2. Academic Validation
  3. KTt-45, a T-type calcium channel blocker, acts as an anticancer agent by inducing apoptosis on HeLa cervical cancer cell line

KTt-45, a T-type calcium channel blocker, acts as an anticancer agent by inducing apoptosis on HeLa cervical cancer cell line

  • Sci Rep. 2023 Dec 13;13(1):22092. doi: 10.1038/s41598-023-47199-1.
Nguyen Huy Du # 1 2 3 4,  Truong Thi Bich Ngoc # 1 2 3,  Huynh Qui Cang 2 3,  Nguyen Thi Thuy Luyen 3 4 5 6,  Tran Linh Thuoc 2 3,  Tran Le Quan 3 4 5 6,  Dang Thi Phuong Thao 7 8 9
Affiliations

Affiliations

  • 1 Department of Molecular and Environmental Biotechnology, Faculty of Biology and Biotechnology, VNU-HCM, University of Science, 227 Nguyen Van Cu, Ho Chi Minh City, 700000, Vietnam.
  • 2 Laboratory of Cancer Research, VNU-HCM, University of Science, Duong so 4, Linh Trung, Thu Duc, Ho Chi Minh City, 700000, Vietnam.
  • 3 Vietnam National University, Ho Chi Minh City, Vo Truong Toan, Linh Trung, Thu Duc, Ho Chi Minh City, 700000, Vietnam.
  • 4 Central Laboratory of Analysis, VNU-HCM, University of Science, 227 Nguyen Van Cu, Ho Chi Minh City, 700000, Vietnam.
  • 5 Department of Hydro-Geology-Engineering Geology and Environmental Geology, Faculty of Geology, VNU-HCM, University of Science, 227 Nguyen Van Cu, Ho Chi Minh City, 700000, Vietnam.
  • 6 Department of Medicinal Chemistry, Faculty of Chemistry, VNU-HCM, University of Science, 227 Nguyen Van Cu, Ho Chi Minh City, 700000, Vietnam.
  • 7 Department of Molecular and Environmental Biotechnology, Faculty of Biology and Biotechnology, VNU-HCM, University of Science, 227 Nguyen Van Cu, Ho Chi Minh City, 700000, Vietnam. [email protected].
  • 8 Laboratory of Cancer Research, VNU-HCM, University of Science, Duong so 4, Linh Trung, Thu Duc, Ho Chi Minh City, 700000, Vietnam. [email protected].
  • 9 Vietnam National University, Ho Chi Minh City, Vo Truong Toan, Linh Trung, Thu Duc, Ho Chi Minh City, 700000, Vietnam. [email protected].
  • # Contributed equally.
PMID: 38086845 DOI: 10.1038/s41598-023-47199-1
Abstract

The abnormal expression in the T-type calcium channels is involved in various Cancer types, thus inhibiting T-type calcium channels is one of approaches in Cancer treatment. The fact that KTt-45 acted as a T-type calcium channel Inhibitor as well as a pain-relief agent prompts us to address if KTt-45 plays any role against Cancer cells. The results showed that KTt-45 caused cytotoxic effects towards HeLa cervical, Raji lymphoma, MCF-7 breast Cancer, and A549 lung Cancer cell lines with IC50 values less than 100 μM, in which highly selective toxicity was against HeLa cells (IC50 = 37.4 μM, SI > 3.2). Strikingly, the KTt-45 induced an accumulation of cytoplasmic vacuoles after 48 h treatment and mitochondrial-dependent Apoptosis activation as evidenced by morphological features, chromatin condensation, nuclear fragmentation, and significant activation of caspase-9 as well as Caspase-3. In conclusion, KTt-45 could inhibit cell growth and trigger mitochondrial-dependent Apoptosis in HeLa cervical Cancer cells. The results, taken together, strongly demonstrated that KTt-45 is a potential agent for further study on Anticancer drug development which not only targets Cancer cells but also helps to relieve neuropathic pain in Cancer patients.

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