scholarly journals Clavukoellians G–K, New Nardosinane and Aristolane Sesquiterpenoids with Angiogenesis Promoting Activity from the Marine Soft Coral Lemnalia sp.

Marine Drugs ◽  
2020 ◽  
Vol 18 (3) ◽  
pp. 171 ◽  
Author(s):  
Qi Wang ◽  
Xuli Tang ◽  
Hui Liu ◽  
Xiangchao Luo ◽  
Ping Jyun Sung ◽  
...  
Keyword(s):  
Quantitative Analysis ◽  
Structure Elucidation ◽  
Soft Coral ◽  
Spectroscopic Techniques ◽  
Dependent Manner ◽  
Zebrafish Model ◽  
Chemical Examination ◽  
Xisha Islands ◽  
New Compounds ◽  
Dose Dependent

The chemical examination of the marine soft coral Lemnalia sp., collected at the Xisha islands in the South China Sea, resulted in the isolation of four new nardosinane-type sesquiterpenoids, namely clavukoellians G–J (1–4), and one new aristolane sesquiterpene, namely clavukoellian K (5), together with five known compounds, 6–10. The structure elucidation of the isolated natural products was based on various spectroscopic techniques including HRESIMS and NMR, while their absolute configurations were resolved on the basis of comparisons of the ECD spectra with the calculated ECD data. The isolated new compounds 1–5 were evaluated for their anti- and pro- angiogenesis activities in a transgenic fluorescent zebrafish (Tg(vegfr2:GFP)) model. Quantitative analysis revealed that compound 5 displayed pro-angiogenesis activity in a PTK787-induced vascular injury zebrafish model at 2.5 μM. Data showed that compound 5 significantly promoted the angiogenesis in a dose-dependent manner.

scholarly journals A Pilot Study on Antimalarial Effects of Moringa oleifera Leaf Extract in Plasmodium berghei Infection in Mice

2017 ◽  
Vol 15 (2) ◽  
pp. 151-156
Author(s):  
Somrudee NAKINCHAT ◽  
Voravuth SOMSAK
Keyword(s):  
Plasma Glucose ◽  
Crude Extract ◽  
Plasmodium Berghei ◽  
Leaf Extract ◽  
Moringa Oleifera ◽  
Dependent Manner ◽  
Glucose Levels ◽  
New Compounds ◽  
Dose Dependent

The emergence and spread of antimalarial drug resistance of Plasmodium parasites, as well as hypoglycemia, during malaria infection, and subsequent death, are critical problems in malaria-endemic areas. Hence, finding new compounds, especially plant extracts having antimalarial and anti-hypoglycemic activities, are urgently needed. The present study aimed to investigate the antimalarial and anti-hypoglycemic effects of Moringa oleifera leaf extract in Plasmodium berghei infection in mice. Aqueous crude extract of M. oleifera leaves was freshly prepared and used for an efficacy test in vivo. Groups of ICR mice (5 mice in each) were infected with 1´107 infected red blood cells of P. berghei ANKA by intraperitoneal injection and given the extract orally with doses of 100, 500, and 1000 mg/kg for 4 consecutive days. Parasitemia and plasma glucose levels were subsequently measured. The results showed that M. oleifera leaf extract presented significant (p < 0.001) inhibition of parasitemia in a dose-dependent manner. Moreover, this extract exerted anti-hypoglycemia effects in infected mice in a dose-dependent manner. The highest degrees of activity were found at a dose of 1000 mg/kg of the extract. Additionally, no effect on plasma glucose was found in normal mice treated with this extract. It can be concluded that aqueous crude extract of M. oleifera leaves exerted antimalarial and anti-hypoglycemic effects in P. berghei infection in mice.

scholarly journals Acetylcholinesterase and Butyrylcholinesterase Inhibitory Compounds from Corydalis Cava (Fumariaceae)

2011 ◽  
Vol 6 (5) ◽  
pp. 1934578X1100600 ◽  
Author(s):  
Jakub Chlebek ◽  
Kateřina Macáková ◽  
Lucie Cahlíková ◽  
Milan Kurfürst ◽  
Jiří Kuneš ◽  
...  
Keyword(s):  
Human Blood ◽  
Inhibitory Activity ◽  
Potent Inhibitor ◽  
The Other ◽  
Spectroscopic Techniques ◽  
Dependent Manner ◽  
Isoquinoline Alkaloids ◽  
Chemical Structures ◽  
Inhibitory Compounds ◽  
Dose Dependent

Tubers of Corydalis cava were extracted with ethanol and fractionated using n-hexane, chloroform and ethanol. Repeated column chromatography, preparative TLC and crystallization led to the isolation of fifteen isoquinoline alkaloids. The chemical structures of the isolated compounds were determined on the basis of spectroscopic techniques and by comparison with literature data. All isolated compounds were tested for human blood acetylcholinesterase (HuAChE) and human plasma butyrylcholinesterase (HuBuChE) inhibitory activity. (+)-Canadaline inhibited acetylcholinesterase as well as butyrylcholinesterase in a dose-dependent manner with IC50 values of 20.1 ± 1.1 μM and 85.2 ± 3.2 μM, respectively. (+)-Canadine, with an IC50 value of 12.4 ± 0.9 μM, was the most potent inhibitor of acetylcholinesterase, whilst (±)-corycavidine and (+)-bulbocapnine were effective inhibitors of butyrylcholinesterase with IC50 values of 46.2 ± 2.4 uM and 67.0 ± 2.1 μM, respectively. The other isolated alkaloids were considered inactive (IC50 > 100 μM).

scholarly journals Fibrinogen Gamma Chain Promotes Aggregation of Vesicular Stomatitis Virus in Saliva

Viruses ◽  
2020 ◽  
Vol 12 (3) ◽  
pp. 282 ◽  
Author(s):  
Valesca Anschau ◽  
Rafael Sanjuán
Keyword(s):  
Quantitative Analysis ◽  
Vesicular Stomatitis Virus ◽  
Rna Virus ◽  
Comparative Proteomics ◽  
Dependent Manner ◽  
Gamma Chain ◽  
Vesicular Stomatitis ◽  
Molecular Components ◽  
Dose Dependent ◽  
Infectious Unit

The spread of viruses among cells and hosts often involves multi-virion structures. For instance, virions can form aggregates that allow for the co-delivery of multiple genome copies to the same cell from a single infectious unit. Previously, we showed that vesicular stomatitis virus (VSV), an enveloped, negative-strand RNA virus, undergoes strong aggregation in the presence of saliva from certain individuals. However, the molecular components responsible for such aggregation remain unknown. Here we show that saliva-driven aggregation is protein dependent, and we use comparative proteomics to analyze the protein content of strongly versus poorly aggregating saliva. Quantitative analysis of over 300 proteins led to the identification of 18 upregulated proteins in strongly aggregating saliva. One of these proteins, the fibrinogen gamma chain, was verified experimentally as a factor promoting VSV aggregation in a dose-dependent manner. This study hence identifies a protein responsible for saliva-driven VSV aggregation. Yet, the possible involvement of additional proteins or factors cannot be discarded.

scholarly journals New Thiazole Nortopsentin Analogues Inhibit Bacterial Biofilm Formation

Marine Drugs ◽  
2018 ◽  
Vol 16 (8) ◽  
pp. 274 ◽  
Author(s):  
Anna Carbone ◽  
Barbara Parrino ◽  
Maria Cusimano ◽  
Virginia Spanò ◽  
Alessandra Montalbano ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Biofilm Formation ◽  
Microbial Growth ◽  
Bacterial Biofilm ◽  
Dependent Manner ◽  
Gram Negative ◽  
Ic50 Values ◽  
Planktonic Form ◽  
New Compounds ◽  
Dose Dependent

New thiazole nortopsentin analogues were conveniently synthesized and evaluated for their activity as inhibitors of biofilm formation of relevant Gram-positive and Gram-negative pathogens. All compounds were able to interfere with the first step of biofilm formation in a dose-dependent manner, showing a selectivity against the staphylococcal strains. The most active derivatives elicited IC50 values against Staphylococcus aureus ATCC 25923, ranging from 0.40–2.03 µM. The new compounds showed a typical anti-virulence profile, being able to inhibit the biofilm formation without affecting the microbial growth in the planktonic form.

scholarly journals Soft Coral Dendronephthya puetteri Extract Ameliorates Inflammations by Suppressing Inflammatory Mediators and Oxidative Stress in LPS-Stimulated Zebrafish

2018 ◽  
Vol 19 (9) ◽  
pp. 2695 ◽  
Author(s):  
Eun-A Kim ◽  
Yuling Ding ◽  
Hye-Won Yang ◽  
Soo-Jin Heo ◽  
Seung-Hong Lee
Keyword(s):  
Cell Death ◽  
Soft Coral ◽  
In Vivo Model ◽  
Dependent Manner ◽  
Soft Corals ◽  
Zebrafish Model ◽  
Inflammatory Agent ◽  
Anti Inflammatory ◽  
Inflammatory Effect

Marine-derived extract and/or bioactive compounds have attracted increasing demand due to their unique and potential uses as cures for various inflammation-based diseases. Several studies revealed anti-inflammatory candidates found in soft corals. However, the effects of soft corals on inflammation in an in vivo model remain to be determined. Therefore, the extract of soft coral Dendronephthya puetteri (DPE) was investigated for an in vivo anti-inflammatory effect in a lipopolysaccharide (LPS)-stimulated zebrafish model to determine its potential use as a natural anti-inflammatory agent. We also investigated whether DPE has toxic effects in a zebrafish model. No significant changes were observed in terms of survival, heart beat rate, or developmental abnormalities in the zebrafish embryos exposed to a concentration below 100 µg/mL of DPE. Treating the zebrafish model with LPS-treatment significantly increased the ROS, NO generation, and cell death. However, DPE inhibited this LPS-stimulated ROS, NO generation, and cell death in a dose-dependent manner. In addition, DPE significantly reduced the mRNA expression of both iNOS and COX-2 and markedly suppressed the expression levels of the proinflammatory cytokines, TNF-α and IL-6, in an LPS-stimulated zebrafish model. These findings demonstrate that DPE has profound anti-inflammatory effect in vivo, suggesting that DPE might be a strong natural anti-inflammatory agent.

scholarly journals Synthesis of new pyrazolone and pyrazole-based adamantyl chalcones and antimicrobial activity

2020 ◽  
Vol 40 (9) ◽  
Author(s):  
Rawan Al-Saheb ◽  
Sami Makharza ◽  
Feras Al-battah ◽  
Rajab Abu-El-Halawa ◽  
Tawfeq Kaimari ◽  
...  
Keyword(s):  
High Dose ◽  
Moderate Activity ◽  
Dependent Manner ◽  
H Nmr ◽  
Ft Ir ◽  
Bacteria And Fungi ◽  
New Compounds ◽  
Dose Dependent ◽  
Ft Ir Spectroscopy ◽  
C Nmr

Abstract Chalcones and their derivatives are becoming increasingly popular due to their various pharmacological effects. Chalcone molecules may be extracted from natural resources, entirely synthesised, or biosynthesised by modifying the natural ones. In the present study, five pyrazole-based adamantyl heterocyclic compounds were synthesised by condensation of 1-adamantyl chalcone with substituted phenylhydrazine. The products were characterised by using ¹H NMR, ¹³C NMR and FT-IR spectroscopy. The microbiological activity of these compounds was investigated against bacteria and fungi. The new compounds showed good to moderate activity against the microbial species used for screening. All developed molecules showed antibacterial activity against Gram-negative and Gram-positive. These molecules showed antifungal activities against Fusarium oxysporum fungus and in a dose-dependent manner, apart from RS-1 molecules which showed compromised antifungal activity and even at a high dose.

scholarly journals Heterocornols from the Sponge-Derived Fungus Pestalotiopsis heterocornis with Anti-Inflammatory Activity

Marine Drugs ◽  
2021 ◽  
Vol 19 (11) ◽  
pp. 585
Author(s):  
Hui Lei ◽  
Xiaoxu Bi ◽  
Xiuping Lin ◽  
Jianglian She ◽  
Xiaowei Luo ◽  
...  
Keyword(s):  
Chemical Study ◽  
Antimicrobial Activities ◽  
Sea Salt ◽  
Inflammatory Activity ◽  
Raw 264.7 Cells ◽  
Dependent Manner ◽  
Inos Protein Expression ◽  
Anti Inflammatory ◽  
New Compounds ◽  
Dose Dependent

One strain-many compounds (OSMAC) manipulation of the sponge-derived fungus Pestalotiopsis heterocornis XWS03F09 resulted in the production of new secondary metabolites. The chemical study of the fermentation, cultivated on 3% artificial sea salt in the rice media, led to the isolation of twelve compounds, including eight new polyketide derivatives, heterocornols Q–X (1–8), one new ceramide (9), and three known analogues (10–12). The structures and absolute configurations of the new compounds were elucidated by spectroscopic data and calculated ECD analysis. Heterocornols Q (1) and R (2) are novel 6/5/7/5 tetracyclic polyketide derivatives featuring dihydroisobenzofuran and benzo-fused dioxabicyclo [4.2.1] nonane system, which might be derived from the acetyl-CoA by epoxidation, polyene cyclization, and rearrangement to form the core skeleton. Compound 12 showed moderate or weak antimicrobial activities against with MIC values ranging from 25 to 100 μg/mL. Heterocornols T and X (7 and 8) could inhibit the production of LPS-induced NO significantly, comparable to dexamethasone. Further Western blotting analysis showed 7 and 8 markedly suppressed the iNOS protein expression in LPS-induced RAW 264.7 cells in a dose-dependent manner. The result showed that 7 and 8 might serve as potential leads for development of anti-inflammatory activity.

A comparison of cholecystokinin-induced changes in gastric emptying and feeding in rats

1988 ◽  
Vol 255 (1) ◽  
pp. R21-R26 ◽  
Author(s):  
K. L. Conover ◽  
S. M. Collins ◽  
H. P. Weingarten
Keyword(s):  
Quantitative Analysis ◽  
Gastric Emptying ◽  
Intraperitoneal Administration ◽  
Delay Gastric Emptying ◽  
Dependent Manner ◽  
Experimental Conditions ◽  
Cholecystokinin Octapeptide ◽  
Feeding Effects ◽  
Induced Changes ◽  
Dose Dependent

We have compared the abilities of the cholecystokinin octapeptide (CCK-8) to delay gastric emptying and to influence feeding under similar experimental conditions in the rat. The effect of CCK-8 on gastric emptying was assessed in 6-h-deprived rats receiving 10-ml intragastric test loads of 0.15 M saline or 15% (wt/vol) sucrose. Analysis of half-emptying times indicated that intraperitoneal administration of CCK-8 in doses of 1.4-22.4 micrograms/kg produced a dose-dependent retardation of emptying of both saline and nutrient. Lower doses of CCK-8, 0.01 and 0.1 micrograms/kg, had no effect on gastric emptying. The effect of CCK-8 on feeding was assessed in normally feeding rats tested under the same experimental conditions used in the gastric emptying studies. Doses of CCK-8 capable of retarding gastric emptying also suppressed eating in a dose-dependent manner. These findings provide necessary correlational support for the hypothesis that the satiety produced by CCK-8 may be mediated by inhibition of gastric emptying. However, a further quantitative analysis of the correspondence of the gastric emptying and feeding effects of CCK-8 suggest that retardation of emptying cannot account entirely for the satiety effect of the peptide.

scholarly journals Isolation of 4,5-O-Dicaffeoylquinic Acid as a Pigmentation Inhibitor Occurring inArtemisia capillarisThunberg and Its ValidationIn Vivo

2016 ◽  
Vol 2016 ◽  
pp. 1-11 ◽  
Author(s):  
Nadia Tabassum ◽  
Ji-Hyung Lee ◽  
Soon-Ho Yim ◽  
Galzad Javzan Batkhuu ◽  
Da-Woon Jung ◽  
...  
Keyword(s):  
Active Component ◽  
Cultured Cells ◽  
Dependent Manner ◽  
Zebrafish Model ◽  
Artemisia Capillaris ◽  
Dicaffeoylquinic Acid ◽  
Dose Dependent ◽  
Tyrosinase Related Protein ◽  
Pigmentation Disorders

There is a continual need to develop novel and effective melanogenesis inhibitors for the prevention of hyperpigmentation disorders. The plantArtemisia capillarisThunberg (Oriental Wormwood) was screened for antipigmentation activity using murine cultured cells (B16-F10 malignant melanocytes). Activity-based fractionation using HPLC and NMR analyses identified the compound 4,5-O-dicaffeoylquinic acid as an active component in this plant. 4,5-O-Dicaffeoylquinic acid significantly reduced melanin synthesis and tyrosinase activity in a dose-dependent manner in the melanocytes. In addition, 4,5-O-dicaffeoylquinic acid treatment reduced the expression of tyrosinase-related protein-1. Significantly, we could validate the antipigmentation activity of this compoundin vivo, using a zebrafish model. Moreover, 4,5-O-dicaffeoylquinic acid did not show toxicity in this animal model. Our discovery of 4,5-O-dicaffeoylquinic acid as an inhibitor of pigmentation that is activein vivoshows that this compound can be developed as an active component for formulations to treat pigmentation disorders.

Synthesis of New Calixarene Derivatives and Evaluation of Their Cytotoxic Activity

2021 ◽  
Author(s):  
Mehmet Oguz ◽  
Ayse Yildirim ◽  
Irem Mukaddes Durmus ◽  
Serdar Karakurt ◽  
Mustafa Yilmaz
Keyword(s):  
Cancer Cells ◽  
Human Cancer ◽  
Carcinoma Cells ◽  
Spectroscopic Techniques ◽  
Dependent Manner ◽  
Human Cancer Cells ◽  
H Nmr ◽  
Cancerous Cells ◽  
Dose Dependent ◽  
Derivatives Of

Abstract Since calixarenes are more easily synthesized and functionalized than other supramolecules, they are compounds of interest in organic chemistry. In this study, the dihydrazide (3a and 3b) and diamino propyl (6a and 6b) derivatives of p-tert-butylcalix[4]arene and calix[4]arene were synthesized. Then the L-proline methyl ester substituted chlorocyclopropenium was reacted with the calix[4]arene derivatives (3a, 3b, 6a, and 6b) at room temperature in CH2Cl2 to obtain calix[4]arene superbase derivatives (4a, 4b, 7a, and 7b) in 75%, 60%, 70% and 55% yield, respectively. The synthesized compounds' structure was elucidated by using spectroscopic techniques (FTIR, 1H NMR, and 13C NMR ). The cytotoxic properties of the calix[4]arene superbase derivatives were investigated against different human cancerous cells, including A549, DLD-1, HEPG2, and PC-3, as well as human healthy epithelium cell line PNT1A. The cytotoxicity results showed that calix[4]arene superbase derivatives inhibited the proliferation of DLD-1, A549, HEPG2, and PC-3 cells in a dose-dependent manner. Compound 7a had the highest toxic effect on colorectal carcinoma (IC50: 4.7 µM), and the IC50 values were 18.5 µM and 74.4µM against human prostate and lung cancer cells, respectively. Furthermore, the compound 4b was found more effective on hepatocellular carcinoma cells (IC50: 210.2 µM). As a result, the synthesized calix[4]arene superbase derivatives can be developed to treat different human cancer cells. They can be considered as a preliminary result for molecular-level research.

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