Unlocking the Multifunctional Therapeutic Potential of Herbacetin: A Flavone derived Scaffold

Herbacetin (HBT), a naturally occurring flavone, exhibits broad therapeutic -- potential, including anti-cancer, anti-inflammatory, antioxidant, antimicrobial, neuroprotective, and anti-diabetic effects, by modulating key signaling pathways such as NF-κB, PI3K/AKT, AP-1, SGK1/FoxO1, AMPK, SIRT1, MMP9, and NLRP3. It also inhibits several critical enzymes, including ornithine decarboxylase, ATP-citrate lyase, SGK1, AChE, α-glucosidase, and CYP3A4. In the context of cancer, HBT has shown particularly promising activity against breast cancer, liver carcinoma, human colon cancer, and epidermal carcinoma. Structurally, HBT shares significant similarity with well-known flavonoids such as quercetin and kaempferol, and the availability of established total synthetic methodologies makes it an attractive candidate for synthetic chemists. However, the structural modification and comprehensive evaluation of ' 'HBT's biological activity remain underexplored. This review highlights its isolation, total synthesis, pharmacological properties, molecular targets, and future directions, emphasizing the versatility of the HBT scaffold as a promising foundation for the development of novel therapeutic agents.

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Journal
Medicinal Chemistry
Published
2025-07-24
DOI
https://doi.org/10.2174/0115734064389091250719051643
Primary Topic
Sirtuins and Resveratrol in Medicine
Type
article
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article

Unlocking the Multifunctional Therapeutic Potential of Herbacetin: A Flavone derived Scaffold

Navin Kumar Tailor
Medicinal Chemistry
Sirtuins and Resveratrol in Medicine
article

Unlocking the Multifunctional Therapeutic Potential of Herbacetin: A Flavone derived Scaffold

Navin Kumar Tailor
article en

Abstract

Herbacetin (HBT), a naturally occurring flavone, exhibits broad therapeutic -- potential, including anti-cancer, anti-inflammatory, antioxidant, antimicrobial, neuroprotective, and anti-diabetic effects, by modulating key signaling pathways such as NF-κB, PI3K/AKT, AP-1, SGK1/FoxO1, AMPK, SIRT1, MMP9, and NLRP3. It also inhibits several critical enzymes, including ornithine decarboxylase, ATP-citrate lyase, SGK1, AChE, α-glucosidase, and CYP3A4. In the context of cancer, HBT has shown particularly promising activity against breast cancer, liver carcinoma, human colon cancer, and epidermal carcinoma. Structurally, HBT shares significant similarity with well-known flavonoids such as quercetin and kaempferol, and the availability of established total synthetic methodologies makes it an attractive candidate for synthetic chemists. However, the structural modification and comprehensive evaluation of ' 'HBT's biological activity remain underexplored. This review highlights its isolation, total synthesis, pharmacological properties, molecular targets, and future directions, emphasizing the versatility of the HBT scaffold as a promising foundation for the development of novel therapeutic agents.

Medicinal ChemistryVol. 21
Chandigarh University (IN)
Good health and well-being
Openalex Percentile: Top 78%
Sirtuins and Resveratrol in Medicine
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Unlocking the Multifunctional Therapeutic Potential of Herbacetin: A Flavone derived Scaffold — Navin Kumar Tailor · Medicinal Chemistry (2025) | TGRS Research Map | TGRS