JOURNAL OF ETHNOPHARMACOLOGY
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2023
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IF 5.4
Zhi-Ting Liu,Ying Zhang,Rui Fang,Monique Simmonds,Xiu-Juan Zhang,Tong-Tong Zhang,Tong-Tong Sun,Xiao-Qiang Chen
Ethnopharmacological relevance In the snake-infested mountainous regions of China, Saxifraga stolonifera [L.] Meeb is widely utilized as an immediate remedy for venomous snake bites. However, the scientific understanding of S. stolonifera 's efficacy in snakebite treatment remains limited and requires further investigation. Aim of the study The aim of this study was to assess the inhibitory effects of Saxifraga stolonifera phenolic extracts (SSPE) on Deinagkistrodon acutus venom (DAV) and explore the potential of S. stolonifera as a valuable candidate for antivenom development. Materials and methods We employed our previously optimized extraction conditions to obtain SSPE. In vitro experiments utilizing diverse models were conducted to assess the inhibitory effects of the extracted phenolic compounds on DAV, specifically targeting phospholipase A 2 (PLA 2 ), proteolytic, fibrinolytic , and hyaluronidase enzymes. Furthermore, in vivo investigations were conducted to evaluate the inhibitory potential of the extracted compounds against DAV-induced hemorrhagic and edematogenic activity. To elucidate the chemical composition of the phenolic extracts, Ultra Performance Liquid Chromatography-mass spectrometry (UPLC-MS) analysis was performed. Results Our in vitro inhibition study showed that S. stolonifera was able to inhibit the activities of PLA 2 enzyme, proteolytic enzyme , hyaluronidase and fibrinogenolytic. The median effective dose (ED 50 ) values of SSPE for inhibiting PLA 2 enzyme, proteolytic enzyme and hyaluronidase activities were 0.115 mg/mL, 0.026 mg/mL and 0.238 mg/mL, respectively. The DAV-induced hemorrhagic and edematogenic effects of the SSPE were also successfully inhibited in vivo , and the high SSPE concentration was able to completely inhibit the hemorrhage and edema. It is noteworthy that the mice suffered no harm from the high SSPE concentration. The composition analysis showed that the phenolic substances contained in SSPE are gallic acid , protocatechuic acid , chlorogenic acid , rutin , kaempferol-3-O-ɑ-L-rhamnoside, kaempferol-3-O-β-D-glucopyranoside, quercetin and kaempferol . Conclusions This study provides scientific validation of the inhibitory efficacy of S. stolonifera as an emergency treatment for venomous snake bites , offering a theoretical foundation for future drug development strategies targeting snakebite.
研究领域:
药理学
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毒理学
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植物化学
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产品关联
DOI
PubMed
高影响因子
BMC Complementary Medicine and Therapies
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2026
·Vol. 26
·期 1
·191
·
IF 4.4
Shen Fukui,Liu Hongyu,Yang Wen,Tong Tian-Tian,Guo Shiyu,Wei Zhihao,Zhang Wenping,Fan Jihui,Zhang Yuqing,Huang Hao
Background Saxifraga stolonifera Curtis (SSC), a highly esteemed Traditional Chinese Medicine with profound ethnomedicinal value, has been historically employed to treat inflammatory ear disorders. Contemporary preclinical studies have verified its effectiveness in combating otitis media (OM). However, the underlying pharmacological mechanisms, particularly its anti-inflammatory and antibacterial properties remain unclear. Purpose This study aimed to systematically elucidate the chemical basis, antibacterial activity and molecular mechanisms underlying SSC’s anti-OM activity. Methods UHPLC-Q-TOF-MS was employed for comprehensive phytochemical profiling of SSC total extracts. Antibacterial assays were conducted against three OM-associated bacterial strains: Staphylococcus aureus (SA), Pseudomonas aeruginosa (PA), and Klebsiella pneumoniae (KP), using SSC total extracts and its total flavonoid (TF). Network pharmacology analysis identified OM-related targets and pathways, followed by molecular docking validation. qPCR was used to assess mRNA expression of inflammatory cytokines ( IL-6 , TNF-α , IL-1 β) in LPS-induced J774A.1 macrophages. Results Twenty-five bioactive compounds were characterized, including 11 newly reported constituents. Antibacterial results showed SSC exhibited the strongest inhibitory effect against KP, while TF showed relatively strong activity against PA; overall, SSC outperformed TF, suggesting contributions from non-flavonoid components. Network pharmacology revealed 11 core targets interconnected with inflammatory pathways. Molecular docking confirmed strong binding affinities between key components (bergenin, 11-O-galloylbergenin) and targets (HSP90AA1, EGFR). SSC total extracts significantly downregulated pro-inflammatory cytokine mRNA levels in vitro. Conclusion SSC exerts anti-OM effects through a “dual mechanism”: antibacterial activity (with SSC total extract showing stronger efficacy than TF) and anti-inflammatory regulation via TNF/MAPK/NF-κB pathways. This integrative study validates SSC’s traditional use and provides a basis for developing SSC-based therapeutics for OM. Graphical The alternative text for this image may have been generated using AI.
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DOI
高影响因子
JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
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2017
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IF 3.255
Yuan Wang,Qing Li,Yue Dai,Ronghua Pan,Yufeng Xia
A specific and sensitive LC–MS/MS method was established for the simultaneous determination of bergenin, protocatechuic acid and gallic acid, the main active constituents of Saxifraga stolonifera (L.) Meerb. herb, in rat plasma. After fully validated, the method was applied to the comparative pharmacokinetic studies of the three compounds orally administered alone and in combination in the S. stolonifera extract, respectively. The results showed that the pharmacokinetic parameters, including C max , T max , AUC, CL z /F, MRT 0-∞ , were significantly different for both bergenin and protocatechuic acid in the extract as compared to the corresponding compounds administered alone. However, the pharmacokinetic behavior of gallic acid in the extract did not differ from that administered alone. Further studies found that quercetin, coexisting in the herb extract, significantly decreased the glucuronidation of bergenin through inhibiting the activities of UGT1A1 and UGT1A3, and reduced the metabolism of protocatechuic acid by inhibiting the activity of catechol-O-methyltransferase. Quercetin and other flavonoids occurring in the S. stolonifera extract might increase the absorption and improve the bioavailability of bergenin and protocatechuic acid by slowing down the liver metabolism. The findings provide a good guidance for the development and clinical application of S. stolonifera .
研究领域:
药理学
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分析化学
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传统医学
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DOI
PubMed
高影响因子
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