Activity-Guided Purification Identifies Lupeol, a Pentacyclic Triterpene, As a Therapeutic Agent Multiple Pathogenic Factors of Acne

Abstract

Acne vulgaris is a nearly universal cutaneous disease characterized by multifactorial pathogenic processes. Because current acne medications have various side effects, investigating new pharmacologically active molecules is important for treating acne. As natural products generally provide various classes of relatively safe compounds with medicinal potentials, we performed activity-guided purification after a series of screenings from the extracts of five medicinal plants to explore alternative acne medications. Lupeol, a pentacyclic triterpene, from the hexane extract of Solanum melongena L. (SM) was identified after instrumental analysis. Lupeol targeted most of the major pathogenic features of acne with desired physicochemical traits. It strongly suppressed lipogenesis by modulating the IGF-1R/phosphatidylinositide 3 kinase (PI3K)/Akt/sterol response element-binding protein-1 (SREBP-1) signaling pathway in SEB-1 sebocytes, and reduced inflammation by suppressing the NF-κB pathway in SEB-1 sebocytes and HaCaT keratinocytes. Lupeol exhibited a marginal effect on cell viability and may have modulated dyskeratosis of the epidermis. Subsequently, histopathological analysis of human patients' acne tissues after applying lupeol for 4 weeks demonstrated that lupeol markedly attenuated the levels of both the number of infiltrated cells and major pathogenic proteins examined in vitro around comedones or sebaceous glands, providing solid evidence for suggested therapeutic mechanisms. These results demonstrate the clinical feasibility of applying lupeol for the treatment of acne.

Atrophic acne scar: a process from altered metabolism of elastic fibres and collagen fibres based on transforming growth factor‐β1 signalling

“…Acne is one of the most prevalent skin diseases, affecting nearly 90% of adolescents worldwide . Acne scars originating from acne are usually the major prolonged concern of patients because they remain permanently.…”

“…Acne is one of the most prevalent skin diseases, affecting nearly 90% of adolescents worldwide. 1 Acne scars originating from acne are usually the major prolonged concern of patients because they remain permanently. The presence of acne scars can cause both severe cosmetic problems and psychosocial dysfunction, thereby resulting in huge negative impacts on patients' quality of life.…”

Cytotoxic Property of Grias neuberthii Extract on Human Colon Cancer Cells: A Crucial Role of Autophagy

“…For instance, lupeol has been widely reported for its anticancer effect against various cancer cells, such as oral cancer, pancreatic cancer, gallbladder cancer, prostate cancer, and colorectal cancer. [38][39][40][41] Also, asiatic acid is known to be cytotoxic to several tumor cell lines. However, asiatic acid-induced cell death was mainly apoptotic, demonstrated in colon cancer RKO cells [42,43].…”

Seeking new acne treatment from natural products, devices and synthetic drug discovery

“…They conducted activity-guided purification after a series of screenings from several medicinal plants to find out a novel anti-acne component. 4 They applied a series of instrumental analysis to isolate a single functional molecule and conducted cellular and histological analysis to find out mechanisms of this molecule on acne treatment.…”

“…Lupeol, which is the final purified molecule, presents in several plant species, and has been reported to possess wide-spectrum pharmacological activities. 4 …”