Harmine inhibits proliferation and migration of glioblastoma via ERK signalling

Kim, Eunhye; Suh, Jung-Soo; Jang, Yoon-Kwan; Kim, Heonsu; Choi, Gyu-Ho; Kim, Tae-Jin

doi:10.1016/j.procbio.2022.09.014

Cited by 2 publications

(4 citation statements)

References 42 publications

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“…Other β‐carbolines have been shown to affect pathways like PI3 K/Akt and Wnt/β‐catenin, which play crucial roles in cancer cell growth and survival (Li et al., 2017; Tarpley et al., 2021). According to Kim, et al., [79] harmine significantly reduced glioblastoma cells′ proliferative and migratory abilities. Kim, et al [79] .…”

Section: β‐Carbolines’ Anticancer Activity Through Modulation Of Hall...mentioning

confidence: 99%

“…Other β-carbolines have been shown to affect pathways like PI3 K/Akt and Wnt/βcatenin, which play crucial roles in cancer cell growth and survival Tarpley et al, 2021). According to Kim, et al, [79] harmine significantly reduced glioblastoma cells' proliferative and migratory abilities. Kim, et al [79] used cell-based real-time FRET imaging to show that harmine causes a prolonged reduction in ERK signaling but does not affect mTOR, Rac1, or JNK.…”

Section: Inhibition Of Cell Proliferationmentioning

confidence: 99%

“…According to Kim, et al, [79] harmine significantly reduced glioblastoma cells' proliferative and migratory abilities. Kim, et al [79] used cell-based real-time FRET imaging to show that harmine causes a prolonged reduction in ERK signaling but does not affect mTOR, Rac1, or JNK. Harmine prevents EGF-induced ERK signaling, which prevents EGF-induced colony formation and cell proliferation.…”

Section: Inhibition Of Cell Proliferationmentioning

confidence: 99%

“…β-carbolines can influence various signaling pathways involved in cancer progression and proliferation. For example, harmine has been found to inhibit ERK signaling, which is essential for cell proliferation and survival (Kim et al, 2022). Other β-carbolines have been shown to affect pathways like PI3 K/Akt and Wnt/βcatenin, which play crucial roles in cancer cell growth and survival Tarpley et al, 2021).…”

Section: Inhibition Of Cell Proliferationmentioning

confidence: 99%

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Anticancer Potential of β‐Carboline Alkaloids: An Updated Mechanistic Overview

Tshikhudo,

Mabhaudhi,

Koorbanally

et al. 2024

Chemistry & Biodiversity

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This comprehensive review is designed to evaluate the anticancer properties of β‐carbolines derived from medicinal plants, with the ultimate goal of assessing their suitability and potential in cancer treatment, management, and prevention. An exhaustive literature survey was conducted on a wide array of β‐carbolines including, but not limited to, harmaline, harmine, harmicine, harman, harmol, harmalol, pinoline, tetrahydroharmine, tryptoline, cordysinin C, cordysinin D, norharmane, and perlolyrine. Various analytical techniques were employed to identify and screen these compounds, followed by a detailed analysis of their anticancer mechanisms. Natural β‐carbolines such as harmaline and harmine have shown promising inhibitory effects on the growth of cancer cells, as evidenced by multiple in vitro and in vivo studies. Synthetically derived β‐carbolines also displayed noteworthy anticancer, neuroprotective, and cognitive‐enhancing effects. The current body of research emphasizes the potential of β‐carbolines as a unique source of bioactive compounds for cancer treatment. The diverse range of β‐carbolines derived from medicinal plants can offer valuable insights into the development of new therapeutic strategies for cancer management and prevention.

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Section: β‐Carbolines’ Anticancer Activity Through Modulation Of Hall...mentioning

confidence: 99%

Section: Inhibition Of Cell Proliferationmentioning

confidence: 99%

Section: Inhibition Of Cell Proliferationmentioning

confidence: 99%

Section: Inhibition Of Cell Proliferationmentioning

confidence: 99%

See 2 more Smart Citations

Anticancer Potential of β‐Carboline Alkaloids: An Updated Mechanistic Overview

Tshikhudo,

Mabhaudhi,

Koorbanally

et al. 2024

Chemistry & Biodiversity

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Unveiling the antiglioblastoma potential of harmicens, harmine and ferrocene hybrids

Poje,

Šakić,

Marinović

et al. 2024

Acta Pharmaceutica

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The poor prognosis of glioblastoma multiforme, inadequate treatment options, and growing drug resistance urge the need to find new effective agents. Due to the significant anti-cancer potential of harmicens, hybrid compounds which comprise harmine/β-carboline and ferrocene moiety, we investigated their antiglioblastoma potential in vitro and mechanism of action (inhibition of DYRK1A, Hsp90, anti-oxidative activity). The results have shown that triazole-type harmicens, namely 5, with a ferrocene moiety in C-3 position of the β-carboline ring (IC 50 = 3.7 ± 0.1 µmol L−1, SI = 12.6) and 9, the C-6 substituted harmicene (IC 50 = 7.4 ± 0.5 µmol L−1, SI = 5.8) exert remarkable activity and selectivity against human malignant glioblastoma cell line (U251) in vitro. On the other hand, amide-type harmicens 10, 12, and 14 exhibited strong, but non-selective activity, in the low micro-molar range. Mechanistic studies revealed that among active compounds, amide-type harmicens 12 and 14 inhibit DYRK1A and Hsp90 CTD, whereas compound 14 showed pronounced antioxidative activity. Therefore, the antiproliferative activity of harmicens might be a combination of complex molecular interactions.

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Harmine inhibits proliferation and migration of glioblastoma via ERK signalling

Cited by 2 publications

References 42 publications

Anticancer Potential of β‐Carboline Alkaloids: An Updated Mechanistic Overview

Anticancer Potential of β‐Carboline Alkaloids: An Updated Mechanistic Overview

Unveiling the antiglioblastoma potential of harmicens, harmine and ferrocene hybrids

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