. Miftakhov
Summary: An asymmetric total synthesis of 15-deoxy-Delta(12,14)-prostaglandin J(2) methyl ester is described. The synthesis involves several key steps, including the formation of a cyclopentenone precursor, construction of the prostaglandin alpha-chain, and alkylation followed by the formation of the omega-chain.
NEW JOURNAL OF CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Su-Jung Kim, Nam-Chul Cho, Bitnara Han, Kyeojin Kim, Young-Il Hahn, Kwang Pyo Kim, Young Ger Suh, Bu Young Choi, Hye-Kyung Na, Young-Joon Surh
Summary: The cyclopentenone prostaglandin 15d-PGJ2 functions as an allosteric inhibitor of STAT3 by covalently modifying STAT3 on Cys259, inhibiting its activity in MCF10A-Ras cells. This results in antiproliferative and pro-apoptotic effects similar to mutation of this amino acid.
Article
Engineering, Biomedical
Yao Jiang, Jia-Mei Liu, Jia-Ping Huang, Ke-Xi Lu, Wei-Lian Sun, Jing-Yi Tan, Bo-Xiu Li, Li-Li Chen, Yan-Min Wu
Summary: This study evaluated the biological properties of decellularized human periodontal ligament cell (dHPDLC) sheets in vitro, showing that dHPDLC sheets can promote periodontal regeneration in an inflammatory environment.
BIOMEDICAL MATERIALS
(2021)
Article
Immunology
Weiyang Li, Jieshi Xie, Le Yang, Yuanru Yang, Lin Yang, Liying Li
Summary: The study found that 15d-PGJ2 can reduce MIF expression in damaged hepatocytes by activating PPARγ, thereby inhibiting macrophage infiltration and inflammatory response, ultimately alleviating acute liver injury.
INTERNATIONAL IMMUNOPHARMACOLOGY
(2023)
Article
Chemistry, Multidisciplinary
Nikolay S. Vostrikov, Vadim V. Zagitov, Alexander N. Lobov, Diana Ishmetova, Yulia V. Vakhitova, Mansur S. Miftakhov
Summary: A series of novel compounds were synthesized through multiple steps in this study, and their anticancer activities were preliminarily explored.
Article
Chemistry, Multidisciplinary
Zaynutdin R. Makaev, Nikolay S. Vostrikov, Natalya K. Selezneva, Mansur S. Miftakhov
Summary: A simple and efficient synthesis of racemic 15-deoxy- increment 12,14- prostaglandin J2 methyl ester from readily available Corey lactone diol in a total of eleven steps was proposed. Standard methods were used to form a fused co-chain and then converted into PGJ2 methyl ester. The transformation to the target prostaglandin was achieved smoothly in TsOH-CH2Cl2 medium by converting the allylic alcohol moiety to an exocyclic diene substituent conjugated with the endocyclic enone system.
MENDELEEV COMMUNICATIONS
(2023)
Article
Immunology
Yuping Ning, Wenfei Wang, Paul M. Jordan, Stefanie A. Barth, Robert Klaus Hofstetter, Jinjin Xu, Ximeng Zhang, Yi Cai, Christian Menge, Xinchun Chen, Oliver Werz
Summary: Tuberculosis caused by Mycobacterium tuberculosis is a global health concern. In this study, it is shown that M. tuberculosis induces COX-2 expression in human macrophages and promotes the formation of anti-inflammatory J2-PGs. These J2-PGs have anti-inflammatory effects in M1-MDMs, downregulating proinflammatory cytokines and upregulating anti-inflammatory cytokines and M2 markers.
JOURNAL OF IMMUNOLOGY
(2023)
Article
Cell Biology
Clovis M. Kumagai, Renata M. Martinez, Barbara B. Colombo, Priscila Saito, Ingrid C. Pinto, Camilla C. A. Rodrigues, David L. Vale, Ricardo L. N. Matos, Ana P. F. R. L. Bracarense, Marcela M. Baracat, Sandra R. Georgetti, Juliana T. Clemente-Napimoga, Marcelo H. Napimoga, Victor Fattori, Waldiceu A. Verri, Rubia Casagrande
Summary: UVB radiation poses a significant threat to the skin, and topical administration of 15-Deoxy-Delta(12,14)-prostaglandin J(2) shows promise in mitigating UVB-induced skin damage. The study suggests that TFcPGJ(2) has therapeutic potential in combating inflammatory and oxidative skin pathologies caused by UVB exposure.
MEDIATORS OF INFLAMMATION
(2021)
Article
Chemistry, Multidisciplinary
Atsushi Nakayama, Tenta Nakamura, Toshihiro Zaima, Saho Fujimoto, Sangita Karanjit, Kosuke Namba
Summary: The concise total synthesis of tronocarpine, a chippiine-type indole alkaloid, was achieved through a one-pot construction of a pentacyclic skeleton. This strategy, controlled by the stereocenter at the C14 position, can be used to synthesize other chippiine-type alkaloids with azabicyclo[3.3.1]nonane skeletons.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2021)
Article
Chemistry, Multidisciplinary
Hai-Hua Lu, Kang-Ji Gan, Fu-Qiang Ni, Zhihan Zhang, Yao Zhu
Summary: The concise total synthesis of salimabromide was achieved using a series of novel reactions, which allowed for the construction of its unique carbon skeleton and stereocenters.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
(2022)
Article
Chemistry, Organic
Huan He, Fanglin Xue, Zhao Hu, Peng Li, Qian Xiao, Maojie Zhang, Fei Xue, Dan Zhang, Hao Song, Xiao-Yu Liu, Zhibing Zheng, Song Li, Wu Zhong, Yong Qin
Summary: Morphine and its related alkaloids are commonly used natural medicines. However, the current industrial manufacturing process of these compounds causes environmental issues. In this study, researchers developed an efficient total synthesis method for opioids such as codeine, oxycodone, naloxone, and naltrexone. The key step in this synthesis is the Pd-catalyzed dearomatization arene coupling reaction using an inexpensive and stable phosphonium ligand.
ORGANIC CHEMISTRY FRONTIERS
(2022)
Article
Chemistry, Multidisciplinary
Gleb A. Chesnokov, Karl Gademann
Summary: The marine-derived compound Peyssonnoside A was successfully synthesized for the first time in a concise, efficient, scalable, and highly diastereoselective manner. The aglucone peyssonnosol was achieved in 21% overall yield after 15 steps, with key reactions including Simmons-Smith cyclopropanation and Mukaiyama hydration controlled by the spatial structure of the substrates.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
(2021)
Article
Chemistry, Multidisciplinary
Fuhao Zhang, Jingwen Zeng, Mohan Gao, Linzhou Wang, Gen-Qiang Chen, Yixin Lu, Xumu Zhang
Summary: A practical synthetic strategy for enantioselective and divergent synthesis of prostaglandins was reported, involving the construction of multiply substituted five-membered rings through key enyne cycloisomerization and installation of crucial chiral centers using asymmetric hydrogenation. Common intermediates allowed for the production of various prostaglandins and related drugs in two steps, with the preparation of fluprostenol on a 20-gram scale.
Review
Biochemistry & Molecular Biology
So-Eun Son, Nam-Jung Kim, Dong-Soon Im
Summary: The discovery of G protein-coupled receptors (GPCRs) for free fatty acids in the early 21st century led to a new field of research and significant implications for drug discovery. Free fatty acid receptor 4 (FFA4, GPR120) plays a crucial role in regulating obesity-induced metaflammation and GLP-1 secretion, making it an important target for drug development. Various FFA4 agonists have been developed and studied for their potential applications in pathophysiology and drug discovery.
BIOMOLECULES & THERAPEUTICS
(2021)
Article
Chemistry, Organic
Young Min Kim, Hyung-Seok Yoo, Seung Hwan Son, Ga Yeong Kim, Hyu Jeong Jang, Dong Hwan Kim, Soo Dong Kim, Boyoung Y. Park, Nam-Jung Kim
Summary: 2-Aryl-2,3-dihydroquinolin-4(1H)-ones have been identified as important structures with potent biological activities. In this study, 25 novel N-Tf 2-aryl-2,3-dihydroquinolin-4(1H)-ones were efficiently synthesized via oxidative aza-Michael cyclization. This methodology offers advantages such as short reaction times and suitable functional group tolerance.
EUROPEAN JOURNAL OF ORGANIC CHEMISTRY
(2021)
Article
Cell Biology
Eun-Hee Kim, Su-Jung Kim, Hye-Kyung Na, Wonshik Han, Nam-Jung Kim, Young-Ger Suh, Young-Joon Surh
Summary: The study found that 15d-PGJ2 activates VEGF expression through NRF2-driven induction of HO-1 in human breast cancer cells, suggesting a novel oncogenic mechanism. Elevated levels of 15d-PGJ2 during the inflammatory response were linked to poor clinical outcomes in breast cancer patients. Levels of 15d-PGJ2, COX-2, NRF2, and HO-1 were found to be increased in human breast cancer tissues.
Article
Pharmacology & Pharmacy
Ji-Min Kim, Seong-Wook Seo, Dong-Gyun Han, Hwayoung Yun, In-Soo Yoon
Summary: The study found that quercetin significantly influences the metabolism of repaglinide, increasing its exposure in the body. This suggests that quercetin may have clinically significant pharmacokinetic interactions with repaglinide depending on intake from foods and dietary supplements.
Article
Chemistry, Medicinal
Seongkeun Jeong, Changyu Kang, Sohee Park, Sanghyun Ju, Jin-Wook Yoo, In-Soo Yoon, Hwayoung Yun, Yunjin Jung
Summary: Tranilast activates the Nrf2-HO-1 pathway by covalently binding to KEAP1, which contributes to alleviating colitis in rats.
Article
Chemistry, Medicinal
Kyoung Song, Nirmal Rajasekaran, Chaithanya Chelakkot, Hun Seok Lee, Seung-Mann Paek, Hobin Yang, Lina Jia, Hee Geon Park, Woo Sung Son, Yu-Jin Kim, Joon-Seok Choi, Hae Min Jeong, Young-Ger Suh, Hwayoung Yun, Young Kee Shin
Summary: MSPA exhibits anti-cancer effects by simultaneously targeting ENO1, ALDOA, and FH enzymes, reducing glucose consumption and lactate release, inhibiting cancer cell proliferation, and inducing apoptosis.
Article
Medicine, Research & Experimental
Eunbi Cho, Kumju Youn, Huiyoung Kwon, Jieun Jeon, Wan-Seob Cho, Se Jin Park, Seung Hwan Son, Dae Sik Jang, Chan Young Shin, Minho Moon, Mira Jun, Nam-Jung Kim, Dong Hyun Kim
Summary: This study investigated the effects of eugenitol in an AD mouse model and found that it inhibits the formation of A beta plaques and reduces neuronal cell death. In silico docking simulation showed that eugenitol may interact with A beta monomers and fibrils.
BIOMEDICINE & PHARMACOTHERAPY
(2022)
Article
Chemistry, Medicinal
Min Jae Jeon, Hyelim Lee, Jeehee Lee, Soo Yeon Baek, Donghee Lee, Seongman Jo, Joo-Youn Lee, Miso Kang, Hee Ra Jung, Soo Bong Han, Nam-Jung Kim, Sanghee Lee, Hyejin Kim
Summary: Stimulator of interferon genes (STING) is an endoplasmic reticulum membrane protein that plays important roles in cancer immunotherapy. Researchers have synthesized and characterized STING modulators that stimulate downstream signaling and promote immune responses, suggesting their therapeutic potential for cancer treatment.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Ju-Hyun Lee, Seung-Hwan Son, Nam-Jung Kim, Dong-Soon Im
Summary: Atopic dermatitis is a chronic inflammatory skin disorder. Traditional Chinese medicines for AD therapy have been found to suppress MAPKs and NF-.B. This study examined the effect of the p38 MAPK inhibitor NJK14047 on AD-like skin lesions induced in mice and found that it effectively suppressed AD symptoms and reduced cytokine levels.
BIOMOLECULES & THERAPEUTICS
(2022)
Article
Chemistry, Multidisciplinary
Soo Lim Kim, Yo-Sep Yang, Sujin Lee, Nam-Jung Kim
Summary: The research team designed and synthesized 16 analogs of EGFR mutant inhibitors, identifying 9a, 9b, and 20b as inhibitors for EGFR L858R/T790M/C797S mutations, and 10a and 10b as inhibitors for multiple mutation types. Additionally, a molecular docking study on a plausible binding mode of the compounds was provided.
BULLETIN OF THE KOREAN CHEMICAL SOCIETY
(2022)
Article
Biochemistry & Molecular Biology
Ju-Hyun Lee, Seung-Hwan Son, Nam-Jung Kim, Dong-Soon Im
Summary: p38 MAPK plays a crucial role in the pathogenesis of asthma. Inhibition of p38 MAPK with NJK14047 can effectively suppress the development of allergic asthma. However, NJK14047 has no effect on ORMDL3 regulation and sphingolipid biosynthesis.
BIOMOLECULES & THERAPEUTICS
(2022)
Article
Biochemistry & Molecular Biology
Hee Jin Jeong, Hye Lim Lee, Sung Joon Kim, Jeong Hyun Jeong, Su Hyun Ji, Han Byeol Kim, Miso Kang, Hwan Won Chung, Chan Sun Park, Hyunah Choo, Hyo Jae Yoon, Nam-Jung Kim, Duck-Hyung Lee, Sang Hee Lee, Seo-Jung Han
Summary: In this study, novel ENPP1 inhibitors were designed and synthesized to stimulate the STING pathway and inhibit tumor growth. The compound 18p showed high potency against ENPP1 and activated the STING pathway, leading to the induction of cytokines and inhibition of tumor growth in a mouse model.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2022)
Article
Pharmacology & Pharmacy
Shwe Phyu Hlaing, Jiafu Cao, Juho Lee, Jihyun Kim, Aruzhan Saparbayeva, Dongmin Kwak, Hyunwoo Kim, Seonghwan Hwang, Hwayoung Yun, Hyung Ryong Moon, Yunjin Jung, Jin-Wook Yoo
Summary: In this study, curcumin-loaded nanoparticles targeted inflamed colitis tissue and demonstrated better therapeutic efficacy compared to non-targeted nanoparticles. The nanoparticles reduced inflammation and accelerated recovery, making them a promising delivery platform for treating ulcerative colitis.
Article
Chemistry, Organic
Yoon Hu Jang, Yo-Sep Yang, Seung Hwan Son, Hyung-Seok Yoo, Jeong-Won Shin, Hyuck-Jae Won, Soo Lim Kim, Changjin Lim, Nam-Jung Kim
Summary: This study reports an unprecedented approach to synthesizing xanthone scaffold from cyclohexyl(2-hydroxyphenyl)methanone through dehydrogenative cyclization and aromatization cascade. This method offers a novel route with a high atom-economic manner and a wide substrate scope.
Article
Chemistry, Organic
Yo-Sep Yang, Sangmin Lee, Seung Hwan Son, Hyung-Seok Yoo, Yoon Hu Jang, Jeong-Won Shin, Hyuck-Jae Won, Jaehoon Sim, Nam-Jung Kim
Summary: A ligand-controlled direct arylation of indoles via Pd(ii)-catalyzed oxidative boron Heck reaction under aerobic conditions is reported. This methodology provides a regiodivergent route for C2 or C3 aryl indoles in a protection-free and acid/base free manner.
ORGANIC CHEMISTRY FRONTIERS
(2022)
