Thalidezine
Thalidezine, a novel AMPK activator, eliminates apoptosis-resistant cancer cells through energy-mediated autophagic cell death, it can inhibit the growth of mouse L1210 cells in vitro. Thalidezine possesses antimicrobial activity against Mycobacterium smegmatis at concentrations of 100 microgram/ml or less.
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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.
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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.
Antibiotics.2022, 11(4), 510.
Front Plant Sci.2017, 8:723
PLoS One.2021, 16(6):e0248479.
Front Microbiol.2022, 13:835463.
Oncol Lett.2020, 20(4):122.
University of Limpopo2016, 1777
Hum Exp Toxicol.2017, 36(11):1169-1176
Sci Rep.2017, 7:40345
Compounds.2023, 3(1), 169-179.
Chemistry of Natural Compounds2018, 204-206
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Yao Xue Xue Bao. 1990;25(5):330-5.
Anti-tumor effect of hernandezine and other components extracted from Thalictrum glandulosissimum。[Pubmed:
2284950]
METHODS AND RESULTS:
The total alkaloids of T. glandulosissimum and its main component hernandezine were found to be effective for treatment of mice bearing P388 leukemia, S180 ascites and C26 colon cancer.
Although hernandezine inhibited the growth of mouse L1210 cells and human oral cancer KB cells in vitro markedly, its inhibitory effect on normal hemopoietic progenitor cells (CFU-GM) in mice was relatively low.
CONCLUSIONS:
Preliminary results showed that hernandezine blocked cell-cycle transfer from G1 to S phase, and its cytocidal action might be cell cycle specific. In addition, two other components, Thalidezine and isoThalidezine, isolated from the same plant exerted similar inhibitory effect on L1210 cells.
Lloydia. 1977 Jul-Aug;40(4):384-94.
Alkaloids of Thalictrum. XXI. Isolation and characterization of alkaloids from the roots of Thalictrum podocarpum.[Pubmed:
331006]
METHODS AND RESULTS:
Thirteen alkaloids, hernandezine, Thalidezine, N-desmethylThalidezine, isoThalidezine, thalistyline, thalistyline methodiiodide, N-desemethylthalistyline, berberine, columbamine, jatrorrhizine, palmatine, thalifendine, magnoflorine and the artifact, 8-trichloromethyldihydroberberine were isolated from the roots of Thalictrum podocarpum Humb. In addition, oxyberberine and thaliglucinone were obtained in very minor amounts and identified by tlc.
CONCLUSIONS:
Of these compounds, N-desmethylThalidezine and isoThalidezine are new bisbenzylisoquinoline alkaloids. Sucrose was isolated from the alcoholic extract. Hernandezine, thalistyline, Thalidezine, thalistyline methodiiodide and N-desmethylthalistyline were found to possess antimicrobial activity against Mycobacterium smegmatis at concentrations of 100 microgram/ml or less.
Oncotarget. 2017 May 2;8(18):30077-30091.
Thalidezine, a novel AMPK activator, eliminates apoptosis-resistant cancer cells through energy-mediated autophagic cell death.[Pubmed:
28404910]
Cancers illustrating resistance towards apoptosis is one of the main factors causing clinical failure of conventional chemotherapy. Innovative therapeutic methods which can overcome the non-apoptotic phenotype are needed.
The AMP-activated protein kinase (AMPK) is the central regulator of cellular energy homeostasis, metabolism, and autophagy.
Our previous study showed that the identified natural AMPK activator is able to overcome apoptosis-resistant cancer via autophagic cell death. Therefore, AMPK is an ideal pharmaceutical target for chemoresistant cancers.
METHODS AND RESULTS:
Here, we unravelled that the bisbenzylisoquinoline alkaloid Thalidezine is a novel direct AMPK activator by using biolayer interferometry analysis and AMPK kinase assays. The quantification of autophagic EGFP-LC3 puncta demonstrated that Thalidezine increased autophagic flux in HeLa cancer cells. In addition, metabolic stress assay confirmed that Thalidezine altered the energy status of our cellular model. Remarkably, Thalidezine-induced autophagic cell death in HeLa or apoptosis-resistant DLD-1 BAX-BAK DKO cancer cells was abolished by addition of autophagy inhibitor (3-MA) and AMPK inhibitor (compound C). The mechanistic role of autophagic cell death in resistant cancer cells was further supported through the genetic removal of autophagic gene7 (Atg7).
CONCLUSIONS:
Overall, Thalidezine is a novel AMPK activator which has great potential to be further developed into a safe and effective intervention for apoptosis- or multidrug-resistant cancers.
