Hymecromone and Its Products as Cytotoxic Candidates for Brain Cancer: A Brief Review

2021 ◽  
Vol 19 (7) ◽  
pp. 175-186
Author(s):  
Yasser Fakri Mustafa ◽  
Noora Thamer Abdulaziz
Keyword(s):  
Side Effects ◽  
Brain Cancer ◽  
Antitumor Agents ◽  
Future Research ◽  
Chemotherapeutic Drugs ◽  
Cancer Resistance ◽  
Tumor Resistance ◽  
Design And Synthesis ◽  
Cancer Breast ◽  
Wide Range

Brain cancer is the 10th cause of death among patients suffering from cancer worldwide. Despite the huge effort put out to extract, design, and synthesize novel chemotherapeutic drugs, medicinal chemists continue to face significant obstacles due to considerable side effects, growing tumor resistance, and poor selectivity. In recent decades, great attention has been paid to the anti-cancer potential of a variety of natural compounds. Coumarin-based compounds, for example, are distinguished by their structural variety and wide range of pharmacological characteristics. Among these, hymecromone, also known as 7-hydroxy-4-methylcoumarin, and its derivatives have shown promise in the treatment of multi-drug cancer resistance, the decrease of chemotherapeutic drug side effects, and the creation of photo-directed cancer therapy. Furthermore, numerous synthetic hymecromone-derived compounds have been demonstrated to have a broad antitumor potential, making them effective against a variety of cancers including leukemia, prostate cancer, lung cancer, breast cancer, and brain cancer. In this review article, the authors evaluated the findings of a number of recently published scientific studies in order to emphasize the structural properties of hymecromone-derived compounds that are crucial in their potential as antitumor agents for brain cancer. The specification of these qualities might help guide future research towards the design and synthesis of newer chemotherapeutic drugs with improved features.

scholarly journals Celastrol: A Review of Useful Strategies Overcoming its Limitation in Anticancer Application

2020 ◽  
Vol 11 ◽  
Author(s):  
Jinfeng Shi ◽  
Jiaxin Li ◽  
Ziyi Xu ◽  
Liang Chen ◽  
Ruifeng Luo ◽  
...  
Keyword(s):  
Side Effects ◽  
Therapeutic Window ◽  
Future Research ◽  
Anticancer Activities ◽  
Research Directions ◽  
Anticancer Efficacy ◽  
Cancer Breast ◽  
Future Research Directions ◽  
Micro Systems ◽  
Anticancer Compound

Celastrol, a natural bioactive ingredient derived from Tripterygium wilfordii Hook F, exhibits significant broad-spectrum anticancer activities for the treatment of a variety of cancers including liver cancer, breast cancer, prostate tumor, multiple myeloma, glioma, etc. However, the poor water stability, low bioavailability, narrow therapeutic window, and undesired side effects greatly limit its clinical application. To address this issue, some strategies were employed to improve the anticancer efficacy and reduce the side-effects of celastrol. The present review comprehensively focuses on the various challenges associated with the anticancer efficiency and drug delivery of celastrol, and the useful approaches including combination therapy, structural derivatives and nano/micro-systems development. The specific advantages for the use of celastrol mediated by these strategies are presented. Moreover, the challenges and future research directions are also discussed. Based on this review, it would provide a reference to develop a natural anticancer compound for cancer treatment.

scholarly journals Recent Advances in Strategies for Addressing Hypoxia in Tumor Photodynamic Therapy

Biomolecules ◽  
2022 ◽  
Vol 12 (1) ◽  
pp. 81
Author(s):  
Liang Hong ◽  
Jiangmin Li ◽  
Yali Luo ◽  
Tao Guo ◽  
Chenshuang Zhang ◽  
...  
Keyword(s):  
Photodynamic Therapy ◽  
Side Effects ◽  
Treatment Modality ◽  
Tumor Metastasis ◽  
State Of The Art ◽  
Tumor Hypoxia ◽  
Future Research ◽  
Tumor Resistance ◽  
Normal Tissues ◽  
Recent Advances

Photodynamic therapy (PDT) is a treatment modality that uses light to target tumors and minimize damage to normal tissues. It offers advantages including high spatiotemporal selectivity, low side effects, and maximal preservation of tissue functions. However, the PDT efficiency is severely impeded by the hypoxic feature of tumors. Moreover, hypoxia may promote tumor metastasis and tumor resistance to multiple therapies. Therefore, addressing tumor hypoxia to improve PDT efficacy has been the focus of antitumor treatment, and research on this theme is continuously emerging. In this review, we summarize state-of-the-art advances in strategies for overcoming hypoxia in tumor PDTs, categorizing them into oxygen-independent phototherapy, oxygen-economizing PDT, and oxygen-supplementing PDT. Moreover, we highlight strategies possessing intriguing advantages such as exceedingly high PDT efficiency and high novelty, analyze the strengths and shortcomings of different methods, and envision the opportunities and challenges for future research.

scholarly journals Cisplatin Mouse Models: Treatment, Toxicity and Translatability

Biomedicines ◽  
2021 ◽  
Vol 9 (10) ◽  
pp. 1406
Author(s):  
Martina Perše
Keyword(s):  
Side Effects ◽  
Mouse Models ◽  
Potential Benefit ◽  
Molecular Mechanisms ◽  
Therapeutic Agents ◽  
Gastrointestinal Toxicity ◽  
Dependent Manner ◽  
Chemotherapeutic Drugs ◽  
Future Studies ◽  
Wide Range

Cisplatin is one of the most widely used chemotherapeutic drugs in the treatment of a wide range of pediatric and adult malignances. However, it has various side effects which limit its use. Cisplatin mouse models are widely used in studies investigating cisplatin therapeutic and toxic effects. However, despite numerous promising results, no significant improvement in treatment outcome has been achieved in humans. There are many drawbacks in the currently used cisplatin protocols in mice. In the paper, the most characterized cisplatin protocols are summarized together with weaknesses that need to be improved in future studies, including hydration and supportive care. As demonstrated, mice respond to cisplatin treatment in similar ways to humans. The paper thus aims to illustrate the complexity of cisplatin side effects (nephrotoxicity, gastrointestinal toxicity, neurotoxicity, ototoxicity and myelotoxicity) and the interconnectedness and interdependence of pathomechanisms among tissues and organs in a dose- and time-dependent manner. The paper offers knowledge that can help design future studies more efficiently and interpret study outcomes more critically. If we want to understand molecular mechanisms and find therapeutic agents that would have a potential benefit in clinics, we need to change our approach and start to treat animals as patients and not as tools.

Thiosemicarbazones as Potent Anticancer Agents and their Modes of Action

2020 ◽  
Vol 20 (8) ◽  
pp. 638-661 ◽  
Author(s):  
Bhushan Shakya ◽  
Paras Nath Yadav
Keyword(s):  
Anticancer Agents ◽  
Antitumor Agents ◽  
Biological Activities ◽  
Heterocyclic Ring ◽  
Side Chain ◽  
Inactive Compound ◽  
Cancer Breast ◽  
Wide Range ◽  
Ring Nitrogen ◽  
Tumor Types

: Thiosemicarbazones (TSCs) are a class of Schiff bases usually obtained by the condensation of thiosemicarbazide with a suitable aldehyde or ketone. TSCs have been the focus of chemists and biologists due to their wide range of pharmacological effects. One of the promising areas in which these excellent metal chelators are being developed is their use against cancer. TSCs have a wide clinical antitumor spectrum with efficacy in various tumor types such as leukemia, pancreatic cancer, breast cancer, non-small cell lung cancer, cervical cancer, prostate cancer and bladder cancer. To obtain better activity, different series of TSCs have been developed by modifying the heteroaromatic system in their molecules. These compounds possessed significant antineoplastic activity when the carbonyl attachment of the side chain was located at a position α to the ring nitrogen atom, whereas attachment of the side chain β or γ to the heterocyclic N atom resulted in inactive antitumor agents. In addition, replacement of the heterocyclic ring N with C also resulted in a biologically inactive compound suggesting that a conjugated N,N,S-tridentate donor set is essential for the biological activities of thiosemicarbazones. Several possible mechanisms have been implemented for the anticancer activity of thiosemicarbazones.

Understanding the side effects of glucocorticoid therapy: shining a light on a drug everyone thinks they know

2012 ◽  
Vol 71 (11) ◽  
pp. 1761-1764 ◽  
Author(s):  
William G Dixon ◽  
Nick Bansback
Keyword(s):  
Decision Making ◽  
Side Effects ◽  
Decision Process ◽  
Future Research ◽  
Decision Making Process ◽  
Wide Range ◽  
Value Judgements ◽  
The Many ◽  
The Relationship ◽  
Higher Doses

Glucocorticoids are one of the most frequently prescribed therapies in rheumatology, a reflection of their effectiveness as a powerful anti-inflammatory drug. Glucocorticoids are also, however, associated with a wide range of adverse events, particularly at higher doses. To make appropriate decisions, doctors and patients need to weigh these benefits against the potential harms. This article describes the many uncertainties which make informed prescribing difficult. We lack knowledge, for example, on the magnitude of risk, the relationship to dose and duration, and what happens to risk on stopping therapy. Beyond safety, we describe how patients may lack understanding of the nature of the benefits and harms, and how to incorporate value judgements which are crucial to the decision making process. We conclude by exploring how future research might fill these knowledge gaps to enable a better informed decision process.

Comparative Effects of High-Tech Visual Scene Displays and Low-Tech Isolated Picture Symbols on Engagement From Students With Multiple Disabilities

2019 ◽  
Vol 50 (4) ◽  
pp. 693-702 ◽  
Author(s):  
Christine Holyfield ◽  
Sydney Brooks ◽  
Allison Schluterman
Keyword(s):  
Language Learning ◽  
Augmentative And Alternative Communication ◽  
Visual Analysis ◽  
Multiple Disabilities ◽  
Visual Scene ◽  
Future Research ◽  
High Tech ◽  
Single Subject ◽  
Wide Range ◽  
The Difference

Purpose Augmentative and alternative communication (AAC) is an intervention approach that can promote communication and language in children with multiple disabilities who are beginning communicators. While a wide range of AAC technologies are available, little is known about the comparative effects of specific technology options. Given that engagement can be low for beginning communicators with multiple disabilities, the current study provides initial information about the comparative effects of 2 AAC technology options—high-tech visual scene displays (VSDs) and low-tech isolated picture symbols—on engagement. Method Three elementary-age beginning communicators with multiple disabilities participated. The study used a single-subject, alternating treatment design with each technology serving as a condition. Participants interacted with their school speech-language pathologists using each of the 2 technologies across 5 sessions in a block randomized order. Results According to visual analysis and nonoverlap of all pairs calculations, all 3 participants demonstrated more engagement with the high-tech VSDs than the low-tech isolated picture symbols as measured by their seconds of gaze toward each technology option. Despite the difference in engagement observed, there was no clear difference across the 2 conditions in engagement toward the communication partner or use of the AAC. Conclusions Clinicians can consider measuring engagement when evaluating AAC technology options for children with multiple disabilities and should consider evaluating high-tech VSDs as 1 technology option for them. Future research must explore the extent to which differences in engagement to particular AAC technologies result in differences in communication and language learning over time as might be expected.

Understanding Limited Use of Amplification in Infants and Children Who Are Hard of Hearing

2015 ◽  
Vol 25 (1) ◽  
pp. 15-23 ◽  
Author(s):  
Ryan W. McCreery ◽  
Elizabeth A. Walker ◽  
Meredith Spratford
Keyword(s):  
Hard Of Hearing ◽  
Hearing Aid ◽  
Management Strategies ◽  
Infants And Children ◽  
Future Research ◽  
Research Needs ◽  
Case Examples ◽  
Hearing Aid Use ◽  
Wide Range ◽  
In Infants And Children

The effectiveness of amplification for infants and children can be mediated by how much the child uses the device. Existing research suggests that establishing hearing aid use can be challenging. A wide range of factors can influence hearing aid use in children, including the child's age, degree of hearing loss, and socioeconomic status. Audiological interventions, including using validated prescriptive approaches and verification, performing on-going training and orientation, and communicating with caregivers about hearing aid use can also increase hearing aid use by infants and children. Case examples are used to highlight the factors that influence hearing aid use. Potential management strategies and future research needs are also discussed.

The Attenuation of Very Low Frequency Brain Oscillations in Transitions from a Rest State to Active Attention

2009 ◽  
Vol 23 (4) ◽  
pp. 191-198 ◽  
Author(s):  
Suzannah K. Helps ◽  
Samantha J. Broyd ◽  
Christopher J. James ◽  
Anke Karl ◽  
Edmund J. S. Sonuga-Barke
Keyword(s):  
Brain Activity ◽  
Sampling Rate ◽  
Low Frequency ◽  
Future Research ◽  
Adhd Symptoms ◽  
Default Mode ◽  
Very Low Frequency ◽  
Wide Range ◽  
Interference Hypothesis ◽  
Mode Interference

Background: The default mode interference hypothesis ( Sonuga-Barke & Castellanos, 2007 ) predicts (1) the attenuation of very low frequency oscillations (VLFO; e.g., .05 Hz) in brain activity within the default mode network during the transition from rest to task, and (2) that failures to attenuate in this way will lead to an increased likelihood of periodic attention lapses that are synchronized to the VLFO pattern. Here, we tested these predictions using DC-EEG recordings within and outside of a previously identified network of electrode locations hypothesized to reflect DMN activity (i.e., S3 network; Helps et al., 2008 ). Method: 24 young adults (mean age 22.3 years; 8 male), sampled to include a wide range of ADHD symptoms, took part in a study of rest to task transitions. Two conditions were compared: 5 min of rest (eyes open) and a 10-min simple 2-choice RT task with a relatively high sampling rate (ISI 1 s). DC-EEG was recorded during both conditions, and the low-frequency spectrum was decomposed and measures of the power within specific bands extracted. Results: Shift from rest to task led to an attenuation of VLFO activity within the S3 network which was inversely associated with ADHD symptoms. RT during task also showed a VLFO signature. During task there was a small but significant degree of synchronization between EEG and RT in the VLFO band. Attenuators showed a lower degree of synchrony than nonattenuators. Discussion: The results provide some initial EEG-based support for the default mode interference hypothesis and suggest that failure to attenuate VLFO in the S3 network is associated with higher synchrony between low-frequency brain activity and RT fluctuations during a simple RT task. Although significant, the effects were small and future research should employ tasks with a higher sampling rate to increase the possibility of extracting robust and stable signals.

COVID-19 Outbreak Prediction with Machine Learning

2020 ◽  
Author(s):  
Sina Faizollahzadeh Ardabili ◽  
Amir Mosavi ◽  
Pedram Ghamisi ◽  
Filip Ferdinand ◽  
Annamaria R. Varkonyi-Koczy ◽  
...  
Keyword(s):  
Machine Learning ◽  
Prediction Models ◽  
Fuzzy Inference ◽  
Control Measures ◽  
Future Research ◽  
Complex Nature ◽  
Inference System ◽  
Wide Range ◽  
Standard Models ◽  
High Level

Several outbreak prediction models for COVID-19 are being used by officials around the world to make informed-decisions and enforce relevant control measures. Among the standard models for COVID-19 global pandemic prediction, simple epidemiological and statistical models have received more attention by authorities, and they are popular in the media. Due to a high level of uncertainty and lack of essential data, standard models have shown low accuracy for long-term prediction. Although the literature includes several attempts to address this issue, the essential generalization and robustness abilities of existing models needs to be improved. This paper presents a comparative analysis of machine learning and soft computing models to predict the COVID-19 outbreak as an alternative to SIR and SEIR models. Among a wide range of machine learning models investigated, two models showed promising results (i.e., multi-layered perceptron, MLP, and adaptive network-based fuzzy inference system, ANFIS). Based on the results reported here, and due to the highly complex nature of the COVID-19 outbreak and variation in its behavior from nation-to-nation, this study suggests machine learning as an effective tool to model the outbreak. This paper provides an initial benchmarking to demonstrate the potential of machine learning for future research. Paper further suggests that real novelty in outbreak prediction can be realized through integrating machine learning and SEIR models.

Small Molecular Gemcitabine Prodrugs for Cancer Therapy

2020 ◽  
Vol 27 (33) ◽  
pp. 5562-5582 ◽  
Author(s):  
He Miao ◽  
Xuehong Chen ◽  
Yepeng Luan
Keyword(s):  
Drug Resistance ◽  
Side Effects ◽  
Anticancer Drug ◽  
Drug Stability ◽  
Effective Means ◽  
Active Form ◽  
Deoxycytidine Kinase ◽  
High Efficacy ◽  
Pyrimidine Nucleoside ◽  
Design And Synthesis

Gemcitabine as a pyrimidine nucleoside analog anticancer drug has high efficacy for a broad spectrum of solid tumors. Gemcitabine is activated within tumor cells by sequential phosphorylation carried out by deoxycytidine kinase to mono-, di-, and triphosphate nucleotides with the last one as the active form. But the instability, drug resistance and toxicity severely limited its utilization in clinics. In the field of medicinal chemistry, prodrugs have proven to be a very effective means for elevating drug stability and decrease undesirable side effects including the nucleoside anticancer drug such as gemcitabine. Many works have been accomplished in design and synthesis of gemcitabine prodrugs, majority of which were summarized in this review.

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