Taspine is the Cicatrizant Principle in Sangre de Grado Extracted from Croton lechleri *

Planta Medica (Impact Factor: 2.15). 05/1989; 55(2):140-3. DOI: 10.1055/s-2006-961907
Source: PubMed


Sangre de Grado extract used by Peruvian natives as a cicatrizant agent, was collected from trees of the species Croton lechleri growing in the Peruvian jungle. The Sangre de Grado was found to contain one alkaloid identified as taspine and which was shown to be the active cicatrizant principle by an in vivo test in mice. This alkaloid exhibited a dose-related cicatrizant effect and an ED50 of 0.375 mg/kg. Experiments with taspine hydrochloride in order to study its mechanism of action in cell culture systems showed that the alkaloid was non-toxic to human foreskin fibroblasts at concentrations below 150 ng/ml and that it had no effect on cell proliferation. On the other hand, taspine hydrochloride was found to increase the migration of human foreskin fibroblasts. This effect on the migration of fibroblasts is probably the mechanism by which Sangre de Grado and taspine hydrochloride accelerate the wound healing process. Using the two-stage mouse skin carcinogenesis system, we have been able to show that neither Sangre de Grado nor taspine hydrochloride had carcinogenic or tumour promoter activity after 17 months of treatment.

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    • "Arg. (Vaisberg et al., 1989). Based on these results taspine could be one of the compound responsible for the AChE inhibition of the extract since it was already described as a strong inhibitor of AChE when investigated in a Magnolia species (Rollinger et al., 2006). "

    Full-text · Conference Paper · Aug 2014
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    • "Despite of some reports that several compounds can be found in the dragon's blood sap (Cai et al., 1993a,b), it has been reported that the bark sap contains fundamentally the alkaloid, Taspine (Bettolo and Scarpati, 1979), and the lignin 3′4′-O-dimethylcedru- sin, which has been claimed to be the active principles responsible for the anti-inflammatory and wound healing activities (Perdue et al., 1979; Vaisberg et al., 1989; Pieters et al., 1993). The complete chemical constituents present in dragon's blood from several sources can be found in a review of Gupta et al. (2008). "
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    ABSTRACT: Ethnopharmacological relevance: Dragon's blood is a dark-red sap produced by species from the genus Croton (Euphorbiaceae), which has been used as a famous traditional medicine since ancient times in many countries, with scarce data about its safe use in humans. In this research, we studied genotoxicity and clastogenicity of Croton palanostigma sap using the comet assay and micronucleus test in cells of mice submitted to acute treatment. Material and methods: HPLC analysis was performed to identify the main components of the sap. The sap was administered by oral gavage at doses of 300 mg/kg, 1,000 mg/kg and 2,000 mg/kg. For the analysis, the comet assay was performed on the leukocytes and liver cells collected 24h after treatment, and the micronucleus test (MN) on bone marrow cells. Cytotoxicity was assessed by scoring 200 consecutive polychromatic (PCE) and normochromatic (NCE) erythrocytes (PCE/NCE ratio). Results and conclusion: The alkaloid taspine was the main compound indentified in the crude sap of Croton palanostigma. The results of the genotoxicity assessment show that all sap doses tested produced genotoxic effects in leukocytes and liver cells and also produced clastogenic/aneugenic effects in bone marrow cells of mice at the two higher doses tested. The PCE/NCE ratio indicated no cytotoxicity. The data obtained suggest caution in the use of Croton palanostigma sap by humans considering its risk of carcinogenesis.
    Full-text · Article · Mar 2013 · Journal of ethnopharmacology
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    • "Croton lechleri has been evaluated in cell lines such as KB, V-79, K562 and HeLa for anticancer activity showing low activity (Alfonso-Castro et al., 2012; Chen et al., 1994; Itokawa et al., 1991; Rossi et al., 2003; Vaisberg et al., 1989). This activity was mainly ascribed to the presence of the alkaloid taspine (Fig. 1) which has also been reported as the active compound with wound healing properties (Porras-Reyes et al., 1993; Vaisberg et al., 1989). Taspine is the main alkaloid which characterizes Croton lechleri sap, but it is also present in Leontice eversmanii Bge (Berberidaceae), Caulophyllum thalictroides (L.) Michx. "
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    ABSTRACT: Ethnopharmacological relevance: Croton lechleri Mull. Arg. (Euphorbiaceae) is a traditional medicinal plant which produces a red sap, traditionally known as "Sangre de Drago"; it is used in folk medicine externally for wounds, fractures, and haemorrhoids, internally for intestinal and stomach ulcers and also for the empirical cure of cancers. Materials and methods: We investigated the effects of Croton lechleri sap and taspine in comparison with taxol and vinblastine on the growth of human cancer cell lines of SK23 (melanoma), LoVo and HT29 (colorectal cancer) using MTT and Trypan blue assays. Further, we studied cell cycle by flow cytometry and detected acetylated-α-tubulin by confocal microscope. Results: Croton lechleri inhibited cell proliferation starting from 1 μg/mL in SK23 cells, whereas 10 times higher concentrations were required for growth inhibition of HT-29 and LoVo cell lines. Also taspine (0.1 μg/mL) inhibited the SK23 and HT29 cell proliferation. Further, assay was assessed on SK23 and HT29 cell lines with 24-48 h treatment with sap and taspine. Both sap and taspine inhibited cancer cell proliferation; taspine showed higher activity on SK23 cells, which was significantly increased after 48 h of SK23 treatment. Using confocal microscopy we observed that Croton lechleri (1 μg/mL) caused a loss of microtubule structure, whereas taspine (0.5 μg/mL) caused an increase in acetylated α-tubulin and a modification of cellular morphology, mainly in SK23 cells. Croton lechleri sap 10 and 50 μg/mL influence cell cycle; 50 μg/mL sap caused a dramatic reduction of cells in G(1)/G(0) and S phases with a great increase of subG(0) cells. Conclusions: The data showed that Croton lechleri and taspine could inhibit cell proliferation with higher potency against melanoma SK23 cells, supporting the empirical use of the sap as anticancer in ethnomedicine and taspine as a possible anticancer agent.
    Full-text · Article · Oct 2012 · Journal of ethnopharmacology
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