A Fresh Look on Bergenin: Vision of Its Novel Drug Delivery Systems and Pharmacological Activities

Abstract

Bergenin (BER), a key constituent of Bergenia crassifolia (Saxifragaceae), has gained extensive attention, owing to its array of pharmacological actions, including anti-infective, anti-cancer, anti-diabetic, neuroprotective, hepatoprotective, anti-urolithiatic, anti-hyperuricemic, and anti-bradykinin properties. Despite ever-intensifying support for its therapeutic features, the poor solubility, lower oral bioavailability, shorter half-life, and more intestinal pH degradation (pH 6.8 or above) of BER have puzzled researchers. To circumvent these pharmaceutical challenges, and to improve its therapeutic efficacy, newer approaches have been adopted by research scientists. Thus, a discussion of the existing literature may provide complete information about the advances in delivery strategies for enhancing its utility. This paper summarizes up-to-date works on the design and development of novel delivery carriers of this bioactive compound, such as phospholipid complexes, extended-release core tablets, prodrugs, herbal gels, polyherbal ointments, nanoparticles, and poly (lactic acid) polymers, with the objective of harnessing its full potential. This review also provides a deep insight into its bioactivities, along with mechanisms. Additionally, the physicochemical attributes, chemistry, and pharmacokinetics of BER are discussed herein. Hence, the comprehensive information documented in this review may introduce new avenues for research advancements of BER.

Anti-Shigellosis Activity and Mechanisms of Action of Extracts from Diospyros gilletii Stem Bark

“…In a recently published review article by Salimo et al [37], the antibacterial activity of bergenins was reported in 15 in vitro studies and 4 in vivo experiments [37]. Noteworthy, bergenin and its congeners participate in several mechanisms, such as lipid-peroxidation inhibitory activity and free-radical-scavenging activity [38], and initiate apoptosis and cell-cycle arrest in the G0/G1 phase [39]. Moreover, these compounds are able to easily cross the complex and multilayer lipopolysaccharide of bacteria cell walls, thereby causing lysis and cell death [40].…”

Combination of selected Thai traditional pain relief medicinal plants with anti-inflammatory abilities in a protein denaturation assay

“…Bergenin was examined in various anti-inflammatory models and was proven to be an efficient anti-inflammatory compound (Oliveira et al 2019). The compound has been thoroughly studied in terms of pharmacology and has emerged as a promising candidate for therapeutic uses (Mehta et al 2022). Due to the anti-inflammatory agents that were identified as chemical constituents of M. siamensis and M. repandus, as well as the abundant lupeol compound found in C. adansonii, there could be a reason to support the anti-inflammatory activity of the mixture of these three plants, which was the most potent in our observation.…”

Biosynthetic pathway of prescription bergenin from Bergenia purpurascens and Ardisia japonica

“…Bergenin reportedly has anti-inflammatory, anti-anxiety, anti-malaria, anti-cancer, anti-diabetes, anti-hepatotoxicity, immunomodulatory, and neuroprotective pharmacological activities ( Rajesh et al., 2011 ; Liang et al., 2014 ; Gao et al., 2015 ; Jitender et al., 2017 ; Barai et al., 2019 ; Kumar et al., 2019 ; Shi et al., 2019 ; Xiang et al., 2020 ). Bergenin is widely distributed in higher plants and has been found in more than 90 plant species belonging to 37 genera in 20 families ( Mehta et al., 2022 ). The Chinese Pharmacopoeia lists the roots of Bergenia purpurascens and Ardisia japonica as natural bergenin resources for the medicinal extraction industry ( China Pharmacopoeia Committee, 2020 ).…”