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The effects of cantharidin analogues on xanthine oxidase.

Norcantharidin[3], the demethylated product of cantharidin[1] has been used for the treatment of hepatoma, carcinomas of esophagus and gastric cardia, leukopenia and hepatitis. Since the enzyme xanthine oxidase is involved in the diseases mentioned above, and the reactive oxygen species produced by the enzyme induces DNA damage and oxidative damage of tissues, fourteen cantharidin analogues and cantharidimide derivatives were tested for their effects on xanthine oxidase. The results showed that these compounds, listed in Figure 1, displayed very weak inhibitory effects on xanthine oxidase. Con…

Treatment of molluscum contagiosum with cantharidin: a practical approach.

Molluscum contagiosum is very common. In this article we discuss the use of cantharidin as a treatment option for molluscum contagiosum and give detailed information about distribution sources, how to apply it, and caveats regarding its use.Molluscum contagiosum is a common viral disease of childhood caused by a poxvirus, which presents with small, firm, dome-shaped, umbilicated papules. It is generally benign and self-limited, with spontaneous resolution within 6 months to several years. Watchful waiting can often be an appropriate management strategy; however, some patients either desire or …

Cantharidin: a double-edged sword in medicine and toxicology.

Cantharidin (CTD), a natural terpenoid toxin secreted by blister beetles, acts as a potent inhibitor of protein phosphatase. As the principal active component of Mylabris, a traditional Chinese medicine, CTD has attracted considerable interest due to its dual properties, combining potent anti-tumor activity with significant toxicity. Contemporary pharmacological research demonstrates that CTD inhibits the growth and proliferation of diverse cancer cells lines. It exhibits antibacterial and antiparasitic properties, and demonstrates pesticidal activity in agricultural applications. Despite thes…

Topical cantharidin use in dermatology: an updated review.

Cantharidin, a natural toxin produced by the blister beetle, is a topical agent that induces acantholysis of the epidermis, breaking down desmosome plaques through the release of serine proteases. Cantharidin is available in three liquid forms: Ycanth (0.7%), Canthacur (0.7%), and Canthacur PS (1% cantharidin, 30% salicylic acid, 2% podophyllotoxin). Ycanth is used to treat molluscum contagiosum (MC). Canthacur is routinely used to treat a variety of dermatologic conditions including MC, plantar warts, and common warts, whereas Canthacur PS is a more potent formulation indicated for treatment …

Religious objection to cantharidin use in Jain patients.

We report a case of a Jain family that was upset with the use of cantharidin for treatment of molluscum contagiosum for religious reasons.

Кантаридин: ценное обращение с моллюскумом одержимости.

Кантаридин в растворе 0,9% или 0,7% является безопасным и эффективным оргтехникой для моллюска. Она упрощает лечение, особенно детей, посредством быстрой, простой и безболезненной процедуры, однако она должна применяться только врачом.

Совпадение в аннотации оригинала
Cantharidin in either a 0.9% or 0.7% solution is a safe and effective office treatment for molluscum contagiosum. It simplifies the treatment, especially of children, by being a quick, simple, and painless procedure, but it should be applied only by the physician.

Cantharidin Causes Hepatotoxicity by Disrupting GSH-Mediated Redox Homeostasis.

Cantharidin (CTD) possesses potent anticancer activity, whereas its prominent hepatotoxicity severely limits its clinical application. Because the detailed molecular mechanisms responsible for CTD-triggered hepatotoxicity have not been fully elucidated, additional investigations are necessary to uncover its toxicological pathways. This study investigated the mechanism of CTD-triggered hepatotoxicity and the protective effects of exogenous glutathione (GSH) supplementation. In vitro results showed that CTD reduced the GSH/glutathione disulfide (GSSG) ratio and the activities of catalase (CAT) a…

Covalent Binding of Reactive Anhydride of Cantharidin to Biological Amines.

Cantharidin is a terpenoid from coleoptera beetles. Cantharidin has been used to treat molluscum contagiosum and some types of tumors. Cantharidin is highly toxic, and cantharidin poisoning and fatal cases have been reported worldwide. The mechanisms underlying cantharidin-induced toxicity remain unclear. Cantharidin contains anhydride, which may react with biologic amines. This study aimed to examine the chemical reactivity of cantharidin toward nucleophiles and characterize adducts of cantharidin with biologic amines in vitro and in mice. Here two types of conjugates were formed in the incub…

Hepatotoxicity of cantharidin is associated with the altered bile acid metabolism.

Cantharidin (CTD) is an effective antitumor agent. However, it exhibits significant hepatotoxicity, the mechanism of which remains unclear. In this study, biochemical and histopathological analyses complemented with ultra-high-performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS)-based targeted metabolomic analysis of bile acids (BAs) were employed to investigate CTD-induced hepatotoxicity in rats. Sixteen male and female Sprague-Dawley rats were randomly divided into two groups: control and CTD (1.0 mg/kg) groups. Serum and liver samples were collected after 28 days of inte…

Cantharidin-Induced Skin Blister as an In Vivo Model of Inflammation.

The cantharidin-induced skin blister is a simple model for investigating cell migration and inflammatory mediator production at a site of inflammation. Application of cantharidin solution to the ear pinna results in formation of a blister with cell influx and induction of inflammatory mediators at the skin site, as well as local swelling of the ear pinna. The model can be used for investigating anti-inflammatory compounds, such as dexamethasone, and for preclinical drug discovery research, especially in areas where neutrophilic inflammation plays a role in disease pathophysiology. The canthari…

Exploring Cantharidin and its Analogues as Anticancer Agents: A Review.

BACKGROUND: Cantharidin (CTD) is a highly toxic substance which can be used to treat a variety of cancers. However, the clinical application of CTD is restricted due to the serious side effects. In recent years, screening its analogues, exploring the mechanism of action and using combinatory therapy with certain substances are considered to be feasible methods which can reduce side effects and improve the therapeutic activity of CTD. This review aims to describe SAR (structure-activity relationship) of CTD analogues, CTD induction mechanisms, and combinatory therapy exploration. METHODS: We s…

Cantharidin triggers cardiotoxicity via reactive anhydride-mediated covalent protein modification.

Cantharidin (CTD), an anhydride-containing natural product from blister beetles, exhibits potent pharmacological activities in the treatment of molluscum contagiosum and tumors. However, CTD exposure induces multi-organ damage, among which CTD-triggered myocardial cell necrosis and electrophysiological abnormalities represent severe adverse reactions and are the primary causes of fatality. Our recent work revealed that the anhydride moiety of CTD possesses reactivity and can covalently modify proteins via lysine residues. This study investigated the mechanistic role of this covalent modificati…

[Pain-relieving effect of cantharidin blister on lumbar spinal stenosis].

OBJECTIVE: Lumbar spinal stenosis (LSS) is a common cause of chronic lumbar pain and disability. Conventional therapy approaches include analgesics and spinal surgery. Topical cantharidin applications are used for the treatment of severe chronic lumbar pain in traditional European medicine (TEM). We tested the pain-relieving effect of lumbar cantharidin blisters in a non-randomised controlled pilot study. PATIENTS AND METHODS: 28 consecutive patients with manifest LSS were included. The first 20 patients received a cantharidin blister, 8 patients served as controls (waiting list). Pain was as…