|Description:||1. Pteropodine acts as a positive modulator of muscarinic M(1) and 5-HT(2) receptors.|
2. Pteropodine shows antigenotoxic, antioxidant and lymphocyte induction effects.
3. Pteropodine shows strong apoptotic effect on acute leukaemic lymphoblasts.
|Targets:||Calcium Channel | 5-HT Receptor | Bcl-2/Bax|
|Source:||The herbs of Uncaria rhynchophylla|
|Solvent:||Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc.|
|Storage:||Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months(2-8C).
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable for up to two weeks. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
Need more advice on solubility, usage and handling? Please email to: firstname.lastname@example.org
|After receiving:||The packaging of the product may have turned upside down during transportation, resulting in the natural compounds adhering to the neck or cap of the vial. take the vial out of its packaging and gently shake to let the compounds fall to the bottom of the vial. for liquid products, centrifuge at 200-500 RPM to gather the liquid at the bottom of the vial. try to avoid loss or contamination during handling.|
|1 mg||5 mg||10 mg||20 mg||25 mg|
|1 mM||2.7142 mL||13.5711 mL||27.1422 mL||54.2844 mL||67.8555 mL|
|5 mM||0.5428 mL||2.7142 mL||5.4284 mL||10.8569 mL||13.5711 mL|
|10 mM||0.2714 mL||1.3571 mL||2.7142 mL||5.4284 mL||6.7855 mL|
|50 mM||0.0543 mL||0.2714 mL||0.5428 mL||1.0857 mL||1.3571 mL|
|100 mM||0.0271 mL||0.1357 mL||0.2714 mL||0.5428 mL||0.6786 mL|
J Biomed Biotechnol. 2005;2005(3):242-7.
|Genotoxic and cytotoxic studies of beta-sitosterol and pteropodine in mouse.[Pubmed: 16192682 ]|
|Beta-sitosterol (BS) and Pteropodine (PT) are constituents of various plants with pharmacological activities potentially useful to man. The chemicals themselves possess biomedical properties related to the modulation of the immune and the nervous systems, as well as to the inflammatory process. Therefore, safety evaluation of the compounds is necessary in regard to their probable beneficial use in human health. The present study evaluates their genotoxic and cytotoxic potential by determining the capacity of the compounds to induce sister chromatid exchanges (SCE), or to alter cellular proliferation kinetics (CPK) and the mitotic index (MI) in mouse bone marrow cells. Besides, it also determines their capacity to increase the rate of micronucleated polychromatic erythrocytes (MNPE) in peripheral mouse blood, and the relationship polychromatic erythrocytes/normochromatic erythrocytes (PE/NE) as an index of cytotoxicity. For the first assay, four doses of each compound were tested: 200, 400, 600, and 1000 mg/kg in case of BS, and 100, 200, 300, and 600 mg/kg for PT. The results in regard to both agents showed no SCE increase induced by any of the tested doses, as well as no alteration in the CPK, or in the MI. With respect to the second assay, the results obtained with the two agents were also negative for both the MNPE and the PE/NE index along the daily evaluation made for four days. In the present study, the highest tested dose corresponded to 80% of the LD(50) obtained for BS and to 78% in the case of PT. The results obtained establish that the studied agents have neither genotoxic nor cytotoxic effect on the model used, and therefore they encourage studies on their pharmacological properties.|
Eur J Pharmacol. 2002 May 24;444(1-2):39-45.
|Pteropodine and isopteropodine positively modulate the function of rat muscarinic M(1) and 5-HT(2) receptors expressed in Xenopus oocyte.[Pubmed: 12191580]|
|Pteropodine and isoPteropodine are heteroyohimbine-type oxindole alkaloid components of Uncaria tomentosa (Willd.) DC, a Peruvian medicinal plant known as cat's claw. In this study, the effects of these alkaloids on the function of Ca(2+)-activated Cl(-) currents evoked by stimulation of G protein-coupled muscarinic M(1) acetylcholine and 5-HT(2) receptors were studied in Xenopus oocytes in which rat cortex total RNA was translated. Pteropodine and isoPteropodine (1-30 microM) failed to induce membrane current by themselves. However, these alkaloids markedly enhanced the current responses evoked by both acetylcholine and 5-hydroxyhyptamine (5-HT) in a concentration-dependent and reversible manner with the maximal effects at 30 microM. Pteropodine and isoPteropodine produced 2.7- and 3.3-fold increases in the acetylcholine response with EC(50) values of 9.52 and 9.92 microM, respectively, and 2.4- and 2.5-fold increases in the 5-HT response with EC(50) values of 13.5 and 14.5 microM, respectively. In contrast, in oocytes injected with total RNA from the rat cerebellum or spinal cord, neither alkaloid had an effect on the metabotropic current responses mediated by glutamate receptor(1 and 5) (mGlu(1/5)) receptors or ionotropic responses mediated by N-methyl-D-aspartate, kainic acid or glycine. Pteropodine and isoPteropodine (10 microM) significantly reduced the EC(50) values of acetylcholine and 5-HT that elicited current responses, but had no effect on the maximal current responses elicited by acetylcholine and 5-HT. On the other hand, mitraphylline, a stereoisomer of Pteropodine, failed to modulate acetylcholine- and 5-HT-induced responses. These results suggest that Pteropodine and isoPteropodine act as positive modulators of muscarinic M(1) and 5-HT(2) receptors.|
Basic Clin Pharmacol Toxicol. 2009 Mar;104(3):222-7.
|Antigenotoxic, antioxidant and lymphocyte induction effects produced by pteropodine.[Pubmed: 19175366 ]|
|Pteropodine is a heterohimbine-type oxindole alkaloid specifically isolated from 'Cat's claw' (Uncaria tomentosa), a plant that has shown cytostatic, anti-inflammatory and antimutagenic properties and is used in traditional medicine to cure a number of diseases. In this report, we studied the ability of Pteropodine to decrease the rate of sister-chromatid exchanges and micronucleated polychromatic erythrocytes in mice administered doxorubicin. We also determined its capacity to induce lymphocyte production in mice as well as its free radical scavenging potential by applying the DPPH assay. We found Pteropodine (100-600 mg/kg) to significantly decrease the frequency of sister-chromatid exchanges and micronucleated polychromatic erythrocytes in mice administered with 10 mg/kg of doxorubicin. Furthermore, we determined that Pteropodine partially corrected bone marrow cytotoxicity induced by doxorubicin, as it showed an improvement in the rate of polychromatic erythrocytes. Besides, 600 mg/kg of Pteropodine increased 25.8% of the production of lymphocytes over the control value along a 96-hr assay, and it exhibited a strong capacity to trap the DPPH-free radical (98.26% with 250 microg/ml). Our results establish that Pteropodine is an effective antimutagen in the model used, and suggest that Pteropodine deserves further research in the area of cell protective potential and its mechanism of action.|
Br J Haematol. 2006 Mar;132(5):615-22.
|Oxindole alkaloids from Uncaria tomentosa induce apoptosis in proliferating, G0/G1-arrested and bcl-2-expressing acute lymphoblastic leukaemia cells.[Pubmed: 16445836]|
|Natural products are still an untapped source of promising lead compounds for the generation of antineoplastic drugs. Here, we investigated for the first time the antiproliferative and apoptotic effects of highly purified oxindole alkaloids, namely isoPteropodine (A1), Pteropodine (A2), isomitraphylline (A3), uncarine F (A4) and mitraphylline (A5) obtained from Uncaria tomentosa, a South American Rubiaceae, on human lymphoblastic leukaemia T cells (CCRF-CEM-C7H2). Four of the five tested alkaloids inhibited proliferation of acute lymphoblastic leukaemia cells. Furthermore, the antiproliferative effect of the most potent alkaloids Pteropodine (A2) and uncarine F (A4) correlated with induction of apoptosis. After 48 h, 100 micromol/l A2 or A4 increased apoptotic cells by 57%. CEM-C7H2 sublines with tetracycline-regulated expression of bcl-2, p16ink4A or constitutively expressing the cowpox virus protein crm-A were used for further studies of the apoptosis-inducing properties of these alkaloids. Neither overexpression of bcl-2 or crm-A nor cell-cycle arrest in G0/G1 phase by tetracycline-regulated expression of p16INK4A could prevent alkaloid-induced apoptosis. Our results show the strong apoptotic effects of Pteropodine and uncarine F on acute leukaemic lymphoblasts and recommend the alkaloids for further studies in xenograft models.|