A new cassane diterpenoid lactone was isolated from the seed of Caesalpinia minax. On the basis of spectral evidences, its structure was established as 12α-methoxyl, 5α, 14β-dihydroxy-1α, 6α, 7β-triacetoxycass-1...A new cassane diterpenoid lactone was isolated from the seed of Caesalpinia minax. On the basis of spectral evidences, its structure was established as 12α-methoxyl, 5α, 14β-dihydroxy-1α, 6α, 7β-triacetoxycass-13（15）-en-16, 12-olide.展开更多
A new homoflavonoid was isolated from the seed of Caesalpinia minax Hance.On the basis of spectral evidences,its structure was established and named as minaxin.
Caesalpinia minax has a long history of use as a Chinese traditional herb medicine in Yunnan Province, China, for the treatment of skin-related diseases. A potent melanoma inhibitor, purified from the seeds of C. mina...Caesalpinia minax has a long history of use as a Chinese traditional herb medicine in Yunnan Province, China, for the treatment of skin-related diseases. A potent melanoma inhibitor, purified from the seeds of C. minaxand termed Caesalpinia minax protein (CMP), is a protein with a relative molecular mass of 19.8×10 3. Experiments were conducted to assay the inhibitive effects of CMP on the proliferation, migration, and adhesion of murine melanoma cell line K1735M2. The results showed that cell proliferation was suppressed by about 60% with treatment of 22 μg/mL CMP. Furthermore, the migration of K1735M2 cells was inhibited by 30% in the presence of 22 μg/mL CMP. The results also demonstrated that the inhibitive effect of CMP on the migration was dose-dependent. Although low-doses of CMP had no obvious inhibitive effect on the adhesion of K1735M2, 22 μg/mL CMP inhibited the adhesion of K1735M2 by 50%. These results suggest that CMP might be a potential medicine for melanoma therapy.展开更多
Trehalose is the principal sugar circulating in the hemolymph of insects,and trehalose synthesis is catalyzed by trehalose-6-phosphate synthase(TPS)and trehalose-6-phosphate phosphatase(TPP).Insect TPS is a fused enzy...Trehalose is the principal sugar circulating in the hemolymph of insects,and trehalose synthesis is catalyzed by trehalose-6-phosphate synthase(TPS)and trehalose-6-phosphate phosphatase(TPP).Insect TPS is a fused enzyme containing both TPS do-main and TPP domain.Thus,many insects do not possess TPP genes as TPSs have re-placed the function of TPPs.However,TPPs are widely distributed across the dipteran insects,while the roles they play remain largely unknown.In this study,3 TPP genes from notorious dipteran pest Bactrocera minax(BmiTPPB,BmiTPPCl,and BmiTPPC2)were identified and characterized.The different temporal-spatial expression patterns of 3 BmiTPPs implied that they exert different functions in B.minax.Recombinant BmiTPPs were heterologously expressed in yeast cells,and all purified proteins exhibited enzy-matic activities,despite the remarkable disparity in performance between BmiTPPB and BmiTPPCs.RNA interference revealed that all BmiTPPs were successfully downregulated after double-stranded RNA injection,leading to decreased trehalose content and increased glucose content.Also,suppression of BmiTPPs significantly affected expression of down-stream genes and increased the mortality and malformation rate.Collectively,these results indicated that all 3 BmiTPPs in B.minax are involved in trehalose synthesis and metamor-phosis.Thus,these genes could be evaluated as insecticidal targets for managing B.minax,andevenforotherdipteranpests.展开更多
To search naturally occurring interleukin-1β(IL-1β) inhibitors,biscaesalmins A(1) and B(2),two highly oxidized dimeric cassane diterpenoids with a newly formed alicyclic skeleton,have been isolated from the traditio...To search naturally occurring interleukin-1β(IL-1β) inhibitors,biscaesalmins A(1) and B(2),two highly oxidized dimeric cassane diterpenoids with a newly formed alicyclic skeleton,have been isolated from the traditional Chinese medicine Kushilian(Caesalpinia minax).Their full structures were determined by comprehensive spectroscopic analysis and quantum chemical TD-DFT(time-dependent density functional theory) calculation.Biosynthetically,1 and 2 were formed via an intermolecular [4+2]Diels-Alder cycloaddition of two monomers,affording an additional six-membered carbon ring linkage.Compounds 1 and 2 inhibited nitric oxide production on lipopolysaccharide-stimulated THP-1 macrophages,with IC_(50) values being at 1.20±0.23 and 2.30±0.15 μmol/L,respectively.Furthermore,compound 1 inhibited NLRP3(NOD-,LRR-and pyrin domain-containing protein 3) inflammasomemediated IL-1β production and blocked the migration of macrophages towards adipocyte conditioned medium.Biscaesalmins A and B might be candidates for treating inflammation-related metabolic diseases.展开更多
基金supported by the science and technology grant of Guangxi province(No.0639039)special purpose of basic scientific research operation grant for commonweal academy and institute of central authorities(No.YZ-1-24).
文摘A new cassane diterpenoid lactone was isolated from the seed of Caesalpinia minax. On the basis of spectral evidences, its structure was established as 12α-methoxyl, 5α, 14β-dihydroxy-1α, 6α, 7β-triacetoxycass-13（15）-en-16, 12-olide.
基金supported by the technological large platform for comprehensive research and development of new drugs in the Eleventh Five-Year"Significant New Drugs Created"Science and Technology Major Projects(No. 2009ZX09301-003)National Natural Science Foundation of China(No.30973626)+2 种基金the Science and Technology Grant of Guangxi Province(No.0639039)special purpose of basic scientific research operation grant for Commonweal Academy and Institute of Central Authorities(No.YZ-1-24)Innovation capacity-building in Guangxi Science and Technology Agency(0443002-2)
文摘A new homoflavonoid was isolated from the seed of Caesalpinia minax Hance.On the basis of spectral evidences,its structure was established and named as minaxin.
基金Supported by the Foundation of Combined ResearchProject of Tsinghua University,Hong Kong BaptistUniversity and Beijing University of Chinese Medicineon Chinese Traditional Medicine
文摘Caesalpinia minax has a long history of use as a Chinese traditional herb medicine in Yunnan Province, China, for the treatment of skin-related diseases. A potent melanoma inhibitor, purified from the seeds of C. minaxand termed Caesalpinia minax protein (CMP), is a protein with a relative molecular mass of 19.8×10 3. Experiments were conducted to assay the inhibitive effects of CMP on the proliferation, migration, and adhesion of murine melanoma cell line K1735M2. The results showed that cell proliferation was suppressed by about 60% with treatment of 22 μg/mL CMP. Furthermore, the migration of K1735M2 cells was inhibited by 30% in the presence of 22 μg/mL CMP. The results also demonstrated that the inhibitive effect of CMP on the migration was dose-dependent. Although low-doses of CMP had no obvious inhibitive effect on the adhesion of K1735M2, 22 μg/mL CMP inhibited the adhesion of K1735M2 by 50%. These results suggest that CMP might be a potential medicine for melanoma therapy.
基金supported by Natural Science Foundation of Chongqing(cstc202ljcyj-msxmX1054)the Fundamental Research Funds forthe Central Universities(XDJK2018C092).
文摘Trehalose is the principal sugar circulating in the hemolymph of insects,and trehalose synthesis is catalyzed by trehalose-6-phosphate synthase(TPS)and trehalose-6-phosphate phosphatase(TPP).Insect TPS is a fused enzyme containing both TPS do-main and TPP domain.Thus,many insects do not possess TPP genes as TPSs have re-placed the function of TPPs.However,TPPs are widely distributed across the dipteran insects,while the roles they play remain largely unknown.In this study,3 TPP genes from notorious dipteran pest Bactrocera minax(BmiTPPB,BmiTPPCl,and BmiTPPC2)were identified and characterized.The different temporal-spatial expression patterns of 3 BmiTPPs implied that they exert different functions in B.minax.Recombinant BmiTPPs were heterologously expressed in yeast cells,and all purified proteins exhibited enzy-matic activities,despite the remarkable disparity in performance between BmiTPPB and BmiTPPCs.RNA interference revealed that all BmiTPPs were successfully downregulated after double-stranded RNA injection,leading to decreased trehalose content and increased glucose content.Also,suppression of BmiTPPs significantly affected expression of down-stream genes and increased the mortality and malformation rate.Collectively,these results indicated that all 3 BmiTPPs in B.minax are involved in trehalose synthesis and metamor-phosis.Thus,these genes could be evaluated as insecticidal targets for managing B.minax,andevenforotherdipteranpests.
基金the financial support of the Science and Technology Development Fund,Macao SAR (No.FDCT 0031/2019/ A1)the National Natural Science Foundation of China (Nos. 81872754 and 81872756)University of Macao,Macao SAR (Nos.MYRG2017-00109-ICMS and MYRG2018-00037-ICMS)。
文摘To search naturally occurring interleukin-1β(IL-1β) inhibitors,biscaesalmins A(1) and B(2),two highly oxidized dimeric cassane diterpenoids with a newly formed alicyclic skeleton,have been isolated from the traditional Chinese medicine Kushilian(Caesalpinia minax).Their full structures were determined by comprehensive spectroscopic analysis and quantum chemical TD-DFT(time-dependent density functional theory) calculation.Biosynthetically,1 and 2 were formed via an intermolecular [4+2]Diels-Alder cycloaddition of two monomers,affording an additional six-membered carbon ring linkage.Compounds 1 and 2 inhibited nitric oxide production on lipopolysaccharide-stimulated THP-1 macrophages,with IC_(50) values being at 1.20±0.23 and 2.30±0.15 μmol/L,respectively.Furthermore,compound 1 inhibited NLRP3(NOD-,LRR-and pyrin domain-containing protein 3) inflammasomemediated IL-1β production and blocked the migration of macrophages towards adipocyte conditioned medium.Biscaesalmins A and B might be candidates for treating inflammation-related metabolic diseases.
