Screening of high efficiency and low toxicity antitumor active components in Macleaya cordata seeds based on the competitive effect of drugs on double targets by a new laminar flow chip

The Analyst ◽  
2021 ◽  
Author(s):  
Yan Gao ◽  
Huaidong Peng ◽  
Lisi Li ◽  
feng Wang ◽  
Jiang Meng ◽  
...  
Keyword(s):  
Laminar Flow ◽  
High Efficiency ◽  
Early Stage ◽  
Targeted Drugs ◽  
Competitive Effect ◽  
Active Components ◽  
G Quadruplex ◽  
Low Toxicity ◽  
Macleaya Cordata ◽  
Double Targets

It is urgent to obtain targeted drugs that selectively bind to pathological targets rather than physiological targets in the early stage of drug screening. G-quadruplex has become one of the...

Metabolism and Distribution of Novel Tumor Targeting Drugs In Vivo

2020 ◽  
Vol 21 (13) ◽  
pp. 996-1008
Author(s):  
Mengli Wang ◽  
Qiuzheng Du ◽  
Lihua Zuo ◽  
Peng Xue ◽  
Chao Lan ◽  
...  
Keyword(s):  
Monoclonal Antibodies ◽  
Small Molecule ◽  
High Efficiency ◽  
Tumor Therapy ◽  
Research Progress ◽  
Future Research ◽  
Pharmacokinetic Parameters ◽  
Molecular Characteristics ◽  
Targeted Drugs

Background: As a new tumor therapy, targeted therapy is becoming a hot topic due to its high efficiency and low toxicity. Drug effects of targeted tumor drugs are closely related to pharmacokinetics, so it is important to understand their distribution and metabolism in vivo. Methods: A systematic review of the literature on the metabolism and distribution of targeted drugs over the past 20 years was conducted, and the pharmacokinetic parameters of approved targeted drugs were summarized in combination with the FDA's drug instructions. Targeting drugs are divided into two categories: small molecule inhibitors and monoclonal antibodies. Novel targeting drugs and their mechanisms of action, which have been developed in recent years, are summarized. The distribution and metabolic processes of each drug in the human body are reviewed. Results: In this review, we found that the distribution and metabolism of small molecule kinase inhibitors (TKI) and monoclonal antibodies (mAb) showed different characteristics based on the differences of action mechanism and molecular characteristics. TKI absorbed rapidly (Tmax ≈ 1-4 h) and distributed in large amounts (Vd > 100 L). It was mainly oxidized and reduced by cytochrome P450 CYP3A4. However, due to the large molecular diameter, mAb was distributed to tissues slowly, and the volume of distribution was usually very low (Vd < 10 L). It was mainly hydrolyzed and metabolized into peptides and amino acids by protease hydrolysis. In addition, some of the latest drugs are still in clinical trials, and the in vivo process still needs further study. Conclusion: According to the summary of the research progress of the existing targeting drugs, it is found that they have high specificity, but there are still deficiencies in drug resistance and safety. Therefore, the development of safer and more effective targeted drugs is the future research direction. Meanwhile, this study also provides a theoretical basis for clinical accurate drug delivery.

scholarly journals Neighborhood Energy Modeling and Monitoring: A Case Study

Energies ◽  
2021 ◽  
Vol 14 (12) ◽  
pp. 3716
Author(s):  
Francesco Causone ◽  
Rossano Scoccia ◽  
Martina Pelle ◽  
Paola Colombo ◽  
Mario Motta ◽  
...  
Keyword(s):  
High Performance ◽  
High Efficiency ◽  
Early Stage ◽  
Energy Performance ◽  
Monitoring Plan ◽  
Performance Targets ◽  
Carrier Energy ◽  
Zero Carbon ◽  
Energy Grid

Cities and nations worldwide are pledging to energy and carbon neutral objectives that imply a huge contribution from buildings. High-performance targets, either zero energy or zero carbon, are typically difficult to be reached by single buildings, but groups of properly-managed buildings might reach these ambitious goals. For this purpose we need tools and experiences to model, monitor, manage and optimize buildings and their neighborhood-level systems. The paper describes the activities pursued for the deployment of an advanced energy management system for a multi-carrier energy grid of an existing neighborhood in the area of Milan. The activities included: (i) development of a detailed monitoring plan, (ii) deployment of the monitoring plan, (iii) development of a virtual model of the neighborhood and simulation of the energy performance. Comparisons against early-stage energy monitoring data proved promising and the generation system showed high efficiency (EER equal to 5.84), to be further exploited.

scholarly journals Pathogenesis and Potential Therapeutic Targets for Triple-Negative Breast Cancer

Cancers ◽  
2021 ◽  
Vol 13 (12) ◽  
pp. 2978
Author(s):  
Chia-Jung Li ◽  
Yen-Dun Tony Tzeng ◽  
Yi-Han Chiu ◽  
Hung-Yu Lin ◽  
Ming-Feng Hou ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Targeted Therapy ◽  
Triple Negative Breast Cancer ◽  
Triple Negative ◽  
High Efficiency ◽  
Early Recurrence ◽  
New Developments ◽  
Great Progress ◽  
Low Toxicity ◽  
Made In

Triple negative breast cancer (TNBC) is a heterogeneous tumor characterized by early recurrence, high invasion, and poor prognosis. Currently, its treatment includes chemotherapy, which shows a suboptimal efficacy. However, with the increasing studies on TNBC subtypes and tumor molecular biology, great progress has been made in targeted therapy for TNBC. The new developments in the treatment of breast cancer include targeted therapy, which has the advantages of accurate positioning, high efficiency, and low toxicity, as compared to surgery, radiotherapy, and chemotherapy. Given its importance as cancer treatment, we review the latest research on the subtypes of TNBC and relevant targeted therapies.

scholarly journals Synthesis and Decontamination Effect on Chemical and Biological Agents of Benzoxonium-Like Salts

Toxics ◽  
2021 ◽  
Vol 9 (9) ◽  
pp. 222
Author(s):  
Aneta Markova ◽  
Michaela Hympanova ◽  
Marek Matula ◽  
Lukas Prchal ◽  
Radek Sleha ◽  
...  
Keyword(s):  
Biological Agents ◽  
Point Of View ◽  
Attractive Potential ◽  
Bacterial Strains ◽  
Active Components ◽  
Biological Warfare Agents ◽  
Warfare Agents ◽  
Single Compound ◽  
Safety Parameter ◽  
Low Toxicity

Benzoxonium chloride belongs to the group of quaternary ammonium salts, which have been widely used for decades as disinfectants because of their high efficacy, low toxicity, and thermal stability. In this study, we have prepared the C10-C18 set of benzoxonium-like salts to evaluate the effect of their chemical and biological decontamination capabilities. In particular, biocidal activity against a panel of bacterial strains including Staphylococcus aureus in biofilm form was screened. In addition, the most promising compounds were successfully tested against Francisella tularensis as a representative of potential biological warfare agents. From a point of view of chemical warfare protection, the efficiency of BOC-like compounds to degrade the organophosphate simulant fenitrothion was examined. Notwithstanding that no single compound with universal effectiveness was identified, a mixture of only two compounds from this group would be able to satisfactorily cover the proposed decontamination spectrum. In addition, the compounds were evaluated for their cytotoxicity as a basic safety parameter for potential use in practice. In summary, the dual effect on chemical and biological agents of benzoxonium-like salts offer attractive potential as active components of decontamination mixtures in the case of a terrorist threat or chemical or biological accidents.

scholarly journals Mitochondria-targeting fluorescent molecules for high efficiency cancer growth inhibition and imaging

2019 ◽  
Vol 10 (34) ◽  
pp. 7946-7951 ◽  
Author(s):  
Hao Chen ◽  
Jing Wang ◽  
Xin Feng ◽  
Mark Zhu ◽  
Simon Hoffmann ◽  
...  
Keyword(s):  
Growth Inhibition ◽  
High Efficiency ◽  
Clinical Translation ◽  
Cancer Growth ◽  
Lipophilic Cations ◽  
Anti Cancer ◽  
Low Toxicity ◽  
Fluorescent Molecules ◽  
Mitochondria Targeting

5BMF is a new fluorescent mitochondria-accumulating delocalized lipophilic cations [DLC] that boasts significantly increased anti-cancer effects and low toxicity in comparison to previous DLCs, addressing current hurdles in DLC clinical translation.

scholarly journals The Development of Functional Non-Viral Vectors for Gene Delivery

2019 ◽  
Vol 20 (21) ◽  
pp. 5491 ◽  
Author(s):  
Patil ◽  
Gao ◽  
Lin ◽  
Li ◽  
Dang ◽  
...  
Keyword(s):  
Gene Therapy ◽  
Targeted Delivery ◽  
Viral Vectors ◽  
High Efficiency ◽  
Transfection Efficiency ◽  
Cationic Lipids ◽  
Gene Vectors ◽  
Potential Applications ◽  
Low Toxicity ◽  
Low Cytotoxicity

Gene therapy is manipulation in/of gene expression in specific cells/tissue to treat diseases. This manipulation is carried out by introducing exogenous nucleic acids, such as DNA or RNA, into the cell. Because of their negative charge and considerable larger size, the delivery of these molecules, in general, should be mediated by gene vectors. Non-viral vectors, as promising delivery systems, have received considerable attention due to their low cytotoxicity and non-immunogenicity. As research continued, more and more functional non-viral vectors have emerged. They not only have the ability to deliver a gene into the cells but also have other functions, such as the performance of fluorescence imaging, which aids in monitoring their progress, targeted delivery, and biodegradation. Recently, many reviews related to non-viral vectors, such as polymers and cationic lipids, have been reported. However, there are few reviews regarding functional non-viral vectors. This review summarizes the common functional non-viral vectors developed in the last ten years and their potential applications in the future. The transfection efficiency and the transport mechanism of these materials were also discussed in detail. We hope that this review can help researchers design more new high-efficiency and low-toxicity multifunctional non-viral vectors, and further accelerate the progress of gene therapy.

scholarly journals Disarmed anthrax toxin delivers antisense oligonucleotides and siRNA with high efficiency and low toxicity

2015 ◽  
Vol 220 ◽  
pp. 316-328 ◽  
Author(s):  
Paul D.R. Dyer ◽  
Thomas R. Shepherd ◽  
Alexander S. Gollings ◽  
Susan A. Shorter ◽  
Monique A.M. Gorringe-Pattrick ◽  
...  
Keyword(s):  
Antisense Oligonucleotides ◽  
High Efficiency ◽  
Anthrax Toxin ◽  
Low Toxicity

Fishing antitumor ingredients by G-quadruplex affinity from herbal extract on a three-phase-laminar-flow microfluidic chip

Talanta ◽  
2020 ◽  
Vol 220 ◽  
pp. 121368 ◽  
Author(s):  
Qidan Cai ◽  
Jiang Meng ◽  
Yuewei Ge ◽  
Yan Gao ◽  
Yu Zeng ◽  
...  
Keyword(s):  
Laminar Flow ◽  
Microfluidic Chip ◽  
Herbal Extract ◽  
Three Phase ◽  
G Quadruplex

scholarly journals Do Consumers Care about the Energy Efficiency of Buildings? Understanding Residential Choice Based on Energy Performance Certificates

2018 ◽  
Vol 10 (11) ◽  
pp. 4297 ◽  
Author(s):  
Hyunjoo Lee ◽  
Misuk Lee ◽  
Sesil Lim
Keyword(s):  
Energy Efficiency ◽  
Energy Demand ◽  
High Efficiency ◽  
Early Stage ◽  
Energy Performance ◽  
Price Premium ◽  
Consumer Decision Making ◽  
Residential Choice ◽  
Performance Information ◽  
The Government

Disclosing the energy performance information for buildings has been expected to become an important policy for controlling energy demand and reducing CO2 emissions, but its effectiveness remains controversial. This study investigates the effect of energy performance information on consumer residential choice by using a discrete choice experiment in South Korea. The estimation results confirmed that the energy efficiency level of the given housing has a significant effect on consumer residential choice when the related information is actually delivered. Combined with evidence from the simulation study, we suggest that obligating the owners to provide energy performance information to potential buyers/tenants would be necessary for enhancing the use of the information during the consumer decision-making process. Additionally, the simulation result implies that the effectiveness of the policy can be underestimated by the price premium related to energy efficiency. Therefore, we suggest that the government should control the price premium for high-efficiency buildings at the early stage so that the policy related to disclosing the energy performance can be on track.

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