Intestinal absorption mechanism of rotundic acid: Involvement of P-gp and OATP2B1

Hong, Shang; Sun, Yinghui; Wang, Ze; Zhou, Ying; Yang, Huajiao; Ci, Xiaoyan; Cui, Tao; Xia, Yuanyuan; Gu, Yuan; Mao-liang, Liao; Li, Quansheng; Si, Duanyun; Liu, Changxiao

doi:10.1016/j.jep.2022.115006

Cited by 3 publications

(10 citation statements)

References 50 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…103 Shang et al recently demonstrated an increase in intestinal absorption of rotundic acid via the paracellular pathway on canine MDCKII-WT cells with ethylene glycol tetraacetic acid (EGTA). 104 of 4 kDa dextran. 105 Chitosan-mediated reversible opening of tight junctions has also been reported in Caco-2 cells, 106 and chitosan-labeled quantum dots were shown to have enhanced paracellular permeability in mice.…”

Section: Can Orally Delivered Nanoparticles Bypass Cellular Uptake?mentioning

confidence: 99%

“…Using the in vitro gut co-culture model of Caco-2 (enterocyte-like cells)/HT29-MTX (goblet-like cells), researchers showed that the bioavailability of oral insulin delivery can be increased with sodium caprate and the short chain fatty acid geranic acid (3,7-dimethyl-2,6-octadienoic acid) with choline . Shang et al recently demonstrated an increase in intestinal absorption of rotundic acid via the paracellular pathway on canine MDCKII-WT cells with ethylene glycol tetraacetic acid (EGTA) . Dening et al have investigated E-cadherin-domain-derived peptides to enhance intestinal bioavailability and observed increased paracellular permeation of 4 kDa dextran .…”

Section: Can Orally Delivered Nanoparticles Bypass Cellular Uptake?mentioning

confidence: 99%

See 1 more Smart Citation

Mechanisms of Nanoparticle Transport across Intestinal Tissue: An Oral Delivery Perspective

2023

View full text Add to dashboard Cite

Oral drug administration has been a popular choice due to patient compliance and limited clinical resources. Orally delivered drugs must circumvent the harsh gastrointestinal (GI) environment to effectively enter the systemic circulation.The GI tract has a number of structural and physiological barriers that limit drug bioavailability including mucus, the tightly regulated epithelial layer, immune cells, and associated vasculature. Nanoparticles have been used to enhance oral bioavailability of drugs, as they can act as a shield to the harsh GI environment and prevent early degradation while also increasing uptake and transport of drugs across the intestinal epithelium. Evidence suggests that different nanoparticle formulations may be transported via different intracellular mechanisms to cross the intestinal epithelium. Despite the existence of a significant body of work on intestinal transport of nanoparticles, many key questions remain: What causes the poor bioavailability of the oral drugs? What factors contribute to the ability of a nanoparticle to cross different intestinal barriers? Do nanoparticle properties such as size and charge influence the type of endocytic pathways taken? In this Review, we summarize the different components of intestinal barriers and the types of nanoparticles developed for oral delivery. In particular, we focus on the various intracellular pathways used in nanoparticle internalization and nanoparticle or cargo translocation across the epithelium. Understanding the gut barrier, nanoparticle characteristics, and transport pathways may lead to the development of more therapeutically useful nanoparticles as drug carriers.

show abstract

Section: Can Orally Delivered Nanoparticles Bypass Cellular Uptake?mentioning

confidence: 99%

Section: Can Orally Delivered Nanoparticles Bypass Cellular Uptake?mentioning

confidence: 99%

Mechanisms of Nanoparticle Transport across Intestinal Tissue: An Oral Delivery Perspective

2023

View full text Add to dashboard Cite

show abstract

“…The main causes of the limited bioavailability of RA are its poor solubility, low membrane permeability, and active efflux transport. [73] According to an in vivo study, the concentration of RA in all tissues diminished to less than 1/10 of the peak concentration at 4 hours after oral administration. This indicates that there was no significant deposition of RA in the tissues and suggests that the liver may have extensively metabolized or eliminated RA, contributing to its poor oral bioavailability.…”

Section: Biopharmaceutical Profile Of Rotundic Acidmentioning

confidence: 99%

“…[71] RA has poor oral bioavailability due to its strong lipophilicity (LogP = 4.1) and low water solubility (12.89 μg/mL). [72,73] In vivo experiments conducted by Shang et al (2022) manifested that the absolute bioavailability of RA varied between 16.1 % and 19.4 %, depending on the administered dose. The absorption of RA was also found to be dose-dependent, and the compound was widely distributed in the liver.…”

Section: Biopharmaceutical Profile Of Rotundic Acidmentioning

confidence: 99%

“…The absorption of RA was also found to be dose-dependent, and the compound was widely distributed in the liver. [73] The most favorable site for RA absorption is the duodenum in the upper small intestine. Absorption of RA occurs through passive diffusion, P-gpinduced active efflux, OATP2B1-induced active uptake, and the paracellular pathway.…”

Section: Biopharmaceutical Profile Of Rotundic Acidmentioning

confidence: 99%

See 1 more Smart Citation

Efficacy of Rotundic Acid and Its Derivatives as Promising Natural Anticancer Triterpenoids: A Literature‐Based Study

Bhuia,

Chowdhury,

Sonia

et al. 2024

Chemistry & Biodiversity

View full text Add to dashboard Cite

Rotundic acid (RA) is a naturally occurring pentacyclic triterpene with a multitude of pharmacological activities. The primary emphasis of this study is on summarizing the anticancer properties with the underlying mechanisms of RA and its derivatives, as well as the pharmacokinetic features. Data was collected (up to date as of November 10, 2023) from various reliable and authentic literatures by searching in different academic search engines, including PubMed, Springer Link, Scopus, Wiley Online, Web of Science, ScienceDirect, and Google Scholar. The findings imply that RA and its synthetic derivatives possess promising anti‐cancer properties against breast, colorectal, liver, and cervical cancers in various preclinical pharmacological test systems. The results also indicate that RA and its derivatives demonstrated anticancer effects via a number of cellular mechanisms, including apoptotic cell death, inhibition of oxidative stress, anti‐inflammatory effect, cytotoxicity, cell cycle arrest, anti‐proliferative effect, anti‐angiogenic effect, and inhibition of cancer cell migration and invasion. It has been proposed that RA and its derived compounds have the capability to serve as a hopeful chemotherapeutic agent, so further extensive clinical research is necessary.

show abstract

A systematic review: Botany, phytochemistry, traditional uses, pharmacology, toxicology, quality control and pharmacokinetics of Ilex rotunda Thunb.

Zeng

Cui

Yang

et al. 2022

Journal of Ethnopharmacology

View full text Add to dashboard Cite

Intestinal absorption mechanism of rotundic acid: Involvement of P-gp and OATP2B1

Cited by 3 publications

References 50 publications

Mechanisms of Nanoparticle Transport across Intestinal Tissue: An Oral Delivery Perspective

Mechanisms of Nanoparticle Transport across Intestinal Tissue: An Oral Delivery Perspective

Efficacy of Rotundic Acid and Its Derivatives as Promising Natural Anticancer Triterpenoids: A Literature‐Based Study

A systematic review: Botany, phytochemistry, traditional uses, pharmacology, toxicology, quality control and pharmacokinetics of Ilex rotunda Thunb.

Contact Info

Product

Resources

About