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The combination of β-tricalcium phosphate (β-TCP) with polycaprolactone (PCL) has been considered a promising strategy for designing scaffolds for bone grafting. This study incorporated PCL with commercially available β-TCP (OsteoceraTM) to fabricate an injectable bone substitute and evaluate the effect of PCL on compressive strength and setting time of the hydraulic cement. The mechanical testing was compliant with the ASTM D695 and ASTM C191-13 standards. Results showed that PCL-TCP composite presented a well-defined architecture with uniform pore distribution and a significant increase in compressive strength compared with β-TCP alone. Eighteen rabbits, each with two surgically created bone defects, were treated using the PCL-TCP composites. The composite materials were resorbed and replaced by newly formed bone tissue. Both PCL-TCP and β-TCP demonstrated equivalent clinical effects on osteoconduction property in terms of the percentage of newly formed bone area measured by histomorphometric analysis. PCL-TCP was proven to be as effective as the commercially available β-TCP scaffold (OsteoceraTM).

Two new cerebrosides, ferocerebrosides A (1) [(2S,3R,4E,8E,2'R)-1-O-(beta-glucopyranosyl)-N-(2'-hydroxydocosanoyl)-4,8-sphingadienine] and B (2) [(2S,3R,4E,8E,2'R)-1-O-(beta-glucopyranosyl)-N-(2'-hydroxytetracosanoyl)-4,8-sphingadienine], two new tocopherol trimers, ferotocotrimers C (5) and D (6), and two known tocopherol trimers, IVb (3) and IVa (4), were isolated from the seeds of Euryale ferox. Their structures were determined on the basis of spectroscopic data, especially 1D and 2D NMR experiments. Compounds 1 and 2 showed cytotoxicity in the brine shrimp lethality bioassay, with LC50 values of 0.17 and 0.20 mM, respectively.

Study design Laboratory study. Objective To evaluate whether blockade of the Substance P (SP) NK1R attenuates its proinflammatory effect on human intervertebral disc cells (IVD), and to evaluate the signaling pathways associated with SP. Summary of background data SP and its receptors are expressed in human IVD cells, and cause upregulation of inflammatory mediators; however, the effects of blocking these receptors have not been studied in human IVD cells. Methods Human annulus fibrosus (AF) and nucleus pulposus (NP) cells were expanded in monolayer, and then suspended in alginate beads. The alginate beads were treated with culture medium first containing a high affinity NK1R antagonist (L-760735) at different concentrations, and then with medium containing both NK1R antagonist and SP at 2 concentrations. Ribonucleic acid was isolated and transcribed into cDNA. Quantitative reverse transcriptase-polymerase chain reaction (RT-PCR) was performed to evaluate expression of interleukin (IL)-1β, IL-6, and IL-8. Western blot analysis was performed to examine levels of the phosphorylated p38 mitogen-activated protein kinase (MAPK), extracellular signal regulated kinase 1/2 (ERK1/2) and nuclear factor kappa-light-chain-enhancer of activated B cells (NFκB p65). The cells were pretreated with specific inhibitors of p38 (SB203580), ERK1/2 (PD98059), and p65 (SM7368) and then stimulated with SP. Results We detected expression of NK1R, neurokinin receptor 2 (NK2R), and neurokinin receptor 3 (NK3R) in AF and NP cells. Treatment of disc cells with the NK1R antagonist was able to suppress expression of IL-1β, IL-6, and IL-8 in a dose-dependent manner. SP stimulation increased phosphorylation of p38-MAPK and ERK1/2, but not of NFκB p65. This indicates that p38-MAPK and ERK1/2 control SP-induced cytokine expression independently from NF-kB p65. Inhibition of p38 and ERK1/2 activation reduced SP-induced IL-6 production in human disc cells. Conclusion NK1R is responsible for the proinflammatory effect of SP on IVD cells and this effect can be blocked by preventing binding of SP to NK1R. This study shows for the first time that SP mediates signaling in disc cells through NK1R and that SP activates the proinflammatory p38-MAPK and ERK1/2 pathways. Level of evidence 4.

Two new phenylpropanoid glycosides, a-L-rhamnopyranosyl-(1→3)-1-O-caffeoyl-β-D-glucopyrano-side and 2",3"'-diacetyl acteoside, together with seven known compounds have been isolated from the parasitic plant, Aeginetia indica Linn. Their structures were established by spectroscopic and chemical methods.

Two new compounds have been isolated from the whole plant of Monochoria vaginalis and characterized as: (10Z)-1-(2,6-dihydroxyphenyl)octadec-10-en-1-one (1) (20R, 24R)-campest-5-ene-3β, 4β-diol (2) together with nine known ones. The structures of these compounds were elucidated on the basis of spectral data and chemical evidence.

Two new neolignans, namely balanophonin 4-O-β-d-glucopyranoside and aegineoside together with four known neolignans have been isolated from the whole plant of Aeginetia indica Linn. (Orobanchaceae). Their structures were established by spectroscopic and chemical methods.

Three new compounds have been isolated from the whole plant of Monochoria vaginalis and characterized as: (2S,3R,4E,8E,2'R)-1-O-(β-D-glucopyranosyl)-N-(2'-hydroxyicosanoyl)-4,8-sphingadienine, (2S,3R,4E,8E,2'R)-1-O-(β-D-glucopyranosyl)-N-(2'-hydroxyoctadecanoyl)-4,8-sphingadienine and 7-oxo-stigmasteryl-3-O-(6'-hexadecanoyl)-β-D-glucopyranoside. Their structures were established by spectral and chemical evidence.

The structure of a mixture of ceramides (1) derived from 2-amino-4(E)-alkene-1,3-diol sphingenines with C 2 2 , C 2 3 , and C 2 4 saturated fatty acid residues from red alga Ceratodictyon spongiosum ZANARDINI (Rhodymeniaceae) containing the symbiotic sponge Sigmadocia symbiotica has been elucidated on the basis of spectroscopic and chemical evidence. In addition, one new sterol, n-nonadecanoic acid 24-methyl-enecholesteryl ester (2), and six known sterols were also isolated from the marine organisms.

Two new flavonoids, kaempferol 7-O-(2-E-p-coumaroyl-alpha-l-rhamnoside) (1) and kaempferol 7-O-(2,3-di-E-p-coumaroyl-alpha-l-rhamnoside) (2), together with 10 known compounds were isolated from the flowers and fruit of Tetrapanax papyriferus. Compounds 1 and 2 showed cytotoxicity by brine shrimp lethality bioassay with LC(50) values of 0.57 and 0.40 mM, respectively.

From the whole plant of Cassytha filiformis Linn. (Lauraceae), two new neolignans, named 4-O-methylbalanophonin and cassyformin together with three known compounds have been isolated. Their structures were established by spectroscopic and chemical methods.

A new withanolide, withangulatin I (2), was isolated from the whole plant of Physalis angulata. Its structure was established as (20S,22R)-15alpha-acetoxy-5beta,6beta-epoxy-14alpha-hydroxy-1,4-dioxo-witha-2,16,24-trienolide on the basis of chemical and spectroscopic methods including 2D-NMR and circular dichroism (CD) experiments. Withangulatin A (1) and withangulatin I (2) were tested for their cytotoxic activities against two human cancer cell lines, colorectal carcinoma COLO 205 and gastric carcinoma AGS, in vitro. Compounds 1 and 2 exhibited inhibitory activities against these two human cancer cells with IC(50) values of 16.6 and 1.8 and 53.6 and 65.4 muM, respectively.

A new withanolide, withangulatin I (2), was isolated from the whole plant of Physalis angulata. Its structure was established as (20S,22R)-15alpha-acetoxy-5beta,6beta-epoxy-14alpha-hydroxy-1,4-dioxo-witha-2,16,24-trienolide on the basis of chemical and spectroscopic methods including 2D-NMR and circular dichroism (CD) experiments. Withangulatin A (1) and withangulatin I (2) were tested for their cytotoxic activities against two human cancer cell lines, colorectal carcinoma COLO 205 and gastric carcinoma AGS, in vitro. Compounds 1 and 2 exhibited inhibitory activities against these two human cancer cells with IC(50) values of 16.6 and 1.8 and 53.6 and 65.4 muM, respectively.

A new sulfated cucurbitacin, cucurbitacin B 2-sulfate (1) and a new cucurbitacin glucoside, cucurbitacin G 2-O-beta-D-glucopyranoside (2) together with two known cucurbitacin glucosides, arvenin I and arvenin III were isolated from the root bark of Helicteres angustifolia. The structures of these compounds were established on the basis of spectroscopic and chemical evidence. These four compounds taste of strong bitterness. Compound 1 is a first sulfated cucurbitacin found in plants.

The Toll-like receptor 4 (TLR4)-signaling pathway is crucial for activating both innate and adaptive immunity. TLR4 is a promising molecular target for immune-modulating drugs, and TLR4 agonists are of therapeutic potential for treating immune diseases and cancers. Several medicinal herb-derived components have recently been reported to act via TLR4-dependent pathways, suggesting that medicinal plants are potential resources for identifying TLR4 activators. We have applied a screening procedure to systematically identify herbal constituents that activate TLR4. To exclude possible LPS contamination in these plant-derived components, a LPS inhibitor, polymyxin B, was added during screening. One of the plant components we identified from the screening was dioscorin, the glycoprotein isolated from Dioscorea alata. It induced TLR4-downstream cytokine expression in bone marrow cells isolated from TLR4-functional C3H/HeN mice but not from TLR4-defective C3H/HeJ mice. Dioscorin also stimulated multiple signaling molecules (NF-kappaB, ERK, JNK, and p38) and induced the expression of cytokines (TNF-alpha, IL-1beta, and IL-6) in murine RAW 264.7 macrophages. Furthermore, the ERK, p38, JNK, and NF-kappaB-mediated pathways are all involved in dioscorin-mediated TNF-alpha production. In summary, our results demonstrate that dioscorin is a novel TLR4 activator and induces macrophage activation via typical TLR4-signaling pathways.

Four oleanane-type triterpenes, 3alpha,21beta,22alpha-trihydroxy-11,13(18)-oleanadien-28-oic acid (1), 3-epi-papyriogenin C (2), 21-O-acetyl-21-hydroxy-3-oxo-11,13(18)-oleanadien-28-oic acid (3) and 3beta-hydroxy-21-oxo-11,13(18)-oleanadien-28-oic acid methyl ester (4), together with four known triterpenes, were isolated from Tetrapanax papyriferus (Hook) K. Koch. Papyriogenin A (8) exhibited anti-HIV activity and low cytotoxicity in acutely infected H9 lymphocytes. Their structures were determined by analysis of spectroscopic data, including by 1D and 2D NMR.

A new 4α-methylsterol, violasterol A, with three known flavonoids-luteolin, luteolin 7-O-β-D-glucoside and tricin-were isolated from ethanolic extract of whole plants of Viola formosana. The structure of vioiasterol A was assigned to be (22E)-4α-methyl-24ξ-isopropenyl-5α-cholesta-7, 22-diene-3β-ol (1) on the basis of spectral and chemical evidence.

Withangulatin A induced cell rounding up and the morphological alteration resulted from the reorganization of all of the major cytoskeletal components, i.e., vimentin, tubulin, and actin, as revealed by immunofluorescence techniques. When the withangulatin A-treated cells changed to a round-up morphology, vimentin intermediate filaments were found to be collapsed and clustered around the nucleus. The alteration was accompanied by characteristic changes of vimentin molecules, including augmentation of phosphorylation, retardation of electrophoretic mobility, and decrease in detergent extractability. The levels of vimentin phosphorylation were augmented by 2.5- and 1.8-fold in cells incubated with 50 microM withangulatin A for 1 and 3 h, respectively. The electrophoretic mobility of vimentin was partially retarded in cells treated with withangulatin A for 1 h at 10 microM and a completely upshift mobility was observed after 5 h treatment at 50 microM. In addition, vimentin molecules became less extractable by nonident P-40 after the cells were treated with withangulatin A and this effect was dose dependent. The decrease in solubility of vimentin was accompanied by the redistribution of HSP72 into the detergent nonextractable fraction and these two events were well correlated. Our results suggest that withangulatin A induced the modification of vimentin, which resulted in the alteration of cell morphology and redistribution of intracellular HSP72, an event that may play an important role in the induction of heat-shock response.

Two new flavonoid glycosides, takakin 8-O-β-D-glucuronide 6″methyl ester (2), takakin 8-O-β-D-glucuronide 2″-sodium sulfate (3) together with a known flavonoid glycoside, takakin 8-O-β-D-glucuronide were isolated from the root bark of Helicteres angustifolia (Sterculiaceae). The stru- ctures of these compounds were established on the basis of spectrosco- pic and chemical evidence

A new sesquiterpene lactone glucoside, 8-epicrepioside G(1) together with two known compounds, 8-epidesacylcynaropicrin glucoside (2) and ixerin D (3) were isolated from the whole plant of Ixeris chinensis. Their structures were determined on the basis of chemical and spectro- scopic evidence. Compounds (1),(2) and (3) taste of strong bitterness

A new withanolide as a topoisomerase II inhibitor, withangulatin A was isolated from the whole herb of Physalis angulata L. (Solanaceae). The structure of withangulatin A was established as (20S, 22R)-15α-acetoxy-5β,6β-epoxy-4β,14α-dihydroxy-1-oxowitha-2,16,24-trienolide on the basis of spectroscopic and chemical evidence

The reaction of indole with propiolic acid ia 1 : 1 mole ratio gave an adduct (I) of 2 : 1 addition with decarboxylation. The reaction of indole with propiolic acid methyl ester gave a 2 : 1 adduct (II). Hydrolysis of adduct II yield the corresponding carboxylic acid (IV). Decarboxylation of IV also gave I. The mechanism of title reaction were fully studied.

Chemical studies of three representatives of the genus Pseudophegopteris (Thelypteridaceae) revealed that the genus is characterized by the occurrence of unusual flavonoids with a modified B-ring related to protogenkwanin (VII). From P. hirtirachis HOLTT., three novel compounds, protogenkwanone (I), tetrahydroprotogenkwanone (II) and tetrahydroprotogenkwanin (III), were isolated, along with protogenkwanin 4'-O-β-D-glucoside (VI). From P. subaurita CHING, two new acylated glucosides of protogenkwanin, protogenkwanin 4'-O- (2-O-acetyl) -β-D-glucoside (IV) and 4'-O- (6-O-acetyl) -β-D-glucoside (V), were obtained, together with I, II and VI. From P. bukoensis HOLTT., IV, V and VI were isolated, in addition to apigenin 7-O-α-L-rhamnoside and kaempferol. The structures of the new compounds were determined by means of spectroscopic methods and chemical transformations.

Five flavonoids, quercetin, quercitrin, hyperin, orientin, and kaempferol, were isolated from Hypericum nagasawai Hayata. The dominant component is quercitrin.

The whole herb of Hypericum subalatum Hayata contains three flavonoids, caffeic acid esters, a pyranoxanthone, and three xanthines, in addition to the previously reported xanthonolignoids. Among these compounds, 2,7-dihydroxy-3,4-dimethoxyxanthone has not been described in the literature before. The co-occurrence of xanthone derivatives and flavonoids in this plant is of chemotaxonomic significance.

Aus den Rhizomen von Woodwardia orientalis Sw. wurden eine Reihe von Phytosterin-Derivaten (freie Sterine, Sterin-Ester, Sterin-Glucoside, veresterte Sterin-Glucoside) und eine neue Triterpen-Verbindung, die wir Woodwardinsaure nannten, isoliert. Die Struktur der Woodwardinsaure wurde als 3β-Hydroxy-21β-H-Δ22(29)-hopen-23-carbonsaure aufgeklart.

The reaction of indole with propiolic acid ia 1 : 1 mole ratio gave an adduct (I) of 2 : 1 addition with decarboxylation. The reaction of indole with propiolic acid methyl ester gave a 2 : 1 adduct (II). Hydrolysis of adduct II yield the corresponding carboxylic acid (IV). Decarboxylation of IV also gave I. The mechanism of title reaction were fully studied.

Withangulatin A, a new compound with a known chemical structure and from the antitumor Chinese herb Physalis angulata L, was found to act on topoisomerase II to induce topoisomerase II-mediated DNA damage in vitro. It has two effective dosage ranges of approximate 0.5 and 20 microM, with about one-third the activity of 20 microM VM-26.