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Targeting Hyperlipidemia: Investigating the Regulatory Roles of NPC1L1 and SREBP-2 and the Therapeutic Potential of

Suresh Kumar Dev1, Rajnish Srivastava2, Aruna Sharma2

  • 1Venkateshwara Institute of Pharmacy, Sai Tirupati University, Udaipur, Rajasthan, India.

Cardiovascular & Hematological Disorders Drug Targets
|May 15, 2026
PubMed
Abstract

Insights

Phytomedicines offer a natural approach to managing hyperlipidemia by inhibiting cholesterol absorption and synthesis. These plant-based compounds also enhance cholesterol excretion, providing an alternative to conventional drugs for cardiovascular health.

Area of Science:

  • Pharmacology and Phytomedicine
  • Cardiovascular Disease Research
  • Lipid Metabolism

Background:

  • Hypercholesterolemia, a prevalent form of dyslipidemia, significantly contributes to cardiovascular disease.
  • The global incidence of dyslipidemias has steadily increased over the last three decades.

Purpose of the Study:

  • To review the scientific evidence on the role of phytomedicine in managing hyperlipidemia.
  • To synthesize information on plant-based bioactives affecting cholesterol metabolism, focusing on mechanisms and efficacy.

Main Methods:

  • A comprehensive literature review was conducted using Google Scholar and PubMed.
  • Keywords included "Herbs, Medicinal plants, Bioactives, Dyslipidemia, Hyperlipidemia, lipid metabolism, NPC1L1, SREBP-2."
  • Studies published between 2000 and 2025, focusing on regulatory roles of NPC1L1 and SREBP-2, were included.

Main Results:

  • Plant-based bioactives modulate lipid levels through transcription factors like LXR, SREBP, PPARα, and PPARγ.
  • Key molecules in these pathways include NPC1L1, HMGCR, PCSK9, and CYP7A1, influencing cholesterol homeostasis.
  • Bioactives affect cholesterol uptake, esterification, synthesis, and excretion.

Conclusions:

  • Lipid-lowering agents are crucial for preventing atherosclerosis, coronary heart disease, and metabolic syndrome.
  • Herbal medicine presents a viable alternative or complementary approach to synthetic drugs for hyperlipidemia treatment.
  • Plant-derived compounds effectively inhibit intestinal cholesterol absorption, reduce hepatic cholesterol synthesis, and promote cholesterol excretion.
Keywords:
Herbalatherosclerosiscardiovascular disease.coronary heart diseasedyslipidemiaenterocyteshypercholesterolaemialipidplasma

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