Bioavailability challenges associated with development of anti-cancer phenolics
Open accessAbstract
Phenolics including many polyphenols and flavonoids have the potentials to become chemoprevention and chemotherapy agents. However, poor bioavailability limits their biological effects in vivo. This paper reviews the factors that affect phenolics absorption and their bioavailabilities from the points of view of their physicochemical properties and disposition in the gastrointestinal tract. The up-to-date research data suggested that solubility and metabolism are the primary reasons that limit phenolic aglycones' bioavailability although stability and poor permeation may also contribute to the poor bioavailabilities of the glycosides. Future investigations should further optimize phenolics' bioavailabilities and realize their chemopreventive and chemotherapeutic effects in vivo.
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It has been proposed that higher molecular weight compounds such as polyphenols are not dissolved well in water.
“It has been proposed that higher molecular weight compounds (such as polyphenols) were not dissolved well in water (263).”
From Phytogenic Additives Can Modulate Rumen Microbiome to Mediate Fermentation Kinetics and Methanogenesis Through Exploiting Diet–Microbe Interaction (2020) · cites this paper as [263]
Section 2.3 reports poor water solubility for some phenolics, including ellagic acid and potentially lignans. It does not say that higher molecular weight makes polyphenols poorly soluble in water; indeed, it says water solubility is usually not a major impediment for flavonoids. (LLM, conf=0.85)
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References 118 · Cited by 242
Research works printed but not linked: 3
- [20]Decker EA Phenolics: prooxidants or antioxidants? Nutr Rev 1997 55 11 Pt 1 396 8 9420450
- [25]Edward H Kerns LD Drug-like Properties: Concepts, Structure Design and Methods for ADME to Toxicity Optimization 2008 56 Elsevier Inc
- [35]Lamblin F Hano C Fliniaux O Mesnard F Fliniaux MA Laine E [Interest of lignans in prevention and treatment of cancers]. Med Sci (Paris) 2008 24 5 511 9 18466729
- Authors
- Gao, S., & Hu, M.
- Affiliations
- University of Houston (US)
- Corresponding author
- Hu, M.
- ORCID
- Hu, M.
- Venue
- Mini-Reviews in Medicinal Chemistry
- Publisher
- Bentham Science Publishers Ltd.
- Published
- 2010-06-01
- Volume
- 10
- Issue
- 6
- Pages
- 550-567
- ISSN
- 1389-5575 (ISSN-L)
- PMC
- PMC2919492
- OpenAlex
- W1967833615
- Cited by
- 242
- References
- 118
- Citations by year
- 2026: 11 · 2025: 18 · 2024: 23 · 2023: 22 · 2022: 15 · 2021: 21 · 2020: 21 · 2019: 16 · 2018: 16 · 2017: 14 · 2016: 10 · 2015: 16 · 2014: 12 · 2013: 12 · 2012: 8
- FWCI
- 5.53
- Type
- journal article
- Language
- en
- Open access
- green
- www.ncbi.nlm.nih.gov
- Locations
- Mini-Reviews in Medicinal Chemistry (publishedVersion)
- PubMed (publishedVersion)
- PubMed Central (acceptedVersion)
- Funders
- National Institute of General Medical Sciences (R01GM070737, GM 070737)
- Topics
- Health Sciences › Medicine › Biochemistry › Phytochemicals and Antioxidant Activities
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Drug Solubulity and Delivery Systems
- Health Sciences › Medicine › Pharmacology › Flavonoids in Medical Research
- Keywords
- phenolic compounds, bioavailability, polyphenols, flavonoids, gastrointestinal absorption, solubility, metabolism, chemoprevention, anticancer agents
- MeSH terms
- Animals, Antineoplastic Agents, Biological Availability, Clinical Trials as Topic, Flavonoids, Humans, Neoplasms, Phenols, Anticarcinogenic Agents, Rats, Polyphenols
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