| Description: |
Nantenine is an acetylcholinesterase inhibitor, it functions as an effective antagonist against a wide range of MDMA-induced effects in mice. Nantenine has anticonvulsant effect, which seems attributable to its stimulation and the resultant decrease of Ca2+-influx into the cell. (+)-Nantenine has antagonistic activities on alpha1-adrenoceptors, alpha2-adrenoceptors and 5-HT2A receptors in pithed rats. Nantenine displays cytotoxicity against SMMC-7721 with the IC50 value of 70.08 ± 4.63 uM. |
| Targets: |
5-HT Receptor | Calcium Channel | Potassium Channel | Beta Amyloid | AChR | ATPase |
| In vitro: |
| Evid Based Complement Alternat Med. 2014;2014:580483. | | Cytotoxicity of Aporphine, Protoberberine, and Protopine Alkaloids from Dicranostigma leptopodum (Maxim.) Fedde.[Pubmed: 24963327] |
METHODS AND RESULTS:
Nine alkaloids with three different structural skeletons were isolated from Dicranostigma leptopodum (Maxim.) Fedde (Papaveraceae) by repeated silica gel column chromatography. Their chemical structures were identified on the basic of physicochemical and spectroscopic data. Among them, 10-O-methylhernovine (1), nantenine (2), corytuberine (3), lagesianine A (4), and dihydrocryptopine (9) were first isolated from this plant.
CONCLUSIONS:
With a series of cytotoxic tests, compounds 2, 3, and 7 displayed cytotoxicity against SMMC-7721 with IC50 values of 70.08 ± 4.63, 73.22 ± 2.35, and 27.77 ± 2.29 μ M, respectively. | | J Pharmacol Sci. 2011;115(2):254-7. | | Biphasic tracheal relaxation induced by higenamine and nantenine from Nandina domestica Thunberg.[Pubmed: 21282929] |
METHODS AND RESULTS:
We compared the effects of the extract from fruits of Nandina domestica Thunberg (NDE) and its constituents, higenamine and nantenine, on contractile responses in isolated guinea-pig trachea. NDE (1 mg/ml) caused biphasic relaxation of the trachea precontracted with high-K(+) stimulation: the fast component was blocked by propranolol and mimicked by higenamine; and the slow was resistant to propranolol and mimicked by nantenine. Ca(2+)-induced contraction under high-K(+) stimulation was antagonized by nantenine or NDE + propranolol.
CONCLUSIONS:
These results suggest that NDE relaxes the trachea quickly through β-adrenoceptor stimulation by higenamine and slowly through Ca(2+) antagonism by nantenine. |
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| In vivo: |
| Eur J Pharmacol. 2003 Sep 5;477(1):53-8. | | (+)-Nantenine isolated from Nandina domestica Thunb. inhibits adrenergic pressor responses in pithed rats.[Pubmed: 14512098] | The effects of (+)-Nantenine on various pressor responses, recently reported exerting competitive antagonistic activity at the alpha1-adrenoceptor/5-hydroxytryptamine (5-HT)2A receptor, were examined in vivo.
METHODS AND RESULTS:
(+)-Nantenine (0.03-3 mg/kg) caused a dose-dependent inhibition of the pressor response to phenylephrine (alpha1-adrenoceptor agonist) or 5-HT (5-HT receptor agonist) in both anesthetized and pithed rats. The pressor response to UK 14304 (5-Bromo-N-[2-imidazolin-2-yl]-6-quinoxalinamine) (an alpha2-adrenoceptor agonist) was inhibited by (+)-Nantenine (0.003-3 mg/kg) in pithed rats in a dose-dependent manner without affecting the angiotensin II-induced pressor response in anesthetized rats. The pressor response to sympathetic nerve stimulation was also inhibited by (+)-Nantenine (0.3-3 mg/kg) in a dose-dependent manner. (+)-Nantenine (3 mg/kg) facilitated the norepinephrine release induced by sympathetic nerve stimulation in pithed rats. In the guinea pig vas deferens, the initial component of contractions induced by electrical field stimulation was enhanced by (+)-Nantenine (1-30 microM) in a concentration-dependent manner, while the later component was inhibited by it.
CONCLUSIONS:
These data suggest that (+)-Nantenine has antagonistic activities on alpha1-adrenoceptors, alpha2-adrenoceptors and 5-HT2A receptors in pithed rats. | | Phytomedicine. 2003;10(6-7):563-8. | | Nantenine alkaloid presents anticonvulsant effect on two classical animal models.[Pubmed: 13678244 ] | The present study investigated the anticonvulsant and convulsant profiles of nantenine, an aporphine alkaloid found in several vegetal species.
METHODS AND RESULTS:
At lower doses (20-50 mg/kg, i.p.) the alkaloid proved to be effective in inhibiting pentylenotetrazol- (PTZ 100 mg/kg, s.c.) and maximal electroshock-induced seizures (80 mA, 50 pulses/s, 0.2 s), suggesting its potential as an anticonvulsant drug. However, at higher doses (> or = 75 mg/kg, i.p.) a convulsant activity was observed.
CONCLUSIONS:
Comparing the present in vivo nantenine effects on seizures with previous in vitro biphasic action on Na+, K+-ATPase activity, the convulsant effect appears to be related to inhibition of these phosphatase at high doses whereas anticonvulsant effect, observed at low doses, seems attributable to its stimulation and the resultant decrease of Ca2+-influx into the cell. |
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