カンタリジン 化学特性,用途語,生産方法
外観
白色〜ほとんど白色, 結晶〜粉末
溶解性
アセトンに溶け、水にほとんど溶けない。
解説
化学式はC1(/0)H12O4。カンタリジンは，ツチハンミョウ，マメハンミョウなどの甲虫が分泌する無水酸。人に触れると皮膚内に浸透し，種々の刺激作用を呈し，排出に際して強く尿路を刺激し腎炎を起こすこともある。日本薬局方のカンタリスは0.6％以上のカンタリジンを含み，皮膚刺激剤，発泡剤として用いられる。→関連項目ツチハンミョウ｜マメハンミョウ
株式会社平凡社 百科事典マイペディアについて 情報
化学的特性
Cantharidin is a brown to black powder.
使用
Cantharidin is a natural toxin produced by blister beetles that moderately inhibits protein phosphatases 1 (PP1) (IC50 = 1.7 μM) and PP2A (IC50 = 0.2 μM) and only weakly inhibits the activity of PP2B (IC50 = 1 mM). It has been shown to stimulate cell cycle progression and induce premature mitosis, used topically (0.7%) as an anti-wart treatment, and has been shown to be active in cervical, tongue, neuroblastoma, bone, leukemia, ovarian, colon, and various other cancer cell lines.
適応症
Cantharidin, from the beetle Cantharis vesicatoria, causes intraepidermal vesiculation
and is used in the treatment of warts and other benign cutaneous lesions.
Cantharidin is extremely toxic if taken internally; it should not be prescribed for
at-home use.
Cantharidin (Cantharone), a mitochondrial poison derived from the blister beetle Cantharis vesicatoria, leads to changes in cell membranes, epidermal cell dyshesion, acantholysis, and blister formation and is also useful. Cantharidin can be compounded with salicylic acid and podophyllin resin; occlusion for only 2 hours is needed with this combination. Thick hyperkeratotic lesions should be pared down before painting. The lesion should then be painted with cantharidin, allowed to dry, and covered with Blenderm or other nonporous occlusive tape; 40% salicylic acid plaster may be used to achieve greater activity. The tape is left on for 24 hours or until the area begins to hurt. A blister, often hemorrhagic, will form, break, crust, and fall off in 7 to 14 days; at this time, the lesion is pared down, and any wart remnants are retreated. Because the effect of cantharidin is entirely intraepidermal, no scarring ensues. Ring-like or "donut configuration" recurrences may be seen occasionally after treatment with cantharidin or, at times, following liquid nitrogen therapy. Owing to this agent’s toxicity, application by a physician is recommended. Verrusol, which contains 30% salicylic acid, 5% podophyllin, and 1% cantharidin, may be used in the same manner.
定義
ChEBI: A monoterpenoid with an epoxy-bridged cyclic dicarboxylic anhydride structure secreted by many species of blister beetle, and most notably by the Spanish fly, Lytta vesicatoria. Natural toxin inhibitor of protein phosphatases 1 and 2A.
一般的な説明
Brown to black powder or plates or scales. Formerly used as a counterirritant and vesicant. Used for the removal of warts. Used as an experimental anti tumor agent. Active ingredient in spanish fly, a reputed aphrodisiac.
反応プロフィール
Organic anhydrides, such as Cantharidin, are incompatible with acids, strong oxidizing agents, alcohols, amines, and bases.
危険性
Extremely toxic; questionable carcinogen;
powerful irritant to all cells and tissues; deadly poi-
son; respiratory failure; death.
健康ハザード
Cantharidin is classified as super toxic. Probable oral lethal dose in humans is less than 5 mg/kg or a taste of less than 7 drops for a 70 kg (150 lb.) person. It is very toxic by absorption through skin.
火災危険
When heated to decomposition Cantharidin emits acrid smoke and irritating fumes.
生物活性
Natural toxin inhibitor of protein phosphatases 1 and 2A (K i values are 1.1 and 0.19 μ M respectively); similar to okadaic acid (9,10-Deepithio-9,10-didehydroacanthifolicin ). Displays > 500-fold selectivity over PP2B.
職業ばく露
Formerly used as a counterirritant and
vesicant. Also used for the removal of benign epithelial
growths, e.g., warts. Used as an experimental antitumor
agent. The active ingredient in “Spanish fly,” a reputed
aphrodisia
輸送方法
Cantharidin is not specifically listed in the DOT
Performance-Oriented Packaging Standards with respect
to labeling requirements or restrictions on shipping
quantities.
廃棄物の処理
It is inappropriate and possibly dangerous to the environment to dispose of expired or
waste drugs and pharmaceuticals by flushing them down
the toilet or discarding them to the trash. Household quantities of expired or waste pharmaceuticals may be mixed
with wet cat litter or coffee grounds, double-bagged in
plastic, discard in trash. Larger quantities shall carefully
take into consideration applicable DEA, EPA, and FDA
regulations. If possible return the pharmaceutical to the
manufacturer for proper disposal being careful to properly
label and securely package the material. Alternatively, the
waste pharmaceutical shall be labeled, securely packaged,
and transported by a state licensed medical waste contractor
to dispose by burial in a licensed hazardous or toxic waste
landfill or incinerator.
カンタリジン 上流と下流の製品情報
原材料
Concentrated hydrochloric acid
drum
green tea
二ステアリン酸マグネシウム
Pioneer Blue Natural Rubber Latex Gloves, Size 9
Oils, animal, mixed with vegetable oil Me esters, sulfurized
1H,3H-4,7-Epoxy-3a,7a-(methanothiomethano)isobenzofuran-1,3-dione, tetrahydro-, (3aR,4R,7S,7aS)-rel-
三ケイ酸マグネシウム
3,4-Thiophenedicarboxylic acid, 2,5-dihydro-, dimethyl ester
3,4-Thiophenedicarboxylic acid, 2,5-dihydro-
Thieno[3,4-c]furan-1,3(4H,6H)-dione
3-Thiophenecarboxylic acid, 4-cyanotetrahydro-4-hydroxy-, methyl ester
4-オキソテトラヒドロチオフェン-3-カルボン酸メチル
3-(2-メトキシ-2-オキソエチルチオ)プロピオン酸メチル
フラン
準備製品