An overview on the biological activity and anti-cancer mechanism of lovastatin

Xie, Liguo; Zhu, Guodong; Shang, Junjie; Zhang, Chun‐Ting; Ji, Xiuling; Zhang, Qi; Wei, Yunlin

doi:10.1016/j.cellsig.2021.110122

Cited by 33 publications

(30 citation statements)

References 81 publications

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“…This could be ascribed to the higher viscosity of formulation A, which could have allowed for more intimate contact with cells. Statins are reported to enhance apoptosis through the activation of the caspase-3 enzyme and the inhibition of geranylgeranyl pyrophosphate (GGPP) biosynthesis, leading to the inhibition of the prenylation of small G-proteins [44]. These findings explain the cytotoxic ability of statins [45].…”

Section: In Vitro Cell Viability and Caspase-3 Enzyme Assaymentioning

confidence: 99%

Repurposing Lovastatin Cytotoxicity against the Tongue Carcinoma HSC3 Cell Line Using a Eucalyptus Oil-Based Nanoemulgel Carrier

Rizg

Hosny

Mahmoud³

et al. 2022

Gels

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Tongue cancer is one of the most common carcinomas of the head and neck region. The antitumor activities of statins, including lovastatin (LV), and the essential oil of eucalyptus (Eu oil), have been adequately reported. The aim of this study was to develop a nanoemulgel containing LV combined with Eu oil that could then be made into a nanoemulsion and assessed to determine its cytotoxicity against the cell line human chondrosarcoma-3 (HSC3) of carcinoma of the tongue. An I-optimal coordinate-exchange quadratic mixture design was adopted to optimize the investigated nanoemulsions. The droplet size and stability index of the developed formulations were measured to show characteristics of the nanoemulsions. The optimized LV loaded self-nanoemulsifying drug delivery system (LV-Eu-SNEDDS) was loaded into the gelling agent Carbopol 934 to develop the nanoemulgel and evaluated for its rheological properties. The cytotoxic efficiency of the optimized LV-Eu-SNEDDS loaded nanoemulgel was tested for cell viability, and the caspase-3 enzyme test was used against the HSC3 cell line of squamous carcinoma of the tongue. The optimized nanoemulsion had a droplet size of 85 nm and a stability index of 93%. The manufactured nanoemulgel loaded with the optimum LV-Eu-SNEDDS exhibited pseudoplastic flow with thixotropic behavior. The developed optimum LV-Eu-SNEDDS‒loaded nanoemulgel had the best half-maximal inhibitory concentration (IC50) and caspase-3 enzyme values of the formulations developed for this study, and these features improved the ability of the nanoemulsion-loaded gel to deliver the drug to the investigated target cells. In addition, the in vitro cell viability studies revealed the synergistic effect between LV and Eu oil in the treatment of tongue cancer. These findings illustrated that the LV-Eu-SNEDDS-loaded gel formulation could be beneficial in the local treatment of tongue cancer.

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Section: In Vitro Cell Viability and Caspase-3 Enzyme Assaymentioning

confidence: 99%

Repurposing Lovastatin Cytotoxicity against the Tongue Carcinoma HSC3 Cell Line Using a Eucalyptus Oil-Based Nanoemulgel Carrier

Rizg

Hosny

Mahmoud³

et al. 2022

Gels

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“…Higher LDL cholesterol concentration can cause the formation of foam cells, which further leads to plaque accumulation and atherosclerosis. Atherosclerosis is considered the most important contributing factor of cardiovascular diseases [20].…”

Section: Hypercholesterolemia Treatmentmentioning

confidence: 99%

Production of Lovastatin and its Lipid-lowering and Anti-Cancer Effects

Du¹,

Liu²,

Zheng³

2022

HSET

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Lovastatin is traditionally used to reduce the amount of cholesterol and lipid levels in many diseases, but its anti-cancer properties are now discovered. By regulating and modulating crucial signaling small G-proteins of cancer cell including Rho, Rac, and Ras, lovastatin can alter cancer cell division, migration, and induce cell death. Lovastatin has a similar structure to HMG-CoA and thus can competitively bind to HMG-CoA reductase (HMGR) and work as a hypolipidemic medicine. The anti-cancer effect of lovastatin had led to extensive research. It had been confirmed based on many in-vitro studies that lovastatin had obvious inhibitory effects on different kinds of cancer. In addition, lovastatin can increase therapeutic effect since it regulates the cell signaling pathway which induces cell cycle arrests. This article covers the application of lovastatin and cancer treatment. Lovastatin has shown promising anti-cancer properties in breast cancers, ovarian cancers and breast cancers, but more evidence is needed to determine its anti-cancer properties in-vivo and in humans.

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“…The predominant enzyme targeted for controlling the cholesterol level is 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, the rate-limiting and regulatory enzyme in cholesterol biosynthesis. The group of compounds that inhibit the enzyme HMG-CoA reductase is the statin group of molecules 1,3 .…”

Section: Introductionmentioning

confidence: 99%

“…It is involved in the inhibition of cholesterol biosynthesis. Lovastatin also works as an in vivo competitive inhibitor of HMG-CoA reductase for humans and animals as well as in plants and is hence used to treat hypercholesterolemia 1,[3][4][5][6][7][8] . Lovastatin is available in the lactone form but converted to β-hydroxy acid invivo, the active state.…”

Section: Introductionmentioning

confidence: 99%

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Production of Lovastatin using Liquid Cheese Whey by Fusarium nectrioides (MH173849), an Endophytic Fungi Isolated from Euphorbia hirta

Manogaran¹,

Kannan²,

Narayanan³

et al. 2022

J. Pure Appl. Microbiol.

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Lovastatin is a naturally produced 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase enzyme inhibitor- used for treating hypercholesterolemia. It was the first statin drug which was approved by the United States Food and Drug Administration (USFDA). In the current study, endophytic fungus Fusarium nectrioides (MH173849) isolated from Euphorbia hirta L. was used for the production of lovastatin. Four different culture media indicated as M1, M2, M3 and M4 were used for the initial production of lovastatin. Liquid cheese whey was used as nitrogen source. Growth morphology of fungi was investigated using Scanning Electron Microscopy analysis. Also, parameters like temperature, pH, inoculum size, incubation time, and RPM were optimized for the obtaining highest lovastatin production. Among the four media, M4 was found to produce the maximum concentration of lovastatin. Parameters such as temperature of 28°C, pH 6, RPM – 180 rpm and inoculum size of 5 x107 spores/mL were optimal for the production of lovastatin by F. nectrioides (MH173849).

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An overview on the biological activity and anti-cancer mechanism of lovastatin

Cited by 33 publications

References 81 publications

Repurposing Lovastatin Cytotoxicity against the Tongue Carcinoma HSC3 Cell Line Using a Eucalyptus Oil-Based Nanoemulgel Carrier

Repurposing Lovastatin Cytotoxicity against the Tongue Carcinoma HSC3 Cell Line Using a Eucalyptus Oil-Based Nanoemulgel Carrier

Production of Lovastatin and its Lipid-lowering and Anti-Cancer Effects

Production of Lovastatin using Liquid Cheese Whey by Fusarium nectrioides (MH173849), an Endophytic Fungi Isolated from Euphorbia hirta

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