生薬紫根の成分Shikonin及びその誘導体, Pentaacetyl Shikonin(MDS-004)の肉芽腫形成促進作用並びに遅延型アレルギー抑制作用(薬理学)

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Of twelve reduced and acetylated derivatives of shikonin, a chemical constituent of Shikon, the accelerating activity on granuloma formation and the inhibitory activity on delayed-type allergy were investigated in order to find a compound having more characteristic effect than shikonin on wound healing in experimental animals. As a result, it was found that a reduced and pentaacetylated derivative of shikonin, MDS-004,has more excellent pharmacological activity. MDS-004 (0.1-1 mg/pellet) accelerated dose-dependently felt-pellet-induced granuloma formation when given topically together with felt-pellets in rats. It also produced strong inhibition against delayed-type allergies (ear edema) caused by oxazolone and dinitrofluorobenzene by topical application of up to 1 mg/ear to the ear skin of mice; its potency was far superior to that of shikonin. Orally administered MDS-004,unlike shikonin, inhibited carrageenan-induced hind paw edema, and exhibited tendency to heal acetic acid-induced gastric ulcer in rats. However, MDS-004,as well as commercial wound healing drugs tested and shikonin, did not show any healing action in the incised and open wound models in rats, if applied topically to the wound as 5 and 10% powders. On the other hand, MDS-004 did not produce irritative action on the ear skin at a topical dose of 1 mg/ear different from shikonin, and any behavioral changes after oral administration of 100 mg/kg in mice. These results suggest that a white powder MDS-004,different from deep purple shikonin, has accelerating action on glanuloma formation without irritative action and stronger inhibitory action on delayed-type allergy by topical application than shikonin.
公益社団法人日本薬学会の論文
1992-04-25

生薬紫根の成分Shikonin及びその誘導体, Pentaacetyl Shikonin(MDS-004)の肉芽腫形成促進作用並びに遅延型アレルギー抑制作用(薬理学)

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