16625-69-7
Chemical Structure
Boldine hydrochloride
- CAS No.: 16625-69-7
- Formula:C19H22ClNO4
- Molecular Weight:363.84
IUPAC Name: (S)-1,10-dimethoxy-6-methyl-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinoline-2,9-diol hydrochloride
InChIKey: MUGNKMCHLPQCMV-ZOWNYOTGSA-N
SMILES: OC1=C(OC)C2=C3C(CCN(C)[C@@]3([H])CC4=CC(O)=C(OC)C=C24)=C1.Cl
Biological Activity: Boldine hydrochloride is an aporphine alkaloid telomerase (telomerase) inhibitor (IC50 of 0.17 μM for TERT) and a pannexin/connexin hemichannel blocker, with oral activity and blood-brain barrier permeability. Boldine hydrochloride inhibits telomerase activity through direct interaction with the telomerase ribonucleoprotein and non-competitive binding near the TERT active site, and downregulates hTERT mRNA while shifting alternative splicing toward non-functional transcripts. Boldine hydrochloride blocks Panx1, Cx43, Cx26, and Cx30 hemichannels as well as P2X7 receptor-mediated calcium influx. Boldine hydrochloride exhibits antioxidant, anti-inflammatory, antiproliferative, and cytotoxic activities by scavenging ROS, inhibiting NFκB, dephosphorylating SGK1, and reducing TNF-alpha levels. Boldine hydrochloride can be used in research on breast cancer, Alzheimer's disease, glioblastoma, diabetes, and spinal cord injury[1][2][3][4][5][6][7][8].
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Boldine hydrochloride | Boldine hydrochloride is an aporphine alkaloid telomerase (telomerase) inhibitor (IC50 of 0.17 μM for TERT) and a pannexin/connexin hemichannel blocker, with oral activity and blood-brain barrier permeability. Boldine hydrochloride inhibits telomerase activity through direct interaction with the telomerase ribonucleoprotein and non-competitive binding near the TERT active site, and downregulates hTERT mRNA while shifting alternative splicing toward non-functional transcripts. Boldine hydrochloride blocks Panx1, Cx43, Cx26, and Cx30 hemichannels as well as P2X7 receptor-mediated calcium influx. Boldine hydrochloride exhibits antioxidant, anti-inflammatory, antiproliferative, and cytotoxic activities by scavenging ROS, inhibiting NFκB, dephosphorylating SGK1, and reducing TNF-alpha levels. Boldine hydrochloride can be used in research on breast cancer, Alzheimer's disease, glioblastoma, diabetes, and spinal cord injury. | |||||||||||||||||||||
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References
- [1]. Kazemi Noureini S, et al. Boldine, a natural aporphine alkaloid, inhibits telomerase at non-toxic concentrations. Chemico-biological interactions. 2015 Apr 25;231:27-34.
- [2]. Catalán M, et al. Boldine prevents the inflammatory response of cardiac fibroblasts induced by SGK1-NFκB signaling pathway activation. Cellular signalling. 2024 Aug;120:111241. [Content Brief]
- [3]. Yi C, et al. Inhibition of glial hemichannels by boldine treatment reduces neuronal suffering in a murine model of Alzheimer's disease. Glia. 2017 Oct;65(10):1607-1625. [Content Brief]
- [4]. Jiménez-Madrona E, et al. Antiproliferative effect of boldine on neural progenitor cells and on glioblastoma cells. Frontiers in neuroscience. 2023;17:1211467.
- [5]. Kazemi Noureini S, et al. Telomerase Inhibition by a New Synthetic Derivative of the Aporphine Alkaloid Boldine. International journal of molecular sciences. 2018 Apr 19;19(4):1239.
- [6]. Jang YY, et al. Protective effect of boldine on oxidative mitochondrial damage in streptozotocin-induced diabetic rats. Pharmacological research. 2000 Oct;42(4):361-71.
- [7]. Asencio M, et al. Biochemical and behavioral effects of boldine and glaucine on dopamine systems. Pharmacology, biochemistry, and behavior. 1999 Jan;62(1):7-13.
- [8]. Toro CA, et al. Boldine modulates glial transcription and functional recovery in a murine model of contusion spinal cord injury. Frontiers in cellular neuroscience. 2023;17:1163436.
