Title:Recent Progress in the Hesperetin Delivery Regimes: Significance of Pleiotropic
Actions and Synergistic Anticancer Efficacy
Volume: 29
Issue: 37
Author(s): Parth Malik, Manju Bernela, Mahima Seth, Priya Kaushal and Tapan Kumar Mukherjee*
Affiliation:
- Institute of Biotechnology, Amity University, Kolkata 700156, West Bengal, India
Keywords:
Hesperetin, hesperidin, aglycone derivative, phytochemical, chemotherapeutic drugs, nanocarrier, structure-function correlation.
Abstract:
Background: In the plant kingdom, flavonoids are widely distributed with multifunctional immunomodulatory
actions. Hesperetin (HST) remains one of the well-studied compounds in this domain, initially
perceived in citrus plants as an aglycone derivative of hesperidin (HDN).
Observations: Natural origin, low in vivo toxicity, and pleiotropic functional essence are the foremost fascinations
for HST use as an anticancer drug. However, low aqueous solubility accompanied with a prompt degradation
by intestinal and hepatocellular enzymes impairs HST physiological absorption.
Motivation: Remedies attempted herein comprise the synthesis of derivatives and nanocarrier (NC)-mediated
delivery. As the derivative synthesis aggravates the structural complexity, NC-driven HST delivery has
emerged as a sustainable approach for its sustained release. Recent interest in HST has been due to its significant
anticancer potential, characterized via inhibited cell division (proliferation), new blood vessel formation
(angiogenesis), forceful occupation of neighboring cell’s space (invasion), migration to erstwhile physiological
locations (metastasis) and apoptotic induction. The sensitization of chemotherapeutic drugs (CDs) by HST
is driven via stoichiometrically regulated synergistic actions.
Purpose and Conclusion: This article sheds light on HST structure-function correlation and pleiotropic anticancer
mechanisms, in unaided and NC-administered delivery in singular and with CDs synergy. The discussion
could streamline the HST usefulness and long-term anticancer efficacy.