Author: Pezzani, Raffaele ; Aldahish, Afaf Ahmed ; Martorell, Miquel ; Sharopov, Farukh ; Tsouh Fokou, Patrick Valere ; Jiménez-Garcia, Manuel ; Calina, Daniela ; Sharifi-Rad, Javad ; Capó, Xavier

HS-1793 is a novel derivative of resveratrol, a compound known for its numerous beneficial effects, including anticancer activity, anti-inflammatory response, antimicrobial, antiaging, anti-cardiovascular disease activity, neuroprotective activity, etc. Despite its wide and interesting properties, resveratrol suffers from a crucial flaw because it is low bioavailable. For this reason, many other derivatives were explored and among them, HS-1793 has caught the attention of researchers. HS-1793 is a synthetic derivative of resveratrol discovered in 2007 that has been shown to have anti-cancer and anti-inflammatory properties. In addition, the compound showed a positive profile in metabolic processes, with adequate pharmacokinetics and pharmacodynamics. This review highlights current research on HS-1793, evaluating in vitro and in vivo works and lays the foundation for novel explorative trials in human diseases.

08 Feb 2023·Journal of the American Chemical Society

Development of a Fluorescent Probe for M2 Macrophages via Gating-Oriented Live-Cell Distinction

Article

Author: Kwon, Haw-Young ; Chang, Young-Tae ; Lee, Sun Hyeok ; Lee, Hong-Guen ; Kang, Nam-Young ; Cho, Heewon

Macrophages are the most plastic immune cells by changing their characters in response to environmental stimuli. Broadly, macrophages are categorized into two different subsets based on M1/M2 paradigm, which exhibit completely contrary phenotypes. Whereas M1 macrophages are aggressive to offend invaders such as bacteria and tumors, M2 are anti-inflammatory cells and seemingly help tumor immunity. Tumor-associated macrophages are typical examples of M2 cells as the key components of forming and maintaining the tumor microenvironment. Despite the intensive interest, monitoring M2 macrophages in real time is hampered by the lack of competent detection tools. Here, we report the first M2 selective probe CDg18 with a novel mechanism of gating-oriented live-cell distinction through M2-favored fatty acid transporters. To demonstrate the potential of CDg18, we visualize the progressive phenotypic change of M2 toward M1 using a resveratrol analogue HS-1793 as a reprogramming effector. Combined together with M1 probe CDr17, the diminishing M2 character and emerging M1 markers could be simultaneously monitored in real time through the multicolor changes during macrophage reprogramming.

01 Apr 2022·Food Science and Biotechnology

Resveratrol analogue, HS-1793, inhibits inflammatory mediator release from macrophages by interfering with the TLR4 mediated NF-κB activation

Article

Author: Lee, Chang Geun ; Jeong, Min Ho ; Jeong, Soo Kyung ; Jo, Wol Soon ; Kim, Sung Dae ; Oh, Su Jung ; ParK, Moon Taek ; Kang, Young-Rok

Resveratrol is known to have anti-inflammatory properties. However, high-dose resveratrol is required for optimal anti-inflammatory effects. HS-1793 is a derivative designed to be metabolically stable and more effective than resveratrol. We tested whether HS-1793 also has anti-inflammatory activity. HS-1793 effectively inhibited the mRNA and protein expression of lipopolysaccharide (LPS)-induced inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) in macrophages. Therefore, the production of nitric oxide (NO) and prostaglandin E₂ (PGE₂) was significantly attenuated. In addition, HS-1793 completely suppressed the production of inflammatory cytokines enhanced by LPS treatment along with a decrease in Toll-like receptor 4 (TLR4) expression. At the same time, the expression of myeloid differentiation factor 88 (MyD88), IL-1 receptor-associated kinase 1 (IRAK1), and TNF receptor-associated factor 6 (TRAF6) signaling molecules and the nuclear translocation of nuclear factor kappa B (NF-κB)/p65 were also downregulated. We conclusively suggest that HS-1793 also exhibits anti-inflammatory properties by effectively inhibiting TLR4-mediated NF-κB activation.

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Indication	Highest Phase	Country/Location	Organization	Date
Breast Cancer	Preclinical	KR	Pusan National University	15 Jul 2016

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