• Animal cells and systems
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• v.11 no.2
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• pp.141-146
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• 2007

Cantharidin is produced by blister beetles (Coleoptera: Meloidae) and smaller oedemerid beetles (Coleopetra: Oedemeridae) and is found in hemolymph and various tissues. The function of cantharidin in the courtship behaviour of meloids had never been fully established. Our studies show a correlation between density of cuticular pores and cantharidin titre of the scape and pedicel segments of male specimens of the East African species of Epicauta nyassensis (Haag-Rutenberg, 1880) (Coleoptera: Meloidae). Light microscopy of semi-thin cross sections of the male scape and pedicel indicates that there are many canal shaped structures that stretch from the antennal hemolymph to the antennomere surface. These structures may be tubules, which transport cantharidin circulating in the hemolymph to the surface, where the compound can be released via cuticular pore openings. Analyses of the head capsule and antennal segments of E. nyassensis females which had been copulated with males revealed low titre of cantharidin in the first two antennal segments. The density of the scape and pedicel pores of females was to some extent higher than the density of these pores on flagellum; however it was considerably lower than that of the males. Interestingly, no tubular cell or other transport structures were found in the cross sectioning of the female antennomeres or on the integument surface. During mating, male antennomeres, as well as cantharidin containing pores which are located on the $1^{st}\;and\;2^{nd}$ antennomeres, come into direct contact with the female antennae and may release cantharidin to their surface. Female E. nyassensis may be able to discriminate the opposite sex with abundant reserves of cantharidin prior to mating. This is another evidence that cantharidin function in close range sexual selection.

• Journal of The Korean Society of Clinical Toxicology
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• v.3 no.1
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• pp.56-59
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• 2005

Blister beetles produce cantharidin, which is toxic to people and animals. Cantharidin has been believed to be an aphrodisiac and an abortifacient based on its tendency to cause marked irritation to the genitourinary system leading to priapism in men and pelvic congestion in women for many years. Cantharidin was used by oriental traditional medicine for more than 2000 years. Typical signs related to cantharidin ingestion are gastrointestinal tract and urinary tract irritation, endotoxemia, shock and myocardial dysfunction. Cantharidin is a severe irritant to epithelial linings (gastrointestinal tract, urinary tract, and skin) and develop systemic inflammatory response syndrome. We report a case of corrosive esophagogastritis and acute renal failure by ingestion of cantharidin.

• Asian Pacific Journal of Cancer Prevention
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• v.15 no.24
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• pp.10977-10979
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• 2015

Background: This systematic analysis was conducted to evaluate the efficacy and safety of cantharidin combined with chemotherapy in treating Chinese patients with metastatic colorectal cancer. Methods: Clinical studies evaluating the efficacy and safety of cantharidin combined with chemotherapy on response and safety for Chinese patients with colorectal cancer were identified using a predefined search strategy. Pooled response rate (RR) of treatment were calculated.Results: When cantharidin combined with chemotherapy, 4 clinical studies which included 155 patients with advanced colorectal cancer were considered eligible for inclusion. The systematic analysis suggested that, in all patients, pooled RR was 46.5% (72/155) in cantharidin combined regimens. Major adverse effects were neutropenia, leukopenia, fatigue, and anemia with cantharidin combined treatment; no treatment related deaths occurred. Conclusion: This systematic analysis suggests that cantharidin combined regimens are associated with high response rate and accepted toxicity in treating Chinese patients with metastatic colorectal cancer suggesting that randomized clinical trials are now warranted.

• Asian Pacific Journal of Cancer Prevention
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• v.15 no.20
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• pp.8603-8605
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• 2014

Objective: To assess the safety of Brucea javanica and Cantharidin combined with chemotherapy in treating patients with non-small-cell lung carcinoma. Method: A consecutive cohort of patients with NSCLC were divided into four groups: experimental group A treated with Brucea javanica injection combined with chemotherapy; experimental group B with Cantharidin injection combined with chemotherapy; experimental group C treated with Brucea javanica and Cantharidin injection combined with chemotherapy; and the control group receiving only chemotherapy. After more than two courses of treatment, safety, quality of life and side effects were evaluated. Results: The incidences of myelosuppression in groups A, B and C were lower than that in Control group (p<0.05), but without significant differences among A, B and C. Adverse effects on the gastrointestinal tract also were lower than in controls (p<0.05) without variation amnog the combined treatment groups. Conclusions: Brucea javanica or Cantharidin combined with chemotherapy could in both cases improve quality of life in our cohort of NSCLC patients without any increase in toxicity. However, further clinical experiments should be conducted to evaluate the efficacy of Brucea javanica and Cantharidin combined with chemotherapy for patients with NSCLC.

• Asian Pacific Journal of Cancer Prevention
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• v.13 no.9
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• pp.4773-4776
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• 2012

Objectives: To assess the efficacy, side effects, and the impact on quality of life with $Qinin^{(R)}$ (Cantharidin sodium) injection combined with chemotherapy for gastric cancer patients. Method: A consecutive cohort of 70 patients were divided into two groups: experimental group with cantharidin sodium injection combined with chemotherapy, while the control group received chemotherapy alone. After more than two courses of treatment, efficacy, quality of life and side effects were evaluated. Results: The response rate of experimental group was not significantly different from that of the control group (P>0.05), but differences were significant in clinical benefit response and KPS score. In addition, gastrointestinal reactions and the incidence of leukopenia were lower than in the control group (P<0.05). Conclusions: $Qinin^{(R)}$ (Cantharidin sodium) injection combined with chemotherapy enhances clinical benefit response, improving quality of life of gastric cancer patients and reducing side effects of chemotherapy. Thus $Qinin^{(R)}$ (Cantharidin sodium) injection deserves to be further investigated in randomized control clinical trails.

• Asian Pacific Journal of Cancer Prevention
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• v.15 no.14
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• pp.5597-5600
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• 2014

Objectives: To assess side effects on Cantharidin sodium and Shenmai injection combined with chemotherapy in treating patients with breast cancer postoperatively. Method: Patients with breast cancer receiving postoperative chemotherapy were retrospectively collected, and divided into four groups: group A with cantharidin sodium injection combined with chemotherapy; group B with Shenmai injection combined with chemotherapy; group C with both cantharidin sodium and Shenmai injection combined with chemotherapy; while group D (control group) received chemotherapy alone. All patients were administered docetaxel at a dose of $75mg/m^2$ on day 1, epirubicin hydrochloride at a dose of $60mg/m^2$ on day 1, and cyclophosphamide at a dose of $500mg/m^2$ on day 1 for 3 cycles (repeated at 21 day intervals). After ${\geq}$ three courses of treatment, quality of life and side effects were evaluated. Results: There were a total of 78 patients in this study, and the incidence of leukopenia and gastrointestinal reactions in groups A and B were lower than those in the control group and lowest in group C (p<0.05). Conclusions: Thus cantharidin sodium and Shenmai injection combined with chemotherapy reduce side effects and deserve to be further investigated in randomized clinical control trials.

• Journal of Physiology & Pathology in Korean Medicine
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• v.22 no.2
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• pp.357-364
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• 2008

Mylabris is the dried body of the chinese blister beetle. The species used in medicine are Mylabris phalerata and M. cichorii. In recent studies, it has been found that Mylabris possesses antitumor properties, increases the number of leukocytes, and has irritant effects on the urinary organs. The crude extracts of Mylabris have been noted for their highly irritant action and other traditional uses of Mylabris include treatment of poor local blood circulation. The active constituent of Mylabris is cantharidin. The chemical is notable for its vesicant properties, but with severe side effects such as nephrotoxicity. This experiment examined the effect of extracts and fractions, obtained from Mylabris phalerata Pall. on hair growth activity of the C57BL/6N mice after topical application to skin. First, we examined the effect of an extracts, obtained from the alcohol extracts of dried Mylabris phalerata Pall. on hair growth activity of the C57BL/6N mice after topical application to skin. Second, we examined on hair growth activity of the cantharidin fraction of Mylabris phalerata Pall. compared to the control and 1% minoxidil groups. Third, we investigated the number of hair follicle and mast cells after topical application of extracts of Mylabris phalerata Pall. to skin for 16 days. The results were as follows: Hair growth effect from the extracts of Mylabris phalerata Pall.(0.312%) was observed in 80% of mice whose hair had been removed in 13 days. Hair growth effect from the extract of Mylabris phalerata Pall.(0.312 and 0.625%) and 1% minoxidil group was observed in 100% of mice whose hair had been clipped in 20 days. Hair growth effect from the cantharidin fraction(0.5%) and water fraction(0.5%) of Mylabris phalerata Pall. was observed in 100% of mice whose hair had been clipped in 24 days. The hair growth effect on the cantharidin fraction(0.125%) was observed to be strong compared with the minoxidil(3%) group, commercial hair growth agents, in mice whose hair had been clipped in 19 days. In the spontaneous alopecia mice model, the hair growth effect from the cantharidin fraction (0.125%) was observed to be strong as compared with the states before the 13 days experiment. These experiments suggest that extracts and fractions of Mylabris phalerata Pall. may stimulate the topical hair growth activity in low doses.

• Korean Journal of Crystallography
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• v.13 no.2
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• pp.91-95
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• 2002

The structure of Cantharidin (Hexahydro-3a,7a-dimethy1-4,7-epoxyisobenzofuran-1,3-dione, C/sub 10/H/sub 12/O/sub 4/)has been determined by X-ray diffraction methods. The crystal system is orthorhombic, space group Pna2/sub 1/, unit cell constants, a＝11.0731(9) (equation omitted), b＝6.7344(4) (equation omitted), c＝12.5000(9) (equation omitted), α＝β＝γ＝90°, V＝932.13(12) (equation omitted), T=296K, Z＝4, D/sub c/＝1.398Mgm/sup -3/. The intensity data were collected on an Enraf-Nonius CAD-4 Diffractometer with graphite monochromated MoKα radiation(λ＝0.71073(equation omitted)). The molecular structure was solved by direct methods and refined by full-matrix least squares to a final R＝4.42% for 759 unique observed F/sub o/>4σ(F/sub o/) reflections and 140 parameters.

• Journal of Haehwa Medicine
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• v.6 no.2
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• pp.471-482
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• 1998

• Molecules and Cells
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• v.39 no.12
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• pp.869-876
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• 2016

Cantharidin (CTD) is an active compound isolated from the traditional Chinese medicine blister beetle and displayed anticancer properties against various types of cancer cells. However, little is known about its effect on human chronic myeloid leukemia (CML) cells, including imatinib-resistant CML cells. The objective of this study was to investigate whether CTD could overcome imatinib resistance in imatinib-resistant CML cells and to explore the possible underlying mechanisms associated with the effect. Our results showed that CTD strongly inhibited the growth of both imatinib-sensitive and imatinib-resistant CML cells. CTD induced cell cycle arrest at mitotic phase and triggered DNA damage in CML cells. The ATM/ATR inhibitor CGK733 abrogated CTD-induced mitotic arrest but promoted the cytotoxic effects of CTD. In addition, we demonstrated that CTD downregulated the expression of the BCR-ABL protein and suppressed its downstream signal transduction. Real-time quantitative PCR revealed that CTD inhibited BCR-ABL at transcriptional level. Knockdown of BCR-ABL increased the cell-killing effects of CTD in K562 cells. These findings indicated that CTD overcomes imatinib resistance through depletion of BCR-ABL. Taken together, CTD is an important new candidate agent for CML therapy.