| Description: |
Proscillaridin A is a cardiac glycoside, it has anticancer, analgesic effects and immunoreactivities. Proscillaridin A induces apoptosis in MDA-MB-231 cells by increasing free calcium concentration and by activating caspase-3. It exerts anti-tumor effects through GSK3β activation and alteration of microtubule dynamics in glioblastoma. |
| Targets: |
GSK3β | Topoisomerase | Caspase | STAT3 | JNK | TrxR1 | JNK | PARP | Src | eIF2α | ATPase | Bcl-2/Bax | Sodium Channel | Potassium Channel | DNA |
| In vitro: |
| Biological & Pharmaceutical Bulletin, 2008, 31(6):1131-1140. | | Antiproliferative Activity of Derivatives of Ouabain, Digoxin and Proscillaridin A in Human MCF7 and MDA-MB-231 Breast Cancer Cells.[Reference: WebLink] | Three derivatives of ouabain, digoxin and proscillaridin A containing the carboxylic group instead of the lactone moiety were synthesized and examined for cytotoxicity in human breast cancer cells.
METHODS AND RESULTS:
Evaluation of the cytotoxicity of these compounds employing an MTT assay and inhibition of [3H]thymidine incorporation into DNA in both MCF-7 and MDA-MB-231 breast cancer cells demonstrated that compound 3, the most active of the series, proved to be only slightly less potent than proscillaridin A. We evaluated the effects of these compounds 1-3 on change in intracellular Ca2+, appearance of apoptosis, inhibition of DNA topoisomerase I and II, and the activity of caspase-3 in breast cancer cells. These studies indicate that the increase in potency for 3 may be related, in part, to an activation of caspase-3, increasing free calcium concentration and topoisomerase II inhibition.
CONCLUSIONS:
All these data emphasize the potential usefulness of these derivatives of cardiac glycosides as anticancer agents. | | Clinical and Experimental Hypertension, 1998, 20(5-6):593-599. | | Proscillaridin A Immunoreactivity: Its Purification, Transport in Blood By A Specific Binding Protein And Its Correlation With Blood Pressure.[Reference: WebLink] |
METHODS AND RESULTS:
A material crossreacting with antibodies against the bufadienolide proscillaridin A and inhibiting the sodium pump was found in human blood plasma. The concentration of the material with a retention time similar to ouabain in a reversed phase HPLC correlated to systolic blood pressure and pulse pressure. Affinity purification of this compound from bovine adrenals resulted in the isolation of a compound with molecular mass of 600 Da that was not identical with ouabain.
CONCLUSIONS:
Consistent with the postulate that endogenous ouabain and proscillaridin A immunoreactivities may belong to a new class of cardiotonic steroid hormones, a protein of Mr = 60 kDa has been found in bovine serum by affinity-labeling with N-hydroxysuccimidyl digoxigenin-3-O-methylcarbonyl-epsilon-aminocaproate. |
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| In vivo: |
| Digest Journal of Nanomaterials & Biostructures, 2010, 5(2):457-465. | | Analgesic effects of scilliroside, proscillaridin-a and taxifolin from squill bulb (Urginea maritima) on pains.[Reference: WebLink] | The aim of the present study was to assess the clinical efficacy of proscillaridin A (C30H42O8), taxifolin (C15H12O7) and scilliroside ( C32H44O12 ) and safety of squill bulb (Urginea maritima) (L.) Baker extract on various pains of spontaneous volunteer patients.
METHODS AND RESULTS:
In this study, 250 patients were monitored in coats. The average age of these patients were between 40 and 74 years old. Of these 100 were male and 150 female patients. Also, 60 % of proscillaridin-A (C30H42O8), taxifolin (C15H12O7) and scilliroside ( C32H44O12 ) solution in pure glycerin was applied as external on the pain area.ASO, CRP and RF higher values of patiens were significantly decreased ( p < 0.05 and p < 0.01). Knee, joint, calf, hip, shoulder, upper back, low back (lumbago), tailbone and fibromyalgia paints of patients were significantly reduced (p < 0.05 and p < 0.01).
CONCLUSIONS:
Squill bulb constituents can reduce the musculoskeletal pains. |
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