Cryptolepine research information, alkaloid info
Cryptolepine is a naturally occurring indoloquinoline alkaloid used as an antimalarial drug in Central and Western Africa.
Cryptolepine comes from the West African shrub Cryptolepis sanguinolenta. Several cryptolepine analogues have been synthesized that have potential antimalarial activity.
Characterization of the cytotoxic activity of the indoloquinoline alkaloid
cryptolepine in human tumour cell lines and primary cultures of tumour cells
from patients.
Invest New Drugs. 2008. Laryea D, Isaksson A, Wright CW, Larsson R. Division of Clinical Pharmacology, Department of Medical Sciences,
University Hospital, Uppsala, Sweden, Laryea D, Isaksson A, Wright CW,
Larsson R, Nygren P.
The plant derived indoloquinoline alkaloid cryptolepine was investigated for its
cytotoxic properties in 12 human tumour cell lines and in primary cultures of
tumour cells from patients. Among patient solid tumour samples, those from
breast cancer were the most sensitive and essentially as sensitive as
haematological malignancies. Cryptolepine activity showed highest correlations
to topoisomerase II and microtubule targeting drugs. In the cell lines
cryptolepine activity was essentially unaffected by established mechanisms of
drug resistance. A number of genes were identified as associated with
cryptolepine activity. In conclusion, cryptolepine shows interesting in vitro
cytotoxic properties and its further evaluation as an anti-cancer
drug seems warranted.
Evaluation of cryptolepine and huperzine derivatives as
lead compounds towards new agents for the treatment of human African
trypanosomiasis.
Nat Prod Commun. 2009. Oluwafemi AJ, Okanla EO, Camps P,
Muņoz-Torrerob D, Mackey ZB, Chiang PK, Seville S, Wright CW. Department of
Zoology, University of Ilorin, Ilorin, Nigeria.
The alkaloid cryptolepine (1) and eight synthetic analogues (2-8) were assessed
for in vitro activities against Trypanosoma brucei. Four of the analogues were
found to be highly potent with IC50 values of less than 3 nM and three of these
were assessed against T. brucei brucei infection in rats. The most effective
compound was 2, 7-dibromocryptolepine (7); a single oral dose of 20 mg/kg
suppressed parasitaemia and increased the mean survival time to 13.6 days
compared with 8.4 days for untreated controls. In addition, four huperzine
derivatives (9-12) were shown to have in vitro antitrypanosomal activities with
IC50 values ranging from 303-377 nM.
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