[A new cinnamic acid ester derivative from Liquidambaris Resina].

Twelve compounds were isolated from Liquidambaris Resina by silica gel column chromatography and thin layer chromatography. Their structures were identified on the basis of spectral data, electron capture detector data, and physicochemical properties as(2'R, 3'R)-2',3'-dihydroxy-hydrocinnamyl-(E)-cinnamate(1),(E)-cinnamyl-(E)-cinnamate(2), cinnamic acid(3), 28-norlup-20(29)-en-3-one-17ß-hydroperoxide(4), erythrodiol(5), 13ß,28-epoxy-30-hydroxyolean-1-en-3-one(6),(3ß)-olean-12-ene-3,23-diol(7), 2α,3α-dihydroxy-olean-12-en-28-oic acid(8), 28-hydroxyolean-12-en-3-one(9), 3-epi-oleanolic acid(10), 3-oxo-oleanolic acid(11), and hederagenin(12). Compound 1 was a new cinnamic acid ester derivative and compounds 2-4,6-8, and 12 were isolated from Liquidambaris Resina for the first time. Compounds 4, 5, 10, and 12 exerted inhibitory effects on the proliferation of human umbilical vein endothelial cells(HUVEC) with the IC_(50) values of(17.43±2.17),(35.32±0.61),(27.50±0.80), and(46.30±0.30) µmol·L~(-1), respectively.

Pentacyclic Triterpenes from the resin of Liquidambar formosana have anti-angiogenic properties.

Phytochemical investigation of the resin of Liquidambar formosana Hanc led to the separation and identification of five undescribed pentacyclic triterpenoids, including two lupane type, one taraxerane type, and two oleanane type triterpenoids, in addition to ten known analogues. Structures and relative or absolute configurations were elucidated by intensive spectroscopic methods, and single-crystal X-ray diffraction analysis. All isolated compounds were evaluated for their anti-angiogenic effects in vitro against VEGF-induced endothelial cell proliferation and migration in HUVECs. Among them, (5R, 8R, 9R, 10R, 13S, 14R, 17R, 18R, 19S)-17,18-epoxy-17,18-seco-28-norlupa-17- hydroxy-20 (29) -ene-3-one, (5R, 8R, 9R, 10R, 13S, 14R, 17S, 18S, 19S, 20S)-17, 20-peroxy-28- norlupa -29 -hydroxy- 3-one, 11α,12α:13ß,28-diepoxyoleanane- 3-one, 28-norlup-20 (29)-ene- 3ß,17ß-diol, liquidambaric lactone and 13,28-epoxy-11- oleanene- 3-one significantly inhibited VEGF-induced HUVECs proliferation with IC50 values ranging from 1.64 ± 0.36 to 7.06 ± 0.28 µM. In addition, they also effectively decreased VEGF-induced cell migration with IC50 values ranging from 1.57 ± 0.60 to 4.77 ± 0.62 µM. The structure-activity relationship of these compounds is discussed. The anti-angiogenic property of (5R, 8R, 9R, 10R, 13S, 14R, 17R, 18R, 19S)-17,18-epoxy-17,18-seco-28-norlupa-17- hydroxy-20 (29) -ene-3-one is mediated by the VEGFR2 - AKT signaling pathway.

Analysis of factors affecting the therapeutic effect of propranolol for infantile haemangioma of the head and neck.

Infantile haemangiomas (IHs) are the most common congenital vascular tumours of infancy. Propranolol has been demonstrated to be effective for IHs; however, the factors affecting its therapeutic effect remain unknown. We enrolled 169 infants with IHs of the head and neck region treated with oral propranolol at a dose of 2.0 mg/kg/day. We evaluated the therapeutic responses 6 months after treatment and the end of treatment, which were categorized into four grades. The type and location of the lesions and the infant age at treatment initiation were analysed. The clinical response rate (III + IV) was 91.72% at 6 months after treatment and 97.63% at the end of treatment. The average treatment duration was 9.99 (2-24) months. The group aged 4-6 months exhibited a greater therapeutic response rate (98.48%). The treatment duration was shorter (9.52 months) for mixed-type IHs. Better therapeutic responses were observed for IHs located around the parotid, periorbital, cheek, and neck regions and for multiple IH lesions. Our study indicated that propranolol is effective for IHs affecting the head and neck. The age at treatment initiation and the location of the lesions had a significant effect on the therapeutic response, whereas the lesion type might affect the treatment duration.

Rapamycin/sodium hyaluronate binding on nano-hydroxyapatite coated titanium surface improves MC3T3-E1 osteogenesis.

Endosseous titanium (Ti) implant failure due to poor biocompatibility of implant surface remains a major problem for osseointegration. Improving the topography of Ti surface may enhance osseointegration, however, the mechanism remains unknown. To investigate the effect of modified Ti surface on osteogenesis, we loaded rapamycin (RA) onto nano-hydroxyapatite (HAp) coated Ti surface which was acid-etched, alkali-heated and HAp coated sequentially. Sodium hyaluronate (SH) was employed as an intermediate layer for the load of RA, and a steady release rate of RA was maintained. Cell vitality of MC3T3-E1 was assessed by MTT. Osteogenesis of MC3T3-E1 on this modified Ti surface was evaluated by alkaline phosphatase (ALP) activity, mineralization and related osteogenesis genes osteocalcin (OCN), osteopontin (OPN), Collagen-I and Runx2. The result revealed that RA/SH-loaded nano-HAp Ti surface was innocent for cell vitality and even more beneficial for cell osteogenesis in vitro. Furthermore, osteogenesis of MC3T3-E1 showed significant association with the mammalian target of rapamycin (mTOR) phosphorylation by RA, which required further study about the mechanism. The approach to this modified Ti surface presented in this paper has high research value for the development of Ti-based implant.

Sesquiterpenoids from Curcuma wenyujin with anti-influenza viral activities.

Five sesquiterpenoids, 1α,8α-epidioxy-4α-hydroxy- 5αH-guai-7(11),9-dien- 12,8-olide. (1), 8,9-seco-4ß-hydroxy-1α,5ßH-7(11)-guaen-8,10-olide (2), 8α-hydroxy-1α, 4ß,7ßH-guai-10(15)-en- 5ß,8ß-endoxide(3), 7ß,8α-dihydroxy-1α,4αH-guai-10(15)-en-5ß,8ß-endoxide(4) and 7-hydroxy-5(10),6,8-cadinatriene-4-one(5), together with seven known analogs were isolated from the rhizomes of Curcuma wenyujin. Their structures and relative configurations were determined on the basis of spectroscopic methods including 2D NMR techniques, and the structures of 1 and 2 were confirmed by single-crystal X-ray diffraction experiment. Compounds 1-10 and 12 showed significant in vitro antiviral activity against the influenza virus A with IC50 values ranged from 6.80 to 39.97 µM, and SI values ranged from 6.35 to 37.25.

[Antioxidant effect of total flavonoids of Hedysarum polybotry on human umbilical vein endothelial cells injury induced by hydrogen peroxide].

OBJECTIVE: To investigate protective effect of total flavonoids of Hedysarum polybotry on human umbilical vein endothelial cells injury induced by hydrogen peroxide. METHODS: Chemical light assay was used to detect the oxygen radicals scavenging capacity of total flavonoids of Hedysarum polybotry. Lactate dehydrogenase (LDH) in the culture medium, malondialdelyde (MDA) and superoxide dismutase (SOD) in the cell were measured by spectroscopy, respectively. The degress of DNA damage was evaluated with single cell gel electrophoresis (SCGE) technique. RESULTS: Total flavonoids of Hedysarum polybortry could scavenge oxygen radicals. After being exposed to 100 micromol/L H2O2 for 4 hours, the level of LDH and MDA was increased significantly while SOD level was decreased. However, total flavonoids of Hedysarum polybotry could decrease the content of LDH, MDA and increase SOD activity significantly and inhibit the damage of DNA. CONCLUSION: Total flavonoids of Hedysarum polybotry has protective effect on human umbilical vein endothelial cells injury induced by hydrogen peroxide,which may be related to increasing the antioxidant capacity of human umbilical vein endothelial cells.

[Study on the chemical constituents in herb of Hypericum attenuatum].

OBJECTIVE: To study the constituents of Hypericum attenatum. METHOD: The compounds were isolated by chromatography on silica gel, the structures were identified by their physical, chemical properties and IR, NMR and MS spectral data respectively. RESULT: Nine compounds were isolated and identified as p-hydroxybenzoic acid (1), 6, 9-dihydroxy-4, 7-megastigmadien-3-one (2), butyl alcohol-O-alpha-D-fructoside (3), 24-ethyl-cholest-7-ene-3 beta, 5 alpha, 6 beta-thtroil (4), hexanol (5), 1 beta, 6 alpha-dihydroxyeudesmane-4(14)-ene (6), beta-sitosterol (7), 5, 5-dimethyl-4-hydroxy-tetrahydrofuran-2-one (8), beta-daucosterol (9). CONCLUSION: All of the compounds were isolated from H. attenuatum for the first time.