Share This Article:

In Vitro Antiprotozoal and Cytotoxic Activity of the Aqueous Extract, the 80% Methanol Extract and Its Fractions from the Seeds of Brucea sumatrana Roxb. (Simaroubaceae) Growing in Democratic Republic of Congo

Abstract Full-Text HTML Download Download as PDF (Size:92KB) PP. 65-71
DOI: 10.4236/cm.2012.31011    4,224 Downloads   8,117 Views   Citations


The in vitro antiprotozoal and cytotoxic activity of the aqueous extract, the 80% methanol extract, and its different soluble fractions and subfractions from Brucea sumatrana seeds were assessed against two Trypanosoma (T. cruzi and T. brucei brucei), Leishmania infantum and chloroquine and pyrimethanine-resistant K1strain of P. falciparum and against MRC-5 cell-lines respectively. Results indicated that the 80% methanol extract showed a cytotoxic effect against MRC-5 cell lines with CC50 value of 0.54 μg/ml. It however exhibited pronounced and non selective activity against T. cruzi (IC50 = 1.52 μg/ml, SI = 0.03) and L. infantum (IC50 = 2.41 μg/ml, SI = 0.22). It however displayed pronounced and selective effect against T. brucei brucei (IC50 < 0.25, SI > 2.16) and chloroquine and pyrimethamine-resistant K1 strain of P. falciparum (IC50 < 0.25 μg/ml, SI > 2.16). All soluble fractions and subfractions from the partition of the 80% methanol extract were found to exhibit an antiprotozoal activity with IC50 values ranging from <0.25 to 30 μg/ml. The most active was the alkaline aqueous soluble fraction exhibiting pronounced antiprotozoal activity against T .cruzi, T. b. brucei, L. infantum and chloroquine and pyrimethamine-resistant K1 strain of P. falciparum with IC50 values of 0.33, <0.25, 0.25, <0.25 μg/ml respectively resulting in high selective index values of 61.36, > 81, 81 and >81 respectively. The chloroform soluble fraction rich in alkaloid was cytotoxic against MRC-5 cell lines (CC50 = 27.09 μg/ml) and showed good activity against T. b. brucei (IC50 = 8.36 and SI = 3.24) and moderate activity against T. cruzi, L. infantum and chloroquine-pyrimethane-resistant K1 strain of P. falciparum (20 < IC50 < 30 μg/ml). Although the aqueous extract (decoction) and the total alkaloids extract showed a cytotoxic effect against MRC-5 cell lines (CC50 = 1.55 and 0.43 μg/ml respectively), they however displayed pronounced antiprotozoal activity against T. cruzi, T. b. brucei and chloroquine and pyrimethamine-resistant K1 strain of P. falciparum with IC50 values ranging from < 0.25 to 0.6 μg/ml with only a selective action against chloroquine and pyrimethamine-resistant K1 strain of P. falciparum (SI = >6.2 and >1.72 respectively). These extracts however showed good and low activity respectively against L. infantum (IC50 = 24.05 and 6.82 μg/ml respectively).

Conflicts of Interest

The authors declare no conflicts of interest.

Cite this paper

M. Ehata, A. Phuati, S. Lumpu, C. Munduki, D. Phongi, G. Lutete, O. Kabangu, R. Kanyanga, A. Matheeussen, P. Cos, S. Apers, L. Pieters, L. Maes and A. Vlietinck, "In Vitro Antiprotozoal and Cytotoxic Activity of the Aqueous Extract, the 80% Methanol Extract and Its Fractions from the Seeds of Brucea sumatrana Roxb. (Simaroubaceae) Growing in Democratic Republic of Congo," Chinese Medicine, Vol. 3 No. 1, 2012, pp. 65-71. doi: 10.4236/cm.2012.31011.


[1] M. O. Hasbi, “Pharmacognostic Study of Brucea amarissima Merr. from Gowa (South Sulawesi, Indonesia), Isolation and Identification of quassinoid Compound by Thin Layer Chromatography,” Research Report, Vol. 1, No. 1, 1979, pp. 6-7.
[2] W. Tang and G. Eisenbrand, “Chinese Drugs of Plant Origin. Chemistry, Pharmacology, and Use Traditional and Modern Medicine,” Springer-Verlag, New York, 1992.
[3] Subeki, H. Matssura, K. Tabahashi, K. Nabeta, M. Yamasaki, Y. Maede and K. Katakura, “Screening of Indonesian Medicinal Plant Extracts for Antibabesial Activity and Isolation of New Quassinoids from Brucea javanica,” Journal of Natural Products, Vol. 70, No. 10, 2007, pp. 1654-1657. doi:10.1021/np070236h
[4] A. NoorShahida, T. W. Wong and C. Y. Choo, “Hypoglycemic Effect of quassinoids from Brucea javanica (L.) Merr. (Simaroubaceae) Seeds,” Journal of Ethnopharmacology, Vol. 124, No. 3, 2009, pp. 586-591. doi:10.1016/j.jep.2009.04.058
[5] M. M. Anderson, M. J. O’Neill, J. D. Phillipson and D. C. Warhurst, “In Vitro Cytotoxic of a Series of Quassinoids from Brucea javanica Fruits against KB Cells,” Planta Medica, Vol. 157, No. 1, 1991, pp. 62-64. doi:10.1055/s-2006-960020
[6] C. Karin, S. B. Liu, S. L. Yang,. M. F. Roberts and J. D. Phillipson, “Production of Canthin-6-One Alkaloids by Cell Suspension Cultures of Brucea javanica (L.) Merr,” Plant Cell Reports, Vol. 9, No. 5, 1990, pp. 261-263.
[7], 2010.
[8] J. M. Watt and M. C. Breyer-Brandwijk, “Medicinal and Poisonous Plants of Southern and Eastern Africa,” Livingstone, Edinburg, 1962.
[9] B. Ngoma and M. Bitengeli, “Therapeutic Application of Brucea sumatrana Roxb. (Simaroubaceae),” Al-Birunya, Vol. 9, No. 1, 1993, pp. 101-108.
[10] K. Pavanand, W. Nutakul, T. Dechatiwongse, K. Yoshihira, K. Yongvanitchit, J. P. Scovill, L. L. Flippen-Anderson, R. Gilardi, C. George, P. Kanchanapee and H. K. Webster, “In Vitro Antimalarial Activity of Brucea Javanica against Multi-Drug Resistant Plasmodium falciparum,” Planta Medica, Vol. 52, No. 1, 1986, pp. 108-111. doi:10.1055/s-2007-969092
[11] M. J. O’Neill, D. H. Bray, P. Boardman, J. D. Phillipson, D. C. Warhurst, W. Peters and M. Suffers, “Plants as Sources of Antimalarial Drugs: In Vitro Antimalarial Activities of Some Quassinoids,” Antimicrobial Agents Chemotherapy, Vol. 30, No. 1, 1986, pp. 101-104.
[12] M. J. O’Neill, D. H. Bray, P. Boardman, L. I. Chan and J. D. Phillipson, “Plants as Sources of Antimalarial Drugs, Parts 4: Activity of Brucea javanica Fruits against Chloroquine-Resistant and Pyrimethamine-Resistant Plasmodium falciparum in Vitro and against Plasmodium berghei in Vivo,” Journal of Natural Products, Vol. 50, No. 1, 1987, pp. 41-48. doi:10.1021/np50049a007
[13] H. S. Kim, Y. Shibata, N. Ko, N. Ikemoto, Y. Ishizuka, N. Murakami, M. Sugimoto, M. Kobayashi and Y. Wataya, “Potent in Vivo Antimalarial Activity of 3,15-Di-O-acetylbruceolide against Plasmodium berghei Infection in Mice,” Parasitology International, Vol. 48, No. 3, 2000, pp. 271-274. doi:10.1016/S1383-5769(99)00023-9
[14] M. D. R. Camacho, J. D. Phillipson, S. L. Croft, P. N. Solis, S. J. Marshall and S. A. Ghazanfar, “Screening of Plant Extracts for Antiprotozoal and Cytotoxic Activities,” Journal of Ethnopharmacology, Vol. 89, No. 2-3, 2003, pp. 185-191. doi:10.1016/S0378-8741(03)00269-1
[15] J. Nguyen-Pouplin, H. Tan, H. Tran, T. A. Phan, C. Dolecek, J. Farrar, T. H. Tran, P. Caron, B. Bodo and P. Grellier, “Antimalarial and Cytotoxic Activities of Ethnopharmacologically Selected Medicinal Plants from South Vietnam,” Journal of Ethnopharmacology, Vol. 109, No. 3, 2007, pp. 417-427. doi:10.1016/j.jep.2006.08.011
[16] N. Sriwilaijaroen, S. Kondo, P. Nanthasri, S. Auparakkitanon, Y. Suzuki and P. Vilairat, “Antiplasmodial Effects of Brucea javanica (L.) Merr. and Eurycoma longifolia Jack and Their Combination with Chloroquine and Quinine on Plasmodium falciparum in Culture,” Tropical Medicine and Health, Vol. 38, No. 1, 2010, pp. 61-68. doi:10.2149/tmh.2009-11
[17] K. H. Lee, Y. Imakura, Y. Sumida, R. Y. Wu, I. H. Hall and H. C. Huang, “Antitumor Agents. 33. Isolation and Structural Elucidation of Bruceoside A and B, Novel Antileukemic Quassinoid Glycosides, and Brucein D and E from Brucea javanica,” Journal of Organic Chemistry, Vol. 47, No. 13, 1979, pp. 2180-2185. doi:10.1021/jo01327a031
[18] K. H. Lee. N. Hayashi, M. Okano and M. Juichi, “Antitumor Agents. 65. Brusatol and Cleomiscosin-A, Antileukemic Principles from Brucea javanica,” Journal of Natural Products, Vol. 47, No. 3, 1984, pp. 550-551. doi:10.1021/np50033a030
[19] T. Sakaki, S. Yoshimura, T. Tsuyuki, T. Takahashi, T. Honda and P. Yadanzioside, “A New Antileukemic Quassinoid Glycoside from Brucea javanica (L.) Merr. with the 3-O-(?-D-glucopyranosyl)-bruceantin Structure,” Chemical and Pharmaceutical Bulletin, Vol. 34, No. 10, 1986, pp. 4447-4450.
[20] L. Luyengi, N. Suh, H. H. S. Fong, J. M. Pezzuto and A. D. Kinghorn, “A Lignan and Four Terpenoids from Brucea javanica That Induce Differentiation with Cultured HL-60 Promyelocytic Leukemia Cells,” Phytochemistry, Vol. 43, No. 2, 1996, pp. 409-412. doi:10.1016/0031-9422(96)00258-0
[21] I. M. Kim, S. Takashima, Y. Hitotsuyanagi, T. Hasuda and K. Takeya, “New Quassinoids Javanicolides C and D and Javanicosides B-F from Seeds of Brucea javanica,” Journal of Natural Products, Vol. 67, No. 1, 2004, pp. 863-868. doi:10.1021/np030484n
[22] Y. Hitotsuyanagi, I. H. Kim, T. Hasuda, Y. Yamauchi and K. Takeya, “A Structure-Activity Relationship Study of Brusatol, an Antitumor Quassinoid,” Tetrahedron, Vol. 62, No. 20, 2006, pp. 4262-4271. doi:10.1016/j.tet.2006.01.083
[23] L. Pan, Y. W. Chin, H. B. Chai, T. N. Ninh, D. D. Soejarto and A. D. Kinghorn, “Bioactivity-Guide Isolation of Cytotoxic Constituents of Brucea javanica Collected in Vietnam,” Bioorganic and Medicinal Chemistry, Vol. 17, No. 6, 2009, pp. 2219-2224. doi:10.1016/j.bmc.2008.10.076
[24] C. W. Wright, M. J. O’Neill, J. D. Phillipson and D. C. Warhurst, “Use of Microdilution to Assess in Vitro Antiamoebic Activities of Brucea javanica Fruits, Simaruba amara, Stem, and a Number of Quassinoids,” Antimicrobial Agents Chemotherapy, Vol. 32, No. 11, 1988, pp. 1725-1729.
[25] C. W. Wright, M. M. Anderson, D. Allen, J. D. Phillipson, G. C. Kirby, D. C. Warhurst and H. R. Chang, “Quassinoid Exhibit Greater Selectivity against Plasmodium falciparum than againt Entamoeba histolytica, Giardia inetstinalis or Toxoplasma gondii in Vitro,” Journal of Eukariotic Microbiology, Vol. 40, No. 3, 1993, pp. 244-246. doi:10.1111/j.1550-7408.1993.tb04910.x
[26] N. Sawangjaroen and K. Sawangjaroen, “The Effect of Extracts from Anti-Diarrheic Thai Medicinal Plants on the in Vitro Growth of the Intestinal Protozoa Parasite Blastocytis hominis,” Journal of Ethnopharmacology, Vol. 98, No. 1-2, 2005, pp. 67-72. doi:10.1016/j.jep.2004.12.024
[27] B. S. Bawm, H. Matsuura, A. Elkhateeb, K. Nabeta, Subeki, N. Nonaka, Y. Oku and K. Katakura, “In Vitro Antitrypanosamal Activities of Quassinoid Compounds from the Fruits of a Medicinal Plant, Brucea javanica,” Veterinary Parasitology, Vol. 158, No. 4, 2008, pp. 288-294. doi:10.1016/j.vetpar.2008.09.021
[28] A. Elkhateeb, M. Yamasaki, M. Maede, K. Katakura, K. Nabeta and H. Matsuura, “Anti-Babesial Quassinoids from the Fruits of Brucea javanica,” Natural Product Communications, Vol. 3, No. 1, 2008, pp. 1-4.
[29] I. H. Hall, K. H. Lee, Y. Imakura, M. Okano and A. Johnson, “Anti-inflammatory Agents. III. Structure-Activity Relationships of Brusatol and Related Quanssinoids,” Journal of Pharmaceutical Science, Vol. 72, No. 11, 1983, pp. 1282-1284. doi:10.1002/jps.2600721111
[30] S. Yoshimura, T. Sakaki, M. Ishibashi, T. Tsuyuki, T. Takahashi, K. Matsushita and T. Honda, “Structures of Yadanziolides A, B, and C, New Bitter Principles from Brucea javanica,” Chemical and Pharmaceutical Bulletin, Vol. 32, No. 11, 1984, pp. 4698-4700. doi:10.1248/cpb.32.4698
[31] S. Yoshimura, T. Sakaki, M. Ishibashi, T. Tsuyuki, T. Takahashi and T. Honda, “Constituents of Seeds of Brucea javanica. Structures of New Bitter Principles, Yandanziolides A, B, C, Yandaziosides F, I, J, and L,” Bulletin of the Chemical Society of Japan, Vol. 58, No. 9, 1985, pp. 2673-2679. doi:10.1246/bcsj.58.2673
[32] M. E. Wagih, G. Alam, S. Wiryodagdo and K. Attia, “Improved Production of the Indole Alkaloid Canthin-One from Cell Suspension Culture of Brucea javanica (L.) Merr.,” India Journal of Science and Technology, Vol. 1, No. 1, 2008, pp. 1-6.
[33] L. A. Mitcher, Y. H. Park, D. Clark and G. W. Clark III, “Antimicrobial Agents from Higher Plants. An Investigation of Hunnemannia fumariaefolia pseudoalcoholates of Sanguinarine and Chelerythrine,” Journal of Natatural Products, Vol. 41, No. 1, 1978, pp. 145-150.
[34] J. B. Harborne, “Phytochemical Methods. A Guide to Modern Techniques of Plants Analysis,” Chapman & Hall, London, 1998.
[35] K. Kuypers, P. Cos, E. Ortega-Barria, D. Vanden Berghe and L. Maes, Bioassays for Some Parasitic Protozoa, Screening Concepts and Standard in Vitro and in Vivo Laboratory Model,” In: M. P. Gupta, S. S. Handa and K. Vanish, Eds., Biological Screening of Plant Constituents, International Centre for Science and High Technology, Trieste, 2006, pp. 7-18.
[36] W. Trager and J. Jensen, “Human Malaria Parasites in Continuous Culture,” Science, Vol. 193, No. 4254, 1976, pp. 673-675. doi:10.1126/science.781840
[37] M. T. Makler, J. M. Ries, J. A. Williams, J. E. Bancroft, R. C. Piper, B. L. Gibbins and D. J. Hinrichs, “Parasite Lactate Dehydrogenase as an Assay for Plasmodium falciparum Drug Sensitivity,” American Journal of Tropical Medicine and Hygiene, Vol. 48, No. 6, 1993, pp. 739-741.
[38] L. G. Tona, K. G. Mesia, T. H. Nanga, K. R. Cimanga, S. Apers, P. Cos, L. Maes, L. Pieters and A. J. Vleitinck, “In Vitro Antiprotozoal and Cytotoxic Activities of Plant Extracts from Democratic Republic of Congo,” Recent Research Development in Plant Science, Vol. 4, No. 1, 2007, pp. 41-60.

comments powered by Disqus

Copyright © 2020 by authors and Scientific Research Publishing Inc.

Creative Commons License

This work and the related PDF file are licensed under a Creative Commons Attribution 4.0 International License.