2. Academic Validation
  3. Anti-inflammatory Quinoline Alkaloids from the Roots of Waltheria indica

Anti-inflammatory Quinoline Alkaloids from the Roots of Waltheria indica

  • J Nat Prod. 2023 Feb 24;86(2):276-289. doi: 10.1021/acs.jnatprod.2c00861.
Feifei Liu 1 2,  Timothy J O'Donnell 3,  Eun-Jung Park 2 4,  Sasha Kovacs 2,  Kenzo Nakamura 2,  Asim Dave 4,  Yuheng Luo 3,  Rui Sun 3,  Marisa Wall 5,  Supakit Wongwiwatthananukit 6,  Dane Kaohelani Silva 7,  Philip G Williams 3,  John M Pezzuto 2 8,  Leng Chee Chang 2
Affiliations

Affiliations

  • 1 School of Life Sciences, Jiangsu Normal University, Xuzhou, Jiangsu 221116, People's Republic of China.
  • 2 Department of Pharmaceutical Sciences, Daniel K. Inouye College of Pharmacy, University of Hawai'i at Hilo, Hilo, Hawaii 96720, United States.
  • 3 Department of Chemistry, University of Hawai'i at Manoa, 2545 McCarthy Mall, Honolulu, Hawaii 96822, United States.
  • 4 Arnold and Marine Schwartz College of Pharmacy and Health Sciences, Long Island University, Brooklyn, New York 11201, United States.
  • 5 Daniel K. Inouye U.S. Pacific Basin Agricultural Research Center, USDA-ARS, Hilo, Hawaii 96720, United States.
  • 6 Department of Pharmacy Practice, Daniel K. Inouye College of Pharmacy, University of Hawai'i at Hilo, Hilo, Hawaii 96720, United States.
  • 7 Hale Ola Pono, LLC, Keaau, Hawaii 96749, United States.
  • 8 College of Pharmacy and Health Sciences, Western New England University, Springfield, Massachusetts 10119, United States.
PMID: 36746775 DOI: 10.1021/acs.jnatprod.2c00861
Abstract

Sixteen new Quinoline Alkaloids (1a-7, 8a, 9, 10, 13-15, 17, and 21) and 10 known analogs (8b, 11, 12, 16, 18-20, and 22-24), along with three known cyclopeptide Alkaloids (25-27), were isolated from the roots of Waltheria indica. The structures of the new compounds were elucidated by detailed NMR and circular dichroism with computational support and mass spectrometry data interpretation. Anti-inflammatory potential of isolates was evaluated based on inhibition of lipopolysaccharide (LPS)-induced nitric oxide (NO) production and tumor necrosis factor-alpha (TNF-α)-induced nuclear factor kappa B (NF-κB) activity with Cell Culture models. In the absence of cell growth inhibition, compounds 6, 8a, 9-11, 13, 21, and 24 reduced TNF-α-induced NF-κB activity with IC50 values ranging from 7.1 to 12.1 μM, comparable to the positive control (BAY 11-7082, IC50 = 9.7 μM). Compounds 6, 8a, 8b, and 11 showed significant NO-inhibitory activity with IC50 values ranging from 11.0 to 12.8 μM, being more active than the positive control (l-NMMA, IC50 = 22.7 μM). Structure-activity relationships indicated that NO inhibitory activity was significantly affected by C-8 substitution. Inhibition of LPS-induced nitric oxide synthase (iNOS) by 8b [(5S)-waltherione M, IC50 11.7 ± 0.8 μM] correlated with inhibition of iNOS mRNA expression. The biological potential of W. indica metabolites supports the traditional use of this plant for the treatment of inflammatory-related disorders.

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