Antituberculosis compounds, Hirsutellones A, B, and C

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

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C435S117000, C548S417000

Reexamination Certificate

active

07414069

ABSTRACT:
Three new alkaloids, Hirsutellones A, B, and C, are produced in cultures of fungus such asHirsutella niveastrain BCC 2594 andTrichodermasp. strain BCC 7579. The Hirsutellones exhibited potent growth inhibitory activity againstMycobacterium tuberculosis(H37Ra strain) with an MIC value of 0.78 μg/ml, while showing weak or no cytotoxicity to mammalian cells. Therefore, Hirsutellones and pharmaceutical compositions containing Hirsutellones may be useful for the treatment of tuberculosis. Also described herein are methods of isolating the Hirsutellones.

REFERENCES:
patent: 2001247574 (2001-09-01), None
Isaka et al. “Hirsutellones A-E, antimycobacterial alkaloids from the insect pathogenic fungusHirsutella niveaBCC 2594” Tetrahedron, 2005, vol. 61, pp. 5577-5583.
Collins, Lisa A. et al. (May 1997) “Microplate Alamar Blue Assay versus BACTEC 460 System for High-Throughput Screening of Compounds againstMycobacterium tuberculosisandMycobacterium avium,” Antimicrobial Agents and Chemotherapy, 41(5): 1004-1009.
He, Haiyin et al. (2002) “Pyrrocidines A and B, new antibiotics produced by a filamentous fungus,” Tetrahedron Letters, 43: 1633-1636.
Hywel-Jones, Nigel L. (1997) “Hirsutellaspecies associated with hoppers (Homoptera) in Thailand,” Mycol. Res., 101(10): 1202-1206.
Skehan, Philip et al. (Jul. 4, 1990) “New Colorimetric Cytotoxicity Assay for Anticancer-Drug Screening,” Natl Cancer Inst, 82(13): 1107-1112.

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