Kahweol Exerts Skin Moisturizing Activities by Upregulating STAT1 Activity

Kahweol is a diterpene present in coffee. Until now, several studies have shown that kahweol has anti-inflammatory and anti-angiogenic functions. Due to the limited research available about skin protection, this study aims to discern the potential abilities of kahweol and the possible regulation targets. First, the cytotoxicity of kahweol was checked by 3-4-5-dimethylthiazol-2-yl)-2-5-diphenyltetrazolium bromide assay, while 2,20-azino-bis (3ethylbenzothiazoline-6-sulphonic acid) diammonium salt and 1-diphenyl-2-picryl-hydrazyl were used to examine the radical scavenging ability. Polymerase chain reaction analysis was performed to explore the proper time points and doses affecting skin hydration and barrier-related genes. Luciferase assay and Western blotting were used to explore the possible transcription factors. Finally, fludarabine (a STAT1 inhibitor) was chosen to discern the relationship between skin-moisturizing factors and STAT1. We found that HaCaT cells experienced no toxicity from kahweol, and kahweol displayed moderate radical scavenging ability. Moreover, kahweol increased the outcome of HAS1, HAS2, occludin, and TGM-1 from six hours in a dose-dependent manner as well as the activation of STAT1 from six hours. Additionally, kahweol recovered the suppression of HAS2, STAT1-mediated luciferase activity, and HA secretion, which was all downregulated by fludarabine. In this study, we demonstrated that kahweol promotes skin-moisturizing activities by upregulating STAT1.

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Water Extractable Phytochemicals from Peppers (Capsicumspp.) Inhibit Acetylcholinesterase and Butyrylcholinesterase Activities and Prooxidants Induced Lipid Peroxidation in Rat BrainIn Vitro

International Journal of Food Science ◽

10.1155/2014/605618 ◽

2014 ◽

Vol 2014 ◽

pp. 1-7 ◽

Cited By ~ 2

Author(s):

Omodesola O. Ogunruku ◽

Ganiyu Oboh ◽

Ayokunle O. Ademosun

Keyword(s):

Lipid Peroxidation ◽

Antioxidant Capacity ◽

Radical Scavenging ◽

Antioxidant Property ◽

Inhibitory Effect ◽

Dependent Manner ◽

Significant Difference ◽

Radical Scavenging Ability ◽

Dose Dependent ◽

Anticholinesterase Properties

Background. This study sought to investigate antioxidant capacity of aqueous extracts of two pepper varieties (Capsicum annuumvar.accuminatum(SM) andCapsicum chinense(RO)) and their inhibitory effect on acetylcholinesterase and butyrylcholinesterase activities.Methods. The antioxidant capacity of the peppers was evaluated by the 2,2′-azino-bis(3-ethylbenzthiazoline-6-sulphonic acid) (ABTS) radical scavenging ability and ferric reducing antioxidant property. The inhibition of prooxidant induced lipid peroxidation and cholinesterase activities in rat brain homogenates was also evaluated.Results. There was no significant difference (P>0.05) in the total phenol contents of the unripe and ripeCapsicumspp. extracts. Ripe and unripe SM samples had significantly higher (P<0.05) ABTS*scavenging ability than RO samples, while the ripe fruits had significantly higher (P<0.05) ferric reducing properties in the varieties. Furthermore, the extracts inhibited Fe2+and quinolinic acid induced lipid peroxidation in rats brain homogenates in a dose-dependent manner. Ripe and unripe samples from SM had significantly higher AChE inhibitory abilities than RO samples, while there was no significant difference in the BuChE inhibitory abilities of the pepper samples.Conclusion. The antioxidant and anticholinesterase properties ofCapsicumspp. may be a possible dietary means by which oxidative stress and symptomatic cognitive decline associated with neurodegenerative conditions could be alleviated.

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Shikonin treatment ameliorates Lipopolysaccharides (LPS) induced acute liver failure in mice via regulating the miR-106/MCL1 and miR-34a/SIRT1/TP53 signaling

Archives of Medical Science ◽

10.5114/aoms/127659 ◽

2021 ◽

Author(s):

Fan Huang ◽

Hua Hai ◽

Buwei Gao

Keyword(s):

Animal Model ◽

Signaling Pathways ◽

Serum Levels ◽

Luciferase Assay ◽

High Dose ◽

Dependent Manner ◽

Protein Levels ◽

The Relationship ◽

Dose Dependent ◽

Different Doses

IntroductionThe treatment with shikonin (SKN) suppresses the expression of miR-106 and miR-34a. Furthermore, SIRT1 and MCL1 are targets of miR-34a and miR-106, respectively. In this study, we treated an animal model of ALF with high dose (1.0 mg/kg) and low dose (0.5 mg/kg) of SKN to investigate its effect on liver functions and signaling pathways of SKN/miR-106/MCL1 and SKN/miR-34a/SIRT1/TP53.Material and methodsALF animal model was established and the serum levels of alanine aminotransferase (ALT) and aspartate aminotransferase (AST) were analyzed to evaluate the effects of different doses of SKN. TUNNEL was performed to assess hepatocyte apoptosis. Luciferase assay, RT-qPCR and Western blot analysis were performed to measure the relationship between miR-106, miR-34a, SIRT1 and MCL1.ResultsIn the ALF mice models, the administration of SKN decreased the levels of ALT and AST in a dose-dependent manner, along with a significantly decreased number of apoptotic hepatocytes. And SKN may protect liver during ALF via reducing the level of inflammation. Luciferase assay showed that the co-transfection of wild-type MCL1/SIRT1 and miR-106/miR-34a significantly decreased the luciferase activity of LO2 cells, thus indicating that MCL1 and SIRT1 are identified as targets of miR-106 and miR-34a, respectively, while SIRT1 could act as a regulator of TP53. Moreover, the expression of miR-106, miR-34a and TP53 was decreased over an increasing concentration of SKN, along with the increasing mRNA and protein levels of MCL1 and SIRT1.ConclusionsIn this study, we showed that SKN alleviated ALF in a dose-dependent manner via regulating the signaling pathways of SKN/miR-106/MCL1 and SKN/miR-34a/SIRT1/TP53.

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Isolation, Characterization and Bioactive Properties of Alkali-Extracted Polysaccharides from Enteromorpha prolifera

Marine Drugs ◽

10.3390/md18110552 ◽

2020 ◽

Vol 18 (11) ◽

pp. 552

Author(s):

Shifeng Zhao ◽

Yuan He ◽

Chungu Wang ◽

Israa Assani ◽

Peilei Hou ◽

...

Keyword(s):

Antioxidant Activities ◽

Radical Scavenging ◽

Helical Structure ◽

Scientific Basis ◽

Dependent Manner ◽

Enteromorpha Prolifera ◽

Molecular Weights ◽

Diphenyltetrazolium Bromide ◽

Dose Dependent

Four new purified polysaccharides (PAP) were isolated and purified from the Enteromorpha prolifera by alkali extraction, and further characterization was investigated. Their average molecular weights of PAP-1, PAP-2, PAP-3, and PAP-4 were estimated as 3.44 × 104, 6.42 × 104, 1.20 × 105, and 4.82 × 104 Da, respectively. The results from monosaccharide analysis indicated that PAP-1, PAP-2, PAP-3 were acidic polysaccharides and PAP-4 was a neutral polysaccharide. PAP-1 and PAP-2 mainly consist of galacturonic acid, while PAP-3 and PAP-4 mainly contained rhamnose. Congo red test showed that no triple helical structure was detected in the four polysaccharides. The antioxidant activities were investigated using 1,1-diphenyl-2-picrylhydrazyl (DPPH), Superoxide, and 2, 2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical assay. In vitro antitumor activities were evaluated by 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. PAP-1 exhibited relatively stronger antioxidant activities among the four polysaccharides in a dose-dependent manner. At a concentration of 1.00 mg/mL, the antioxidant activities of PAP-1 on the DPPH radical scavenging rate, superoxide anion radical scavenging rate, and ABTS radical rate at 1.00 mg/mL were 56.40%, 54.27%, and 42.07%, respectively. They also showed no significant inhibitory activity against MGC-803, HepG2, T24, and Bel-7402 cells. These investigations of polysaccharides provide a scientific basis for the use of E. prolifera as an ingredient in functional foods and medicines.

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MiR-125a-5p Alleviates Dysfunction and Inflammation of Pentylenetetrazol- induced Epilepsy Through Targeting Calmodulin-dependent Protein Kinase IV (CAMK4)

Current Neurovascular Research ◽

10.2174/1567202616666190906125444 ◽

2019 ◽

Vol 16 (4) ◽

pp. 365-372 ◽

Cited By ~ 4

Author(s):

Qishuai Liu ◽

Li Wang ◽

Guizhen Yan ◽

Weifa Zhang ◽

Zhigang Huan ◽

...

Keyword(s):

Protein Kinase ◽

Target Gene ◽

Luciferase Assay ◽

Enzyme Linked Immunosorbent Assay ◽

Inflammatory Factor ◽

Dependent Protein Kinase ◽

Expression Levels ◽

Dependent Protein ◽

Polymerase Chain ◽

The Relationship

Background: MicroRNAs (miRNA) are known to play a key role in the etiology and treatment of epilepsy through controlling the expression of gene. However, miR-125a-5p in the epilepsy is little known. Epilepsy in rat models was induced by Pentylenetetrazol (PTZ) and miR- 125a-5p profiles in the hippocampus were investigated in our experiment. Also, the relationship between miR-125a-5p and calmodulin-dependent protein kinase IV (CAMK4) was identified and the related mechanism was also illustrated. Methods: The miR-125a-5p mRNA expression levels were evaluated by quantitative real time polymerase chain reaction (qRT-PCR). Western Blot (WB) was used to analyze the CAMK4 protein expression levels. Seizure score, latency and duration were determined based on a Racine scale. The enzyme-linked immunosorbent assay (ELISA) was used to analyze the inflammatory factor expression. The relationship between miR-125a-5p and CAMK4 was detected through dual luciferase assay. Results: Downregulation of miR-125a-5p was observed in the hippocampus of PTZ-induced epilepsy rats. The overexpression of miR-125a-5p attenuated seizure and decreased inflammatory factor level in the hippocampus of PTZ-induced rats. The miR-125a-5p alleviated epileptic seizure and inflammation in PTZ-induced rats by suppressing its target gene, CAMK4. Conclusion: miR-125a-5p may represent a novel therapeutic treatment for PTZ-induced epilepsy by preventing the activation of CAMK4.

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IN VITRO CYTOTOXIC AND APOPTOTIC EFFECT OF PASSIFLORA FOETIDA AGAINST CERVICAL CANCER CELLS AND ITS FOURIER TRANSFORM INFRARED PROFILING

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2017.v10i11.20226 ◽

2017 ◽

Vol 10 (11) ◽

pp. 46

Author(s):

Dheeban Shankar ◽

Basker S ◽

Karthik S

Keyword(s):

Fourier Transform ◽

Functional Groups ◽

Fourier Transform Infrared ◽

Dependent Manner ◽

Diphenyltetrazolium Bromide ◽

Cervical Cancer Cells ◽

Apoptotic Effect ◽

Passiflora Foetida ◽

Dose Dependent

Objective: This study was aimed on the analysis of cytotoxic and apoptotic action of Passiflora foetida followed by identification of the functional groups responsible for the activity.Methods: In this study, cytotoxic and apoptotic effect of methanol extract of P. foetida were analyzed by treating HeLa cell line cultures with different concentrations of the extract (25, 50, 75, 100, and 125 μg/ml), and thereby the activity was ratified by 3-(4,5-dimethylthiazol-2-yl)-2,5- diphenyltetrazolium bromide (MTT) assay and propidium iodide staining. The functional groups of the bioactive compounds for the effectiveness of the treatment were known by Fourier transform infrared spectroscopy analysis (FTIR).Results: The cytotoxic activity was found to be increased in a dose-dependent manner with inhibitory concentration value of 21.55 μg/ml and showed an effective apoptosis. Further, FTIR analysis confirmed the presence of functional groups of alkaloids, flavonoids, saponins, steroids, terpenoids, phenols and cardiac glycosides which might be responsible for the aforesaid activity.Conclusion: The cytotoxic and apoptotic action of P. foetida was proved to be very effective, and the tenable functional groups were identified.

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Insulin-responsive cultured foetal-rat hepatocytes. Their preparation and characterization

Biochemical Journal ◽

10.1042/bj2230039 ◽

1984 ◽

Vol 223 (1) ◽

pp. 39-46 ◽

Cited By ~ 14

Author(s):

D C DeSante ◽

L Little ◽

D E Peavy ◽

F Vinicor

Keyword(s):

Monolayer Culture ◽

Cultured Cells ◽

Rat Hepatocytes ◽

Dependent Manner ◽

Deoxyribonuclease I ◽

Haematopoietic Cells ◽

Foetal Rat ◽

The Relationship ◽

Dose Dependent ◽

Scatchard Plots

An improved non-perfusion method for the preparation of cultured foetal-rat hepatocytes is described. Digestion of the liver with collagenase and deoxyribonuclease I gave yields of 40 × 10(6) hepatocytes/g of liver. The plating efficiency of hepatocytes in medium with 10 microM-cortisol was 50%. Cell morphology and metabolism were maintained through 3 days of monolayer culture, with minimal contamination by haematopoietic cells or fibroblasts. The cultured cells bound and degraded 125I-insulin in a time- and dose-dependent manner. The estimated ED50 for competitive binding at 37 degrees C was 1.1 nM. Curvilinear Scatchard plots were observed, with estimates of 16 500 high-affinity sites (Kd = 813 pM) and 53 000 low-affinity sites (Kd = 23 nM) per cell. The cultured cells demonstrated a glycogenic response to insulin, with an estimated ED50 of 120 pM. The degree of glycogenic response to insulin varied with time in culture: 500% above basal on day 1, 200% on day 2, and only 150% on day 3. Cultured foetal cells also exhibited a time-dependent uptake of 2-aminoisobutyric acid, which, in contrast with previous reports with adult cells, was not stimulated by the presence of 10 nM-insulin. Cultured foetal hepatocytes may provide an interesting model with which to study the relationship between insulin-receptor binding and insulin action.

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Betulinic acid induces apoptosis of gallbladder cancer cells via repressing SCD1

Acta Biochimica et Biophysica Sinica ◽

10.1093/abbs/gmz148 ◽

2020 ◽

Vol 52 (2) ◽

pp. 200-206 ◽

Cited By ~ 2

Author(s):

Hongfei Wang ◽

Fangxiao Dong ◽

Ye Wang ◽

Xu’an Wang ◽

Defei Hong ◽

...

Keyword(s):

Gallbladder Cancer ◽

Betulinic Acid ◽

Polymerase Chain Reaction Analysis ◽

Inhibitory Effect ◽

Dependent Manner ◽

Antitumor Effects ◽

Concentration Dependent Manner ◽

Polymerase Chain ◽

Induced Apoptosis ◽

Scd1 Expression

Abstract Gallbladder cancer (GBC) is the most common and aggressive malignancy of the biliary tract. Betulinic acid (BetA) has been reported to have anti-inflammatory and antitumor effects; however, the effect of BetA on GBC is still unknown. In this study, we investigated the effect of BetA on five GBC cell lines and found that BetA significantly inhibited the proliferation of NOZ cells but had little inhibitory effect on other GBC cells. BetA disturbed mitochondrial membrane potential and induced apoptosis in NOZ cells. Real-time polymerase chain reaction analysis revealed that stearoyl-coenzyme A desaturase 1 (SCD1) was highly expressed in NOZ cells but low expressed in other GBC cells. BetA inhibited SCD1 expression in a concentration-dependent manner in NOZ cells. Downregulation of SCD1 expression by RNA interference inhibited the proliferation of NOZ cells and induced cell apoptosis. Moreover, BetA inhibited the growth of xenografted tumors and suppressed SCD1 expression in nude mice. Thus, our results showed that BetA induced apoptosis through repressing SCD1 expression in GBC, suggesting that BetA might be an effective agent for the treatment of patients with GBC that highly expresses SCD1.

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Chondroprotective Activity ofMurraya exoticathrough Inhibitingβ-Catenin Signaling Pathway

Evidence-based Complementary and Alternative Medicine ◽

10.1155/2013/752150 ◽

2013 ◽

Vol 2013 ◽

pp. 1-8 ◽

Cited By ~ 4

Author(s):

Longhuo Wu ◽

Haiqing Liu ◽

Rui Zhang ◽

Linfu Li ◽

Jialin Li ◽

...

Keyword(s):

Degenerative Joint Disease ◽

Joint Disease ◽

Chondrocyte Apoptosis ◽

Dependent Manner ◽

Chain Reaction ◽

Protein Expressions ◽

Murraya Exotica ◽

Oa Chondrocytes ◽

Polymerase Chain ◽

Dose Dependent

Osteoarthritis (OA) is a degenerative joint disease that affects millions of people. Currently, there is no effective drug treatment for it. The purpose of this study is to investigate the chondroprotective effects ofMurraya exotica(L.) on OA. The rat OA models were duplicated to prepare for separating OA chondrocytes, synovial fluid (SF), and serum containingM. exotica(50 mg/kg, 100 mg/kg, and 200 mg/kg),M. exoticashowed the activity of decreasing the contents of TNF-αand IL-1βin SF and the chondrocyte apoptosis in a dose-dependent manner. To investigate the probable mechanism, quantitative real-time polymerase chain reaction (qRT-PCR) and western blotting were used to determine gene expression and protein profiles, respectively. The results reveal thatM. exoticacan downregulate mRNA and protein expressions ofβ-catenin and COX-2 and reporter activity significantly. Conclusively,M. exoticaexhibits antiapoptotic chondroprotective activity probably through inhibitingβ-catenin signaling.

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Cutaneous Adverse Effects With HER1/EGFR-Targeted Agents: Is There a Silver Lining?

Journal of Clinical Oncology ◽

10.1200/jco.2005.00.6916 ◽

2005 ◽

Vol 23 (22) ◽

pp. 5235-5246 ◽

Cited By ~ 359

Author(s):

Román Peréz-Soler ◽

Leonard Saltz

Keyword(s):

Surrogate Marker ◽

Growth Factor Receptor ◽

Dependent Manner ◽

Activity Data ◽

Egfr Inhibition ◽

The Face ◽

Epidermal Growth ◽

Management Recommendations ◽

The Relationship ◽

Dose Dependent

The human epidermal growth factor receptor (HER1/EGFR) is dysregulated in many solid tumors, making it an attractive target for anticancer therapy. A number of agents that target this receptor are in use or in development. A specific adverse effect common to this class of agent is a papulopustular rash, usually on the face and upper torso, which generally occurs in a dose-dependent manner. Little is known about the etiology of this rash, and there are no clear evidence-based management recommendations. Histologic data indicate that rash may be caused by HER1/EGFR inhibition in skin, although this has not been confirmed. Findings suggest that there is a relationship between the development of rash and response and/or survival, making rash a potential surrogate marker of activity. Data from multiple studies with cetuximab and erlotinib show a consistent relationship between rash and response, as well as between rash and survival. The relationship between rash and clinical outcome is currently less consistent for gefitinib. Some studies report a correlation, whereas others do not. The cause of the possible relationship between rash and clinical benefit remains unclear at this time, and additional studies are needed to determine the clinical utility of this observation.

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Chemical characterization, antioxidant and cytotoxic activities of the methanolic extract of Hymenocrater longiflorus grown in Iraq

Zeitschrift für Naturforschung C ◽

10.1515/znc-2015-4145 ◽

2015 ◽

Vol 70 (9-10) ◽

pp. 227-235 ◽

Cited By ~ 4

Author(s):

Rafal S.A. Al-Anee ◽

Ghassan M. Sulaiman ◽

Khulood W. Al-Sammarrae ◽

Giuliana Napolitano ◽

Renzo Bagnati ◽

...

Keyword(s):

Antioxidant Activities ◽

Radical Scavenging Activity ◽

Radical Scavenging ◽

Chemical Characterization ◽

Cytotoxic Activities ◽

Dependent Manner ◽

Histone H2ax ◽

Northern Iraq ◽

Polyphenolic Composition ◽

Diphenyltetrazolium Bromide

Abstract Hymenocrater longiflorus was collected from northern Iraq, and the chemical composition and antioxidant and cytotoxic activities of this plant were investigated. Ten compounds detected by HPLC-ESI/MS were identified as flavonoids and phenolic acids. The free radical scavenging activity of the 70% methanol extract was evaluated using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay. The antioxidant activities of the extract may be attributed to its polyphenolic composition. The cytotoxicity of the plant extract against the osteosarcoma (U2OS) cell line was assessed with the 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) assay. The extract significantly reduced the viability of cells in a concentration- and time-dependent manner. Cells were arrested during the S-phase of the cell cycle, and DNA damage was revealed by antibodies against histone H2AX. The apoptotic features of cell shrinkage and decrease in cell size were also observed. Western blot analysis revealed cleavage of poly (ADP-ribose)-polymerase 1 (PARP-1), in addition to increases in the proteins p53, p21, and γ-H2AX. Collectively, our findings demonstrate that the H. longiflorus extract is highly cytotoxic to U2OS cells, most likely due to its polyphenolic composition.

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