Statins—From Fungi to Pharmacy: A Comprehensive Review of Natural and Synthetic Statins

Summary

This research traces the remarkable journey of statins from their discovery in fungi to their development as essential medicines for treating high cholesterol. These medications, which began as natural compounds produced by various fungi, have evolved into both natural and synthetic versions that help millions of people manage their cardiovascular health. The study explains how these drugs work, their benefits, and potential side effects. Impacts on everyday life: • Provides safe and effective treatment options for people with high cholesterol • Helps prevent heart attacks and strokes in at-risk populations • Demonstrates how natural compounds from fungi can be developed into life-saving medicines • Offers multiple medication options allowing doctors to personalize treatment based on individual patient needs • Shows the importance of continuing research into natural sources for new drug development

Background

Statins are a class of cholesterol-lowering medications that originated from fungal sources. The first statin, compactin (mevastatin), was discovered by Akira Endo and colleagues at Sankyo pharmaceutical company in Japan through screening of fungal metabolites. Natural statins are produced through fermentation of fungi like Monascus spp., Penicillium spp., Aspergillus terreus, and Pleurotus ostreatus.

Objective

This review aims to describe the processes of obtaining natural fungal statins, provide detailed information on the pharmacokinetics and pleiotropic properties of both natural and synthetic statins, and examine their side effects and drug interactions. The paper focuses on tracing the evolution from fungal-derived compounds to modern synthetic statins while comparing their properties and clinical applications.

Results

The review found that statins can be categorized as natural (fungal-derived), semi-synthetic derivatives, or fully synthetic compounds. Natural statins like lovastatin and compactin share a hexahydro-naphthalene structure, while synthetic statins have different ring structures but maintain the HMG-CoA-like moiety responsible for enzyme inhibition. All statins effectively reduce LDL cholesterol but differ in their pharmacokinetic properties, potency, and pleiotropic effects. The review documented various beneficial effects beyond cholesterol reduction, including anti-inflammatory, antithrombotic, and potential neuroprotective properties.

Conclusion

Statins represent a crucial class of medications for treating dyslipidemia and hypercholesterolemia, with their development spanning from fungal metabolites to synthetic compounds. While sharing the common mechanism of HMG-CoA reductase inhibition, different statins exhibit varying pharmacokinetic parameters, potencies, and pleiotropic effects. Understanding these differences is essential for optimal clinical application. Ongoing research continues to explore the extensive biological effects of fungal sources to discover novel therapeutic alternatives.
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