Osteoporosis is a bone metabolic disease caused by the imbalance between osteoblasts and osteoclasts due to excess osteoclastogenesis,manifesting in the decrease of bone density and bone strength.Scutellariae Radix sh...Osteoporosis is a bone metabolic disease caused by the imbalance between osteoblasts and osteoclasts due to excess osteoclastogenesis,manifesting in the decrease of bone density and bone strength.Scutellariae Radix shows good anti-osteoporosis activity,but the effective component is still unclear.Cell membrane chromatography(CMC)is a biological affinity chromatography with membrane immobilized on a silica carrier as the stationary phase.It can realize a dynamical simulation of interactions between drugs and receptors on cell membrane,which is suitable for screening active compounds from complex systems.In this study,the components of Scutellariae Radix with potential anti-osteoporosis activity through inhibiting the differentiation from bone marrow mononuclear cells(BMMCs)to osteoclast were screened by a BMMC/CMC analytical system.Firstly,a new3-mercaptopropyltrimethoxysilane(MPTS)-modified BMMC/CMC stationary phase was developed to realize covalent binding with cell membrane fractions.By investigating the retention time(tR)of the positive drug,the life span of the MPTS-modified CMC columns was significantly improved from 3 to 12 days.Secondly,6 components of Scutellariae Radix were screened to show affinity to membrane receptors on BMMCs by a two-dimensional BMMC/CMC-TOFMS analytical system.Among them,tectochrysin demonstrated the best anti-osteoporosis effect in vitro,which has never been reported.We found that tectochrysin could inhibit the differentiation of BMMCs into osteoclasts induced by receptor activator of nuclear factor-κB ligand(RANKL)and macrophage colony-stimulating factor(M-CSF)in a concentration-dependent manner in vitro.In vivo,it significantly reduced the loss of bone trabeculae in ovariectomized mice,and decreased the level of C-terminal cross-linking telopeptides of type 1 collagen(CTX-1),tartrate-resistant acid phosphatase 5 b(TRAP-5 b),interleukin 6(IL-6)in serum.In conclusion,tectochrysin serves as a potential candidate in the treatment of osteoporosis.The proposed twodimensional MPTS-modified BMMC/CMC-TOFMS analytical system shows the advantages of longlife span and fast recognition ability,which is very suitable for infrequent cell lines.展开更多
Over the past decades,epidemiological studies have concluded that a diet rich in plant-derived products plays a pivotal role in human health.Fisetin(3,3’,4’,7-tetrahydroxyflavone)is a hydrophobic polyphenolic compou...Over the past decades,epidemiological studies have concluded that a diet rich in plant-derived products plays a pivotal role in human health.Fisetin(3,3’,4’,7-tetrahydroxyflavone)is a hydrophobic polyphenolic compound primarily found in edible plants(e.g.strawberry,blueberry,apple,grape,persimmon,kiwi,and cucumber).Various preclinical studies have revealed that fisetin exhibits a wide range of pharmacological effects such as antioxidant,antiinflammatory,anti-carcinogenic,anti-osteoporotic,antimicrobial,and anti-diabetic properties.Therefore,the pharmacological in vitro and in vivo studies on fisetin are discussed in this review.Additionally,this review would be useful for further study regarding the potential of natural products,notably fisetin,and its therapeutic potential for the prevention and treatment of diseases.展开更多
A simple and efficient procedure for synthesis of 1-hydroxymethylene-1,1-bisphos- phoates from aldehydes is described. This method was applied to the synthesis of novel catechol substituted bisphosphonates as the a...A simple and efficient procedure for synthesis of 1-hydroxymethylene-1,1-bisphos- phoates from aldehydes is described. This method was applied to the synthesis of novel catechol substituted bisphosphonates as the anti-osteoporosis agents.展开更多
Background: Alpinia officinarum Hance is valued as an edible medicinal plant. The rhizome is widely reported to have anticancer activity whereas little information is available on the aerial part. This study investiga...Background: Alpinia officinarum Hance is valued as an edible medicinal plant. The rhizome is widely reported to have anticancer activity whereas little information is available on the aerial part. This study investigates chemical composition, proapoptotic and anti-osteoporosis activities of essential oil from aerial parts of A. officinarum (APEO). Methods: In this study, APEO was extracted by hydrodistillation and analyzed using GC-MS. The inhibitive activity of 0 - 2.5 μL/mL. APEO was investigated using MTT assay, while in vivo effect was evaluated in nude mice. The cell cycle, apoptosis, Δψm and expression of proteins analyses influenced by 0 - 0.313 μL/mL APEO were detected by PI, Annexin V/PI, JC-1, and Western blot, respectively. Alkaline phosphatase activity and mineralized nodules formation of rat osteoblasts with 0 - 0.156 μL/mL APEO were assayed using colorimetric method and alizarin red staining, respectively. Results: Total 45 constituents were identified accounting for 91.1% of APEO (sesquiterpene hydrocarbons for 44.4%). APEO significantly inhibited cancer cells growth in a dose-dependent manner. APEO also inhibited cancer growth in vivo. The percentage of S phase cells is up to 64.846% with 0.313 μL/mL APEO. The proportion of total apoptotic cells significantly increased to 79.6% at 0.313 μL/mL concentration. APEO treated cells accompanied with Bcl-2 and Δψm decrease, and caspase-3 and p53 upregulation. Furthermore, addition of APEO in rat osteoblasts led to a dose-dependent increase in ALP activity and formation of mineralized bone nodules. Conclusions: Our data suggest that APEO could be developed as an agent against human lung cancer and osteoporosis, especially cancer-induced bone loss.展开更多
基金supported by the National Natural Science Foundation of China(Grant Nos.81973291 to Xiaofei Chen,81573396 to Yifeng Chai,81973275 to Yongfang Yuan,81703674 to Yue Liu,81703779 to Rong Wang,81803815 to Shaozhan Wang and 81871099 to Xiao Chen)Fund of Shanghai Science and Technology Committee,China(19QA1411500 to Xiaofei Chen,17401900800 to Yongfang Yuan and 17YF1424700 to Yue Liu)
文摘Osteoporosis is a bone metabolic disease caused by the imbalance between osteoblasts and osteoclasts due to excess osteoclastogenesis,manifesting in the decrease of bone density and bone strength.Scutellariae Radix shows good anti-osteoporosis activity,but the effective component is still unclear.Cell membrane chromatography(CMC)is a biological affinity chromatography with membrane immobilized on a silica carrier as the stationary phase.It can realize a dynamical simulation of interactions between drugs and receptors on cell membrane,which is suitable for screening active compounds from complex systems.In this study,the components of Scutellariae Radix with potential anti-osteoporosis activity through inhibiting the differentiation from bone marrow mononuclear cells(BMMCs)to osteoclast were screened by a BMMC/CMC analytical system.Firstly,a new3-mercaptopropyltrimethoxysilane(MPTS)-modified BMMC/CMC stationary phase was developed to realize covalent binding with cell membrane fractions.By investigating the retention time(tR)of the positive drug,the life span of the MPTS-modified CMC columns was significantly improved from 3 to 12 days.Secondly,6 components of Scutellariae Radix were screened to show affinity to membrane receptors on BMMCs by a two-dimensional BMMC/CMC-TOFMS analytical system.Among them,tectochrysin demonstrated the best anti-osteoporosis effect in vitro,which has never been reported.We found that tectochrysin could inhibit the differentiation of BMMCs into osteoclasts induced by receptor activator of nuclear factor-κB ligand(RANKL)and macrophage colony-stimulating factor(M-CSF)in a concentration-dependent manner in vitro.In vivo,it significantly reduced the loss of bone trabeculae in ovariectomized mice,and decreased the level of C-terminal cross-linking telopeptides of type 1 collagen(CTX-1),tartrate-resistant acid phosphatase 5 b(TRAP-5 b),interleukin 6(IL-6)in serum.In conclusion,tectochrysin serves as a potential candidate in the treatment of osteoporosis.The proposed twodimensional MPTS-modified BMMC/CMC-TOFMS analytical system shows the advantages of longlife span and fast recognition ability,which is very suitable for infrequent cell lines.
文摘Over the past decades,epidemiological studies have concluded that a diet rich in plant-derived products plays a pivotal role in human health.Fisetin(3,3’,4’,7-tetrahydroxyflavone)is a hydrophobic polyphenolic compound primarily found in edible plants(e.g.strawberry,blueberry,apple,grape,persimmon,kiwi,and cucumber).Various preclinical studies have revealed that fisetin exhibits a wide range of pharmacological effects such as antioxidant,antiinflammatory,anti-carcinogenic,anti-osteoporotic,antimicrobial,and anti-diabetic properties.Therefore,the pharmacological in vitro and in vivo studies on fisetin are discussed in this review.Additionally,this review would be useful for further study regarding the potential of natural products,notably fisetin,and its therapeutic potential for the prevention and treatment of diseases.
文摘A simple and efficient procedure for synthesis of 1-hydroxymethylene-1,1-bisphos- phoates from aldehydes is described. This method was applied to the synthesis of novel catechol substituted bisphosphonates as the anti-osteoporosis agents.
文摘Background: Alpinia officinarum Hance is valued as an edible medicinal plant. The rhizome is widely reported to have anticancer activity whereas little information is available on the aerial part. This study investigates chemical composition, proapoptotic and anti-osteoporosis activities of essential oil from aerial parts of A. officinarum (APEO). Methods: In this study, APEO was extracted by hydrodistillation and analyzed using GC-MS. The inhibitive activity of 0 - 2.5 μL/mL. APEO was investigated using MTT assay, while in vivo effect was evaluated in nude mice. The cell cycle, apoptosis, Δψm and expression of proteins analyses influenced by 0 - 0.313 μL/mL APEO were detected by PI, Annexin V/PI, JC-1, and Western blot, respectively. Alkaline phosphatase activity and mineralized nodules formation of rat osteoblasts with 0 - 0.156 μL/mL APEO were assayed using colorimetric method and alizarin red staining, respectively. Results: Total 45 constituents were identified accounting for 91.1% of APEO (sesquiterpene hydrocarbons for 44.4%). APEO significantly inhibited cancer cells growth in a dose-dependent manner. APEO also inhibited cancer growth in vivo. The percentage of S phase cells is up to 64.846% with 0.313 μL/mL APEO. The proportion of total apoptotic cells significantly increased to 79.6% at 0.313 μL/mL concentration. APEO treated cells accompanied with Bcl-2 and Δψm decrease, and caspase-3 and p53 upregulation. Furthermore, addition of APEO in rat osteoblasts led to a dose-dependent increase in ALP activity and formation of mineralized bone nodules. Conclusions: Our data suggest that APEO could be developed as an agent against human lung cancer and osteoporosis, especially cancer-induced bone loss.
