Showing papers by "Wen-Cai Ye published in 2019"
TL;DR: B5G1, a new derivative of BA, induces cell death in multidrug resistant cancer cells HepG2/ADM and MCF-7/ADR through mitochondrial-apoptosis pathway and provides the first demonstration that B5G 1, as a novel mitophagy inducer, has the potential to be developed into a drug candidate for treating multidrog resistant cancer.
Abstract: Betulinic acid (BA) and its derivatives are a class of high-profile drug candidates, but their anticancer effects on resistant cancer have rarely been reported. Although a few studies indicated mitophagy is related with drug resistance, its role in different cancer types and anticancer agents treatment remains largely unclear. Here, we find that B5G1, a new derivative of BA, induces cell death in multidrug resistant cancer cells HepG2/ADM and MCF-7/ADR through mitochondrial-apoptosis pathway. B5G1 also triggers mitophagy independent on Atg5/Beclin 1. Further mechanistic study indicates that B5G1 upregulates PTEN-induced putative kinase 1 (PINK1) to recruit Parkin to mitochondria followed by ubiquitination of Mfn2 to initiate mitophagy. Inhibition of mitophagy by PINK1 siRNA, mdivi-1, or bafilomycin A1 (Baf A1) promotes B5G1-induced cell death. In addition, ROS production and mitochondrial damage in B5G1-treated HepG2/ADM cells cause mitochondrial apoptosis and mitophagy. In vivo study shown that B5G1 dramatically inhibits HepG2/ADM xenograft growth accompanied by apoptosis and mitophagy induction. Together, our results provide the first demonstration that B5G1, as a novel mitophagy inducer, has the potential to be developed into a drug candidate for treating multidrug resistant cancer.
77 citations
TL;DR: GF1-induced activation of the IGF-1/IGF1R pathway to promote angiogenesis is an effective approach to alleviate cerebral ischemia, and GF1 is a potential agent that improves cerebrovascular function and promotes recovery from ischemic stroke.
47 citations
TL;DR: The anti-inflammatory activities of 1-11 were investigated by monitoring their inhibitory effects on nitric oxide production in lipopolysaccharide-stimulated RAW 264.7 cells and the correlations of the chemical shifts of the relevant carbons and the configurations of C-2, C-13, and C-14 of their flexible macrocyclic ring were considered.
Abstract: Guided by 1H NMR spectroscopic experiments using the aromatic protons as probes, 11 macrocyclic diterpenes (1-11) were isolated from the aerial parts of Euphorbia helioscopia. Their full three-dimensional structures, including absolute configurations, were established unambiguously by spectroscopic analysis and single-crystal X-ray crystallographic experiments. Among the isolated compounds, compound 1 is the third member thus far of a rare class of Euphorbia diterpenes featuring an unusual 5/10 fused ring system, and 2-4 are new jatrophane diterpenes. Based on the NMR data of the jatrophane diterpenes obtained in this study as well as those with crystallographic structures reported in the literature, the correlations of the chemical shifts of the relevant carbons and the configurations of C-2, C-13, and C-14 of their flexible macrocyclic ring were considered. Moreover, the anti-inflammatory activities of 1-11 were investigated by monitoring their inhibitory effects on nitric oxide production in lipopolysaccharide-stimulated RAW 264.7 cells. Compound 1 showed an IC50 of 7.4 ± 0.6 μM, which might be related to the regulation of the NF-κB signaling pathway by suppressing the translocation of the p65 subunit and the consequent reduction of IL-6 and TNF-α secretions.
33 citations
TL;DR: Two novel phloroglucinol-terpenoid adducts, featuring a rare 2,2,4-trimethyl-cinnamyl-β-triketone unit, isolated from the buds of Cleistocalyx operculatus exhibited significant in vitro antiviral activities against respiratory syncytial virus (RSV).
32 citations
TL;DR: The contribution of angiogenesis to tumor metastasis is introduced and the application of Food and Drug Administration-approved vessel targeting drugs for metastatic tumors are summarized.
Abstract: Tumor vessels provide essential paths for tumor cells to escape from the primary tumor and form metastatic foci in distant organs. The vessel targeting strategy has been widely used as an important clinical cancer chemotherapeutic strategy for patients with metastatic tumors. Our review introduces the contribution of angiogenesis to tumor metastasis and summarizes the application of Food and Drug Administration (FDA)-approved vessel targeting drugs for metastatic tumors. We recommend the application and mechanisms of vascular targeting drugs for inhibiting tumor metastasis and discuss the risk and corresponding countermeasures after vessel targeting treatment.
24 citations
TL;DR: In this paper, 17 diterpenoid lactones, including two new compounds, were identified by spectroscopic methods, and most of them attenuated the generation of TNF-α and IL-6 in LPS-induced RAW 274.7 cells examined by ELISA.
Abstract: Andrographis paniculata (AP) has been widely used in China for centuries to treat various diseases, and especially to treat inflammation. Diterpenoid lactones are the main anti-inflammatory components of AP. However, systematic chemical composition and biological activities, as well as key pharmacophores, of these diterpenoid lactones from AP have not yet been clearly understood. In this study, 17 diterpenoid lactones, including 2 new compounds, were identified by spectroscopic methods, and most of them attenuated the generation of TNF-α and IL-6 in LPS-induced RAW 274.7 cells examined by ELISA. Pharmacophores of diterpenoid lactones responsible for the anti-inflammatory activities were revealed based on the quantitative structure-activity relationship (QSAR) models. Moreover, new compounds (AP-1 and AP-4) exerted anti-inflammatory activity in LPS microinjection-induced zebrafish, which might be correlated with the inhibition of the translocation of NF-κB p65 from cytoplasm to nucleus. Our study provides guidelines for future structure modification and rational drug design of diterpenoid lactones with anti-inflammatory properties in medical chemistry.
21 citations
TL;DR: Interestingly, lycorine treatment decreased the levels of the nuclear pore complex protein 93 (Nup93, E2RSV7), which is associated with nuclear–cytoplasmic transport, and may provide new insights into how Lycorine may trap vRNPs in the nucleus and suggest new potential therapeutic targets for influenza virus.
Abstract: Highly pathogenic H5N1 influenza viruses (HPAIV) cause rapid systemic illness and death in susceptible animals, leading to a disease with high morbidity and mortality rates. Although vaccines and drugs are the best solution to prevent this threat, a more effective treatment for H5 strains of influenza has yet to be developed. Therefore, the development of therapeutics/drugs that combat H5N1 influenza virus infection is becoming increasingly important. Lycorine, the major component of Amaryllidaceae alkaloids, exhibits better protective effects against A/CK/GD/178/04 (H5N1) (GD178) viruses than the commercial neuraminidase (NA) inhibitor oseltamivir in our prior study. Lycorine demonstrates outstanding antiviral activity because of its inhibitory activity against the export of viral ribonucleoprotein complexes (vRNPs) from the nucleus. However, how lycorine affects the proteome of AIV infected cells is unknown. Therefore, we performed a comparative proteomic analysis to identify changes in protein expression in AIV-infected Madin-Darby Canine Kidney cells treated with lycorine. Three groups were designed: mock infection group (M), virus infection group (V), and virus infection and lycorine-treated after virus infection group (L). The multiplexed tandem mass tag (TMT) approach was employed to analyze protein level in this study. In total, 5,786 proteins were identified from the three groups of cells by using TMT proteomic analysis. In the V/M group, 1,101 proteins were identified, of which 340 differentially expressed proteins (DEPs) were determined during HPAIV infection; among the 1,059 proteins identified from the lycorine-treated group, 258 proteins presented significant change. Here, 71 proteins showed significant upregulation or downregulation of expression in the virus-infected/mock and virus-infected/lycorine-treated comparisons, and the proteins in each fraction were functionally classified further. Interestingly, lycorine treatment decreased the levels of the nuclear pore complex protein 93 (Nup93, E2RSV7), which is associated with nuclear-cytoplasmic transport. In addition, Western blot experiments confirmed that the expression of Nup93 was significantly downregulated in lycorine treatment but induced after viral infection. Our results may provide new insights into how lycorine may trap vRNPs in the nucleus and suggest new potential therapeutic targets for influenza virus.
20 citations
TL;DR: Affinity-based protein profiling has proven to be a powerful method in target identification of bioactive molecules and was applied in two photoreactive anticancer inhibitors, arenobufagin and HM30181, which validated to be involved in the function of the anticancer effects.
Abstract: Affinity-based protein profiling has proven to be a powerful method in target identification of bioactive molecules. Here, this technology was applied in two photoreactive anticancer inhibitors, arenobufagin and HM30181. Using UV irradiation, these photoreactive reagents can covalently cross-link to target proteins, leading to a covalent binding with target proteins. Moreover, the cellular on/off targets of these two molecules, including ATP1A1, MDR1, PARP1, DDX5, NOP2, RAB6A, and ERGIC1 were first identified by affinity-based protein profiling and bioimaging approaches. The protein hit, PARP1, was further validated to be involved in the function of the anticancer effects.
19 citations
TL;DR: A pair of enantiomeric triketone-phloroglucinol hybrids, (+)- and (-)-myrtuspirone A (1), featuring an unprecedented 3-isopropyl-3 H-spiro[benzofuran-2,1'-cyclohexane] backbone, isolated from the leaves of Myrtus communis exhibited antibacterial activities against Gram-positive bacteria including multidrug-resistant strains.
19 citations
TL;DR: Five new phloroglucinol derivatives, eucalyptins C-G (1-5), together with 13 known analogues (6-18) were isolated from the fruits of EucalyPTus globulus and it was demonstrated that 1 exhibited an immunosuppressive effect through inducing apoptosis and inhibiting cytokine secretion.
Abstract: Five new phloroglucinol derivatives, eucalyptins C-G (1-5), together with 13 known analogues (6-18) were isolated from the fruits of Eucalyptus globulus. The structures and absolute configurations of 1-5 were established by means of spectroscopic data analysis, computational calculation methods, and single-crystal X-ray diffraction. Compounds 1-18 were investigated for their immunosuppressive effects in vitro, and 1, 2, 6, and 7 displayed moderate inhibitory activities with IC50 values of 11.8, 10.2, 18.2, and 19.1 μM, respectively. The stimulation index (SI) of 1 was 64.2 and was compared to that of cyclosporine A (SI = 149.57). Further study demonstrated that 1 exhibited an immunosuppressive effect through inducing apoptosis and inhibiting cytokine secretion.
17 citations
TL;DR: The stereoisomers of Sch B, especially (+)-2 and (-)-2, were found to be potential selective ATP-competitive GSK-3β inhibitors, which further affected their anti-AD effects.
Abstract: Glycogen synthase kinase-3β (GSK-3β) is a key enzyme in hyperphosphorylation of tau proteins and is a promising therapeutic target in Alzheimer’s disease (AD). Here, we reported, for the first time, that the stereoisomers of Schisandrin B (Sch B), (+)-1, (−)-1, (+)-2, and (−)-2, were potent GSK-3β inhibitors. They were demonstrated to selectively target GSK-3β in an orthosteric binding mode, with IC50 values of 340, 290, 80, and 70 nM, respectively. Further study showed that these stereoisomers can significantly increase the expression of p-GSK-3β (Ser9) and decrease the expressions of p-GSK-3β (Tyr216) and p-GSK-3β (Tyr279). Finally, these compounds can alleviate the cell injury induced by Aβ, and the cognitive disorders in AD mice, especially (+)-2 and (−)-2. Collectively, the stereoisomers of Sch B, especially (+)-2 and (−)-2, were found to be potential selective ATP-competitive GSK-3β inhibitors, which further affected their anti-AD effects. These promising findings explained the biological target of ...
TL;DR: Most of bufadienolides could significantly inhibit the proliferation of cancer cells, and compounds 1, 8, 12, 18 and 19 showed the most potent inhibitory activity against four types of human tumor cells.
TL;DR: Psiguadiols A-J (1-10), new meroterpenoids with rearranged skeletons, were isolated from the leaves of Psidium guajava and a putative biosynthetic pathway for 1-10 is discussed.
Abstract: Psiguadiols A-J (1-10), new meroterpenoids with rearranged skeletons, were isolated from the leaves of Psidium guajava. Compounds 1-3 represent the first examples of 6,8-diformyl-5,7-dihydroxy-4-phenylchromane-coupled sesquiterpenoids with an unprecedented C-8-spiro-fused 6/6/9/4 tetracyclic ring system. Compounds 4 and 5 represent two unusual scaffolds featuring 1β,6β- and 3α,5α-epoxy rings, respectively. The combination of spectroscopic data analyses, comparison of experimental and calculated ECD data, and single-crystal X-ray diffraction data of 1, 6, and 8 allowed for the assignment of the structures. A putative biosynthetic pathway for 1-10 is discussed. Compounds 1, 7, and 8 exhibited inhibitory activities against PTP1B with IC50 values of 4.7, 6.2, and 9.2 μM, respectively. In addition, molecular docking was performed to investigate the mechanism of action.
TL;DR: Five new matrine-type alkaloid dimers were isolated from the aerial parts of Sophora alopecuroides and exhibited the most significant activity, better than that of matrine, the representative compound from S. alopECuroides.
Abstract: Five new matrine-type alkaloid dimers, alopecuroides A-E, were isolated from the aerial parts of Sophora alopecuroides. Alopecuroides A and B represent the first dimeric matrine-type alkaloids possessing a cyano group and an epoxy moiety. Alopecuroides C and D are dimeric matrine-type alkaloids connected via C-2-C-9' and C-10-C-3' bonds, respectively. The chemical structures of alopecuroides A-E were elucidated by spectroscopic methods combined with single-crystal X-ray diffraction analysis. The anti-inflammatory effects of alopecuroides A-E were evaluated, and alopecuroide B exhibited the most significant activity, better than that of matrine, the representative compound from S. alopecuroides.
TL;DR: Results suggested that 1 might be an effective candidate for PD therapy, and oral administration of 1 was demonstrated to possess anti-PD effect through alleviating apoptosis and oxidative stress in vitro and in vivo.
TL;DR: Three new monoterpenoid indole alkaloids (MIAs), hunterines A-C (1-3), were isolated from Hunteria zeylanica and alkaloid 1 showed moderate cytotoxic activity against HepG2 cell line.
Abstract: Three new monoterpenoid indole alkaloids (MIAs), hunterines A-C (1-3), were isolated from Hunteria zeylanica. Compound 1 possesses a unique skeleton with an unprecedented azabicyclo[4.3.1]decane ring system. Compounds 2 and 3 are a pair of epimeric vobasinylindole alkaloid heterodimers. Their structures including absolute configurations were established by spectroscopic analyses, X-ray diffraction, computational calculation, and the modified Mosher's method. Plausible biogenetic pathways of 1-3 were also proposed. Alkaloid 1 showed moderate cytotoxic activity against the HepG2 cell line.
TL;DR: Three pairs of dimeric phenylpropanoyl-phloroglucinol enantiomers, (+)- and (-)-xanthchrysones A-C, as well as their postulated biosynthetic precursors were isolated and identified from the leaves of Xanthostemon chrysanthus.
Abstract: Three pairs of dimeric phenylpropanoyl–phloroglucinol enantiomers, (+)- and (−)-xanthchrysones A–C [(+)- and (−)-1–3], as well as their postulated biosynthetic precursors, were isolated and identified from the leaves of Xanthostemon chrysanthus. Compound 1 featured an unprecedented bis-phenylpropanoyl-benzo[b]cyclopent[e] oxepine tricyclic backbone. Compounds 2 and 3 represent the first examples of 1-(cyclopentylmethyl)-3-(3-phenylpropanoyl)benzene scaffold. The structures and absolute configurations of 1–3 were determined by spectroscopic and X-ray diffraction analysis as well as electronic circular dichroism (ECD) calculation. Both (+)-2 and (−)-2 showed moderate antibacterial activities including several multidrug-resistant strains.
TL;DR: Both IVIM-DWI and R2* mapping can adequately detect the vascular-disrupting effect of DAVLBH as early as 1 hour after injection in a mouse xenograft model and are the two most sensitive hemodynamic parameters and can monitor the hyperacute changes associated with DAV LBH treatment in vivo.
Abstract: OBJECTIVE. This study aimed to investigate the feasibility of intravoxel incoherent motion (IVIM) DWI and R2* (transverse relaxation rate) mapping to monitor the hyperacute therapeutic efficacy of ...
TL;DR: In this paper, total flavonoid C-glycosides derived from the extracts of Abrus pulchellus subsp. mollis (Hance) Verdc. (Leguminosae) were firstly found to prevent nonalcoholic fatty liver disease both in vitro and in vivo.
Abstract: Abrus pulchellus subsp. mollis (Hance) Verdc. (Leguminosae) is a well-known edible plant usually added to soups and beverages. In this study, vicenin-2 (1), isoschaftoside (2), schaftoside (3), and their enrichment fraction, total flavonoid C-glycosides, derived from the extracts of A. mollis, were firstly found to prevent nonalcoholic fatty liver disease both in vitro and in vivo. In the in vitro study, total flavonoid C-glycosides decreased the lipid accumulation in oleic acid-treated HepG2 cells. The mechanisms of total flavonoid C-glycosides are involved in the regulation of peroxisome proliferator-activated receptor α and its downstream, and the reduction of proinflammatory cytokines. In high-fat diet-induced fatty liver rats, total flavonoid C-glycosides decreased the levels of glutamic-oxalacetic transaminease and glutamic-pyruvic transaminase, and decreased the lipid accumulation both in the liver and blood without affecting food intake. In addition, total flavonoid C-glycosides also increased the activities of the antioxidant enzyme system in vivo. In conclusion, total flavonoid C-glycosides are active components of A. mollis on nonalcoholic fatty liver disease, and can be used in functional food and supplements for nonalcoholic fatty liver disease prevention and treatment.
TL;DR: Nine known compounds along with two new flavonoids, along with nine known compounds, were isolated from the nuts of Areca catechu (Palmae), and new structures were established by a combination of spectroscopic data and electronic circular dichroism (ECD) calculation.
Abstract: Two new flavonoids, calquiquelignan M (1), calquiquelignan N (2), along with nine known compounds (3–11), were isolated from the nuts of Areca catechu (Palmae). The new structures, including absolute configurations, were established by a combination of spectroscopic data and electronic circular dichroism (ECD) calculation. The known compounds were identified by comparing their spectroscopic data with reported in the literature. The flavonoids compounds (1–8) were evaluated for their cytotoxicity activities against three human cancer cell lines. Compounds 1 and 2 exhibited a moderate cytotoxic activity against HepG2 cell lines with IC50 values of 49.8 and 53.6 μM, respectively.
TL;DR: Three new linear peptides containing d-leucine, named whitmantides A-C (1-3), were isolated from the dried whole bodies of Whitmania pigra Whitman and displayed neuroprotective activities against oxygen-glucose deprivation/reperfusion injury on Neuro-2a cells.
Abstract: Three new linear peptides containing d-leucine, named whitmantides A-C (1-3), were isolated from the dried whole bodies of Whitmania pigra Whitman. Their structures with absolute configurations were elucidated by Edman degradation, mass spectrometry, Marfey's analysis, and solid-phase synthesis. It is the first time that peptides containing d-amino acid in leeches were discovered. Compounds 1-3 displayed neuroprotective activities against oxygen-glucose deprivation/reperfusion injury on Neuro-2a cells. In addition, ex vivo serum stability tests showed that 1-3 were resistant to protease degradation.
TL;DR: Interestingly, the strain GGF16‐1‐2 can produce enantiomers, and these compounds were evaluated for their antibacterial, cytotoxic and inhibitory activities against PDE4D2.
Abstract: One new racemic mixture, penicilliode A (1) and four pairs of enantiomeric polyketides, penicilliode B and C (2 and 3) and coniochaetone B and C (4 and 5), were obtained from the starfish-derived symbiotic fungus Penicillium sp. GGF16-1-2. Interestingly, the strain GGF16-1-2 can produce enantiomers. The absolute configuration of 1 was determined by X-ray diffraction (XRD) analysis, and the absolute configurations of 2-4 were determined by the optical rotation (OR) values and electronic circular dichroism (ECD) calculations. Compounds 1-5 were firstly isolated from the marine-derived fungus Penicillium as racemates, and 2-5 were separated by HPLC with a chiral stationary phase. All the compounds were evaluated for their antibacterial, cytotoxic and inhibitory activities against PDE4D2.
TL;DR: A pair of new glycosidic epimers, cablinosides A and B, were isolated from the leaves of Pogostemon cablin and showed moderate α‐glucosidase inhibitory activity and no significant cytotoxic activity against HepG2 cells.
Abstract: A pair of new glycosidic epimers, cablinosides A (1a) and B (1b) were isolated from the leaves of Pogostemon cablin. The structures with absolute configurations of 1a and 1b were elucidated by extensive NMR investigation, and quantum chemical CD calculations. The epimer mixture 1 showed moderate α-glucosidase inhibitory activity and no significant cytotoxic activity against HepG2 cells.
TL;DR: It is demonstrated that PHMH exerts anti-angiogenic activity both in vitro and in vivo, and its findings provide new insights into the potential application of PHMH as a therapeutic agent for anti-ANGiogenesis.
Abstract: The rhizome of Alpinia officinarum Hance, a popular spice used as a condiment in China and Europe, has various reported bioactivities, including anticancer, anti-inflammatory and antioxidant effects. However, its anti-angiogenic activity has not previously been reported. In this study, a diarylheptanoid was isolated from Alpinia officinarum and identified as 1-phenyl-7-(4-hydroxy-3-methoxyphenyl)-4E-en-3-heptanone (PHMH). We demonstrated that PHMH exerts anti-angiogenic activity both in vitro and in vivo. PHMH inhibited vascular endothelial growth factor (VEGF)-induced viability, migration, invasion and tube formation in human umbilical vein endothelial cells (HUVECs) in vitro, and also suppressed VEGF-induced sprout formation of rat aorta ex vivo. Furthermore, PHMH was found to block VEGF-induced vessel formation in mice and suppress angiogenesis in both zebrafish and chorioallantoic membrane models. Mechanistic studies indicated that PHMH inhibited VEGF-induced VEGF receptor-2 (VEGFR-2) auto-phosphorylation and resulted in the blockage of VEGFR-2-mediated signaling cascades in HUVECs, including the Akt/mTOR, ERK1/2, and FAK pathways. Our findings provide new insights into the potential application of PHMH as a therapeutic agent for anti-angiogenesis.
TL;DR: It is demonstrated that PDG FR-β may be a potential therapeutic target for pterygium, and inhibition of PDGFR-β by sunitinib is a promising and effective approach for p lotterygium treatment.
Abstract: Background: Pterygium, a common eye disease with high postoperative recurrence, lacks effective therapeutic strategies. Therefore, it's urgent to identify specific targets to develop rationally targeted molecular drugs for the pterygial therapy. Methods: The cell proliferation and motility were studied in both the primary human pterygial fibroblasts (hPFs) and an ex vivo pterygium model. hPFs transfected with the pCMV3-PDGFRB plasmid, PDGFRB siRNA and CRISPR/Cas9 system were used to determine the role of PDGFR-β in pterygial fibroblasts functions. Western blotting, immunohistochemistry and immunofluorescence were performed to evaluate the expression of the key proteins. Results: PDGFR-β expression in the pterygial stroma and primary hPFs was significantly higher than that in the conjunctiva and human conjunctival fibroblasts. PDGF-BB promoted the proliferation, migration and invasion of hPFs, which can be significantly suppressed by sunitinib via inhibition of the PDGFR-β/extracellular signal-regulated kinase (ERK) pathway. In the ex vivo model, the knockout of PDGFRB and sunitinib treatment blocked the proliferation and motility of fibroblasts in the pterygial stroma via the suppression of PDGFR-β/ERK pathway. Conclusion: This study demonstrates that PDGFR-β may be a potential therapeutic target for pterygium, and inhibition of PDGFR-β by sunitinib is a promising and effective approach for pterygium treatment.
TL;DR: Five new trans‐2,3,5,4′‐tetrahydroxystilbene 2‐O‐β‐d‐glucopyranoside (TSG)‐based stilbenes glycoside oligomers (1–5) were isolated from the roots of Polygonum multiflorum and exhibited moderate inhibitory activities against NO production in LPS‐stimulated RAW264.7 cells.
Abstract: Five new trans-2,3,5,4'-tetrahydroxystilbene 2-O-β-d-glucopyranoside (TSG)-based stilbene glycoside oligomers (1-5) were isolated from the roots of Polygonum multiflorum. Their structures were elucidated by comprehensive spectroscopic analyses and chemical evidences. The absolute configurations of 1, 2, 4, and 5 were established by quantum-chemical electronic circular dichroism (ECD) calculations. Putative biosynthetic pathways of 1-5 were proposed using TSG as the key precursor. In addition, compounds 1 (multiflorumiside H) and 3 (multiflorumiside J) exhibited moderate inhibitory activities against NO production in LPS-stimulated RAW264.7 cells.
TL;DR: All the saponins isolated showed no significant effects against respiratory syncytial virus (RSV) and lipopolysaccharide‐induced nitric oxide production in Raw264.7 macrophages.
Abstract: Asprellosides A-K, nine new ursane-type triterpenoid glycosides (1-9), and two new oleanane-type triterpenoid glycosides (10 and 11), including six rare sulfated triterpenoid glycosides, were isolated from the roots of Ilex asprella. Their structures were determined on the basis of comprehensive spectroscopic analysis and chemical methods. Among these compounds, asprelloside B (2) and asprelloside C (3) are the first examples of triterpenoid glycosides bearing a rare 3,4-O-disulfo-xylopyranosyl residue. All the saponins isolated showed no significant effects against respiratory syncytial virus (RSV) and lipopolysaccharide-induced nitric oxide production in Raw264.7 macrophages.
01 Jan 2019
TL;DR: Several tumor angiogenesis inhibitors (TAIs) have appeared in the market or in different stages of clinical trials, and several of them have been commonly applied in cancer treatment alone, or in combination with other chemotherapeutic agents (CTAs) or radiotherapy as discussed by the authors.
Abstract: It has been known that the VEGF/VEGFR signaling pathway plays an important role in angiogenesis and it is overactive in many types of solid tumors. Since tumor angiogenesis is vital for tumor cell survival, proliferation, migration, and invasion, antiangiogenic therapy has been extensively explored. Currently, a lot of tumor angiogenesis inhibitors (TAIs) have appeared in the market or in different stages of clinical trials, and several of them have been commonly applied in cancer treatment alone, or in combination with other chemotherapeutic agents (CTAs) or radiotherapy. This chapter will introduce several of the angiogenesis inhibitors, their antiangiogenic pharmacological mechanisms, new indications, and clinical trial results in chemotherapy, with a focus on bevacizumab, ramucirumab, sorafenib, and sunitinib.