| Description: |
4-Methoxy-5- hydroxycanthin-6-one has anti-inflammatory effect, it can significantly inhibit the production of NO and the release of TNF-α induced by LPS in macrophage RAW 264.7, it has protective effect on dextran sulfate sodium -induced rat colitis. After oral administration, 4-methoxy-5- hydroxycanthin-6-one (3, 9, and 27 mg/kg) can reduce the development of carrageenan-induced paw edema and complete Freund's adjuvant (CFA)-induced chronic arthritis in rats. 5-Hydroxy-4-methoxycanthin-6-one exhibits significant cytotoxic activity against CNE2 cell line.
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| Targets: |
NO | TNF-α | NOS |
| In vitro: |
| J Asian Nat Prod Res. 2008 Nov-Dec;10(11-12):1009-12. | | Canthin-6-one alkaloids from Picrasma quassioides and their cytotoxic activity.[Pubmed: 19031238] |
METHODS AND RESULTS:
A new alkaloid, 4,5-dimethoxy-10-hydroxycanthin-6-one (1), was isolated from the stem of Picrasma quassioides Bennet (Simaroubaceae) together with four known canthin-6-one alkaloids, 8-hydroxycanthin-6-one (2), 4,5-dimethoxycanthin-6-one (3), 5-hydroxy-4-methoxycanthin-6-one (4), and 3-methylcanthin-5,6-dione (5). Their structures were elucidated on the basis of spectroscopic data. The cytotoxic activity of the canthin-6-one alkaloids was evaluated using human nasopharyngeal carcinoma (CNE2) and human liver cancer (Bel-7402) cell lines.
CONCLUSIONS:
Among these isolates, compounds 1-4 exhibited significant cytotoxic activity against CNE2 cell line. |
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| In vivo: |
| Phytomedicine. 2013 Feb 15;20(3-4):319-23. | | In vitro and in vivo anti-inflammatory effects of 4-methoxy-5- hydroxycanthin-6-one, a natural alkaloid from Picrasma quassioides.[Pubmed: 23271002 ] | In the present study, we evaluated the anti-inflammatory effect of 4-methoxy-5- hydroxycanthin-6-one (5-Hydroxy-4-methoxycanthin-6-one,CAN), a natural alkaloid isolated from Picrasma quassioides.
METHODS AND RESULTS:
CAN significantly inhibited the production of NO and the release of TNF-α induced by LPS in macrophage RAW 264.7. Western blot showed that CAN can downregulate the expression of iNOS protein. After oral administration, CAN (3, 9, and 27 mg/kg) reduced the development of carrageenan-induced paw edema and complete Freund's adjuvant (CFA)-induced chronic arthritis in rats.
CONCLUSIONS:
The observed results indicated that pre-treatment with CAN might be an effective therapeutic intervention against inflammatory diseases including chronic arthritis. | | Planta Med. 2009 Feb;75(2):142-5. | | Protective effect of 4-methoxy-5-hydroxycanthin-6-one, a natural alkaloid, on dextran sulfate sodium-induced rat colitis.[Pubmed: 19085815] |
METHODS AND RESULTS:
In the present study, we evaluated the effect of 4-methoxy-5-hydroxycanthin-6-one (5-Hydroxy-4-methoxycanthin-6-one, CAN), a natural alkaloid isolated from Picrasma quassioides (D.Don) Benn., on ulcerative colitis induced by dextran sulfate sodium (DSS) in rats in comparison with the positive control drug, sulfasalazine (SASP). Given orally for several days, CAN significantly reduced the severity of colitis and mitigated changes in colon length, colon mucosa myeloperoxidase (MPO) activity, and the level of tumor necrosis factor-alpha (TNF-alpha) in serum. The effect of CAN was similar to that of SASP.
CONCLUSIONS:
These results suggest that CAN treatment might be an effective therapeutic intervention against ulcerative colitis induced by DSS. |
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