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1.
Plants (Basel) ; 13(7)2024 Apr 06.
Article in English | MEDLINE | ID: mdl-38611563

ABSTRACT

In this study, the antioxidant (DPPH and ABTS radical-scavenging, ferric-reducing, iron (II)-chelating), anti-inflammatory (LPS-induced Raw 264.7 cell line), and cytotoxic activities (Du145 and A549 cell lines) of raw fruit, ripe fruit and leaves of the Lycium ferocissimum species were examined. By using high-pressure liquid chromatography, p-OH benzoic acid, caffeic acid, and rutin were detected in the ethanol and water extracts. For the most active raw fruit ethanol extract, the IC50 in terms of the DPPH-scavenging activity was 0.57 mg/mL, and the ABTS inhibition percentage was 88.73% at a 3 mg/mL concentration. The raw fruit ethanol extract exhibited significant inhibition of viability in the Du145 cell line in the concentration range of 62.5-1000 µg/mL. Additionally, the extract effectively reduced the LPS-induced inflammation parameters (TNF-α, IFN-γ, PGE 2, and NO) at a concentration of 31.25 µg/mL. The biological activities of L. ferocissimum, which have been elucidated for the first time, have yielded promising results.

2.
Toxicol Res (Camb) ; 13(2): tfae046, 2024 Apr.
Article in English | MEDLINE | ID: mdl-38533180

ABSTRACT

Breast cancer is one of the most common types of cancer causing high mortality rates among women worldwide. This study was aimed to evaluate the effect of Pistacia terebinthus (terebinth) resin extract (TRE) on the MDA-MB-231 breast cancer cell line. In the study, the cytotoxic dose of the resin extract in MDA-MB-231 cells was evaluated by MTS analysis. The effect of TRE on apoptosis was examined by Hoechst staining. Caspase-3 and cleaved caspase-3 protein expressions were determined by western blot analysis. Based on the outcomes of our MTS analysis, the IC50 dose of TRE was calculated at 56.54 µg/mL during a 24-h application period. With Hoechst staining analysis, an increase was observed in cells that underwent apoptotic change at 10 and 100 µg/ml TRE concentrations compared to the control. At 25 and 50 µg/mL TRE concentrations, no apoptotic change was found in comparison to the control; however, a significant drop in the number of viable cells was observed because 200, 300, and 500 µg/mL TRE concentrations were above the toxic dose. The caspase-3 protein expression level was significantly higher in cells treated with 100 µg/ml TRE compared to the control group, while there was no significant change in cleaved caspase-3 protein expression. It was thought that P. terebinthus resin might cause cell death in MDA-MB-231 cells via caspase-independent apoptosis pathway or other cell death pathways, and it was concluded that it could be a supportive treatment for breast cancer treatment.

3.
Plants (Basel) ; 12(17)2023 Aug 28.
Article in English | MEDLINE | ID: mdl-37687327

ABSTRACT

The essential oil of Pelargonium graveolens L. is valuable for its therapeutic benefits, so this study aimed to determine the synergistic effect of the combination of the essential oil of this plant with antibiotics instead of the extracts prepared with various solvents. In addition, the second goal of this study was to determine whether the essential oil combined with various antibiotics increased the overall killing activity in mouse macrophage cells with the aim of introducing an immunotherapeutic approach to the infection treatments used today. Herein, the volatile profile of Geranium oil (G.O) was analyzed using GC/MS. The current study sought to assess the synergistic characteristics of several antibiotic combinations using G.O against pneumococci, as well as the oil's antioxidant and antimicrobial activities. The major components of the oil were citronellol, geraniol, and isomenthone. In the combinations of G.O and antibiotics, the synergism of the Streptococcus pneumoniae to antibiotics advanced. When the time-kill data were evaluated, G.O + antibiotic combinations quickly diminished the viable cell count of S. pneumoniae from the 6th h. In this study, the combined use of existing antibiotics used in infection treatments with G.O could improve antibiotic effectiveness and thus prevent bacteria from developing antibiotic resistance.

4.
Chem Biodivers ; 20(1): e202200816, 2023 Jan.
Article in English | MEDLINE | ID: mdl-36482033

ABSTRACT

The present study is focused on the antimicrobial, antioxidant, cytotoxic, and DNA protective effects of methanol extract obtained from R. digitellata, R. fastigiata, R. fraxinea, and R. polymorpha species that are distributed in Turkey. The highest total phenol content was determined in R. digitellata (144.6 mgGAE/gextract ), and the highest total amount of flavonoids was found in R. fastigiata (20.40 mgGAE/gextract ). The content of usnic acid was determined by High-Performance Liquid Chromatography (HPLC) and the highest amount was found in R. digitellata. DPPH (1,1-diphenyl-2-picrylhydrazyl) and ABTS [2,2'-azinobis(3-ethylbenzathiazoline-6-sulfonic acid)] radical scavenging methods were used for antioxidant activity. R. fraxinea showed the highest DPPH⋅ and ABTS+ ⋅ scavenging activity. In addition, the DNA protective effect was investigated using pBR322 plasmid DNA, and; all studied species were found to have DNA protective effects. The antibacterial activity was investigated using the disc diffusion method, and the R. digitellata methanol extract showed the best results with a 12.35 mm zone on Proteus mirabilis. On the human lung cancer (A549) and breast cancer (MDA-MB-231) cell lines, cytotoxic activity was assessed using an MTT assay. All lichen extracts were found to have a significant cytotoxic effect on both cancer cell lines at 1000 µg/mL concentration. These results suggest that Ramalina species may be potential candidates for developing new phytopharmaceuticals and functional components.


Subject(s)
Anti-Infective Agents , Antineoplastic Agents , Humans , Antioxidants/chemistry , Methanol , Plant Extracts/pharmacology , Plant Extracts/chemistry , Anti-Infective Agents/pharmacology , DNA
5.
Molecules ; 27(23)2022 Nov 26.
Article in English | MEDLINE | ID: mdl-36500342

ABSTRACT

Centaurea pichleri subsp. pichleri, Conyza canadensis, and Jasminum fruticans are traditionally used plants grown in Turkey. Methanol extracts were obtained from these plants and pharmacological activity studies and phytochemical analyses were carried out. To evaluate the phytochemical composition, spectrophotometric and chromatographic techniques were used. The extracts were evaluated for antioxidant activity by DPPH●, ABTS●+ radical scavenging, and FRAP assays. The cytotoxic effects of the extracts were investigated on DU145 prostate cancer and A549 lung cancer cell lines. The anti-inflammatory effects of extracts were investigated on the NO amount, TNF-α, IFN-γ, and PGE 2 levels in lipopolysaccharide-stimulated Raw 264.7 cells. The richest extract in terms of phenolic compounds (98.19 ± 1.64 mgGAE/gextract) and total flavonoids (21.85 ± 0.64 mgCA/gextract) was identified as C. pichleri subsp. pichleri methanol extract. According to antioxidant activity determinations, the C. pichleri subsp. pichleri extract was found to be the most active extract. Finally, the C. pichleri subsp. pichleri methanol extract was revealed to be the most effective inhibitor of viability in the cytotoxic activity investigation, and the extract with the best anti-inflammatory action. The findings point to C. pichleri subsp. pichleri as a promising source of bioactive compounds in the transition from natural sources to industrial uses, such as new medications, cosmeceuticals, and nutraceuticals.


Subject(s)
Centaurea , Conyza , Erigeron , Oleaceae , Plants, Medicinal , Antioxidants/chemistry , Centaurea/chemistry , Plants, Medicinal/chemistry , Methanol , Plant Extracts/pharmacology , Plant Extracts/chemistry , Phytochemicals/pharmacology , Anti-Inflammatory Agents/pharmacology
6.
Antioxidants (Basel) ; 11(10)2022 Sep 20.
Article in English | MEDLINE | ID: mdl-36290576

ABSTRACT

Arctium minus (Hill) Bernh. (Asteraceae), which has a wide distribution area in Turkey, is a medicinally important plant. Eighty percent methanol extracts of the leaf, flower head, and root parts of A. minus were prepared and their sub-fractions were obtained. Spectrophotometric and chromatographic (high-performance liquid chromatography) techniques were used to assess the phytochemical composition. The extracts were evaluated for antioxidant activity by diphenyl-2-picrylhydrazil radical (DPPH●), 2,2'-Azino-bis 3-ethylbenzothiazoline-6-sulfonic acid (ABTS●+) radical scavenging, and ß-carotene linoleic acid bleaching assays. Furthermore, the extracts were subjected to α-amylase, α-glucosidase, lipoxygenase, and tyrosinase enzyme inhibition tests. The cytotoxic effects of extracts were investigated on MCF-7 and MDA-MB-231 breast cancer cell lines. The richest extract in terms of phenolic compounds was identified as the ethyl acetate sub-fraction of the root extract (364.37 ± 7.18 mgGAE/gextact). Furthermore, chlorogenic acid (8.855 ± 0.175%) and rutin (8.359 ± 0.125%) were identified as the primary components in the leaves' ethyl acetate sub-fraction. According to all methods, it was observed that the extracts with the highest antioxidant activity were the flower and leaf ethyl acetate fractions. Additionally, ABTS radical scavenging activity of roots' ethyl acetate sub-fraction (2.51 ± 0.09 mmol/L Trolox) was observed to be as effective as that of flower and leaf ethyl acetate fractions at 0.5 mg/mL. In the ß-carotene linoleic acid bleaching assay, leaves' methanol extract showed the highest antioxidant capacity (1422.47 ± 76.85) at 30 min. The enzyme activity data showed that α-glucosidase enzyme inhibition of leaf dichloromethane extract was moderately high, with an 87.12 ± 8.06% inhibition value. Lipoxygenase enzyme inhibition was weakly detected in all sub-fractions. Leaf methanol extract, leaf butanol, and root ethyl acetate sub-fractions showed 99% tyrosinase enzyme inhibition. Finally, it was discovered that dichloromethane extracts of leaves, roots, and flowers had high cytotoxic effects on the MDA-MB-231 cell line, with IC50 values of 21.39 ± 2.43, 13.41 ± 2.37, and 10.80 ± 1.26 µg/mL, respectively. The evaluation of the plant extracts in terms of several bioactivity tests revealed extremely positive outcomes. The data of this study, in which all parts of the plant were investigated in detail for the first time, offer promising results for future research.

7.
Front Pharmacol ; 13: 902551, 2022.
Article in English | MEDLINE | ID: mdl-36133811

ABSTRACT

Ginger (Zingiber officinale Roscoe), a member of the Zingiberaceae family, is one of the most popular spices worldwide, known since ancient times, and used both as a spice and a medicinal plant. The phenolic compounds found in ginger are predominantly gingerols, shogaols, and paradols. Gingerols are the major phenolic compounds found in fresh ginger and contain mainly 6-gingerol as well as 4-, 5-, 8-, 10-, and 12-gingerols. Gingerols possess a wide array of bioactivities, such as antioxidant and anticancer, among others. Regarding the different array of biological activities and published data on the mechanisms underlying its action, the complex interaction between three key events, including inflammation, oxidative stress, and immunity, appears to contribute to a plethora of pharmacological activities of this compound. Among these, the immunomodulatory properties of these compounds, which attract attention due to their effects on the immune system, have been the focus of many studies. Gingerols can alleviate inflammation given their ability to inhibit the activation of protein kinase B (Akt) and nuclear factor kappa B (NF-κB) signaling pathways, causing a decrease in proinflammatory and an increase in anti-inflammatory cytokines. However, given their low bioavailability, it is necessary to develop new and more effective strategies for treatment with gingerols. In order to overcome this problem, recent studies have addressed new drug delivery systems containing gingerols. In this review, the immunomodulatory activities of gingerol and its underlying mechanisms of action combined with the contributions of developed nanodrug delivery systems to this activity will be examined.

8.
S Afr J Bot ; 146: 36-47, 2022 May.
Article in English | MEDLINE | ID: mdl-35210693

ABSTRACT

Salvia ekimiana Celep & Dogan is an endemic species of Turkey. To our knowledge, the number of studies on biological activities and phytochemical profiling of this plant is quite limited. Therefore, this study aimed to analyze its activities and phytochemical content in detail. The qualitative-quantitative compositions were determined via spectrophotometric and chromatographic (LC-MS/MS and HPLC) techniques. 1,1-Diphenyl-2-picrylhydrazyl radical (DPPH•) and 2,2'-Azino-bis 3-ethylbenzothiazoline-6-sulfonic acid (ABTS•+) radical scavenging and ascorbate-iron (III)-catalyzed phospholipid peroxidation experiments were performed to measure antioxidant capacity. Hyaluronidase, collagenase, and elastase enzyme inhibition tests were determined in vitro using a spectrophotometer. Antiproliferative activity was evaluated in human lung cancer (A549) and human breast cancer (MCF7) cells. The murine fibroblast (L929) cell line was used as a normal control cell. While the subextract rich in phenolic compounds was n-butanol extract, rosmarinic acid was defined as the main secondary metabolite. The highest antioxidant activity observed for the n-butanol subextract included the following: DPPH• EC50: 0.08±0.00 mg/mL, TEAC/ABTS: 2.19±0.09 mmol/L Trolox, MDA EC50: 0.42±0.03 mg/mL. The methanolic extract, the ethyl acetate, and n-butanol subextracts displayed significant inhibitory activity on collagenase, while the other subextracts did not show any inhibitory activity on hyaluronidase and elastase. Due to strong interactions with their active sites, molecular docking showed luteolin 7-glucuronide, apigenin 7-glucuronide, and luteolin 5-glucoside had the highest binding affinity with target enzymes. The chloroform subextract showed significant cytotoxicity in all cell lines. These novel results revealed that S. ekimiana has strong antioxidant, collagenase enzyme inhibitory, and cytotoxic potential.

9.
Article in English | MEDLINE | ID: mdl-35176983

ABSTRACT

The article has been withdrawn at the request of the author of the journal Current Pharmaceutical Biotechnology.Bentham Science apologizes to the readers of the journal for any inconvenience this may have caused. Bentham Science Disclaimer: It is a condition of publication that manuscripts submitted to this journal have not been published and will not be simultaneously submitted or published elsewhere. Furthermore, any data, illustration, structure or table that has been published elsewhere must be reported, and copyright permission for reproduction must be obtained. Plagiarism is strictly forbidden, and by submitting the article for publication the authors agree that the publishers have the legal right to take appropriate action against the authors, if plagiarism or fabricated information is discovered. By submitting a manuscript the authors agree that the copyright of their article is transferred to the publishers if and when the article is accepted for publication.

10.
CNS Neurol Disord Drug Targets ; 21(9): 795-817, 2022.
Article in English | MEDLINE | ID: mdl-34872486

ABSTRACT

Parkinson's Disease (PD) is a multifaceted disorder with various factors suggested to play a synergistic pathophysiological role, such as oxidative stress, autophagy, pro-inflammatory events, and neurotransmitter abnormalities. While it is crucial to discover new treatments in addition to preventing PD, recent studies have focused on determining whether nutraceuticals will exert neuroprotective actions and pharmacological functions in PD. Quercetin, a flavonol-type flavonoid, is found in many fruits and vegetables and is recognised as a complementary therapy for PD. The neuroprotective effect of quercetin is directly associated with its antioxidant activity, in addition to stimulating cellular defence against oxidative stress. Other related mechanisms are activating Sirtuins (SIRT1) and inducing autophagy, in addition to induction of Nrf2-ARE and Paraoxonase 2 (PON2). Quercetin, whose neuroprotective activity has been demonstrated in many studies, unfortunately, has a disadvantage because of its poor water solubility, chemical instability, and low oral bioavailability. It has been reported that the disadvantages of quercetin have been eliminated with nanocarriers loaded with quercetin. The role of nanotechnology and nanodelivery systems in reducing oxidative stress during PD provides an indisputable advantage. Accordingly, the present review aims to shed light on quercetin's beneficial effects and underlying mechanisms in neuroprotection. In addition, the contribution of nanodelivery systems to the neuroprotective effect of quercetin is also discussed.


Subject(s)
Neuroprotective Agents , Parkinson Disease , Antioxidants/metabolism , Antioxidants/pharmacology , Antioxidants/therapeutic use , Humans , Neuroprotective Agents/pharmacology , Neuroprotective Agents/therapeutic use , Oxidative Stress , Parkinson Disease/drug therapy , Quercetin/pharmacology , Quercetin/therapeutic use
11.
Curr Neuropharmacol ; 20(3): 594-610, 2022 Mar 04.
Article in English | MEDLINE | ID: mdl-34561984

ABSTRACT

Neuromuscular junction (NMJ) disorders result from damage, malfunction or absence of one or more key proteins involved in neuromuscular transmission, comprising a wide range of disorders. The most common pathology is antibody-mediated or downregulation of ion channels or receptors, resulting in Lambert-Eaton myasthenic syndrome, myasthenia gravis, and acquired neuromyotonia (Isaac's syndrome), and rarely congenital myasthenic syndromes caused by mutations in NMJ proteins. A wide range of symptomatic treatments, immunomodulating therapies, or immunosuppressive drugs have been used to treat NMJ diseases. Future research must be directed at a better understanding of the pathogenesis of these diseases, and developing novel disease-specific treatments. Numerous secondary metabolites, especially alkaloids isolated from plants, have been used to treat NMJ diseases in traditional and clinical practices. An ethnopharmacological approach has provided leads for identifying new treatments for NMJ diseases. In this review, we performed a literature survey in Pubmed, Science Direct, and Google Scholar to gather information on drug discovery from plant sources for NMJ disease treatments. To date, most research has focused on the effects of herbal remedies on cholinesterase inhibitory and antioxidant activities. This review provides leads for identifying potential new drugs from plant sources for the treatment of NMJ diseases.


Subject(s)
Biological Products , Lambert-Eaton Myasthenic Syndrome , Myasthenia Gravis , Biological Products/pharmacology , Biological Products/therapeutic use , Humans , Lambert-Eaton Myasthenic Syndrome/therapy , Myasthenia Gravis/drug therapy , Neuromuscular Junction , Synaptic Transmission
12.
Front Biosci (Landmark Ed) ; 26(11): 1089-1096, 2021 11 30.
Article in English | MEDLINE | ID: mdl-34856755

ABSTRACT

Aim: The aim of this study is the synthesis of nanosilver particles (AgNPs) from Pelargonium quercetorum Agnew. (Geraniaceae) and evaluation of the antimicrobial and the cytotoxic potential of AgNPs. Methods: The synthesized AgNPs were evaluated for antimicrobial and anticancer efficacy using the minimum inhibition concentration method and MTT (3-(4,5-Dimethylthiazol-2-yl)-2,5-Diphenyltetrazolium bromide) assay. Results: The AgNPs inhibited approximately 90% the growth of gram-positive Staphylococcus aureus and gram-negative Esherichia coli and yeast Candida albicans pathogens at a concentration of 500 µg/mL. The synthesized AgNPs showed excellent toxicity in MCF-7 cells, and specifically, pq70 AgNP inhibited the growth of MCF-7 cells by 52% at a concentration of 3.125 µg/mL. Conclusion: It was determined that the AgNPs, which had been synthesized from extracts that contained a high phenolic composition, were smaller in size, and showed high anticancer and antimicrobial properties.


Subject(s)
Anti-Infective Agents , Metal Nanoparticles , Pelargonium , Anti-Bacterial Agents/pharmacology , Anti-Infective Agents/pharmacology , Microbial Sensitivity Tests , Plant Extracts/pharmacology
13.
Cancers (Basel) ; 13(11)2021 May 31.
Article in English | MEDLINE | ID: mdl-34073059

ABSTRACT

Many anticancer active compounds are known to have the capacity to destroy pathologically proliferating cancer cells in the body, as well as to destroy rapidly proliferating normal cells. Despite remarkable advances in cancer research over the past few decades, the inclusion of natural compounds in researches as potential drug candidates is becoming increasingly important. However, the perception that the natural is reliable is an issue that needs to be clarified. Among the various chemical classes of natural products, anthraquinones have many biological activities and have also been proven to exhibit a unique anticancer activity. Emodin, an anthraquinone derivative, is a natural compound found in the roots and rhizomes of many plants. The anticancer property of emodin, a broad-spectrum inhibitory agent of cancer cells, has been detailed in many biological pathways. In cancer cells, these molecular mechanisms consist of suppressing cell growth and proliferation through the attenuation of oncogenic growth signaling, such as protein kinase B (AKT), mitogen-activated protein kinase (MAPK), HER-2 tyrosine kinase, Wnt/-catenin, and phosphatidylinositol 3-kinase (PI3K). However, it is known that emodin, which shows toxicity to cancer cells, may cause kidney toxicity, hepatotoxicity, and reproductive toxicity especially at high doses and long-term use. At the same time, studies of emodin, which has poor oral bioavailability, to transform this disadvantage into an advantage with nano-carrier systems reveal that natural compounds are not always directly usable compounds. Consequently, this review aimed to shed light on the anti-proliferative and anti-carcinogenic properties of emodin, as well as its potential toxicities and the advantages of drug delivery systems on bioavailability.

14.
Mar Drugs ; 18(8)2020 Aug 13.
Article in English | MEDLINE | ID: mdl-32823595

ABSTRACT

Carotenoids are natural fat-soluble pigments synthesized by plants, algae, fungi and microorganisms. They are responsible for the coloration of different photosynthetic organisms. Although they play a role in photosynthesis, they are also present in non-photosynthetic plant tissues, fungi, and bacteria. These metabolites have mainly been used in food, cosmetics, and the pharmaceutical industry. In addition to their utilization as pigmentation, they have significant therapeutically applications, such as improving immune system and preventing neurodegenerative diseases. Primarily, they have attracted attention due to their antioxidant activity. Several statistical investigations indicated an association between the use of carotenoids in diets and a decreased incidence of cancer types, suggesting the antioxidant properties of these compounds as an important factor in the scope of the studies against oxidative stress. Unusual marine environments are associated with a great chemical diversity, resulting in novel bioactive molecules. Thus, marine organisms may represent an important source of novel biologically active substances for the development of therapeutics. Marine carotenoids (astaxanthin, fucoxanthin, ß-carotene, lutein but also the rare siphonaxanthin, sioxanthin, and myxol) have recently shown antioxidant properties in reducing oxidative stress markers. Numerous of bioactive compounds such as marine carotenoids have low stability, are poorly absorbed, and own very limited bioavailability. The new technique is nanoencapsulation, which can be used to preserve marine carotenoids and their original properties during processing, storage, improve their physiochemical properties and increase their health-promoting effects. This review aims to describe the role of marine carotenoids, their potential applications and different types of advanced nanoformulations preventing and treating oxidative stress related disorders.


Subject(s)
Antioxidants/pharmacology , Aquatic Organisms/chemistry , Carotenoids/pharmacology , Nanoparticles , Oxidative Stress/drug effects , Animals , Antioxidants/chemistry , Antioxidants/isolation & purification , Antioxidants/pharmacokinetics , Biological Availability , Carotenoids/chemistry , Carotenoids/isolation & purification , Carotenoids/pharmacokinetics , Drug Compounding , Fresh Water , Humans , Molecular Structure , Nanotechnology , Seawater , Structure-Activity Relationship
15.
Molecules ; 25(11)2020 May 31.
Article in English | MEDLINE | ID: mdl-32486408

ABSTRACT

Combretastatins are a class of closely related stilbenes (combretastatins A), dihydrostilbenes (combretastatins B), phenanthrenes (combretastatins C) and macrocyclic lactones (combretastatins D) found in the bark of Combretum caffrum (Eckl. & Zeyh.) Kuntze, commonly known as the South African bush willow. Some of the compounds in this series have been shown to be among the most potent antitubulin agents known. Due to their structural simplicity many analogs have also been synthesized. Combretastatin A4 phosphate is the most frequently tested compounds in preclinical and clinical trials. It is a water-soluble prodrug that the body can rapidly metabolize to combretastatin A4, which exhibits anti-tumor properties. In addition, in vitro and in vivo studies on combretastatins have determined that these compounds also have antioxidant, anti-inflammatory and antimicrobial effects. Nano-based formulations of natural or synthetic active agents such as combretastatin A4 phosphate exhibit several clear advantages, including improved low water solubility, prolonged circulation, drug targeting properties, enhanced efficiency, as well as fewer side effects. In this review, a synopsis of the recent literature exploring the combretastatins, their potential effects and nanoformulations as lead compounds in clinical applications is provided.


Subject(s)
Antineoplastic Agents, Phytogenic/chemistry , Stilbenes/chemistry , Animals , Anti-Infective Agents/pharmacology , Anti-Inflammatory Agents/pharmacology , Antineoplastic Agents, Phytogenic/pharmacology , Antioxidants/chemistry , Antiparasitic Agents/pharmacology , Caco-2 Cells , Cell Line, Tumor , Cell Proliferation , Combretum/chemistry , Drug Delivery Systems , HT29 Cells , Humans , Melanoma, Experimental/metabolism , Solubility , Stereoisomerism , Stilbenes/pharmacology , Structure-Activity Relationship , Tubulin/chemistry , Tubulin Modulators/pharmacology , Water/chemistry
16.
Antioxidants (Basel) ; 9(4)2020 Apr 01.
Article in English | MEDLINE | ID: mdl-32244734

ABSTRACT

Salvia aramiensis Rech. f. is a species that grows only in Hatay, Turkey and is used as a traditional stomachic tea. Neither the chemical composition nor the potential bioactivity of the plant has been investigated before. Antioxidant activity (1,1-Diphenyl-2-picrylhydrazyl Radical (DPPH●) and 2,2'-Azino-bis (3-ethylbenzothiazoline-6-sulfonic acid (ABTS+●) radical scavenging and ß-carotene/linoleic acid co-oxidation) of 70% methanol, 70% ethanol extracts, and 2% infusion obtained from S. aramiensis aerial parts were determined. The effect of 70% methanol extract on collagenase and elastase enzyme inhibition and its chemical composition via chromatographic methods (LC-MS/MS and HPLC) were analyzed. Nanoliposomes were developed with 70% methanol extract, were characterized, and were evaluated. The key parameters for the most active 70% methanol extract included the following DPPH•EC50: 28.4 µg/mL, Trolox equivalent antioxidant capacity (TEAC)/ABTS: 1.77 ± 0.09 mmol/L/Trolox. Furthermore 70% methanol extract showed more than 50% inhibition on collagenase and elastase enzymes at all the concentrations. The main component of the extract, rich in phenolic compounds, has been identified as rosmarinic acid; 83.7 µg/mL extract was released from the nanoliposomal formulation. The extract and its formulation are found to be nontoxic on the L929 fibroblast cell line. This study successfully developed a long-term antioxidant and enzyme inhibitory formulation containing S. aramiensis, which has been used safely among the public for years.

17.
Adv Exp Med Biol ; 1152: 283-292, 2019.
Article in English | MEDLINE | ID: mdl-31456190

ABSTRACT

Based on the insights gleaned from decades of research, it seems clear that mechanistic target of rapamycin (mTOR) is an essential signaling node that integrates environmental clues for regulation of cell survival, metabolism and proliferation of the cells. However, overwhelmingly increasing scientific evidence has added a new layer of intricacy to already complicated and versatile signaling pathway of mTOR. Deregulation of spatio-temporally controlled mTOR-driven pathway played contributory role in breast cancer development and progression. Pharmacologists and molecular biologists have specifically emphasized on the identification and development of mTOR-pathway inhibitors. In this chapter we have attempted to provide an overview of the most recent findings related to therapeutic targeting of mTOR-associated mTORC1 and mTORC2 in breast cancer. We have also comprehensively summarized regulation of mTOR and its partners by microRNAs in breast cancer.


Subject(s)
Breast Neoplasms/drug therapy , Drug Resistance, Neoplasm , Mechanistic Target of Rapamycin Complex 1/metabolism , Mechanistic Target of Rapamycin Complex 2/metabolism , TOR Serine-Threonine Kinases/metabolism , Female , Humans , MicroRNAs/genetics , Molecular Targeted Therapy , Neoplasm Metastasis
18.
Cell Mol Biol (Noisy-le-grand) ; 64(11): 102-107, 2018 Aug 30.
Article in English | MEDLINE | ID: mdl-30213297

ABSTRACT

Piperlongumine is a biologically and pharmacologically active constituent of the plant Piper longum. This compound is gradually gaining attention because of its ability to inhibit/prevent different cancers. Modern era of molecular oncology is incomplete without ground-breaking discoveries made in the field of cell signaling pathways. High-throughput technologies have considerably improved our understanding about wide ranging signal transduction cascades which play crucial role in cancer development and progression. It is exciting to note that piperlongumine has been shown to pleiotropically modulate different oncogenic signaling pathways. We partition this multi-component review into discrete sections and categorically summarize key findings related to excellent ability of piperlongumine to therapeutically target JAK-STAT, NF-kB and PI3K/AKT/mTOR pathways. We also set spotlight on regulation of TRAIL pathway and autophagy by piperlongumine in different cancers. On the basis of the current understanding of piperlongumine, molecular biologists and pharmacologists will develop the next generation of translational studies, which will prove to be helpful in improving the clinical outcome and getting a step closer to personalized medicine.


Subject(s)
Antineoplastic Agents/pharmacology , Dioxolanes/pharmacology , Animals , Apoptosis/drug effects , Humans , Reactive Oxygen Species/metabolism , Signal Transduction/drug effects
19.
J Cancer Res Ther ; 14(2): 314-320, 2018.
Article in English | MEDLINE | ID: mdl-29516912

ABSTRACT

OBJECTIVE: The aim of study was to investigate anticancer effect of Viburnum opulus (VO) on Ehrlich ascites carcinoma (EAC) bearing mice that treated with different concentrations of VO. MATERIALS AND METHODS: For tumor transplantation; mice were inoculated with 1 × 106 EAC cells intraperitoneally and than divided into five groups (n = 9). Two hours after inoculation; experimental groups were treated daily with VO extract at doses of 1000 mg/kg, 2000 mg/kg, 4000 mg/kg. RESULTS: Extracts obtained from gilaburu juice can have hinder effect on tumor cell growth. CONCLUSION: As far as we known, this is the first study about in vivo antitumoral activity of VOon Ehrlich ascites tumor model, and consequently VO extract exhibited anticancer activity against EAC-bearing mice.


Subject(s)
Antineoplastic Agents, Phytogenic/pharmacology , Carcinoma, Ehrlich Tumor/metabolism , Carcinoma, Ehrlich Tumor/pathology , Plant Extracts/pharmacology , Viburnum/chemistry , Allografts , Animals , Antioxidants/pharmacology , Biomarkers , Carcinoma, Ehrlich Tumor/drug therapy , Cell Survival/drug effects , Disease Models, Animal , Immunohistochemistry , Kidney/drug effects , Kidney/metabolism , Liver/drug effects , Liver/metabolism , Male , Mice
20.
J Nanosci Nanotechnol ; 18(6): 3856-3864, 2018 Jun 01.
Article in English | MEDLINE | ID: mdl-29442719

ABSTRACT

Diabetes mellitus (DM) is a chronic metabolic disease and the subgroup of DM is called type II which is the most common form. The incidence of type II is increasing worldwide and it focuses on several new approaches to efficiently treatment of diabetes. Resveratrol (RSV) is known to be strong antioxidant and has an insulin-like effect in streptozotocin (STZ)-induced diabetic cells. It plays an active role at treatment of diabetes with reducing the oxidative stress, lowering glucose levels and protection of beta cells which are responsible for insulin secretion. In our study, we prepared two different RSV-loaded nanoliposomes (LPs), characterized in vitro and evaluated efficiencies of LPs on diabetes and related oxidative stress. Release and transport studies of RSV through dialyse membrane and pancreatic beta TC (ß TC) cells were investigated from its solution and LPs. Stability studies were performed at two different conditions (4 °C and 25 °C ± 60% relative humidity) for 3 months. Particle size (PS), zeta potential (ZP), polydispersity index (PDI), encapsulation efficiency (EE) and type of the formulations were determined. ß TC cell line was used in cell culture studies and cell viability was measured with using 3-(4,5-dimethyldiazol-2-yl)-2,5 diphenyl tetrazolium bromide (MTT) cytotoxicity test. The antidiabetic effects of RSV LPs were investigated on ß TC cell induced with glucose and STZ and we evaluated relationship between glucose and insulin concentration before and after incubation with LPs containing RSV. Antioxidant and preventive effects of RSV-loaded LPs against diabetes-associated oxidative stress were determined with superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px) enzyme assay. When all results were evaluated together, these new developed liposomal formulations significantly decreased high glucose levels in diabetic cell groups synchronous with increasing insulin levels and they showed prolonged antioxidant activity against oxidative stress for 24 hours compared to RSV solution.


Subject(s)
Antioxidants/administration & dosage , Diabetes Mellitus/drug therapy , Stilbenes/administration & dosage , Animals , Antioxidants/chemistry , Blood Glucose , Diabetes Mellitus, Experimental , Drug Delivery Systems , Insulin , Liposomes , Nanoparticles , Oxidative Stress , Rats, Wistar , Resveratrol , Stilbenes/chemistry , Streptozocin
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