The aromatic Baeckea frutescens leaves(BFL)known as“Gang-Song-Cha”is a popular drink(Tea)in South China.To explore the healthcare value,a systematic and in-depth study on BFL alleviating rheumatoid arthritis(RA)was ...The aromatic Baeckea frutescens leaves(BFL)known as“Gang-Song-Cha”is a popular drink(Tea)in South China.To explore the healthcare value,a systematic and in-depth study on BFL alleviating rheumatoid arthritis(RA)was carried out by integrating network pharmacology,molecular docking,and experimental verification.The efficacy was first evaluated,and the BFL extract could ameliorate RA by inhibiting articular swelling,lowering immune organ index,improving the ankle pathologies,and regulating serum levels of tumor necrosis factorα(TNF-α),interleukin(IL)-6,and IL-10 in CIA rats.Then the anti-RA mechanism of BFL was investigated by leveraging the high-content and active component 5-hydroxy-7-methoxy-2-isopropylchromone(Chro),and the potential signaling pathway and related target proteins for Chro acting on RA were analyzed by Kyoto Encyclopedia of Genes and Genomes(KEGG)enrichment and docking simulation.Finally,the experimental validations were conducted on rheumatoid arthritis fibroblast-like synoviocytes(RAFLS),and compound Chro could inhibit cell invasion and migration,block cell cycle at G2/M phase and induce apoptosis,and reduce the secretion of inflammatory cytokines by suppressing the PI3K-Akt pathway.These results provided pharmacological basis for the folk usage of“Gang-Song-Cha”for intervening RA.展开更多
[Objectives]This study was conducted to investigate the inhibitory effects of different extraction fractions of Baeckea frutescens L.on the proliferation of human colon cancer LOVO cells in vitro.[Methods]Leaves were ...[Objectives]This study was conducted to investigate the inhibitory effects of different extraction fractions of Baeckea frutescens L.on the proliferation of human colon cancer LOVO cells in vitro.[Methods]Leaves were separated from the aerial part of B.frutescens,immersed in distilled water and treated by ultrasound for half an hour.The volatile oil in B.frutescens leaves was extracted by steam distillation.The leaves after removing the volatile oil were extracted by reflux condensation,and then the extract was concentrated into fluid extract.The organic solvent extraction method was applied to extract the fluid extract until the organic phase was nearly colorless,and the extracts were combined,and concentrated into fluid extract,which was then freeze-dried into powder for later use.A cytotoxicity experiment was carried out on human colon cancer LOVO cells with different extraction fractions of B.frutescens as test drugs.Cell activity was detected by MTT assay.[Results]The petroleum ether fraction and chloroform fraction of B.frutescens had no inhibitory effect on the proliferation of human intestinal cancer LOVO cells in vitro.The ethyl acetate fraction and n-butanol fraction of B.frutescens had inhibitory effects on the proliferation of human colon cancer LOVO cells in vitro in a dose-dependent manner.The IC_(50)of ethyl acetate was 398.94μg/ml,and that of n-butanol was 617.02μg/ml.[Conclusions]The ethyl acetate and n-butanol extraction fractions from B.frutescens have inhibitory effects on the proliferation of human colon cancer LOVO cells in vitro in a dose-dependent manner.展开更多
In the present study,we carried out a phytochemical investigation of the ethanol extract of the aerial parts of Baeckea frutescens,which resulted in the isolation of two new flavonoid glycosides,myricetin 3-O-(5'-...In the present study,we carried out a phytochemical investigation of the ethanol extract of the aerial parts of Baeckea frutescens,which resulted in the isolation of two new flavonoid glycosides,myricetin 3-O-(5'-O-galloyl)-α-L-arabinofuranoside(1),6-methylquercetin 7-O-β-D-glucopyranoside(2),one new methylchromone glycoside,7-O-(4',6'-digalloyl)-β-D-glucopyranosyl-5-hydroxy-2-methylchromone(3),together with three known compounds(4-6).The structures of these isolated compounds were established on the basis of 1 D and 2 D NMR techniques and chemical methods.The anti-inflammatory activities of the compounds 1-6 were evaluated for their inhibitory effects against cyclooxygenases-1 and-2 in vitro.Compounds 1-6 showed potent COX-1 and COX-2 inhibiting activities in vitro with IC50 values ranging from 1.95 to 5.54 μmol·L^(-1) and ranging from 1.01 to 2.27 μmol·L^(-1),respectively.展开更多
Phytochemical investigation of the MeOH extract of twigs and leaves of Baeckea frutescens led to the isolation of seven new polymethylated phloroglucinol meroterpenoids(PPMs),named baeckfrutones M-S(1-7).Their structu...Phytochemical investigation of the MeOH extract of twigs and leaves of Baeckea frutescens led to the isolation of seven new polymethylated phloroglucinol meroterpenoids(PPMs),named baeckfrutones M-S(1-7).Their structures and absolute configurations were determined by spectroscopic analyses,chiral-phase HPLC analysis,and electronic circular dichroism(ECD)calculations.PPM 1 is a novel meroterpenoid possessing a 6/6/5/3 tetracyclic skeleton in PPMs,whereas 3 and 4 are the first hydroxytasmanone type phloroglucinol-monoterpene hybrids.(+)-2 and 7 displayed potent antiinflammatory activity with IC50 values of 20.86±0.60 and 36.21±1.18 lL,respectively.展开更多
[Objectives] This study aimed to investigate the anti-inflammatory effects of Baeckea frutescence L.in vitro and in vivo.[Methods]The anti-inflammatory activity of B.frutescence was measured by mouse peritoneal capill...[Objectives] This study aimed to investigate the anti-inflammatory effects of Baeckea frutescence L.in vitro and in vivo.[Methods]The anti-inflammatory activity of B.frutescence was measured by mouse peritoneal capillary permeability test,mouse auricle swelling test and rat cotton granuloma test.The RAW264.7 macrophage model was stimulated by lipopolysaccharide(LPS),and the effects of B.frutescence on tumor necrosis factor-α(TNF-α) and interleukin-6(IL-6) were detected by enzyme-linked immunosorbent assay(ELISA),and the relative expression of inducible nitric oxide synthase(i NOS) and cyclooxygenase-2(COX-2) proteins was detected by Western blot.Thus,the in vitro anti-inflammatory activity of B.frutescence was studied.[Results] B.frutescence significantly inhibited mouse peritoneal capillary permeability,inhibited xylene-induced mouse auricle swelling and rat cotton granuloma,significantly inhibited TNF-α and IL-6 levels,and down-regulated the expression of i NOS and COX-2 proteins in cells.[Conclusions]B.frutescence showed good anti-inflammatory activity both in vitro and in vivo,and the mechanism may be related to the release inhibition of inflammatory factors TNF-α and the regulation of COX-2.展开更多
Phytochemical investigation of the aerial parts of Baeckea frutescens resulted in the isolation of three new mono-or sesquiterpene-based meroterpenoids, frutescones S-U(1-3), and one pair of new(±)-5,7-dihydroxy-...Phytochemical investigation of the aerial parts of Baeckea frutescens resulted in the isolation of three new mono-or sesquiterpene-based meroterpenoids, frutescones S-U(1-3), and one pair of new(±)-5,7-dihydroxy-8-isobutyryl-6-methyldihydroflavonol(4). Their structures and absolute configurations were established by HR-ESI-MS, 1D and 2D NMR, and quantum chemical ECD calculation. Compound 1 exhibited inhibitory effect on NO production in LPS-activated RAW 264.7 macrophages with an IC50 value being 0.81 μmol·L–1.展开更多
基金supported by the National Natural Science Foundation of China(U1804182)the Basic Research(Natural Science)Cultivation Project of Zhengzhou University(JC23852095).
文摘The aromatic Baeckea frutescens leaves(BFL)known as“Gang-Song-Cha”is a popular drink(Tea)in South China.To explore the healthcare value,a systematic and in-depth study on BFL alleviating rheumatoid arthritis(RA)was carried out by integrating network pharmacology,molecular docking,and experimental verification.The efficacy was first evaluated,and the BFL extract could ameliorate RA by inhibiting articular swelling,lowering immune organ index,improving the ankle pathologies,and regulating serum levels of tumor necrosis factorα(TNF-α),interleukin(IL)-6,and IL-10 in CIA rats.Then the anti-RA mechanism of BFL was investigated by leveraging the high-content and active component 5-hydroxy-7-methoxy-2-isopropylchromone(Chro),and the potential signaling pathway and related target proteins for Chro acting on RA were analyzed by Kyoto Encyclopedia of Genes and Genomes(KEGG)enrichment and docking simulation.Finally,the experimental validations were conducted on rheumatoid arthritis fibroblast-like synoviocytes(RAFLS),and compound Chro could inhibit cell invasion and migration,block cell cycle at G2/M phase and induce apoptosis,and reduce the secretion of inflammatory cytokines by suppressing the PI3K-Akt pathway.These results provided pharmacological basis for the folk usage of“Gang-Song-Cha”for intervening RA.
基金Supported by Social Development Program of Guilin Science and Technology Bureau(20210227-9-3)Guangxi Medical and Health Appropriate Technology Development and Application of the Project(S202310601143)University-Level Undergraduate Innovation and Entrepreneurship Training Program(X202410601223).
文摘[Objectives]This study was conducted to investigate the inhibitory effects of different extraction fractions of Baeckea frutescens L.on the proliferation of human colon cancer LOVO cells in vitro.[Methods]Leaves were separated from the aerial part of B.frutescens,immersed in distilled water and treated by ultrasound for half an hour.The volatile oil in B.frutescens leaves was extracted by steam distillation.The leaves after removing the volatile oil were extracted by reflux condensation,and then the extract was concentrated into fluid extract.The organic solvent extraction method was applied to extract the fluid extract until the organic phase was nearly colorless,and the extracts were combined,and concentrated into fluid extract,which was then freeze-dried into powder for later use.A cytotoxicity experiment was carried out on human colon cancer LOVO cells with different extraction fractions of B.frutescens as test drugs.Cell activity was detected by MTT assay.[Results]The petroleum ether fraction and chloroform fraction of B.frutescens had no inhibitory effect on the proliferation of human intestinal cancer LOVO cells in vitro.The ethyl acetate fraction and n-butanol fraction of B.frutescens had inhibitory effects on the proliferation of human colon cancer LOVO cells in vitro in a dose-dependent manner.The IC_(50)of ethyl acetate was 398.94μg/ml,and that of n-butanol was 617.02μg/ml.[Conclusions]The ethyl acetate and n-butanol extraction fractions from B.frutescens have inhibitory effects on the proliferation of human colon cancer LOVO cells in vitro in a dose-dependent manner.
基金supported by the National Natural Science Foundation of China(No.81573309)
文摘In the present study,we carried out a phytochemical investigation of the ethanol extract of the aerial parts of Baeckea frutescens,which resulted in the isolation of two new flavonoid glycosides,myricetin 3-O-(5'-O-galloyl)-α-L-arabinofuranoside(1),6-methylquercetin 7-O-β-D-glucopyranoside(2),one new methylchromone glycoside,7-O-(4',6'-digalloyl)-β-D-glucopyranosyl-5-hydroxy-2-methylchromone(3),together with three known compounds(4-6).The structures of these isolated compounds were established on the basis of 1 D and 2 D NMR techniques and chemical methods.The anti-inflammatory activities of the compounds 1-6 were evaluated for their inhibitory effects against cyclooxygenases-1 and-2 in vitro.Compounds 1-6 showed potent COX-1 and COX-2 inhibiting activities in vitro with IC50 values ranging from 1.95 to 5.54 μmol·L^(-1) and ranging from 1.01 to 2.27 μmol·L^(-1),respectively.
基金This work was financially supported by the National Natural Science Foundation of China(Nos.31570363 and 31770391)Key Research and Development Plan of Yunnan Province–Special Project of Science and Technology in Yunnan Province(2017IB007)+2 种基金Major Biomedical Project of Yunnan Province(2018ZF005)Innovation Team of the Ministry of Education(No.IRT-17R49)the Foundation of State Key Laboratory of Phytochemistry and Plant Resources in West China(P2017-ZZ04 and P2017-KF06),Kunming Institute of Botany,Chinese Academy of Sciences.
文摘Phytochemical investigation of the MeOH extract of twigs and leaves of Baeckea frutescens led to the isolation of seven new polymethylated phloroglucinol meroterpenoids(PPMs),named baeckfrutones M-S(1-7).Their structures and absolute configurations were determined by spectroscopic analyses,chiral-phase HPLC analysis,and electronic circular dichroism(ECD)calculations.PPM 1 is a novel meroterpenoid possessing a 6/6/5/3 tetracyclic skeleton in PPMs,whereas 3 and 4 are the first hydroxytasmanone type phloroglucinol-monoterpene hybrids.(+)-2 and 7 displayed potent antiinflammatory activity with IC50 values of 20.86±0.60 and 36.21±1.18 lL,respectively.
基金Supported by Key Science and Technology Project of Guangxi(Gui Ke Zhong1355001-4)Youth Innovation Fund Project of Guangxi Key Laboratory of Traditional Chinese Medicine Quality Standards(Gui Zhong Zhong Xi 201105)Open Project of Guangxi Key Laboratory of Traditional Chinese Medicine Quality Standards(Gui Zhong Zhong Kai 201303)
文摘[Objectives] This study aimed to investigate the anti-inflammatory effects of Baeckea frutescence L.in vitro and in vivo.[Methods]The anti-inflammatory activity of B.frutescence was measured by mouse peritoneal capillary permeability test,mouse auricle swelling test and rat cotton granuloma test.The RAW264.7 macrophage model was stimulated by lipopolysaccharide(LPS),and the effects of B.frutescence on tumor necrosis factor-α(TNF-α) and interleukin-6(IL-6) were detected by enzyme-linked immunosorbent assay(ELISA),and the relative expression of inducible nitric oxide synthase(i NOS) and cyclooxygenase-2(COX-2) proteins was detected by Western blot.Thus,the in vitro anti-inflammatory activity of B.frutescence was studied.[Results] B.frutescence significantly inhibited mouse peritoneal capillary permeability,inhibited xylene-induced mouse auricle swelling and rat cotton granuloma,significantly inhibited TNF-α and IL-6 levels,and down-regulated the expression of i NOS and COX-2 proteins in cells.[Conclusions]B.frutescence showed good anti-inflammatory activity both in vitro and in vivo,and the mechanism may be related to the release inhibition of inflammatory factors TNF-α and the regulation of COX-2.
基金the National Natural Science Foundation of China (Nos.81803392, 81573309 and 81973206)the Local Innovative and Research Teams Project of Guangdong Pearl River Talents Program (No. 2017BT01Y036)+3 种基金the National Key R&D Program of China (No. 2017YFC1703802)theNatural Science Foundation of Jiangsu Province (No. BK20180566)the Funding of Double First-rate Discipline Innovation Team (Nos.CPU2018GF05 and CPU2018GY11)the China Postdoctoral Science Foundation funded project (No. 2018M630644)。
文摘Phytochemical investigation of the aerial parts of Baeckea frutescens resulted in the isolation of three new mono-or sesquiterpene-based meroterpenoids, frutescones S-U(1-3), and one pair of new(±)-5,7-dihydroxy-8-isobutyryl-6-methyldihydroflavonol(4). Their structures and absolute configurations were established by HR-ESI-MS, 1D and 2D NMR, and quantum chemical ECD calculation. Compound 1 exhibited inhibitory effect on NO production in LPS-activated RAW 264.7 macrophages with an IC50 value being 0.81 μmol·L–1.
