scholarly journals Gallnuts: A Potential Treasure in Anticancer Drug Discovery

2018 ◽  
Vol 2018 ◽  
pp. 1-9 ◽  
Author(s):  
Jiayu Gao ◽  
Xiao Yang ◽  
Weiping Yin ◽  
Ming Li
Keyword(s):  
Anticancer Drugs ◽  
Case Reports ◽  
Bioactive Metabolites ◽  
Anticancer Activities ◽  
Web Based ◽  
Scientific Databases ◽  
Anticancer Properties ◽  
Rhus Chinensis ◽  
Pharmacological Studies ◽  
Fundamental Understanding

Introduction. In the discovery of more potent and selective anticancer drugs, the research continually expands and explores new bioactive metabolites coming from different natural sources. Gallnuts are a group of very special natural products formed through parasitic interaction between plants and insects. Though it has been traditionally used as a source of drugs for the treatment of cancerous diseases in traditional and folk medicinal systems through centuries, the anticancer properties of gallnuts are barely systematically reviewed. Objective. To evidence the traditional uses and phytochemicals and pharmacological mechanisms in anticancer aspects of gallnuts, a literature review was performed. Materials and Methods. The systematic review approach consisted of searching web-based scientific databases including PubMed, Web of Science, and Science Direct. The keywords for searching include gallnut, Galla Chinensis, Rhus chinensis, Rhus potaninii, Rhus punjabensis, nutgall, gall oak, Quercus infectoria, Quercus lusitanica, and galla turcica. Two reviewers extracted papers independently to remove the papers unrelated to the anticancer properties of gallnuts. Patents, abstracts, case reports, and abstracts in symposium and congress were excluded. Results and Conclusion. As a result, 14 articles were eligible to be evaluated. It is primarily evident that gallnuts contain a number of bioactive metabolites, which account for anticancer activities. The phytochemical and pharmacological studies reviewed strongly underpin a fundamental understanding of anticancer properties for gallnuts (Galla Chinensis and Galla Turcica) and support their ongoing clinical uses in China. The further bioactive compounds screening and evaluation, pharmacological investigation, and clinical trials are expected to progress gallnut-based development to finally transform the wild medicinal gallnuts to the valuable authorized anticancer drugs.

scholarly journals From Traditional Usage to Pharmacological Evidence: A Systematic Mini-Review of Spina Gleditsiae

2016 ◽  
Vol 2016 ◽  
pp. 1-6 ◽  
Author(s):  
Jiayu Gao ◽  
Xiao Yang ◽  
Weiping Yin
Keyword(s):  
Chemical Constituents ◽  
Pharmacological Activities ◽  
Traditional Use ◽  
Web Based ◽  
Scientific Databases ◽  
Pharmacological Studies ◽  
Fundamental Understanding ◽  
Medicinal Properties ◽  
Gleditsia Sinensis ◽  
Phytochemical Components

Spina Gleditsiae is an important herb with various medicinal properties in traditional and folk medicinal systems of East Asian countries. In China through the centuries, it has been traditionally used as a source of drugs for anticancer, detoxication, detumescence, apocenosis, and antiparasites effects. Recently, an increasing number of studies have been reported regarding its chemical constituents and pharmacological activities. To further evidence the traditional use, phytochemicals, and pharmacological mechanisms of this herb, a systematic literature review was performed herein for Spina Gleditsiae. The review approach consisted of searching several web-based scientific databases including PubMed, Web of Science, and Elsevier using the keywords “Spina Gleditsiae”, “Zao Jiao Ci”, and “Gleditsia sinensis”. Based on the proposed criteria, 17 articles were evaluated in detail. According to the reviewed data, it is quite evident that Spina Gleditsiae contains a number of bioactive phytochemical components, which account for variety medicinal values including anticancer, anti-inflammatory, antiatherogenic, antimicrobial, antiallergic, and antivirus activities. The phytochemical and pharmacological studies reviewed herein strongly underpin a fundamental understanding of herbal Spina Gleditsiae and support its ongoing clinical uses in China. The further phytochemical evaluation, safety verification, and clinical trials are expected to progress Spina Gleditsiae-based development to finally transform the traditional TCM herb Spina Gleditsiae to the valuable authorized drug.

scholarly journals Improved Anticancer Activities of a New Pentafluorothio-Substituted Vorinostat-Type Histone Deacetylase Inhibitor

2021 ◽  
Vol 14 (12) ◽  
pp. 1319
Author(s):  
Nils Goehringer ◽  
Yayi Peng ◽  
Bianca Nitzsche ◽  
Hannah Biermann ◽  
Rohan Pradhan ◽  
...  
Keyword(s):  
Anticancer Drugs ◽  
Histone Deacetylases ◽  
Parent Compound ◽  
Hdac Inhibitors ◽  
Drug Candidate ◽  
Anticancer Activities ◽  
Drug Candidates ◽  
Anticancer Properties ◽  
Ic50 Values ◽  
Potent Drug

The development of new anticancer drugs is necessary in order deal with the disease and with the drawbacks of currently applied drugs. Epigenetic dysregulations are a central hallmark of cancerogenesis and histone deacetylases (HDACs) emerged as promising anticancer targets. HDAC inhibitors are promising epigenetic anticancer drugs and new HDAC inhibitors are sought for in order to obtain potent drug candidates. The new HDAC inhibitor SF5-SAHA was synthesized and analyzed for its anticancer properties. The new compound SF5-SAHA showed strong inhibition of tumor cell growth with IC50 values similar to or lower than that of the clinically applied reference compound vorinostat/SAHA (suberoylanilide hydroxamic acid). Target specific HDAC inhibition was demonstrated by Western blot analyses. Unspecific cytotoxic effects were not observed in LDH-release measurements. Pro-apoptotic formation of reactive oxygen species (ROS) and caspase-3 activity induction in prostate carcinoma and hepatocellular carcinoma cell lines DU145 and Hep-G2 seem to be further aspects of the mode of action. Antiangiogenic activity of SF5-SAHA was observed on chorioallantoic membranes of fertilized chicken eggs (CAM assay). The presence of the pentafluorothio-substituent of SF5-SAHA increased the antiproliferative effects in both solid tumor and leukemia/lymphoma cell models when compared with its parent compound vorinostat. Based on this preliminary study, SF5-SAHA has the prerequisites to be further developed as a new HDAC inhibitory anticancer drug candidate.

scholarly journals The Aquaporin-3-Inhibiting Potential of Polyoxotungstates

2020 ◽  
Vol 21 (7) ◽  
pp. 2467 ◽  
Author(s):  
Catarina Pimpão ◽  
Inês V. da Silva ◽  
Andreia F. Mósca ◽  
Jacinta O. Pinho ◽  
Maria Manuela Gaspar ◽  
...  
Keyword(s):  
Cell Migration ◽  
Cell Growth ◽  
Anticancer Drugs ◽  
Inhibitory Concentration ◽  
Yeast Cells ◽  
Anticancer Activities ◽  
Cancer Cell Growth ◽  
Aquaporin 3 ◽  
Anticancer Properties ◽  
First Time

Polyoxometalates (POMs) are of increasing interest due to their proven anticancer activities. Aquaporins (AQPs) were found to be overexpressed in tumors bringing particular attention to their inhibitors as anticancer drugs. Herein, we report for the first time the ability of polyoxotungstates (POTs), such as of Wells–Dawson P2W18, P2W12, and P2W15, and Preyssler P5W30 structures, to affect aquaporin-3 (AQP3) activity and impair melanoma cell migration. The tested POTs were revealed to inhibit AQP3 function with different effects, with P2W18, P2W12, and P5W30 being the most potent (50% inhibitory concentration (IC50) = 0.8, 2.8, and 3.2 µM), and P2W15 being the weakest (IC50 > 100 µM). The selectivity of P2W18 toward AQP3 was confirmed in yeast cells transformed with human aquaglyceroporins. The effect of P2W12 and P2W18 on melanoma cells that highly express AQP3 revealed an impairment of cell migration between 55% and 65% after 24 h, indicating that the anticancer properties of these compounds may in part be due to the blockage of AQP3-mediated permeability. Altogether, our data revealed that P2W18 strongly affects AQP3 activity and cancer cell growth, unveiling its potential as an anticancer drug against tumors where AQP3 is highly expressed.

scholarly journals A Comprehensive Mini-Review of Curcumae Radix: Ethnopharmacology, Phytochemistry, and Pharmacology

2021 ◽  
Vol 16 (5) ◽  
pp. 1934578X2110206
Author(s):  
Dongyi Hu ◽  
Jiayu Gao ◽  
Xiao Yang ◽  
Ying Liang
Keyword(s):  
Therapeutic Potential ◽  
Curcuma Longa ◽  
Web Based ◽  
Medicinal Uses ◽  
Scientific Databases ◽  
Wide Range ◽  
Fundamental Understanding ◽  
Medicinal Properties ◽  
Curcuma Kwangsiensis ◽  
Anti Inflammation

Curcumae Radix is an efficacious ingredient with various medicinal properties empirically used in traditional Chinese medicine (TCM) formula for the treatment of cancer, depression, chest pain, dysmenorrhea, epilepsy, and jaundice. However, either phytochemical or pharmacological information of Curcumae Radix underlying its traditionally medicinal uses is rarely summarized and systematically analyzed. To provide evidence for clinical trials, a comprehensive literature review has been prepared of the phytochemicals, and ethnopharmacological and pharmacological mechanisms of this herb. The review approach consisted of searching several web-based scientific databases, including PubMed, Web of Science, and Elsevier. The keywords included “Curcumae Radix,” “ Curcuma wenyujin,” “ Curcuma longa,” “ Curcuma kwangsiensis,” and “ Curcuma phaeocaulis.” Based on the proposed criteria, 57 articles were evaluated in detail. The accumulated data indicate that Curcumae Radix contains a number of bioactive phytochemicals, mainly sesquiterpenes, diarylheptanoids, and diarylpentanoids, which account for a variety of medicinal values, such as anticancer, anti-inflammation, anti-hepatic fibrosis, and antioxidant. A wide range of apoptotic proteins, cell adhesion molecules, inflammatory cytokines, and enzymic and nonenzymic antioxidants could be modulated by either Curcumae Radix or its bioactive compounds, thus underpinning a fundamental understanding for the pharmacological effects of this herb. This review highlights the therapeutic potential of Curcumae Radix to progress the development of versatile adjuvants or therapeutic agents in the future.

scholarly journals Ellagic Acid and Schisandrins: Natural Biaryl Polyphenols with Therapeutic Potential to Overcome Multidrug Resistance in Cancer

Cells ◽  
2021 ◽  
Vol 10 (2) ◽  
pp. 458
Author(s):  
Sabesan Yoganathan ◽  
Anushan Alagaratnam ◽  
Nikita Acharekar ◽  
Jing Kong
Keyword(s):  
Multidrug Resistance ◽  
Small Molecules ◽  
Anticancer Drugs ◽  
Abc Transporters ◽  
Ellagic Acid ◽  
Therapeutic Potential ◽  
Anticancer Activities ◽  
Glycoprotein P ◽  
Major Mechanism ◽  
Anticancer Properties

Multidrug resistance (MDR) is one of the major clinical challenges in cancer treatment and compromises the effectiveness of conventional anticancer chemotherapeutics. Among known mechanisms of drug resistance, drug efflux via ATP binding cassette (ABC) transporters, namely P-glycoprotein (P-gp) has been characterized as a major mechanism of MDR. The primary function of ABC transporters is to regulate the transport of endogenous and exogenous small molecules across the membrane barrier in various tissues. P-gp and similar efflux pumps are associated with MDR because of their overexpression in many cancer types. One of the intensively studied approaches to overcome this mode of MDR involves development of small molecules to modulate P-gp activity. This strategy improves the sensitivity of cancer cells to anticancer drugs that are otherwise ineffective. Although multiple generations of P-gp inhibitors have been identified to date, reported compounds have demonstrated low clinical efficacy and adverse effects. More recently, natural polyphenols have emerged as a promising class of compounds to address P-gp linked MDR. This review highlights the chemical structure and anticancer activities of selected members of a structurally unique class of ‘biaryl’ polyphenols. The discussion focuses on the anticancer properties of ellagic acid, ellagic acid derivatives, and schisandrins. Research reports regarding their inherent anticancer activities and their ability to sensitize MDR cell lines towards conventional anticancer drugs are highlighted here. Additionally, a brief discussion about the axial chirality (i.e., atropisomerism) that may be introduced into these natural products for medicinal chemistry studies is also provided.

scholarly journals Natural Phytochemicals in Bladder Cancer Prevention and Therapy

2021 ◽  
Vol 11 ◽  
Author(s):  
Yong Xia ◽  
Ruijiao Chen ◽  
Guangzhen Lu ◽  
Changlin Li ◽  
Sen Lian ◽  
...  
Keyword(s):  
Bladder Cancer ◽  
Anticancer Drugs ◽  
Anticancer Activities ◽  
First Line ◽  
Anticancer Properties ◽  
Bladder Cancer Cells ◽  
Cancer Types ◽  
Available Information ◽  
New Anticancer Drugs

Phytochemicals are natural small-molecule compounds derived from plants that have attracted attention for their anticancer activities. Some phytochemicals have been developed as first-line anticancer drugs, such as paclitaxel and vincristine. In addition, several phytochemicals show good tumor suppression functions in various cancer types. Bladder cancer is a malignant tumor of the urinary system. To date, few specific phytochemicals have been used for bladder cancer therapy, although many have been studied in bladder cancer cells and mouse models. Therefore, it is important to collate and summarize the available information on the role of phytochemicals in the prevention and treatment of bladder cancer. In this review, we summarize the effects of several phytochemicals including flavonoids, steroids, nitrogen compounds, and aromatic substances with anticancer properties and classify the mechanism of action of phytochemicals in bladder cancer. This review will contribute to facilitating the development of new anticancer drugs and strategies for the treatment of bladder cancer using phytochemicals.

Design of Lamivudine Loaded Nanoparticles for Oral Application by Nano Spray Drying Method: A New Approach to use an Antiretroviral Drug for Lung Cancer Treatment

2020 ◽  
Vol 23 (10) ◽  
pp. 1064-1079
Author(s):  
Ahmet Alper Öztürk ◽  
İrem Namlı ◽  
Kadri Güleç ◽  
Şennur Görgülü
Keyword(s):  
Lung Cancer ◽  
Cancer Treatment ◽  
Anticancer Activity ◽  
Cell Line ◽  
Anticancer Drugs ◽  
Release Kinetics ◽  
Prolonged Release ◽  
Lung Cancer Treatment ◽  
Anticancer Properties ◽  
Ft Ir

Aims: To prepare lamivudine (LAM)-loaded-nanoparticles (NPs) that can be used in lung cancer treatment. To change the antiviral indication of LAM to anticancer. Background: The development of anticancer drugs is a difficult process. One approach to accelerate the availability of drugs is to reclassify drugs approved for other conditions as anticancer. The most common route of administration of anticancer drugs is intravenous injection. Oral administration of anticancer drugs may considerably change current treatment modalities of chemotherapy and improve the life quality of cancer patients. There is also a potentially significant economic advantage. Objective: To characterize the LAM-loaded-NPs and examine the anticancer activity. Methods: LAM-loaded-NPs were prepared using Nano Spray-Dryer. Properties of NPs were elucidated by particle size (PS), polydispersity index (PDI), zeta potential (ZP), SEM, encapsulation efficiency (EE%), dissolution, release kinetics, DSC and FT-IR. Then, the anticancer activity of all NPs was examined. Results: The PS values of the LAM-loaded-NPs were between 373 and 486 nm. All NPs prepared have spherical structure and positive ZP. EE% was in a range of 61-79%. NPs showed prolonged release and the release kinetics fitted to the Weibull model. NPs structures were clarified by DSC and FT-IR analysis. The results showed that the properties of NPs were directly related to the drug:polymer ratio of feed solution. NPs have potential anticancer properties against A549 cell line at low concentrations and non-toxic to CCD 19-Lu cell line. Conclusion: NPs have potential anticancer properties against human lung adenocarcinoma cells and may induce cell death effectively and be a potent modality to treat this type of cancer. These experiments also indicate that our formulations are non-toxic to normal cells. It is clear that this study would bring a new perspective to cancer therapy.

scholarly journals Plant-Derived Nano and Microvesicles for Human Health and Therapeutic Potential in Nanomedicine

Pharmaceutics ◽  
2021 ◽  
Vol 13 (4) ◽  
pp. 498
Author(s):  
Mariaevelina Alfieri ◽  
Antonietta Leone ◽  
Alfredo Ambrosone
Keyword(s):  
Therapeutic Potential ◽  
Biological Activities ◽  
Plant Biotechnology ◽  
Bioactive Metabolites ◽  
Anticancer Activities ◽  
Long Distance ◽  
In Vivo Models ◽  
Therapeutic Tools

Plants produce different types of nano and micro-sized vesicles. Observed for the first time in the 60s, plant nano and microvesicles (PDVs) and their biological role have been inexplicably under investigated for a long time. Proteomic and metabolomic approaches revealed that PDVs carry numerous proteins with antifungal and antimicrobial activity, as well as bioactive metabolites with high pharmaceutical interest. PDVs have also been shown to be also involved in the intercellular transfer of small non-coding RNAs such as microRNAs, suggesting fascinating mechanisms of long-distance gene regulation and horizontal transfer of regulatory RNAs and inter-kingdom communications. High loading capacity, intrinsic biological activities, biocompatibility, and easy permeabilization in cell compartments make plant-derived vesicles excellent natural or bioengineered nanotools for biomedical applications. Growing evidence indicates that PDVs may exert anti-inflammatory, anti-oxidant, and anticancer activities in different in vitro and in vivo models. In addition, clinical trials are currently in progress to test the effectiveness of plant EVs in reducing insulin resistance and in preventing side effects of chemotherapy treatments. In this review, we concisely introduce PDVs, discuss shortly their most important biological and physiological roles in plants and provide clues on the use and the bioengineering of plant nano and microvesicles to develop innovative therapeutic tools in nanomedicine, able to encompass the current drawbacks in the delivery systems in nutraceutical and pharmaceutical technology. Finally, we predict that the advent of intense research efforts on PDVs may disclose new frontiers in plant biotechnology applied to nanomedicine.

scholarly journals The relationship between Google search interest for pulmonary symptoms and COVID-19 cases using dynamic conditional correlation analysis

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Halit Cinarka ◽  
Mehmet Atilla Uysal ◽  
Atilla Cifter ◽  
Elif Yelda Niksarlioglu ◽  
Aslı Çarkoğlu
Keyword(s):  
Case Reports ◽  
Time Varying ◽  
Conditional Correlation ◽  
Web Based ◽  
Specific Symptom ◽  
Sliding Windows ◽  
Dynamic Conditional Correlation ◽  
The United Kingdom ◽  
Correlation Models ◽  
Google Search

AbstractThis study aims to evaluate the monitoring and predictive value of web-based symptoms (fever, cough, dyspnea) searches for COVID-19 spread. Daily search interests from Turkey, Italy, Spain, France, and the United Kingdom were obtained from Google Trends (GT) between January 1, 2020, and August 31, 2020. In addition to conventional correlational models, we studied the time-varying correlation between GT search and new case reports; we used dynamic conditional correlation (DCC) and sliding windows correlation models. We found time-varying correlations between pulmonary symptoms on GT and new cases to be significant. The DCC model proved more powerful than the sliding windows correlation model. This model also provided better at time-varying correlations (r ≥ 0.90) during the first wave of the pandemic. We used a root means square error (RMSE) approach to attain symptom-specific shift days and showed that pulmonary symptom searches on GT should be shifted separately. Web-based search interest for pulmonary symptoms of COVID-19 is a reliable predictor of later reported cases for the first wave of the COVID-19 pandemic. Illness-specific symptom search interest on GT can be used to alert the healthcare system to prepare and allocate resources needed ahead of time.

Annona muricata silver nanoparticles exhibit strong anticancer activities against cervical and prostate adenocarcinomas through regulation of CASP9 and the CXCL1/CXCR2 genes axis

Tumor Biology ◽  
2021 ◽  
Vol 43 (1) ◽  
pp. 37-55
Author(s):  
Yahaya Gavamukulya ◽  
Esther N. Maina ◽  
Hany A. El-Shemy ◽  
Amos M. Meroka ◽  
Geoffrey K. Kangogo ◽  
...  
Keyword(s):  
Silver Nanoparticles ◽  
Anticancer Drugs ◽  
Hela Cells ◽  
Selectivity Index ◽  
Annona Muricata ◽  
Anticancer Activities ◽  
Apoptosis Pathway ◽  
Migration Assay ◽  
Intrinsic Apoptosis Pathway ◽  
In Cells

BACKGROUND: Green synthesized nanoparticles have been earmarked for use in nanomedicine including for the development of better anticancer drugs. OBJECTIVE: The aim of this study was to undertake biochemical evaluation of anticancer activities of green synthesized silver nanoparticles (AgNPs) from ethanolic extracts of fruits (AgNPs-F) and leaves (AgNPs-L) of Annona muricata. METHODS: Previously synthesized silver nanoparticles were used for the study. The effects of the AgNPs and 5-Fluorouracil were studied on PC3, HeLa and PNT1A cells. The resazurin, migration and colonogenic assays as well as qRT-PCR were employed. RESULTS: The AgNPs-F displayed significant antiproliferative effects against HeLa cells with an IC50 of 38.58μg/ml and PC3 cells with an IC50 of 48.17μg/ml but selectively spared normal PNT1A cells (selectivity index of 7.8), in comparison with first line drug 5FU and AgNPs-L whose selectivity index were 3.56 and 2.26 respectively. The migration assay revealed potential inhibition of the metastatic activity of the cells by the AgNPs-F while the colonogenic assay indicated the permanent effect of the AgNPs-F on the cancer cells yet being reversible on the normal cells in contrast with 5FU and AgNPs-L. CASP9 was significantly over expressed in all HeLa cells treated with the AgNPs-F (1.53-fold), AgNPs-L (1.52-fold) and 5FU (4.30-fold). CXCL1 was under expressed in HeLa cells treated with AgNPs-F (0.69-fold) and AgNPs-L (0.58-fold) and over expressed in cells treated with 5FU (4.95-fold), but the difference was not statistically significant. CXCR2 was significantly over expressed in HeLa cells treated with 5FU (8.66-fold) and AgNPs-F (1.12-fold) but under expressed in cells treated with AgNPs-L (0.76-fold). CONCLUSIONS: Here we show that biosynthesized AgNPs especially AgNPs-F can be used in the development of novel and better anticancer drugs. The mechanism of action of the AgNPs involves activation of the intrinsic apoptosis pathway through upregulation of CASP9 and concerted down regulation of the CXCL1/ CXCR2 gene axis.

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