Effects of the Antiulcer Drug Geranylgeranylacetone on Aspirin-Induced Gastric Ulcers in Rats

Murakami, Manabu; Oketani, Kiyoshi; Fujisaki, Hideaki; Wakabayashi, Tsuneo; Ohgo, Toshiharu; Okabe, Susumu

doi:10.1016/s0021-5198(19)52695-6

Cited by 4 publications

(4 citation statements)

References 13 publications

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“…Previous studies have reported that GGA acts as an inducer of Hsp70, which interacts with CHIP to promote protein degradation by polyubiquitination. 5,13 We have confirmed that CHIP could decrease PRMT1 level in HEK293 cells via the ubiquitinationproteasome pathway. 14 Here, we detected the levels of Hsp70 and PRMT1 in GGA-stimulated U-2 OS cells.…”

Section: The Level Of Prmt1 Was Decreased In Ggatreated U-2 Os Cells ...supporting

confidence: 56%

“…Geranylgeranylacetone (GGA) is an oral anti‐ulcer drug with no major adverse effects 4 . Previous studies have shown that GGA acts as an inducer of heat shock protein 70 (Hsp70), which rapidly accumulates in cells after heat stress 5 .…”

Section: Introductionmentioning

confidence: 99%

“…as an inducer of heat shock protein 70 (Hsp70), which rapidly accumulates in cells after heat stress. 5 At the same time, GGA inhibits cell survival and induces apoptosis in multiple types of cancer, such as leukaemia, colon cancer and melanoma. [6][7][8] GGA also exerts antiinvasion effects on ovarian cancer and breast carcinoma cells.…”

mentioning

confidence: 99%

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Geranylgeranylacetone promotes human osteosarcoma cell apoptosis by inducing the degradation of PRMT1 through the E3 ubiquitin ligase CHIP

Jiang

Liao

Liu

et al. 2021

J Cellular Molecular Medi

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Geranylgeranylacetone (GGA), an inducer of heat shock proteins, exerts anticancer activity in some tumours. However, the effect of GGA on human osteosarcoma (OS) has not been reported. This work is designed to evaluate the effect of GGA on the proliferation and apoptosis of human OS cells and to explore the underlying mechanisms. It was found that GGA markedly inhibited the proliferation and induced apoptosis of U‐2 OS cells in a dose‐dependent manner and also up‐regulated the expression of heat shock protein 70 (Hsp70). The degradation and ubiquitination of protein arginine N‐methyltransferase 1 (PRMT1) were obviously enhanced in U‐2 OS cells with CHIP overexpression and GGA treatment. The expression of PRMT1 was reversed in GGA‐treated cell after CHIP knockdown. The turnover of PRMT1 was obviously faster in cells overexpressing CHIP than that in control cells. The methylation and activity of STAT3 were induced by PRMT1, resulting in the inhibition of FAS transcription. Overexpression of PRMT1 reversed the effect of GGA on activation of apoptosis‐related proteins and U‐2 OS cell apoptosis. The expressions of PRMT1 were significantly up‐regulated in OS tissues compared with the adjacent normal tissues and benign bone tumours. In conclusion, GGA promotes the degradation of PRMT1 through the Hsp70‐CHIP‐mediated proteasome pathway, thereby inducing the FAS‐triggered cell apoptosis. Inhibition of PRMT1 may be a potential therapeutic strategy for OS patients.

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Section: The Level Of Prmt1 Was Decreased In Ggatreated U-2 Os Cells ...supporting

confidence: 56%

Section: Introductionmentioning

confidence: 99%

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Geranylgeranylacetone promotes human osteosarcoma cell apoptosis by inducing the degradation of PRMT1 through the E3 ubiquitin ligase CHIP

Jiang

Liao

Liu

et al. 2021

J Cellular Molecular Medi

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“…This involves increasing the number of important macromolecule proteins and phospholipids as a defense factor in gastric mucosa and gastric mucus by enhancing the biosynthesis of glycolipids in microsomes of gastric mucosal cells. Teprenone has been reported to protect against ulcers induced by hydrochloric acid, aspirin, and ethanol, and to improve the poor proliferative capacity of gastric mucosal proliferation cells in hydrocortisone-induced ulcers (Arakawa et al 1988;Murakami et al 1982). It maintained the homeostasis of gastric mucosal proliferation cells to promote the healing of mucosal injury, and enhanced the biosynthesis of prostaglandin E2 in the gastric body and esophageal mucosa of normal rats.…”

Section: Introductionmentioning

confidence: 99%

Enhancement of teprenone isomer separation by subcritical fluid chromatography using porous graphitic carbon column

et al. 2021

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Teprenone is a therapeutic anti-ulcer agent developed in Japan. As described in the Japanese Pharmacopoeia (JP) 17th Edition, gas chromatography/hydrogen flame ionization detection (GC/FID) and high-performance liquid chromatography/ultraviolet detection (HPLC/UV) have been used for the assay of active pharmaceutical ingredients (APIs) and teprenone capsules, respectively. The critical aspect of the assay is a separation of the structural isomers (mono-cis and all-trans) of teprenone. Herein, we propose an improved quantitative method for the quality control of teprenone in APIs and capsules via subcritical fluid chromatography/photo diode array detection (SubFC/PDA) using a porous graphitic carbon column. SubFC conditions, i.e., type and content of the organic modifier in the mobile phase, column temperature, injection volume, and flow rate, were optimized. The developed SubFC/PDA method was validated according to ICH guidelines Q2(R1) in terms of accuracy, precision (repeatability and intermediate precision), specificity, linearity, quantification range, robustness, and stability. Comparison of SubFC/PDA method with the GC/FID or HPLC/UV method (described in JP) revealed that the SubFC/PDA method gave better resolution and run time than the JP methods. The developed SubFC/PDA method is expected to be useful for pharmaceutical analysis or quality control of teprenone isomers.

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Biologically active derivatives of polyprenylacetic acids and related compounds (review)

Serebryakov

Nigmatov

1990

Pharm Chem J

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Effects of the Antiulcer Drug Geranylgeranylacetone on Aspirin-Induced Gastric Ulcers in Rats

Cited by 4 publications

References 13 publications

Geranylgeranylacetone promotes human osteosarcoma cell apoptosis by inducing the degradation of PRMT1 through the E3 ubiquitin ligase CHIP

Geranylgeranylacetone promotes human osteosarcoma cell apoptosis by inducing the degradation of PRMT1 through the E3 ubiquitin ligase CHIP

Enhancement of teprenone isomer separation by subcritical fluid chromatography using porous graphitic carbon column

Biologically active derivatives of polyprenylacetic acids and related compounds (review)

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