scholarly journals Isolation of Monovalerianester A, an Inhibitor of Fat Accumulation, from Valeriana Fauriei

2015 ◽  
Vol 10 (8) ◽  
pp. 1934578X1501000
Author(s):  
Keiji Yuki ◽  
Mariko Ikeda ◽  
Shosuke Yoshida ◽  
Osamu Ohno ◽  
Kiyotake Suenaga ◽  
...  
Keyword(s):  
Crude Extract ◽  
Aqueous Ethanol ◽  
Therapeutic Potential ◽  
Inhibitory Effects ◽  
Chromatographic Purification ◽  
Fat Accumulation ◽  
Treatment Of Obesity

The rhizomes and roots of Valeriana fauriei were extracted with 80% aqueous ethanol. This extract was found to exhibit potent inhibitory effects on fat accumulation in 3T3-L1 murine adipocytes. After several steps of chromatographic purification, we succeeded in identifying monovalerianester A as an inhibitor of fat accumulation. Thus, monovalerianester A and the crude extract of the rhizomes and roots of V. fauriei may have therapeutic potential for the treatment of obesity.

scholarly journals Inhibitory Effects of Stilbene Derivatives from Parthenocissus Tricuspidata on Adipocyte Differentiation and Pancreatic Lipase

2013 ◽  
Vol 8 (10) ◽  
pp. 1934578X1300801 ◽  
Author(s):  
Sang Hoon Lee ◽  
Qing Liu ◽  
Bang Yeon Hwang ◽  
Mi Kyeong Lee
Keyword(s):  
Pancreatic Lipase ◽  
Lipase Activity ◽  
Adipocyte Differentiation ◽  
Fat Absorption ◽  
Inhibitory Effects ◽  
Fat Accumulation ◽  
Prevention And Treatment ◽  
Stilbene Derivatives ◽  
Parthenocissus Tricuspidata ◽  
Treatment Of Obesity

Obesity, which is characterized by excessive fat accumulation, occurs by fat absorption by lipase and sequential fat accumulation in adipocytes through adipocyte differentiation. Thus, inhibition of pancreatic lipase activity and adipocyte differentiation would be crucial for the prevention and treatment of obesity. Investigation of anti-obesity compounds from Parthenocissus tricuspidata stems resulted in the isolation of nineteen compounds including five acetophenones, five flavonoids and nine stilbene derivatives. Among them, the stilbene derivatives showed the most potent anti-obesity effects. Stilbene monomers showed strong inhibitory activity on both adipocyte differentiation and pancreatic lipase, followed by stilbene dimer and trimer. Flavonoids showed mild inhibition on adipocyte differentiation, whereas acetophenones showed little effect in our assay system. Taken together, P. tricuspidata might be a new candidate for the development of obesity treatment.

scholarly journals Inhibitory Effects of seco-Triterpenoids from Acanthopanax sessiliflorus Fruits on HUVEC Invasion and ACE Activity

2015 ◽  
Vol 10 (9) ◽  
pp. 1934578X1501000 ◽  
Author(s):  
Jin-Won Lee ◽  
Nam-In Baek ◽  
Dae-Young Lee
Keyword(s):  
Blood Flow ◽  
Crude Extract ◽  
Umbilical Vein ◽  
Inhibitory Effect ◽  
Inhibitory Effects ◽  
Ace Inhibitory Activity ◽  
Dioic Acid ◽  
Acanthopanax Sessiliflorus ◽  
Ace Activity ◽  
Very High

This study was conducted to investigate the effects of the crude extract from Acanthopanax sessiliflorus fruits and the isolated seco-triterpenoids from the crude extract on blood flow in human umbilical vein endothelial cell (HUVEC) invasion assay and angiotensin converting enzyme (ACE) inhibitory activity assay. On the basis of DMSO, the extent of HUVECs'invasion was remarkably decreased with crude extract concentrations of 400 and 1000 μg/mL. Additionally, the extent of the HUVEC invasion inhibitory effect in 400 and 1000 μg/mL of acanthosessilioside F were 55.8% and 72.4%, respectively. In addition, the maximum extent of the HUVEC invasion inhibitory effect of 22-α-hydroxychiisanoside was 88.9%. The IC50 value of the inhibitory effect on ACE activity in the crude extract was 4 μg/mL. The isolated seco-triterpenoids, 22α-hydroxychiisanogenin, 3,4- seco-lupan-20(30)-en-3,28-dioic acid, (1 R)-1,4-epoxy-11α,22α-hydroxy-3,4- seco-lupan-20(30)-en-3,28-dioicacid, (+)-divaroside, and chiisanosidehad showed very high inhibitory effects on ACE activity, ranging from 1.8 to 2.9 üg/mL, which is much higher than the 150.0 üg/mL effect of aspirin. These results suggest that the crude extract from Acanthopanax sessiliflorus fruits and the isolated seco-triterpenoids from the crude extract enhance the blood flow effect by decreasing ACE activity.

scholarly journals Alantolactone: A Natural Plant Extract as a Potential Therapeutic Agent for Cancer

2021 ◽  
Vol 12 ◽  
Author(s):  
Yuan Cai ◽  
Kewa Gao ◽  
Bi Peng ◽  
Zhijie Xu ◽  
Jinwu Peng ◽  
...  
Keyword(s):  
Molecular Mechanisms ◽  
Cancer Colorectal ◽  
Therapeutic Potential ◽  
Inhibitory Effects ◽  
Cytotoxic Effects ◽  
Cancer Breast ◽  
Anticancer Effects ◽  
Inula Helenium

Alantolactone (ALT) is a natural compound extracted from Chinese traditional medicine Inula helenium L. with therapeutic potential in the treatment of various diseases. Recently, in vitro and in vivo studies have indicated cytotoxic effects of ALT on various cancers, including liver cancer, colorectal cancer, breast cancer, etc. The inhibitory effects of ALT depend on several cancer-associated signaling pathways and abnormal regulatory factors in cancer cells. Moreover, emerging studies have reported several promising strategies to enhance the oral bioavailability of ALT, such as combining ALT with other herbs and using ALT-entrapped nanostructured carriers. In this review, studies on the anti-tumor roles of ALT are mainly summarized, and the underlying molecular mechanisms of ALT exerting anticancer effects on cells investigated in animal-based studies are also discussed.

scholarly journals Studies on antidiarrheal and laxative activities of aqueous-ethanol extract of Asphodelus tenuifolius and underlying mechanisms

2019 ◽  
Vol 19 (1) ◽  
Author(s):  
Naveed Aslam ◽  
Khalid Hussain Janbaz
Keyword(s):  
Crude Extract ◽  
Castor Oil ◽  
Aqueous Ethanol ◽  
Intestinal Transit ◽  
In Vivo Studies ◽  
Control Group ◽  
Phytochemical Screening ◽  
Response Curves ◽  
Aqueous Fraction ◽  
Spasmolytic Activity

Abstract Background Asphodelus tenuifolius Cav. (Asphodelaceae) has traditional reputability in treatment of diarrhea and constipation but no scientific study has been reported for its gastrointestinal effects. Present study was conducted to evaluate antidiarrheal and laxative activities of the plant. Methods Aqueous-ethanol crude extract of Asphodelus tenuifolius (At.Cr) was subjected to phytochemical screening and liquid-liquid fractionation. In vivo studies of charcoal meal intestinal transit test, antidiarrheal activity against castor oil induced diarrhea and laxative activity were performed in mice. In vitro experiments were conducted upon rabbit jejunum preparations using standard tissue bath techniques. Results Phytochemical screening indicated presence of alkaloids, anthraquinones, flavonoids, saponins, steroids, tannins and phenols in At.Cr. In charcoal meal intestinal transit test, At.Cr increased (p < 0.001) intestinal motility at 100 mg/kg dose, but decreased (p < 0.001) it at 500 mg/kg dose, when compared to the control group. At.Cr (300–700 mg/kg) provided protection from castor oil induced diarrhea in mice, which was significant (p < 0.001) at 500 and 700 mg/kg doses, as compared to the saline treated control group. At.Cr (50 and 100 mg/kg) enhanced total and wet feces counts in normal mice, as compared to saline treated control. In jejunum preparations, At.Cr inhibited spontaneous, K+ (80 mM) and K+ (25 mM) mediated contractions, similar to verapamil. Pre-incubation of jejunum preparations with At.Cr resulted in rightward nonparallel shift in Ca+ 2 concentration response curves, similar to verapamil. The spasmolytic activity was concentrated in ethylacetate fraction. Aqueous fraction exhibited spasmogenicity upon spontaneous contractions, which was blocked in presence of verapamil, but remained unaffected by other tested antagonists. Conclusion The Asphodelus tenuifolius crude extract possesses gut modulatory activity, which may normalize gut functions in diarrhea and constipation. The spasmolytic activity of the extract was found to be mediated through Ca+ 2 channel blocking action. The spasmogenic activity, found partitioned in aqueous fraction, possibly involves Ca+ 2 influx through voltage gated Ca+ 2 channels. The study supports ethnic uses of the plant in diarrhea and constipation.

scholarly journals Antibacterial and Antiparasitic Effects of Bothropoides lutzi venom

2012 ◽  
Vol 7 (1) ◽  
pp. 1934578X1200700
Author(s):  
Ramon R.P.P.B. de Menezes ◽  
Alba F. C. Torres ◽  
Thiala S. J. da Silva ◽  
Daniel F. de Sousa ◽  
Danya B. Lima ◽  
...  
Keyword(s):  
Chagas Disease ◽  
Antibacterial Effect ◽  
Therapeutic Potential ◽  
Chronic Phase ◽  
Public Health Problem ◽  
Peritoneal Macrophages ◽  
Inhibitory Effects ◽  
Antimicrobial Drugs ◽  
Viable Cells ◽  
Therapeutic Value

The therapeutic potential of toxins has aroused great interest in the scientific community. Microbial resistance is a serious current public health problem, in part because of the wide use of antimicrobial drugs. Furthermore, there are several problems in the treatment of parasitic diseases such as leishmaniosis and Chagas’ disease, including the low efficacy in some clinical phases of the diseases and the loss of effectiveness of benzonidazole in the chronic phase of Chagas’ disease. In this context, the aim of this work was to study the antimicrobial and antiparasitic effects of Bothropoides lutzi total venom (BltTV). The venom exerted an antibacterial effect on S. aureus, with MIC=MLC=200 μg/mL. The inhibitory effects of BltTV on promastigote forms of Leishmania amazonensis and L. chagasi were assessed by counting of viable cells after incubation with BltTV. IC50 values of 234.6 μg/mL and 61.2 μg/mL, were obtained, respectively. Furthermore, the venom repressed epimastigote forms of Trypanosoma cruzi growth. Finally, BltTV was verified to affect murine peritoneal macrophages, causing a cytotoxic effect at the highest concentrations (100 and 50 μg/mL). In conclusion, Bothropoides lutzi venom demonstrated antibacterial and antiparasite effects, suggesting that the venom contains some substance(s) of therapeutic value.

scholarly journals Pharmacological Inhibition of Caspase-8 Suppresses Inflammation-Induced Angiogenesis in the Cornea

Biomolecules ◽  
2020 ◽  
Vol 10 (2) ◽  
pp. 210
Author(s):  
Yunzhe Tian ◽  
He Li ◽  
Xiuxing Liu ◽  
Lihui Xie ◽  
Zhaohao Huang ◽  
...  
Keyword(s):  
Molecular Mechanisms ◽  
Therapeutic Potential ◽  
Corneal Neovascularization ◽  
Caspase 8 ◽  
Inhibitory Effects ◽  
Toll Like Receptor 4 ◽  
Pharmacological Inhibition ◽  
Cytokines And Chemokines ◽  
Tnf Α

Inflammation-induced angiogenesis is closely related to many diseases and has been regarded as a therapeutic target. Caspase-8 has attracted increasing attention for its immune properties and therapeutic potential in inflammatory disorders. The aim of our study is to investigate the clinical application of pharmacological inhibition of caspase-8 and the underlying molecular mechanisms in inflammation-induced angiogenesis in the cornea. A model of alkali burn (AB)-induced corneal neovascularization (CNV) in C57BL/6 wild-type (WT) mice and toll-like receptor 4 knockout (Tlr4-/-) mice was used. We found that AB increased caspase-8 activity and the pharmacological inhibition of caspase-8 exerted substantial inhibitory effects on CNV, with consistent decreases in caspase-8 activity, inflammatory cell infiltration, macrophage recruitment and activation, VEGF-A, TNF-α, IL-1β, MIP-1, and MCP-1 expression in the cornea. In vitro, caspase-8 mediated TLR4–dependent chemokines and VEGF-A production by macrophages. The TLR4 knockout significantly alleviated CNV, suppressed caspase-8 activity and downregulated expression of inflammatory cytokines and chemokines after AB. Taken together, these findings provide the first demonstration that the pharmacological inhibition of caspase-8 suppresses inflammation-induced angiogenesis and support the use of a pharmacological caspase-8 inhibitor as a novel clinical treatment for CNV and other angiogenic disorders.

scholarly journals Secondary Metabolites from the Culture of the Marine-derived Fungus Paradendryphiella salina PC 362H and Evaluation of the Anticancer Activity of Its Metabolite Hyalodendrin

Marine Drugs ◽  
2020 ◽  
Vol 18 (4) ◽  
pp. 191
Author(s):  
Ambre Dezaire ◽  
Christophe H. Marchand ◽  
Marine Vallet ◽  
Nathalie Ferrand ◽  
Soraya Chaouch ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Cancer Cells ◽  
Crude Extract ◽  
High Throughput Screening ◽  
Therapeutic Potential ◽  
Cancer Cell Line ◽  
Anticancer Activities ◽  
Chemical Library ◽  
Altered Expression ◽  
Cancer Aggressiveness

High-throughput screening assays have been designed to identify compounds capable of inhibiting phenotypes involved in cancer aggressiveness. However, most studies used commercially available chemical libraries. This prompted us to explore natural products isolated from marine-derived fungi as a new source of molecules. In this study, we established a chemical library from 99 strains corresponding to 45 molecular operational taxonomic units and evaluated their anticancer activity against the MCF7 epithelial cancer cell line and its invasive stem cell-like MCF7-Sh-WISP2 counterpart. We identified the marine fungal Paradendryphiella salina PC 362H strain, isolated from the brown alga Pelvetia caniculata (PC), as one of the most promising fungi which produce active compounds. Further chemical and biological characterizations of the culture of the Paradendryphiella salina PC 362H strain identified (-)-hyalodendrin as the active secondary metabolite responsible for the cytotoxic activity of the crude extract. The antitumor activity of (-)-hyalodendrin was not only limited to the MCF7 cell lines, but also prominent on cancer cells with invasive phenotypes including colorectal cancer cells resistant to chemotherapy. Further investigations showed that treatment of MCF7-Sh-WISP2 cells with (-)-hyalodendrin induced changes in the phosphorylation status of p53 and altered expression of HSP60, HSP70 and PRAS40 proteins. Altogether, our study reveals that this uninvestigated marine fungal crude extract possesses a strong therapeutic potential against tumor cells with aggressive phenotypes and confirms that members of the epidithiodioxopiperazines are interesting fungal toxins with anticancer activities.

scholarly journals The Application of Simulated Moving-Bed Chromatography for the Separation of Ginsenosides in Sanchi Ginseng and American Ginseng

2020 ◽  
Vol 15 (10) ◽  
pp. 1934578X2096467
Author(s):  
Tai Thi Ngoc Dong ◽  
Chih-Hsiung Lin ◽  
Ming-Tsai Liang
Keyword(s):  
Crude Extract ◽  
Large Scale ◽  
Aqueous Ethanol ◽  
American Ginseng ◽  
Simulated Moving Bed ◽  
Moving Bed ◽  
Pharmaceutical Ingredients ◽  
Antisolvent Precipitation ◽  
Simulated Moving Bed Chromatography ◽  
Significant Difference

In this study, the separation of ginsenosides from the crude extract of Sanchi ginseng and American ginseng, obtained by aqueous ethanol extraction, was conducted in a simulated moving bed (SMB) with cleaning in place (CIP) design. Concentrated products with 86.2%, w/w, and 91.5%, w/w, of ginsenosides were obtained by the utilization of CIP-SMB for Sanchi and American ginseng, respectively. This study reveals that CIP-SMB could enrich ginsenosides by removing the retained impurities, which were initially extracted by aqueous ethanol and not removed by either the antisolvent precipitation for Sanchi ginseng or the ethyl acetate extraction for American ginseng. Although the ginsenosides in both ginsengs are similar, the difficulty in applying chromatography to the crude extract differs. A natural crude extract normally contains compounds with significant difference in retention. A traditional SMB with 4 sections will be, consequently, unable to continuously separate the natural products. This study develops methods for pretreating the crude extract and demonstrates the feasibility of continuously separating ginsenosides by using SMB. SMB is an effective technology for large-scale chromatography and can generally resolve solvent and energy consumption problems. This is expected to promote the industrial use of SMB for the production of concentrated ginsenosides as active pharmaceutical ingredients.

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