Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – C-o-group doai
Reexamination Certificate
1999-05-21
2001-08-07
Naff, David M. (Department: 1651)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
C-o-group doai
C514S560000, C514S546000, C514S762000
Reexamination Certificate
active
06271267
ABSTRACT:
BACKGROUND OF THE INVENTION
1. Field of Invention
The present invention relates to agents having regulatory activity for the morphological transition of dimorphic fungi which can grow both as yeast form cells and as mycelial form cells.
2. Description of Related Art
Most fungi take the form, through their life cycle, of either a spherical single cell growing through budding (or cell division) (yeast form fungus) or a filamentous multicellular organism growing through apical growth (filamentous fungus). However, some yeasts can reversibly take yeast form (Y form) and mycelial form (M form). This phenomena in which such a reversible transition occurs due to a specific nutritional, physical or chemical factor is called as dimorphism. The dimorphic fungi generally belong to Subdivision Deuteromycotina. and typically include genus Candida. The dimorphic fungi such as genus Candida are indigenous microbes with respect to humans, which generally exist in human bodies or in a living environment. They are not pathogenic to healthy humans but become pathogenic to patients whose immunity is deteriorated by some cause, and such an infection is called as an opportunistic infection. By taking
Candida albicans
belonging to genus Candida as an example, it has been known, in fact, that a multiplicity of mycelial form cells are present in combination with yeast form cells in infectious foci of candidiasis, indicating that being mycelial form cells is one of the pathogenic factors of this fungi. This is supposedly because mycelia of the mycelium form cells readily adhere to animal tissues and advantageously serve to invade mechanically into the inside of host tissues, and in addition hardly suffer from mycophagy activities of phagocytes (Arai, T., et al., Sabouraudia 15, 171-177(1977)).
SUMMARY OF THE INVENTION
Practical findings on factors of the reversible transition between yeast form cells and mycelial form cells, however, have not yet been obtained. If mycelial form cells, which are considered to be pathogenic, can be transited to yeast form cells with efficiency, opportunistic infections caused by these dimorphic fungi may be mitigated. To patients whose biophylaxis functions are deteriorated, such as the elderly, patients with cancers, or patients who have been subjected to organ transplantation or those infected with HIV, a variety of antibiotics are administered for phylaxis against bacteria, but infections of molds, yeasts or other fungi induced by microbial substitution cannot be prevented under present circumstances. In particular, medically significant demands have been made to develop drugs that are effective to dimorphic fungi generally exiting in vivo and have less adverse drug reactions.
Accordingly, the present invention provides an agent having regulatory activity on the morphological transition of dimorphic fungi, which includes a compound containing at least one geranyl group represented by the following formula (1) as its main structure:
(CH
3
)
2
C═CH—CH
2
—CH
2
—C(CH
3
)═CH—CH
2
—
In this agent, the compound containing at least one geranyl group may preferably be a terpene or its isomer, or a derivative thereof.
The terpene in the above agent may be a monoterpene composed of one geranyl group, a sesquiterpene containing one geranyl group or a diterpene containing two geranyl groups.
In this agent, when the dimorphic fungi are genus Candida, the regulatory activity on morphologic transition may be inhibitory activity on transition of yeast form cells to mycelial form cells or promoting activity on transition of mycelial form cells to yeast form cells.
REFERENCES:
patent: 3595975 (1971-07-01), Gauvreau
patent: 4220665 (1980-09-01), Klein
Arai, T. et al., “Phagocytosis ofCandida albicansby Rabbit Alveolar Macrophages and Guinea Pig Neutrophils,”Sabouraudia15, pp. 171-177 (1977).
Jorge Neto, Rev. Fac. Farm. Odontol. Araraquara, 10(2), 317-327, 1976.*
Duve et al., J. Insect. Physiol. , 38(8), 575-585, 1992.*
Andersen et al., Chem. Res. Toxicol., 10(2), 156-164, 1997.*
Lunz et al., Physiol. Entomol., 22(4), 365-372, 1997.
Matsuoka Hideaki
Oh Ki-Bong
Bio-Giken, Inc.
Meller Mike
Naff David M.
Oliff & Berridg,e PLC
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