To study the chemical constituents of Sappan Lignum. Chemical constituents were isolated by method of solvent extraction, repeated chromatography with silica gel, Sephadex LH-20, and ODS. The structures were elucidate...To study the chemical constituents of Sappan Lignum. Chemical constituents were isolated by method of solvent extraction, repeated chromatography with silica gel, Sephadex LH-20, and ODS. The structures were elucidated based on spectro- scopic data. Fourteen compounds were isolated and their structures were identified as brazilin （1）, sappanone B （2）, （E）-3-（3,4- dihydroxybenzylidene）-7-hydroxychroman-4-one （3）, 3-deoxysappanone B （4）, brazilide A （5）, euxanthone （6）, quercetin （7）, rhamnetin （8）, sappanchalcone （9）, 3-deoxysappanchalcone （10）, butein （11）, 2,4,5-trihydroxybenzaldehyde （12）, 3,8,9-trihydroxy- 6H-benzo[c]chromen-6-one （13） and 13-sitosterol （14）. Compounds 12 and 13 were two new natural compounds, and the ^13C NMR data of compound 13 were reported for the first time. Compound 6 was the first xanthone isolated from the genus Caesalpinia.展开更多
AIM: To investigate the active constituents of Lignum Sappan(Caesalpinia sappan L.) on growth-related signaling and cell mitosis. METHOD: The influence of the ethyl acetate(EtOAc) extract of Lignum Sappan and its cons...AIM: To investigate the active constituents of Lignum Sappan(Caesalpinia sappan L.) on growth-related signaling and cell mitosis. METHOD: The influence of the ethyl acetate(EtOAc) extract of Lignum Sappan and its constituents on growth-related signaling were evaluated by a luciferase assay in cells stably- transfected with NF-κB, STAT1, or STAT3 responsive luciferase reporter plasmid. The inhibitory effect on the cell cycle was determined by flow cytometric analysis. The anti-tumor activities were assessed in vitro and in vivo. RESULTS: The EtOAc extract of Lignum Sappan had inhibitory activities on growth-related signaling and cell mitosis. Three major active compounds were sappanchalcone, brazilin, and butein. Sappanchalcone blocked cell cycle progression in the G2/M phase, brazilin inhibited TNFα/NF-κB signaling, while butein inhibited IL-6/STAT3 signaling, as well as TNFα/NF-κB signaling. The three compounds all demonstrated cytotoxic activities against human tumor cells in vitro. In a S180 tumor cell-bearing mice model, the anti-tumor efficacy of the EtOAc extract was better than the individual compounds acting alone. CONCLUSION: These results indicate that Lignum Sappan contains multiple active compounds with different antitumor activities, which act synergistically to enhance their anti-tumor effects. The EtOAc extract of Lignum Sappan may be better than individual active constituent as a novel medicine for the treatment of cancer.展开更多
Determination of brazilin by High Performance Liquid Chromatography （HPLC） method and measurement of the antioxidative and lipase inhibition effects in the Caesalpinia sappan wood from various locations in Indonesia...Determination of brazilin by High Performance Liquid Chromatography （HPLC） method and measurement of the antioxidative and lipase inhibition effects in the Caesalpinia sappan wood from various locations in Indonesia is described in this paper. Brazilin was separated from sample matrix using a reversed phase C 18, Shim-pack VP column with the mobile phase in a gradient elution for45 min from 5% to 100% methanol in 0.05% aqueous trifluoroacetic acid. Brazilin in ethanolic extracts ofC. sappan wood was in the range of 5.81 to 24.85 mg/g on dry-weight basis. Antioxidant and lipase inhibition activities expressed by IC50 values from all samples were in the range from 6.60 to 11.53 μg/mL and 50.76 to 203.21 μg/mL, respectively. Antioxidative and lipase inhibition potency of all ethanolic extracts were compared to vitamin C and chloramphenicol, isopropyl methylphenol and tetracyclin, respectively.展开更多
Caesalpinia sappan L.(CS) is a plant of Leguminosae family,commonly known as Brazil or Sappan wood.CS is distributed in Southeast Asia and its dried heartwood has been used as traditional ingredient of food or beverag...Caesalpinia sappan L.(CS) is a plant of Leguminosae family,commonly known as Brazil or Sappan wood.CS is distributed in Southeast Asia and its dried heartwood has been used as traditional ingredient of food or beverages and has a wide variety of medicinal properties.Higher extraction yield of CS wood was achieved with 95% ethanol for 2 h.Chemical constituent's investigation of sappan wood resulled in the isolation of various structural types of phenolic components including one xanihone,one coumarin,three chalcones,two flavones three homoisoflavonoids and brazilin.Brazilin[(6a S-cis)-7,11b-dihydrobcnz[b]indeno[1.2-d]pyran-3.6a.9.10(6H)- tetroll.a major and active compound found in CS heartwood.Most of the folkloric uses of brazilin were validated by the scientific studies such as antioxidant,antibacterial,anti-inflammatory,anti-photoaging.hypoglycemic,vasorelaxant,hepatoproteetive and anti-acne activity.CS heartwood extract is safe and did not produce any acute or subacute toxicity in both male and female rats.Brazilin is the safe natural compound having potential to develop as a medicinal compound with application in food,beverage,cosmetics and pharmaceutical industries to screen its clinical use in modern medicine.The information gained could provide the important and potential approach for pharmaceutical researcher to implicate the knowledge of brazilin in the formulation of new drug and to reveal therapeutic and gaps requiring future research opportunities.More studies are needed to evaluate the potential application of brazilin as preservative and coloring agent in food processing industries.展开更多
Caesalpinia sappan L., belonging to the family Leguminosae, is a medicinal plant that is distributed in Southeast Asia. The dried heartwood of this plant is used as a traditional ingredient of food, red dyes, and folk...Caesalpinia sappan L., belonging to the family Leguminosae, is a medicinal plant that is distributed in Southeast Asia. The dried heartwood of this plant is used as a traditional ingredient of food, red dyes, and folk medicines in the treatment of diarrhea, dysentery, tuberculosis, skin infections, and inflammation. Brazilin is the major active compound, which has exhibited various phar- macological effects, including anti-platelet activity, anti-hepatotoxicity, induction of immunological tolerance, and anti-inflammatory and antioxidant activities. The present study aimed to evaluate the antioxidant activity and expression of antioxidant enzymes of C. sappan L. extract and its major compound, brazilin, in human epidermal keratinocytes exposed to UVA irradiation. Our results indi- cated that C. sappan L. extract reduced UVA-induced H202 production via GPX7 activation. Moreover, brazilin exhibited anfioxidant effects that were similar to those of C. sappan L. via glutathione peroxidase 7 （GPX7）, suggesting that C. sappan L. extract and its natural compound represent potential treatments for oxidative stress-induced photoaging of skin.展开更多
Objective: The objective of the work was to optimize the extraction conditions of Caesalpinia sappan L.heartwood in order to maximize the brazilin content and antibacterial activity of the extract.Methods: Two indepen...Objective: The objective of the work was to optimize the extraction conditions of Caesalpinia sappan L.heartwood in order to maximize the brazilin content and antibacterial activity of the extract.Methods: Two independent factors were studied: extraction temperature(45–95 °C) and extraction time(30–60 min). In addition, five dependent factors were monitored, including extraction yield, brazilin content, and clear zones against Staphylococcus aureus TISTR 1466, Staphylococcus epidermidis TISTR 518 and Propionibacterium acnes DMST 14961. The brazilin content was quantified by high-performance liquid chromatography and antibacterial activity was determined by disk diffusion assay.Results: The high temperature provided high total extract yield as well as brazilin content, while extraction time had little effect on yield or brazilin content. Extraction time had a positive effect, while extraction temperature had little effect on clear zone against S. aureus. The largest clear zone against S. epidermidis was achieved at low extraction temperature and long extraction time. Conversely, short extraction time and high extraction temperature provided the largest clear zone against P. acnes. The optimal conditions providing the highest brazilin content was an extraction temperature and extraction time of 95 °C and 30 min, respectively.The same optimal conditions also provided the simultaneous greatest antibacterial activity against the three bacteria. Modeled optimal conditions were validated be conducting extraction using these values. Yield and antibacterial activity of the resulting extract demonstrated that the model had a low percentage error.Conclusion: The optimal condition will be used as a standard condition for extraction of C. sappan heartwood to maximize brazilin content and antibacterial activity.展开更多
OBJECTIVE: To investigate the inhibitory effect of Sumu(Lignum Sappan) plus Fuzi(Radix Aconiti Lateralis Praeparata)(SF) on the growth and metastasis of Lewis lung carcinoma.METHODS: A lung carcinoma model was establi...OBJECTIVE: To investigate the inhibitory effect of Sumu(Lignum Sappan) plus Fuzi(Radix Aconiti Lateralis Praeparata)(SF) on the growth and metastasis of Lewis lung carcinoma.METHODS: A lung carcinoma model was established by subcutaneously inoculating Lewis lung carcinoma cells into C57 BL/6 mice. The mice were randomly divided into four groups of 13 mice(control, low-dose, moderate-dose, and high-dose), and gavaged once-daily for 21 consecutive days. The rates of tumor inhibition, metastasis, and metastasis inhibition were observed. The differential expressions of s P-selectin and vascular endothelial growth factor C(VEGFC) were compared between the treatment groups and the control group.RESULTS: The tumor weights differed significantly between the treatment groups and the control group(P < 0.05). Administration of SF in the moderate-dosage and low-dose groups significantly inhibited the expression of s P-selectin and VEGFC(both P < 0.05), suggesting anti-tumor activity.CONCLUSION: SF can inhibit the growth and metastasis of Lewis lung carcinoma.展开更多
Two new rearranged diterpenoids, tomocinol C （1） and spirocaesalmin C （2） were isolated from the seeds of Caesalpinia sappan. Their structures were elucidated based on comprehensive analysis of spectroscopic data,...Two new rearranged diterpenoids, tomocinol C （1） and spirocaesalmin C （2） were isolated from the seeds of Caesalpinia sappan. Their structures were elucidated based on comprehensive analysis of spectroscopic data, and their absolute configurations were established by single crystal X-ray crystallography.展开更多
Phytochemical investigation on the seeds of Caesalpinia sappan led to the isolation of five new cassanetype diterpenoids, named 11-oxo-phanginin A（1）, caesalsappanins O–Q（2–4） and phanginin U（5）,together with ...Phytochemical investigation on the seeds of Caesalpinia sappan led to the isolation of five new cassanetype diterpenoids, named 11-oxo-phanginin A（1）, caesalsappanins O–Q（2–4） and phanginin U（5）,together with five known compounds. The structures of the new compounds were elucidated by extensive analysis of mass spectrometric and 1D and 2D NMR spectroscopic data. All the new compounds showed moderate cytotoxic effects on human breast cancer MCF-7 and human colon cancer HCT116 cell lines.展开更多
Natural dyes taken from the barks of the tree Caesalpinia sappan has been used in many consumer products.Hence it is imperative to test the toxicity of this dye.In the present study an investigation was conducted to f...Natural dyes taken from the barks of the tree Caesalpinia sappan has been used in many consumer products.Hence it is imperative to test the toxicity of this dye.In the present study an investigation was conducted to find out the toxic effect of aqueous extract of the dye C.sappan in test animal Wister albino rats.Acute oral toxicity showed no clinical signs of toxicity and no mortality even at a dose level of 100–2000 mg/kg in 14 days observation period.When a dose level above 2500 mg/kg was given for 28 days,no death was noticed up to the dose level 5000 mg/kg body weight.The weight of the tested rats was not significantly reduced,when compared with the control group.The organ-body weight ratio of kidney,liver and abdomen did not change when compared to the control group in the observation period.The less toxicity of the dyes of C.sappan.展开更多
Antioxidant activities of the 95% ethanol extract from Caesalpinia sappan heartwood （ECS）, protosappanin A, protosappanin B, and brazilein were studied in vitro. The inhibition of the formation of malondialdehyde （...Antioxidant activities of the 95% ethanol extract from Caesalpinia sappan heartwood （ECS）, protosappanin A, protosappanin B, and brazilein were studied in vitro. The inhibition of the formation of malondialdehyde （MDA） and the scavenging of superoxide anions, hydrogen peroxide, and hydroxyl radicals were assayed. The experimental results show that all four substances had antioxidant activity in vitro but their capabilities differed for the different indicators. ECS, protosappanin A, and protosappanin B show more inhibition of MDA and scavenging of hydrogen peroxide, while brazilein shows more scavenging of hydroxyl radicals. All the samples show little scavenging of superoxide anions.展开更多
Objective:To clarify the active constituents of the heartwoods of Caesalpinia sappan,a traditional Chinese medicine with the functions of promoting blood circulation(Huoxue in Chinese)and removing blood stasis(Quyu in...Objective:To clarify the active constituents of the heartwoods of Caesalpinia sappan,a traditional Chinese medicine with the functions of promoting blood circulation(Huoxue in Chinese)and removing blood stasis(Quyu in Chinese).Methods:The chemical constituents were isolated and purified by combination of silica gel and Sephadex LH-20 column chromatography,along with semipreparative HPLC.Their chemical structures were established by multiple spectroscopic methods and comparison with literature data.The in vitro antiplatelet aggregation activities were evaluated using mouse platelet induced by AYPGKF-NH2,a gold agonist of protease-activated receptor 4(PAR4).Results:Two new phenols,methyl 2-(4,4’,5’-trihydroxy-2’-(methoxymethyl)biphenyl-2-yloxy)acetate(1)and 1’-methylcaesalpin J(2),together with 24 known compounds(3-26),were isolated from the heartwoods of C.sappan.Among them,sappanchalcone(16)and brazilin(20)showed inhibitory activities against mouse platelet aggregation with IC50 values of 114.8μmol/L and 100.8μmol/L,respectively.Conclusion:Antiplatelet compounds from C.sappan targeting at PAR4 are reported for the first time.展开更多
文摘To study the chemical constituents of Sappan Lignum. Chemical constituents were isolated by method of solvent extraction, repeated chromatography with silica gel, Sephadex LH-20, and ODS. The structures were elucidated based on spectro- scopic data. Fourteen compounds were isolated and their structures were identified as brazilin （1）, sappanone B （2）, （E）-3-（3,4- dihydroxybenzylidene）-7-hydroxychroman-4-one （3）, 3-deoxysappanone B （4）, brazilide A （5）, euxanthone （6）, quercetin （7）, rhamnetin （8）, sappanchalcone （9）, 3-deoxysappanchalcone （10）, butein （11）, 2,4,5-trihydroxybenzaldehyde （12）, 3,8,9-trihydroxy- 6H-benzo[c]chromen-6-one （13） and 13-sitosterol （14）. Compounds 12 and 13 were two new natural compounds, and the ^13C NMR data of compound 13 were reported for the first time. Compound 6 was the first xanthone isolated from the genus Caesalpinia.
基金supported by the China National Natural Science Foundation Grant(Nos.9112970181102848+1 种基金31129004)the China National Science and Technology 973 grant(No.2012CB910704)
文摘AIM: To investigate the active constituents of Lignum Sappan(Caesalpinia sappan L.) on growth-related signaling and cell mitosis. METHOD: The influence of the ethyl acetate(EtOAc) extract of Lignum Sappan and its constituents on growth-related signaling were evaluated by a luciferase assay in cells stably- transfected with NF-κB, STAT1, or STAT3 responsive luciferase reporter plasmid. The inhibitory effect on the cell cycle was determined by flow cytometric analysis. The anti-tumor activities were assessed in vitro and in vivo. RESULTS: The EtOAc extract of Lignum Sappan had inhibitory activities on growth-related signaling and cell mitosis. Three major active compounds were sappanchalcone, brazilin, and butein. Sappanchalcone blocked cell cycle progression in the G2/M phase, brazilin inhibited TNFα/NF-κB signaling, while butein inhibited IL-6/STAT3 signaling, as well as TNFα/NF-κB signaling. The three compounds all demonstrated cytotoxic activities against human tumor cells in vitro. In a S180 tumor cell-bearing mice model, the anti-tumor efficacy of the EtOAc extract was better than the individual compounds acting alone. CONCLUSION: These results indicate that Lignum Sappan contains multiple active compounds with different antitumor activities, which act synergistically to enhance their anti-tumor effects. The EtOAc extract of Lignum Sappan may be better than individual active constituent as a novel medicine for the treatment of cancer.
文摘Determination of brazilin by High Performance Liquid Chromatography （HPLC） method and measurement of the antioxidative and lipase inhibition effects in the Caesalpinia sappan wood from various locations in Indonesia is described in this paper. Brazilin was separated from sample matrix using a reversed phase C 18, Shim-pack VP column with the mobile phase in a gradient elution for45 min from 5% to 100% methanol in 0.05% aqueous trifluoroacetic acid. Brazilin in ethanolic extracts ofC. sappan wood was in the range of 5.81 to 24.85 mg/g on dry-weight basis. Antioxidant and lipase inhibition activities expressed by IC50 values from all samples were in the range from 6.60 to 11.53 μg/mL and 50.76 to 203.21 μg/mL, respectively. Antioxidative and lipase inhibition potency of all ethanolic extracts were compared to vitamin C and chloramphenicol, isopropyl methylphenol and tetracyclin, respectively.
文摘Caesalpinia sappan L.(CS) is a plant of Leguminosae family,commonly known as Brazil or Sappan wood.CS is distributed in Southeast Asia and its dried heartwood has been used as traditional ingredient of food or beverages and has a wide variety of medicinal properties.Higher extraction yield of CS wood was achieved with 95% ethanol for 2 h.Chemical constituent's investigation of sappan wood resulled in the isolation of various structural types of phenolic components including one xanihone,one coumarin,three chalcones,two flavones three homoisoflavonoids and brazilin.Brazilin[(6a S-cis)-7,11b-dihydrobcnz[b]indeno[1.2-d]pyran-3.6a.9.10(6H)- tetroll.a major and active compound found in CS heartwood.Most of the folkloric uses of brazilin were validated by the scientific studies such as antioxidant,antibacterial,anti-inflammatory,anti-photoaging.hypoglycemic,vasorelaxant,hepatoproteetive and anti-acne activity.CS heartwood extract is safe and did not produce any acute or subacute toxicity in both male and female rats.Brazilin is the safe natural compound having potential to develop as a medicinal compound with application in food,beverage,cosmetics and pharmaceutical industries to screen its clinical use in modern medicine.The information gained could provide the important and potential approach for pharmaceutical researcher to implicate the knowledge of brazilin in the formulation of new drug and to reveal therapeutic and gaps requiring future research opportunities.More studies are needed to evaluate the potential application of brazilin as preservative and coloring agent in food processing industries.
基金supported by the Technological Innovation R&D Program(No.S2443581)funded by the Small and Medium Business Administration(SMBA,Korea)
文摘Caesalpinia sappan L., belonging to the family Leguminosae, is a medicinal plant that is distributed in Southeast Asia. The dried heartwood of this plant is used as a traditional ingredient of food, red dyes, and folk medicines in the treatment of diarrhea, dysentery, tuberculosis, skin infections, and inflammation. Brazilin is the major active compound, which has exhibited various phar- macological effects, including anti-platelet activity, anti-hepatotoxicity, induction of immunological tolerance, and anti-inflammatory and antioxidant activities. The present study aimed to evaluate the antioxidant activity and expression of antioxidant enzymes of C. sappan L. extract and its major compound, brazilin, in human epidermal keratinocytes exposed to UVA irradiation. Our results indi- cated that C. sappan L. extract reduced UVA-induced H202 production via GPX7 activation. Moreover, brazilin exhibited anfioxidant effects that were similar to those of C. sappan L. via glutathione peroxidase 7 （GPX7）, suggesting that C. sappan L. extract and its natural compound represent potential treatments for oxidative stress-induced photoaging of skin.
基金the Research Institute of Rangsit University for financial support (Grant No. 14/2560)
文摘Objective: The objective of the work was to optimize the extraction conditions of Caesalpinia sappan L.heartwood in order to maximize the brazilin content and antibacterial activity of the extract.Methods: Two independent factors were studied: extraction temperature(45–95 °C) and extraction time(30–60 min). In addition, five dependent factors were monitored, including extraction yield, brazilin content, and clear zones against Staphylococcus aureus TISTR 1466, Staphylococcus epidermidis TISTR 518 and Propionibacterium acnes DMST 14961. The brazilin content was quantified by high-performance liquid chromatography and antibacterial activity was determined by disk diffusion assay.Results: The high temperature provided high total extract yield as well as brazilin content, while extraction time had little effect on yield or brazilin content. Extraction time had a positive effect, while extraction temperature had little effect on clear zone against S. aureus. The largest clear zone against S. epidermidis was achieved at low extraction temperature and long extraction time. Conversely, short extraction time and high extraction temperature provided the largest clear zone against P. acnes. The optimal conditions providing the highest brazilin content was an extraction temperature and extraction time of 95 °C and 30 min, respectively.The same optimal conditions also provided the simultaneous greatest antibacterial activity against the three bacteria. Modeled optimal conditions were validated be conducting extraction using these values. Yield and antibacterial activity of the resulting extract demonstrated that the model had a low percentage error.Conclusion: The optimal condition will be used as a standard condition for extraction of C. sappan heartwood to maximize brazilin content and antibacterial activity.
基金Supported by Beijing University of Chinese Medicine Fundamental Research Funds for Young and Middle-aged Teachers in 2015(No.2015-JYB-JSMS006)
文摘OBJECTIVE: To investigate the inhibitory effect of Sumu(Lignum Sappan) plus Fuzi(Radix Aconiti Lateralis Praeparata)(SF) on the growth and metastasis of Lewis lung carcinoma.METHODS: A lung carcinoma model was established by subcutaneously inoculating Lewis lung carcinoma cells into C57 BL/6 mice. The mice were randomly divided into four groups of 13 mice(control, low-dose, moderate-dose, and high-dose), and gavaged once-daily for 21 consecutive days. The rates of tumor inhibition, metastasis, and metastasis inhibition were observed. The differential expressions of s P-selectin and vascular endothelial growth factor C(VEGFC) were compared between the treatment groups and the control group.RESULTS: The tumor weights differed significantly between the treatment groups and the control group(P < 0.05). Administration of SF in the moderate-dosage and low-dose groups significantly inhibited the expression of s P-selectin and VEGFC(both P < 0.05), suggesting anti-tumor activity.CONCLUSION: SF can inhibit the growth and metastasis of Lewis lung carcinoma.
基金financial support of the National Science & Technology Major Project ‘‘Key New Drug Creation and Manufacturing Program’’ (No.2012ZX09301001-001)the National Natural Science Funds (No.81302657,81473112,81573305)+1 种基金the Chinese Academy of Sciences (No.KSZD-EW-Z-004-01)the Shanghai Commission of Science and Technology (No.12JC1410300)
文摘Two new rearranged diterpenoids, tomocinol C （1） and spirocaesalmin C （2） were isolated from the seeds of Caesalpinia sappan. Their structures were elucidated based on comprehensive analysis of spectroscopic data, and their absolute configurations were established by single crystal X-ray crystallography.
基金Financial support by Science and Technology Development Fund, Macao S.A.R (No. FDCT 120/2013/A3)the Research Fund of University of Macao (Nos. MYRG2014-00020-ICMS-QRCM and MYRG2015-00153-ICMS-QRCM)
文摘Phytochemical investigation on the seeds of Caesalpinia sappan led to the isolation of five new cassanetype diterpenoids, named 11-oxo-phanginin A（1）, caesalsappanins O–Q（2–4） and phanginin U（5）,together with five known compounds. The structures of the new compounds were elucidated by extensive analysis of mass spectrometric and 1D and 2D NMR spectroscopic data. All the new compounds showed moderate cytotoxic effects on human breast cancer MCF-7 and human colon cancer HCT116 cell lines.
文摘Natural dyes taken from the barks of the tree Caesalpinia sappan has been used in many consumer products.Hence it is imperative to test the toxicity of this dye.In the present study an investigation was conducted to find out the toxic effect of aqueous extract of the dye C.sappan in test animal Wister albino rats.Acute oral toxicity showed no clinical signs of toxicity and no mortality even at a dose level of 100–2000 mg/kg in 14 days observation period.When a dose level above 2500 mg/kg was given for 28 days,no death was noticed up to the dose level 5000 mg/kg body weight.The weight of the tested rats was not significantly reduced,when compared with the control group.The organ-body weight ratio of kidney,liver and abdomen did not change when compared to the control group in the observation period.The less toxicity of the dyes of C.sappan.
基金the National Natural Science Foundation of China(No. 30572340)the Fund for Doctoral Station of the Ministry of Education, China (No. 20060003072)the Key Technologies Research and Development Program of the 11th Five-Year Plan of China (No. 2006BAI08B03-09)
文摘Antioxidant activities of the 95% ethanol extract from Caesalpinia sappan heartwood （ECS）, protosappanin A, protosappanin B, and brazilein were studied in vitro. The inhibition of the formation of malondialdehyde （MDA） and the scavenging of superoxide anions, hydrogen peroxide, and hydroxyl radicals were assayed. The experimental results show that all four substances had antioxidant activity in vitro but their capabilities differed for the different indicators. ECS, protosappanin A, and protosappanin B show more inhibition of MDA and scavenging of hydrogen peroxide, while brazilein shows more scavenging of hydroxyl radicals. All the samples show little scavenging of superoxide anions.
基金supported by the International Partnership Program of Chinese Academy of Sciences(153631KYSB20160004)the Southeast Asia Biodiversity Research Institute,Chinese Academy of Sciences(Y4ZK111B01).
文摘Objective:To clarify the active constituents of the heartwoods of Caesalpinia sappan,a traditional Chinese medicine with the functions of promoting blood circulation(Huoxue in Chinese)and removing blood stasis(Quyu in Chinese).Methods:The chemical constituents were isolated and purified by combination of silica gel and Sephadex LH-20 column chromatography,along with semipreparative HPLC.Their chemical structures were established by multiple spectroscopic methods and comparison with literature data.The in vitro antiplatelet aggregation activities were evaluated using mouse platelet induced by AYPGKF-NH2,a gold agonist of protease-activated receptor 4(PAR4).Results:Two new phenols,methyl 2-(4,4’,5’-trihydroxy-2’-(methoxymethyl)biphenyl-2-yloxy)acetate(1)and 1’-methylcaesalpin J(2),together with 24 known compounds(3-26),were isolated from the heartwoods of C.sappan.Among them,sappanchalcone(16)and brazilin(20)showed inhibitory activities against mouse platelet aggregation with IC50 values of 114.8μmol/L and 100.8μmol/L,respectively.Conclusion:Antiplatelet compounds from C.sappan targeting at PAR4 are reported for the first time.
