Flavonoids are by far the most dominant class of phenolic compounds isolated from Morus alba leaves(MAL). Other classes of compounds are benzofurans, phenolic acids, alkaloids, coumarins, chalcones and stilbenes. Majo...Flavonoids are by far the most dominant class of phenolic compounds isolated from Morus alba leaves(MAL). Other classes of compounds are benzofurans, phenolic acids, alkaloids, coumarins, chalcones and stilbenes. Major flavonoids are kuwanons, moracinflavans, moragrols and morkotins. Other major compounds include moracins(benzofurans), caffeoylquinic acids(phenolic acids) and morachalcones(chalcones). Research on the anticancer properties of MAL entailed in vitro and in vivo cytotoxicity of extracts or isolated compounds. Flavonoids, benzofurans, chalcones and alkaloids are classes of compounds from MAL that have been found to be cytotoxic towards human cancer cell lines. Further studies on the phytochemistry and anticancer of MAL are suggested. Sources of information were Pub Med,Pub Med Central, Science Direct, Google, Google Scholar, J-Stage, Pub Chem and China National Knowledge Infrastructure.展开更多
The root bark of Morus alba L. or white mulberry is widely used as traditional medicine in China, Japan and Korea. Major classes and types of phenolic compounds isolated from the root bark are flavonoids(kuwanons, mor...The root bark of Morus alba L. or white mulberry is widely used as traditional medicine in China, Japan and Korea. Major classes and types of phenolic compounds isolated from the root bark are flavonoids(kuwanons, morusin, cyclomorusin and sanggenons), benzofurans(moracins and mulberrofurans), and stilbenoids(mulberrosides). Some of the flavonoids and benzofurans are products of Diel-Alder type adducts. Other classes of compounds include triterpenes, phenolic acids and coumarins. Morusin, a prenylated flavonoid, was first isolated from the root bark of M. alba, and later from the leaf, stem bark and twig of the plant. The potent anti-cancer properties of morusin have attracted much attention with research on-going and new findings being published. The compound inhibits angiogenesis, tumour progression and tumour migration, and triggers apoptosis, cell cycle arrest and autophagy in colorectal, cervical, prostate, breast, hepatoma, pancreatic, glioblastoma, gastric, ovarian and lung cancer cell lines. The anti-cancer activities of morusin are executed via various molecular targets and signalling pathways. It is anticipated that on-going in vitro studies will progress gradually to in vivo studies using animal models before efforts towards drug development can be initiated for clinical trials.展开更多
Benzofuran is an essential structural component found in a wide range of natural products,agrochemicals and drugs,possessing a range of biological activities.In recent years,there have been numerous reports of success...Benzofuran is an essential structural component found in a wide range of natural products,agrochemicals and drugs,possessing a range of biological activities.In recent years,there have been numerous reports of successful syntheses of benzofuran derivatives via intra-and inter-molecular cyclizations using diverse catalysts.This review gives an exhaustive and methodical survey of the procedures for making benzofurans.展开更多
AIM:To investigate the pathway(s)mediating rat antral circular smooth muscle contractile responses to the cholinomimetic agent,bethanechol and the subtypes of muscarinic receptors mediating the cholinergic contraction...AIM:To investigate the pathway(s)mediating rat antral circular smooth muscle contractile responses to the cholinomimetic agent,bethanechol and the subtypes of muscarinic receptors mediating the cholinergic contraction. METHODS:Circular smooth muscle strips from the antrum of Sprague-Dawley rats were mounted in muscle baths in Krebs buffer.Isometric tension was recorded.Cumulative concentration-response curves were obtained for(+)-cis- dioxolane(cD),a nonspecific muscarinic agonist,at 10^(-8)- 10^(-4)mol/L,in the presence of tetrodotoxin(TTX,10^(-7)mol/L). Results were normalized to cross sectional area.A repeat concentration-response curve was obtained after incubation of the muscle for 90 min with antagonists for M1(pirenzepine), M2(methoctramine)and M3(darifenadn)muscarinic receptor subtypes.The sensitivity to PTX was tested by the ip injection of 100 mg/kg of PTX 5 d before the experiment.The antral circular smooth muscles were removed from PTX-treated and non-treated rats as strips and dispersed smooth muscle cells to identify whether PTX-linked pathway mediated the contractility to bethanechol. RESULTS:A dose-dependent contractile response observed with bethanechol,was not affected by TTx.The pretreatment of rats with pertussis toxin decreased the contraction induced by bethanechol.Lack of calcium as well as the presence of the L-type calcium channel blocker,nifedipine,also inhibited the cholinergic contraction,with a reduction in response from 2.5±0.4 g/mm^2 to 1.2±0.4 g/mm^2(P<0.05).The dose- response curves were shifted to the right by muscarinic antagonists in the following order of affinity:darifenacin (M_3)>methocramine(M_2)>pirenzepine(M_1). CONCLUSION:The muscarinic receptors-dependent contraction of rat antral circular smooth muscles was linked to the signal transduction pathway(s)involving pertussis-toxin sensitive GTP-binding proteins and to extracellular calcium via L-type voltage gated calcium channels.The presence of the residual contractile response after the treatment with nifedipine,sugges展开更多
Chemodivergent synthesis of benzofurans and 2,3-dihydrobenzofurans has been realized.Under a reaction system consisting of DBDMH and K_(2)CO_(3) as promotors,controlled conditions enabled the formation of two sets of ...Chemodivergent synthesis of benzofurans and 2,3-dihydrobenzofurans has been realized.Under a reaction system consisting of DBDMH and K_(2)CO_(3) as promotors,controlled conditions enabled the formation of two sets of valuable heterocycles from the tandem transformation of enaminones and salicylaldehydes.The key to success was the identification of the reaction parameters,in which the imine intermediate which was formed by transient halogenation coupling and substitution processes underwent either aldol condensation/annulation or imine hydrolysis/aldol condensation.The additives NH_(4)Cl or Fe_(2)(SO_(4))_(3) controlled the unique selectivity of this reaction.A broad substrate scope of enaminones and salicylaldehydes has been employed in this reaction,demonstrating excellent functional group tolerance and versatility.展开更多
A new and convenient visible-light-induced method has been developed for the synthesis of sulfonylated benzofurans via oxidative cyclization reaction of 1,6-enynes and arylsulfinic acids.This reaction was carried out ...A new and convenient visible-light-induced method has been developed for the synthesis of sulfonylated benzofurans via oxidative cyclization reaction of 1,6-enynes and arylsulfinic acids.This reaction was carried out under metal-free and mild conditions,in which the C-S,C-C and C=O bonds could be sequentially formed in one pot operation.展开更多
以3,4-二羟基苯丙烯酸（咖啡酸）为原料,经酯化和仿生氧化偶联反应得到苯并呋喃类化合物2-（3′,4′-二羟基苯基）-3-甲氧羰基-5-甲氧羰基乙烯基-7-羟基-2,3-二氢苯并呋喃（1）和苯并二氧六环类化合物2-（3′,4′-二羟基苯基）-3-甲氧羰...以3,4-二羟基苯丙烯酸（咖啡酸）为原料,经酯化和仿生氧化偶联反应得到苯并呋喃类化合物2-（3′,4′-二羟基苯基）-3-甲氧羰基-5-甲氧羰基乙烯基-7-羟基-2,3-二氢苯并呋喃（1）和苯并二氧六环类化合物2-（3′,4′-二羟基苯基）-3-甲氧羰基-6-甲氧羰基乙烯基-2,3-二氢-1,4-苯并二氧六环（2）,然后经乙酰化、DDQ氧化脱氢、Pd/C 催化氢化、氢化铝锂还原、碱性条件下脱乙酰基等反应,合成了一系列苯并呋喃新木脂素类化合物3~7和苯并二氧六环新木脂素类化合物8~10.所合成化合物的结构已由核磁共振法（1 H NMR,13 C NMR）、质谱法（MS）进行了表征.其中5~7,9和10是未见文献报道的新化合物,8为天然产物异美商陆醇A.采用MTT法对所合成的苯并呋喃新木脂素类化合物1,3~5进行了生物活性测试.结果表明：化合物1,3,4和5对白血病细胞（HL-60）、肺癌细胞（A-549）、乳腺癌细胞（MCF-7）、结肠癌细胞（SW-480）、肝癌细胞（SMMC-7721）有良好的体外生长抑制活性.展开更多
The deconstructive reorganization strategy for the synthesis of benzene-containing products from the kojic acid-and maltol-derived alkynes has been recently reported.In this strategy,kojic acid and maltol are analogou...The deconstructive reorganization strategy for the synthesis of benzene-containing products from the kojic acid-and maltol-derived alkynes has been recently reported.In this strategy,kojic acid and maltol are analogous to the"Transformers",which can transform into benzofurans and benzaldehydes via annulation reactions.Under the synthetic standpoint,this deconstructive reorganization strategy features high atom economy,innate scalability and functional group tolerance.In the near future,we believe that this unique method will be widely investigated a nd other novel transformations of kojic acid and maltol will be discovered.展开更多
文摘Flavonoids are by far the most dominant class of phenolic compounds isolated from Morus alba leaves(MAL). Other classes of compounds are benzofurans, phenolic acids, alkaloids, coumarins, chalcones and stilbenes. Major flavonoids are kuwanons, moracinflavans, moragrols and morkotins. Other major compounds include moracins(benzofurans), caffeoylquinic acids(phenolic acids) and morachalcones(chalcones). Research on the anticancer properties of MAL entailed in vitro and in vivo cytotoxicity of extracts or isolated compounds. Flavonoids, benzofurans, chalcones and alkaloids are classes of compounds from MAL that have been found to be cytotoxic towards human cancer cell lines. Further studies on the phytochemistry and anticancer of MAL are suggested. Sources of information were Pub Med,Pub Med Central, Science Direct, Google, Google Scholar, J-Stage, Pub Chem and China National Knowledge Infrastructure.
文摘The root bark of Morus alba L. or white mulberry is widely used as traditional medicine in China, Japan and Korea. Major classes and types of phenolic compounds isolated from the root bark are flavonoids(kuwanons, morusin, cyclomorusin and sanggenons), benzofurans(moracins and mulberrofurans), and stilbenoids(mulberrosides). Some of the flavonoids and benzofurans are products of Diel-Alder type adducts. Other classes of compounds include triterpenes, phenolic acids and coumarins. Morusin, a prenylated flavonoid, was first isolated from the root bark of M. alba, and later from the leaf, stem bark and twig of the plant. The potent anti-cancer properties of morusin have attracted much attention with research on-going and new findings being published. The compound inhibits angiogenesis, tumour progression and tumour migration, and triggers apoptosis, cell cycle arrest and autophagy in colorectal, cervical, prostate, breast, hepatoma, pancreatic, glioblastoma, gastric, ovarian and lung cancer cell lines. The anti-cancer activities of morusin are executed via various molecular targets and signalling pathways. It is anticipated that on-going in vitro studies will progress gradually to in vivo studies using animal models before efforts towards drug development can be initiated for clinical trials.
文摘Benzofuran is an essential structural component found in a wide range of natural products,agrochemicals and drugs,possessing a range of biological activities.In recent years,there have been numerous reports of successful syntheses of benzofuran derivatives via intra-and inter-molecular cyclizations using diverse catalysts.This review gives an exhaustive and methodical survey of the procedures for making benzofurans.
文摘AIM:To investigate the pathway(s)mediating rat antral circular smooth muscle contractile responses to the cholinomimetic agent,bethanechol and the subtypes of muscarinic receptors mediating the cholinergic contraction. METHODS:Circular smooth muscle strips from the antrum of Sprague-Dawley rats were mounted in muscle baths in Krebs buffer.Isometric tension was recorded.Cumulative concentration-response curves were obtained for(+)-cis- dioxolane(cD),a nonspecific muscarinic agonist,at 10^(-8)- 10^(-4)mol/L,in the presence of tetrodotoxin(TTX,10^(-7)mol/L). Results were normalized to cross sectional area.A repeat concentration-response curve was obtained after incubation of the muscle for 90 min with antagonists for M1(pirenzepine), M2(methoctramine)and M3(darifenadn)muscarinic receptor subtypes.The sensitivity to PTX was tested by the ip injection of 100 mg/kg of PTX 5 d before the experiment.The antral circular smooth muscles were removed from PTX-treated and non-treated rats as strips and dispersed smooth muscle cells to identify whether PTX-linked pathway mediated the contractility to bethanechol. RESULTS:A dose-dependent contractile response observed with bethanechol,was not affected by TTx.The pretreatment of rats with pertussis toxin decreased the contraction induced by bethanechol.Lack of calcium as well as the presence of the L-type calcium channel blocker,nifedipine,also inhibited the cholinergic contraction,with a reduction in response from 2.5±0.4 g/mm^2 to 1.2±0.4 g/mm^2(P<0.05).The dose- response curves were shifted to the right by muscarinic antagonists in the following order of affinity:darifenacin (M_3)>methocramine(M_2)>pirenzepine(M_1). CONCLUSION:The muscarinic receptors-dependent contraction of rat antral circular smooth muscles was linked to the signal transduction pathway(s)involving pertussis-toxin sensitive GTP-binding proteins and to extracellular calcium via L-type voltage gated calcium channels.The presence of the residual contractile response after the treatment with nifedipine,sugges
基金the Science and Technology Foundation of Henan Province(222102310580)Innovation and Entrepreneurship Training Program for College StudentsHenan University of Science and Technology(2023180).
文摘Chemodivergent synthesis of benzofurans and 2,3-dihydrobenzofurans has been realized.Under a reaction system consisting of DBDMH and K_(2)CO_(3) as promotors,controlled conditions enabled the formation of two sets of valuable heterocycles from the tandem transformation of enaminones and salicylaldehydes.The key to success was the identification of the reaction parameters,in which the imine intermediate which was formed by transient halogenation coupling and substitution processes underwent either aldol condensation/annulation or imine hydrolysis/aldol condensation.The additives NH_(4)Cl or Fe_(2)(SO_(4))_(3) controlled the unique selectivity of this reaction.A broad substrate scope of enaminones and salicylaldehydes has been employed in this reaction,demonstrating excellent functional group tolerance and versatility.
基金supported by the Natural Science Foundation of Shandong Province (No. ZR2018MB009)the International Cooperation Project of Qinghai Province (No. 2018-HZ-806)+1 种基金the Qinghai Key Laboratory of Tibetan Medicine Research (No. 2017-ZJ-Y11)the National Natural Science Foundation of China (No. 21302109)
文摘A new and convenient visible-light-induced method has been developed for the synthesis of sulfonylated benzofurans via oxidative cyclization reaction of 1,6-enynes and arylsulfinic acids.This reaction was carried out under metal-free and mild conditions,in which the C-S,C-C and C=O bonds could be sequentially formed in one pot operation.
文摘以3,4-二羟基苯丙烯酸（咖啡酸）为原料,经酯化和仿生氧化偶联反应得到苯并呋喃类化合物2-（3′,4′-二羟基苯基）-3-甲氧羰基-5-甲氧羰基乙烯基-7-羟基-2,3-二氢苯并呋喃（1）和苯并二氧六环类化合物2-（3′,4′-二羟基苯基）-3-甲氧羰基-6-甲氧羰基乙烯基-2,3-二氢-1,4-苯并二氧六环（2）,然后经乙酰化、DDQ氧化脱氢、Pd/C 催化氢化、氢化铝锂还原、碱性条件下脱乙酰基等反应,合成了一系列苯并呋喃新木脂素类化合物3~7和苯并二氧六环新木脂素类化合物8~10.所合成化合物的结构已由核磁共振法（1 H NMR,13 C NMR）、质谱法（MS）进行了表征.其中5~7,9和10是未见文献报道的新化合物,8为天然产物异美商陆醇A.采用MTT法对所合成的苯并呋喃新木脂素类化合物1,3~5进行了生物活性测试.结果表明：化合物1,3,4和5对白血病细胞（HL-60）、肺癌细胞（A-549）、乳腺癌细胞（MCF-7）、结肠癌细胞（SW-480）、肝癌细胞（SMMC-7721）有良好的体外生长抑制活性.
基金the National Natural Science Foundation of China(Nos.21871053 and 21532001)the Leading Innovative and Entrepreneur Team Introduction Program of Zhejiang(No.2019R01005)。
文摘The deconstructive reorganization strategy for the synthesis of benzene-containing products from the kojic acid-and maltol-derived alkynes has been recently reported.In this strategy,kojic acid and maltol are analogous to the"Transformers",which can transform into benzofurans and benzaldehydes via annulation reactions.Under the synthetic standpoint,this deconstructive reorganization strategy features high atom economy,innate scalability and functional group tolerance.In the near future,we believe that this unique method will be widely investigated a nd other novel transformations of kojic acid and maltol will be discovered.
