MC1R modulators(Melanocortin receptor 1 modulators), MITF inhibitors(melanocyte inducing transcription factor inhibitors), SIK1 inhibitors(salt inducible kinase 1 inhibitors)

Therapeutic Areas

Skin and Musculoskeletal Diseases

Active Indication

Skin Pigmentation

Inactive Indication-

Originator Organization

Chungbuk National University

Active Organization

Chungbuk National University

Inactive Organization-

License Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC20H24O3

InChIKeyTXELARZTKDBEKS-UHFFFAOYSA-N

CAS Registry78954-23-1

100 Clinical Results associated with Yakuchinone A

100 Translational Medicine associated with Yakuchinone A

100 Patents (Medical) associated with Yakuchinone A

Literatures (Medical) associated with Yakuchinone A

01 Oct 2024·Chinese Journal of Natural Medicines

Four new diarylheptanoids and two new terpenoids from the fruits of Alpinia oxyphylla and their anti-inflammatory activities

Article

Author: ZHOU, Mi ; Geng, Jianliang ; DONG, Jie ; Yao, Xinsheng ; Li, Haibo ; LI, Haibo ; Dong, Jie ; Zhou, Mi ; YU, Yang ; Yu, Yang ; GENG, Jianliang ; YAO, Xinsheng

Four previously unreported diarylheptanoids (1a/1b-2a/2b), one undescribed sesquiterpenoid (8), one new diterpenoid (12), and twelve known analogs were isolated from the fruits of Alpinia oxyphylla. The structural elucidation of these compounds was achieved through a comprehensive analysis of spectroscopic data, single-crystal X-ray diffraction, electronic circular dichroism (ECD), and modified Mosher's method. Enantiomeric mixtures (1a/1b, 2a/2b, 3a/3b, 4a/4b, and 5a/5b) were separated on a chiral column using acetonitrile-water mixtures as eluents. Among them, compounds 3a/3b and 4a/4b were isolated as optically pure enantiomers in the initial chiral separation. Furthermore, most of the isolates were evaluated for their inhibitory effects against the production of nitric oxide (NO) and interleukin-6 (IL-6) in lipopolysaccharide (LPS)-induced RAW264.7 macrophages. Interestingly, 2 and 4 showed significant inhibitory activities against NO production with IC₅₀ values of 33.65 and 9.88 μmol·L^-1 (hydrocortisone: IC₅₀ 34.26 μmol·L^-1), respectively. Additionally, they also partially reduced the secretion of IL-6.

01 Sep 2024·Journal of Pharmaceutical and Biomedical Analysis

Comparisons of pharmacokinetics and tissue distribution of six major bioactive components of the herbal pair Alpinia officinarum-Cyperus rotundus in normal and primary dysmenorrhea rats

Article

Author: Ren, Xikang ; Li, Yonghui ; Wei, Na ; Li, Hailong ; Zhang, Junqing ; Huang, Yufang ; Tan, Yinfeng

The Liangfu formula, as described in 'Liangfang Jiye', is well-known for its efficacy in treating stomach pain, abdominal pain, and dysmenorrhea. This research aimed to investigate the pharmacokinetics and tissue distribution of 5-hydroxy-7-(4-hydroxy-3-methoxyphenyl)-1-phenyl-3-heptanone (DPHA), Galangin, Kaempferide, 5-Hydroxy-1,7-diphenyl-3-heptanone (DPHC), α-Cyperone, and Nootkatone in vivo using an LC-MS/MS method. The method successfully separated the six active components and internal standards (Chrysin and Yakuchinone-A) on an XB-C18 column with a mobile phase of 0.2 ‰ formic acid water-acetonitrile. It demonstrated good linearity with a correlation coefficient (r²) ≥ 0.9911 and a lower limit of quantification (LLOQ) of 5-80 ng/mL for the different components. Precision, accuracy, matrix effects, and recovery rates were within acceptable ranges. Pharmacokinetic analysis revealed significant differences in parameters between primary dysmenorrhea (PD) and normal rats (especially AUC, T_max, and CL_z/F). Tissue distribution showed that the six active components of the herbal pair Alpinia officinarum Hance-Cyperus rotundus L. (HPAC) extract was primarily distributed in the liver, lung, and kidney. This study offers valuable insights into the potential mechanisms of action and drug development for treating PD.

01 Sep 2024·Journal of Cereal Science

A multi-omics-based investigation into the regulation of phenolics in fresh maize kernels at different developmental stages

Author: Guo, Yuqiu ; Liu, Kaichang ; Tian, Xiaomin ; Chen, Lirong ; Han, Di ; Sun, Linlin ; Gong, Kuijie

In this study, a total of 33 key differential metabolites related to phenolic synthesis were obtained in the fresh-eating and maturity stages by LC-MS anal. using UNIFY with a self-constructed database.Based on KEGG pathway anal., three pathways related to phenolic metabolite synthesis were identified.The differential genes selected from the transcriptome and the differential metabolites selected from the target metabolism were correlated in the anal., revealing the existence of 7 enzymes involved in the synthesis of phenolic compounds in secondary metabolismAmong which the fresh-eating stage promotes phenolics synthesis by up-regulation of the activities of the two enzymes, CCoAOMT and 4CL, and the enzymes, DFR, C3H, DFR, CHI, REF1 and F3H were expressed at higher levels during the maturity stage than fresh-eating stage, thus improving the tolerance and stress resistance of the plant itself and its ability to respond to the external environment, which has an important impact on the regulation of phenolic accumulation.

100 Deals associated with Yakuchinone A

R&D Status

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Indication	Highest Phase	Country/Location	Organization	Date
Skin Pigmentation	Preclinical	South Korea	Chungbuk National University	06 Jun 2024

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