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ETHNOPHARMACOLOGICAL RELEVANCE: The roots and rhizomes of Bergenia purpurascens (Hook. f. et Thomson) Engl., was used as a sunscreen to protect against ultraviolet rays in Tibet of China historically, but its skin whitening constituents and pharmacological effects of this plant remained unknown. AIM OF THE STUDY: To investigate the anti-melanogenesis effect of B. purpurascens in vitro and in vivo, and then explore the preliminary mechanism. MATERIALS AND METHODS: An ultraviolet B (UVB)-induced skin injury model of mice was used to verify the ameliorative effect of B. purpurascens extract (BPE) on ultraviolet damage. Then, alpha-melanocyte stimulating hormone (α-MSH)-induced murine melanoma cell line (B16F10) melanin generation model was further adopted to approval the effects of BPE and its bioactive compound, cuscutin, in vitro. Moreover, α-MSH stimulated melanogenesis model in zebrafish was employed to confirm the anti-pigmentation effect of cuscutin. Then, proteins expressions associated with melanin production were observed using western blotting assay to explore preliminary mechanism. RESULTS: BPE inhibited UVB-induced mice injury and restored skin barrier function observably in vivo. BPE and cuscutin suppressed the overproduction of melanin in α-MSH induced B16F10 significantly, in which cuscutin exhibited better effect than well-known whitening agent α-arbutin at same 10 µg/mL concentration. Moreover, the pigmentation of zebrafish embryo was decreased by cuscutin. Finally, cuscutin showed significant downregulation of expressions of tyrosinase (TYR) and tyrosinase related protein-1 (TRP-1), TRP-2 and microphthalmia-associated transcription factor (MITF) in the melanogenic signaling pathway. CONCLUSION: B. purpurascens extract and its major bioactive constituent, cuscutin, showed potent anti-melanogenesis and skin-whitening effect by targeting TYR and TRP-2 proteins for the first time, which supported its traditional use.

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Bergenia purpurascens is an important medicinal, edible and ornamental plant. It generally grows in high-altitude areas with complex climates. There have been no reports about how B. purpurascens survives under cold stress. Here, the B. purpurascens under low temperature were subjected to transcriptomics analysis to explore the candidate genes and pathways that involved in the cold tolerance of B. purpurascens. Compared with the control treatment, we found 9,600 up-regulated differentially expressed genes (DEGs) and 7,055 down-regulated DEGs. A significant number of DEGs were involved in the Ca2+ signaling pathway, mitogen-activated protein kinase (MAPK) cascade, plant hormone signaling pathway, and lipid metabolism. A total of 400 transcription factors were found to respond to cold stress, most of which belonged to the MYB and AP2/ERF families. Five novel genes were found to be potential candidate genes involved in the cold tolerance of B. purpurascens. The study provide insights into further investigation of the molecular mechanism of how B. purpurascens survives under cold stress.

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Bergenia purpurascens (Hook. f. et Thoms.) Engl. is one species of traditional Chinese medicinal plant. This is the first publication of its complete chloroplast (cp) genome. The whole cp genome has 157,246 base pairs in length with 132 annotated genes, of which were 87 protein-coding genes, 37 tRNAs, and 8 rRNAs. According to the phylogenetic study, B. purpurascens and Bergenia scopulosa T. P. Wang. 1974 had a sister relationship. This genomic data and conclusions from B. purpurascens phylogenetic research will provide useful information and throw light on more in-depth investigations of the systematics and evolutionary patterns of Saxifragaceae.

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Phytopathogenic fungi have been considered as being an enormous threat in the agricultural system. In our search of new antifungal natural products, nine new halogenated cyclopentenones, bicolorins A-I (1-3, and 5-10), along with three known cyclopentenones (4, 11, and 12) were isolated from the endophytic fungus Saccharicola bicolor of Bergenia purpurascens by the one strain-many compounds strategy. Their structures and absolute configurations were elucidated based on extensive spectroscopic analysis, X-ray crystallographic analysis, and time-dependent density functional theory-equivalent circulating density calculations. Compounds 1-12 showed antifungal activities against five phytopathogenic fungi (Uromyces viciae-fabae, Pythium dissimile, Gibberella zeae, Aspergillus niger, and Sclerotinia sclerotiorum). Especially, bicolorins B and D (2 and 5) exhibited strong antifungal activities against P. dissimile with the MIC values of 6.2 and 8.5 µg/mL, respectively, compared with the positive control cycloheximide (MIC of 8.6 µg/mL). Additionally, bicolorin D was proven to be potently antifungal against S. sclerotiorum in vitro and in vivo. This work provides an effective strategy for searching antifungal candidate agents.

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Chemical investigation of the ethanolic extracts of the dried leaves of Bergenia purpurascens led to the isolation and identification of a new aromatic glycoside, 1-O-ß-D-glucopyranosyl-2-methoxy-3-hydroxyl-phenylethene (1), along with other 19 known compounds (2-20). The structure of compound 1 was determined by a detailed analysis using various analytical techniques, including 1D and 2D NMR. In vitro anti-proliferative activities of compound 1 on five human cancer cell lines were evaluated. The results showed that compound 1 possessed the most potent effects with the IC50 values of 14.36 ± 1.04 µM against T24 cells. The further bioactivity analysis showed that compound 1 induced apoptosis of T24 cells, and altered anti- and pro-apoptotic proteins, leading to mitochondrial dysfunction and activation of caspase-3 for causing cell apoptosis. The present investigation illustrated compound 1 might be used as a potential antitumour chemotherapy candidate.

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BACKGROUND: Bergenia purpurascens has tonic, haemostatic and anti-tussive actions. Anti-inflammatory and anti-bacterial activities of Bergenia purpurascens have not been reported so far. The objective of this paper is to provide experimental basis for the clinical application of Bergenia purpurascens through the pharmacodynamic study on its anti-inflammatory and anti-bacterial effects. METHODS: Experimental models of xylene-induced ear edema in mice, cotton pellet granuloma in rats, and acetic acid-induced peritoneal capillary permeability in mice were used to investigate the anti-inflammatory effect of Bergenia purpurascens; bacteriostatic and bactericidal effects of Bergenia purpurascens extract on Staphylococcus aureus (SA), methicillin-resistant Staphylococcus aureus (MRSA), and ß-lactamase positive Staphylococcus aureus (ESBLs-SA), were observed in vitro. RESULTS: The results show that Bergenia purpurascens extract could markedly inhibit xylene-induced mouse ear edema, cotton pellet granulation tissue hyperplasia, and increased capillary permeability. Bergenia purpurascens extract has an inhibitory effect on SA, MRSA and ESBLs-SA. CONCLUSION: We conclude that Bergenia purpurascens extract has certain anti-inflammatory and anti-bacterial effects.

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Bergenin, a C-glucoside of 4-O-methyl gallic acid from Bergenia purpurascens, is a naturally antitussive and expectorant agent. A rapid and sensitive liquid chromatography tandem mass spectrometry (LC-MS/MS) method has been developed and validated for the determination of the active component-bergenin, in rat plasma after oral administration of aqueous B. purpurascens extract. The plasma samples were pretreated by protein precipitation with acetonitrile and chromatographic separation was achieved on a Diamonsil® C18 column (150 mm×4.6 mm, 5 µm) with isocratic elution using a mobile phase consisting of water-methanol (30:70, v/v) at a flow rate of 0.6 mL/min. The detection was accomplished by a triple-quadrupole tandem mass spectrometer in multiple-reaction monitoring (MRM) scanning via an electrospray ionization (ESI) source operating in the negative mode. The optimized mass transition ion-pairs (m/z) for quantitation were 327.3/192.0 for bergenin, and 431.1/311.1 for IS. The time for each analysis run was only 3.5 min between injections. The calibration curve exhibited good linearity (r2>0.99) over a range of 1.00-2000 ng/mL for bergenin. The lower limit of quantitation (LLOQ) was 1.00 ng/mL. The intra- and inter-day precisions were no more than 11.8%, and relative errors (RE) were within the range of 0.0-4.4%. The validated method was successfully applied to investigate the pharmacokinetics of bergenin after oral administration of B. purpurascens extract in rats.

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OBJECTIVE: To develop a method for the determination of arbutin, gallic acid, bergenin, protocatechuic acid, chlorogenic acid, catechin, epicatechin, epicatechin gallate, and ferulic acid in Bergenia purpurascens by HPLC-MS/MS. METHODS: The samples were separated on a Diamonsil C18 column (4.6 mm × 150 mm, 5 μm) by gradient elution using methanol and 0.2‰(V/V) formic acid aqueous solution as the mobile phase at a flow rate of 0.8 mL · min-1. The column temperature was room temperature. Multiple-reaction monitoring (MRM) scanning was employed for quantification with switching electrospray ion source polarity in negative mode. RESULTS: Complete separation was achieved within 10 min for the nine compounds (arbutin, gallic acid, bergenin, protocatechuic acid, chlorogenic acid, catechin, epicatechin, epicatechin gallate, ferulic acid): The nine regression equations showed linear relationships between peak areas and contents of each compound. The average recoveries (n=9) of the compounds listed above were 100.2%, 100.0%, 99.8%, 99.9%, 97.9%, 101.2%, 99.8%, 101.7%, 102.4% and RSD were 0.80%, 3.06%, 2.72%, 3.28%, 3.58%, 1.44%, 0.95%, 0.96%, 0.48%, respectively. CONCLUSION: The method is simple, accurate and has good reproducibility, thus can be used for the determination of the nine compounds in Bergenia purpurascens.