Journal of ethnopharmacology · 2024
Chemical profiling and anti-inflammatory effect of phenolic extract of Gentiana rigescens Franch.
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Gao Qiao, Li Yi, Zhong Yao, Zhang Shu-Xian, Yu Chang-Yuan, Chen Guang
Аннотация
ETHNOPHARMACOLOGICAL RELEVANCE: Gentiana rigescens Franch. (G. rigescens), known as "Dian Long Dan" in Southern Yunnan Herbal, has a long history in traditional Chinese medicine for treating hepatitis, allergies, postherpetic neuralgia, cholecystitis and rheumatism.
AIM OF THE STUDY: This study aims to comprehensively analyze the phenolic composition of G. rigescens, evaluate its potential anti-inflammatory effects, elucidate underlying mechanisms, and identify its in vivo bioactive phenolic constituents.
MATERIALS AND METHODS: The extraction of G. rigescens phenolic compounds (GRP) was optimized using the Box-Behnken response surface method, with four phenolic compounds (mangiferin, esculetin, ferulic acid and kaempferol) used as quality index markers. GRP's phytochemical composition was subsequently profiled via UPLC-Q-TOF-MS/MS analysis. Anti-inflammatory activity and mechanisms were assessed in LPS-stimulated RAW264.7 cells and murine models, utilizing NO production assays, ELISA, qRT-PCR, Western blotting and histopathological analysis. Bioactive phenolic compounds in blood were identified post-oral administration for in vivo activity prediction.
RESULTS: The optimal extraction conditions for GRP were determined as follows: Soxhlet extraction using acetone with hydrochloric acid 0.06 mol/L, at a liquid-to-solid ratio of 132: l. for 6.6 h. Seventy-one of phenolic compounds were identified in GRP using UPLC-Q-TOF-MS/MS. GRP significantly inhibited LPS-induced NO production in RAW 264.7 macrophages and reduced pro-inflammatory cytokines IL-6, IL-1β, and TNF-α while increasing anti-inflammatory IL-10. In the carrageenan-induced inflammatory model, GRP exhibited a 69.81% inhibition rate of toe swelling at high doses (1 g/kg), along with protective effects against joint injury, as observed in histological assessments. Mechanistically, GRP downregulated mRNA levels of inflammatory cytokines and reduced the expression of inflammatory proteins iNOS, COX-2, p65, p-p65 and P-IκB as shown by Western blotting. Twenty-five of phenolic compounds, including mangiferin, swertianolin, acacetin, umbelliferone and caffeic acid, were identified in vivo in the blood, indicating potential bioactive roles.
CONCLUSIONS: This study provides the first comprehensive profile of the phenolic composition of G. rigescen, alongside a detailed investigation of its anti-inflammatory activity, mechanisms, and in vivo bioactive components. These findings highlight the therapeutic potential of Dian Long Dan's phenolic constituents and support further research on G. rigescens.
AIM OF THE STUDY: This study aims to comprehensively analyze the phenolic composition of G. rigescens, evaluate its potential anti-inflammatory effects, elucidate underlying mechanisms, and identify its in vivo bioactive phenolic constituents.
MATERIALS AND METHODS: The extraction of G. rigescens phenolic compounds (GRP) was optimized using the Box-Behnken response surface method, with four phenolic compounds (mangiferin, esculetin, ferulic acid and kaempferol) used as quality index markers. GRP's phytochemical composition was subsequently profiled via UPLC-Q-TOF-MS/MS analysis. Anti-inflammatory activity and mechanisms were assessed in LPS-stimulated RAW264.7 cells and murine models, utilizing NO production assays, ELISA, qRT-PCR, Western blotting and histopathological analysis. Bioactive phenolic compounds in blood were identified post-oral administration for in vivo activity prediction.
RESULTS: The optimal extraction conditions for GRP were determined as follows: Soxhlet extraction using acetone with hydrochloric acid 0.06 mol/L, at a liquid-to-solid ratio of 132: l. for 6.6 h. Seventy-one of phenolic compounds were identified in GRP using UPLC-Q-TOF-MS/MS. GRP significantly inhibited LPS-induced NO production in RAW 264.7 macrophages and reduced pro-inflammatory cytokines IL-6, IL-1β, and TNF-α while increasing anti-inflammatory IL-10. In the carrageenan-induced inflammatory model, GRP exhibited a 69.81% inhibition rate of toe swelling at high doses (1 g/kg), along with protective effects against joint injury, as observed in histological assessments. Mechanistically, GRP downregulated mRNA levels of inflammatory cytokines and reduced the expression of inflammatory proteins iNOS, COX-2, p65, p-p65 and P-IκB as shown by Western blotting. Twenty-five of phenolic compounds, including mangiferin, swertianolin, acacetin, umbelliferone and caffeic acid, were identified in vivo in the blood, indicating potential bioactive roles.
CONCLUSIONS: This study provides the first comprehensive profile of the phenolic composition of G. rigescen, alongside a detailed investigation of its anti-inflammatory activity, mechanisms, and in vivo bioactive components. These findings highlight the therapeutic potential of Dian Long Dan's phenolic constituents and support further research on G. rigescens.