Acanthoic acid, unique potential pimaradiene diterpene isolated from Acanthopanax koreanum Nakai (Araliaceae): A review on its pharmacology, molecular mechanism, and structural modification

Q2 · BIOLOGY

Review

Author: Dou, Jia-Yi ; Jiang, Yu-Chen ; Lian, Li-Hua ; Cui, Zhen-Yu ; Nan, Ji-Xing ; Wu, Yan-Ling

Acanthoic acid (AA) is a pimaradiene diterpene isolated from the root bark of Acanthopanax koreanum Nakai (Araliaceae) with a wide range of pharmacological activities, including anti-cancer, anti-inflammatory, anti-diabetes, liver protection, gastrointestinal protection, and cardiovascular protection. In addition, AA promotes its pharmacological effects by targeting liver X receptors (LXRs), nuclear factor-kappa B (NF-κB), Toll-Like Receptor 4 (TLR4) and IL-1 receptor-associated kinase (IRAK) signaling pathways, or AMP-activated protein kinase (AMPK) signaling pathway, etc. Also, some studies focus on the structural modification of AA to improve its pharmacological activities. The review summarizes the pharmacological activities, molecular mechanism, and the structural modification of AA, which might supply information for the development of AA in the future.

01 Dec 2021·Phytotherapy ResearchQ2 · MEDICINE

Antitumor effect of acanthoic acid against primary effusion lymphoma via inhibition of c‐FLIP

Q2 · MEDICINE

Article

Author: Kasemsuk, Teerapich ; Sittithumcharee, Gunya ; Kariya, Ryusho ; Saeeng, Rungnapha ; Okada, Seiji

AbstractAcanthoic acid (AA) is an active substance that is extracted from Croton oblongifolius Roxb., a traditional plant in Thailand. The antiinflammatory effect of AA on NF‐κB pathway has been exclusively reported, however, its anticancer effect is still lacking. PEL is a B cell lymphoma that is mostly found in HIV patients. The prognosis and progression of PEL patients are terribly poor with a median survival time less than 6 months, so the new effective treatment is urgently needed. In this study, we found that AA effectively inhibited PEL cell proliferation with IC50s at 120–130 μM in well‐representative cells, while the IC50s of AA in PBMC were higher (>200 μM). AA increased percentages of Annexin V/PI positive cells, whereas adding of caspase inhibitor (Q‐VD‐OPh) prevented AA‐induced cell death. The antiapoptotic protein, c‐FLIP, was downregulated by AA which leading to the activation of caspase‐8 and ‐3. Combination of AA and TRAIL dramatically enhanced apoptotic cell death. In PEL xenograft model, AA at the dose of 250 mg/kg effectively inhibited PEL tumor growth without detectable toxicities assessed by mice weight and appearance.

01 Jan 2021·Bioorganic & Medicinal ChemistryQ3 · MEDICINE

A novel synthetic acanthoic acid analogues and their cytotoxic activity in cholangiocarcinoma cells

Q3 · MEDICINE

Article

Author: Okada, Seiji ; Sittithumcharee, Gunya ; Kasemsuk, Teerapich ; Arsakhant, Patcharee ; Saeeng, Rungnapha ; Saehlim, Natthiya

A novel series of acanthoic acid analogues containing triazole moiety were synthesized through esterification and CuAAC reaction. Evaluation of their biological activities against four cell lines of cholangiocarcinoma cells showed that 3d exhibited the strongest activity with an IC₅₀ value of 18 µM against KKU-213 cell line, which was 8 fold more potent than acanthoic acid. Interestingly, the triazole ring and nitro group on benzyl ring play very significant role in cytotoxic activity. The computational studies revealed that 3d occupies the binding energy of -12.7 and -10.8 kcal/mol with CDK-2 and EGFR protein kinases, respectively. This result might provide a beginning for the development of acanthoic acid analogues as an anticancer agent.

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Indication	Highest Phase	Country/Location	Organization	Date
Infertility, Male	Preclinical	South Korea	Kyungpook National University	13 Jul 2024

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