Leishmanicidal, antiplasmodial and cytotoxic activity of indole alkaloids from Corynanthe pachyceras

D Staerk; E Lemmich; J Christensen; A Kharazmi; C E Olsen; J W Jaroszewski

Leishmanicidal, antiplasmodial and cytotoxic activity of indole alkaloids from Corynanthe pachyceras

D Staerk, E Lemmich, J Christensen, A Kharazmi, C E Olsen, J W Jaroszewski

Centre for Medical Parasitology

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Abstract

Five indole alkaloids, corynantheidine, corynantheine, dihydrocorynantheine, alpha-yohimbine and corynanthine were isolated from bark of Corynanthe pachyceras K. Schum. (Rubiaceae). The structures were established by spectroscopic methods, including previously unreported assignment of all 1H-NMR resonances by COSY and NOESY experiments. These and related alkaloids showed pronounced activity against Leishmania major promastigotes (IC50 at the micromolar level) but no significant in vitro antiplasmodial activity (against chloroquine-sensitive Plasmodium falciparum). Cytotoxicity assessed with drug sensitive KB-3-1 and multidrug-resistant KB-V1 cell lines was low; the alkaloids are apparently not substrates for the P-glycoprotein (P-170) efflux pump.

Originalsprog	Engelsk
Tidsskrift	Planta Medica
Vol/bind	66
Sider (fra-til)	531-536
ISSN	0032-0943
Status	Udgivet - 2000

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@article{1cebc56021f211df8ed1000ea68e967b,

title = "Leishmanicidal, antiplasmodial and cytotoxic activity of indole alkaloids from Corynanthe pachyceras",

abstract = "Five indole alkaloids, corynantheidine, corynantheine, dihydrocorynantheine, alpha-yohimbine and corynanthine were isolated from bark of Corynanthe pachyceras K. Schum. (Rubiaceae). The structures were established by spectroscopic methods, including previously unreported assignment of all 1H-NMR resonances by COSY and NOESY experiments. These and related alkaloids showed pronounced activity against Leishmania major promastigotes (IC50 at the micromolar level) but no significant in vitro antiplasmodial activity (against chloroquine-sensitive Plasmodium falciparum). Cytotoxicity assessed with drug sensitive KB-3-1 and multidrug-resistant KB-V1 cell lines was low; the alkaloids are apparently not substrates for the P-glycoprotein (P-170) efflux pump.",

author = "D Staerk and E Lemmich and J Christensen and A Kharazmi and Olsen, {C E} and Jaroszewski, {J W}",

note = "Keywords: Alkaloids; Animals; Antineoplastic Agents, Phytogenic; Antiprotozoal Agents; Humans; Indoles; Leishmania major; Plants, Medicinal; Plasmodium falciparum; Tumor Cells, Cultured",

year = "2000",

language = "English",

volume = "66",

pages = "531--536",

journal = "Planta Medica",

issn = "0032-0943",

publisher = "GeorgThieme Verlag",

}

TY - JOUR

T1 - Leishmanicidal, antiplasmodial and cytotoxic activity of indole alkaloids from Corynanthe pachyceras

AU - Staerk, D

AU - Lemmich, E

AU - Christensen, J

AU - Kharazmi, A

AU - Olsen, C E

AU - Jaroszewski, J W

N1 - Keywords: Alkaloids; Animals; Antineoplastic Agents, Phytogenic; Antiprotozoal Agents; Humans; Indoles; Leishmania major; Plants, Medicinal; Plasmodium falciparum; Tumor Cells, Cultured

PY - 2000

Y1 - 2000

N2 - Five indole alkaloids, corynantheidine, corynantheine, dihydrocorynantheine, alpha-yohimbine and corynanthine were isolated from bark of Corynanthe pachyceras K. Schum. (Rubiaceae). The structures were established by spectroscopic methods, including previously unreported assignment of all 1H-NMR resonances by COSY and NOESY experiments. These and related alkaloids showed pronounced activity against Leishmania major promastigotes (IC50 at the micromolar level) but no significant in vitro antiplasmodial activity (against chloroquine-sensitive Plasmodium falciparum). Cytotoxicity assessed with drug sensitive KB-3-1 and multidrug-resistant KB-V1 cell lines was low; the alkaloids are apparently not substrates for the P-glycoprotein (P-170) efflux pump.

AB - Five indole alkaloids, corynantheidine, corynantheine, dihydrocorynantheine, alpha-yohimbine and corynanthine were isolated from bark of Corynanthe pachyceras K. Schum. (Rubiaceae). The structures were established by spectroscopic methods, including previously unreported assignment of all 1H-NMR resonances by COSY and NOESY experiments. These and related alkaloids showed pronounced activity against Leishmania major promastigotes (IC50 at the micromolar level) but no significant in vitro antiplasmodial activity (against chloroquine-sensitive Plasmodium falciparum). Cytotoxicity assessed with drug sensitive KB-3-1 and multidrug-resistant KB-V1 cell lines was low; the alkaloids are apparently not substrates for the P-glycoprotein (P-170) efflux pump.

M3 - Journal article

C2 - 10985079

SN - 0032-0943

VL - 66

SP - 531

EP - 536

JO - Planta Medica

JF - Planta Medica

ER -

Leishmanicidal, antiplasmodial and cytotoxic activity of indole alkaloids from Corynanthe pachyceras

Abstract

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