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1. Introducing a squaramide-based self-immolative spacer for controlled drug release

Author:
Ximenis, Marta; Sampedro, Angel; Martínez-Crespo, Luis; Ramis, Guillem; Orvay, Francisca; Costa, Antonio; Rotger, Carmen
Source:
Chemical communications 2021 v.57 no.22 pp. 2736-2739
ISSN:
1364-548X
Subject:
drug delivery systems; drugs,   etc   ; alkylation agents; glioblastoma;     Show all 4 Subjects
Abstract:
... Herein we report the design, synthesis and assessment of the first example of a squaramide-based self-immolative system triggered by an enzymatic reduction. We have proved that the release of the alkylating agent N′,N′-(bis(2-chloroethyl)benzene)-1,4-diamine (ANM) provokes a dramatic reduction of the survival factor in glioblastoma cells, evidencing the suitability of the squaramide-based spacer f ...
DOI:
10.1039/d0cc07683j

2. Targeting neuroinflammation: The therapeutic potential of ω-3 PUFAs in substance abuse

Author:
Peng, Sha; Peng, Zhuang; Qin, Meng; Huang, Lu; Zhao, Bin; Wei, Lai; Ning, Jie; Tuo, Qin-hui; Yuan, Ti-fei; Shi, Zhe; Liao, Duan-fang
Source:
Nutrition 2021 v.83 pp. 111058
ISSN:
0899-9007
Subject:
drug abuse; drug development,   etc   ; brain; nutrition; therapeutics;     Show all 5 Subjects
Abstract:
... Substance abuse is a chronic relapsing disorder that results in serious health and socioeconomic issues worldwide. Addictive drugs induce long-lasting morphologic and functional changes in brain circuits and account for the formation of compulsive drug-seeking and drug-taking behaviors. Yet, there remains a lack of reliable therapy. In recent years, accumulating evidence indicated that neuroinflam ...
DOI:
10.1016/j.nut.2020.111058

3. Current State and Promising Opportunities on Pharmaceutical Approaches in the Treatment of Polymicrobial Diseases

Author:
Sartini, Sartini; Permana, Andi Dian; Mitra, Saikat; Tareq, Abu Montakim; Salim, Emil; Ahmad, Islamudin; Harapan, Harapan; Emran, Talha Bin; Nainu, Firzan
Source:
Pathogens 2021 v.10 no.2
ISSN:
2076-0817
Subject:
drug therapy; multiple drug resistance,   etc   ; biofilm;     Show all 3 Subject
Abstract:
... In recent years, the emergence of newly identified acute and chronic infectious disorders caused by diverse combinations of pathogens, termed polymicrobial diseases, has had catastrophic consequences for humans. Antimicrobial agents have been clinically proven to be effective in the pharmacological treatment of polymicrobial diseases. Unfortunately, an increasing trend in the emergence of multi-dr ...
DOI:
10.3390/pathogens10020245

4. Electrophoresis of a highly charged dielectric fluid droplet in electrolyte solutions

Author:
Wu, Yvonne; Fan, Leia; Jian, Elaine; Lee, Eric
Source:
Journal of colloid and interface science 2021 v.598 pp. 358-368
ISSN:
0021-9797
Subject:
drugs,   etc   ; droplets; electrolytes; electrophoresis;     Show all 4 Subjects
Abstract:
... Electrophoresis of a dielectric fluid droplet with arbitrary surface potentials is investigated theoretically in this study. A pseudo-spectral method based on Chebyshev polynomials is adopted to solve the governing electrokinetic equations. Droplet mobilities are expressed as functions of electrolyte strength for fluid droplets with various viscosities and surface potentials. Effects of various el ...
DOI:
10.1016/j.jcis.2021.03.179

5. Microfluidic synthesis of curcumin loaded polymer nanoparticles with tunable drug loading and pH-triggered release

Author:
Baby, Thejus; Liu, Yun; Yang, Guangze; Chen, Dong; Zhao, Chun-Xia
Source:
Journal of colloid and interface science 2021 v.594 pp. 474-484
ISSN:
0021-9797
Subject:
drugs,   etc   ; curcumin; pH; polymers;     Show all 4 Subjects
Abstract:
... Polymer nanoparticles (NPs) have attracted significant interest in the past years for drug delivery and triggered release. However, it remains a significant challenge to produce polymer NPs with controlled properties and tunable drug loading. Traditional nanoprecipitation often leads to low drug loading. This study reports the development of a new microfluidic nanoprecipitation approach for making ...
DOI:
10.1016/j.jcis.2021.03.035

6. Redefining the “rational use of medicines”

Author:
Orive, Gorka; Domingo-Echaburu, Saioa; Lertxundi, Unax
Source:
Sustainable chemistry and pharmacy 2021 v.20 pp. 100381
ISSN:
2352-5541
Subject:
drugs,   etc   ; green chemistry; philosophy;     Show all 3 Subjects
Abstract:
... For a long time, the definition of “Rational Use of Drugs” has set the basic conceptual framework for health providers worldwide to implement relevant recommendations about drug use, improving the quality of the lives of patients. However, we believe this definition needs an urgent update to incorporate One-Health's philosophy. ...
DOI:
10.1016/j.scp.2021.100381

7. Direct ligand screening against membrane proteins on live cells enabled by DNA-programmed affinity labelling

Author:
Huang, Yiran; Deng, Yuqing; Zhang, Jianfu; Meng, Ling; Li, Xiaoyu
Source:
Chemical communications 2021 v.57 no.31 pp. 3769-3772
ISSN:
1364-548X
Subject:
drugs,   etc   ; DNA; hydrophobicity; ligands;     Show all 4 Subjects
Abstract:
... Membrane proteins are important drug targets; however, ligand discovery for membrane proteins is highly challenging due to their hydrophobic nature. We show that membrane proteins may be specifically labelled with a DNA tag by DNA-programmed affinity labelling (DPAL), thereby enabling the screening of chemical compounds against membrane proteins directly on live cells. ...
DOI:
10.1039/d1cc00961c

8. Exploring the utility of hybrid siloxane-phosphocholine (SiPC) liposomes as drug delivery vehicles

Author:
Frampton, Mark B.; Blais, Andrea; Raczywolski, Zachary; Castle, Alan; Zelisko, Paul M.
Source:
RSC advances 2021 v.11 no.21 pp. 13014-13023
ISSN:
2046-2069
Subject:
drugs,   etc   ; encapsulation; extrusion; hybrids;     Show all 4 Subjects
Abstract:
... Hybrid siloxane-phosphocholines (SiPCs) are a unique class of lipids that possess the capacity to spontaneously form unilamellar vesicles (ULVs) that are ∼100 nm in diameter upon exposure to aqueous media without the need for extrusion. These hybrid SiPCs do not negatively impact the growth of a number of bacterial strains and were subsequently explored as candidates for the delivery of a model co ...
DOI:
10.1039/d0ra10052h

9. Offline preparative three-dimensional HPLC for systematic and efficient purification of alkaloids from Gelsemium elegans Benth

Author:
Liu, Dian; Han, Yang; Zhou, Han; Jin, Hongli; Kang, Hongjian; Huang, FeiFei; Liu, Yanfang; Liang, Xinmiao
Source:
Journal of chromatography 2021 v.1640 pp. 461935
ISSN:
0021-9673
Subject:
drugs,   etc   ; Gelsemium elegans; pH;     Show all 3 Subjects
Abstract:
... The natural compound library is the most productive source in drug discovery and alkaloids are the most potential drug leads in natural compounds. Presently, systematic purification of alkaloids remains a substantial challenge. In this study, we developed an offline preparative three-dimensional HPLC (3D-HPLC) method to resolve the problem of systematic purification of alkaloids. Ten Gelsemium sta ...
DOI:
10.1016/j.chroma.2021.461935

10. Melting point prediction of organic molecules by deciphering the chemical structure into a natural language

Author:
Mi, Weiming; Chen, Huijun; Zhu, Donghua (Alan); Zhang, Tao; Qian, Feng
Source:
Chemical communications 2021 v.57 no.21 pp. 2633-2636
ISSN:
1364-548X
Subject:
drugs,   etc   ; models; prediction;     Show all 3 Subjects
Abstract:
... Establishing quantitative structure–property relationships for the rational design of small molecule drugs at the early discovery stage is highly desirable. Using natural language processing (NLP), we proposed a machine learning model to process the line notation of small organic molecules, allowing the prediction of their melting points. The model prediction accuracy benefits from training upon d ...
DOI:
10.1039/d0cc07384a

11. Controlled induction of immune tolerance by mesenchymal stem cells transferred by maternal microchimerism

Author:
Iwai, Sayuri; Okada, Aiko; Sasano, Kei; Endo, Masayuki; Yamazaki, Sho; Wang, Xin; Shimbo, Takashi; Tomimatsu, Takuji; Kimura, Tadashi; Tamai, Katsuto
Source:
Biochemical and biophysical research communications 2021 v.539 pp. 83-88
ISSN:
0006-291X
Subject:
drugs,   etc   ; immunosuppression; pregnancy; research;     Show all 4 Subjects
Abstract:
... Feto-maternal immune tolerance is established during pregnancy; however, its mechanism and maintenance remain underexplored. Here, we investigated whether mesenchymal stem/stromal cells (MSCs) as non-inherited maternal antigens (NIMAs) transferred by maternal microchimerism could induce immune tolerance. We showed that MSCs had a potential equivalent to hematopoietic stem and progenitor cells (HSP ...
DOI:
10.1016/j.bbrc.2020.12.032

12. Programmable Transformations of DNA Origami Made of Small Modular Dynamic Units

Author:
Wang, Dongfang; Yu, Lei; Huang, Chao-Min; Arya, Gaurav; Chang, Shuai; Ke, Yonggang
Source:
Journal of the American Chemical Society 2021 v.143 no.5 pp. 2256-2263
ISSN:
1520-5126
Subject:
drugs,   etc   ; DNA; nanocarriers;     Show all 3 Subjects
Abstract:
... Dynamic DNA origami has been employed for generating a rich repository of molecular nanomachines that are capable of sensing various cues and changing their conformations accordingly. The common design principle of the existing DNA origami nanomachines is that each dynamic DNA origami is programmed to transform in a specific manner, and the nanomachine needs to be redesigned to achieve a different ...
DOI:
10.1021/jacs.0c10576

13. Recent advancement in the synthesis of diverse spiro-indeno[1,2-b]quinoxalines: a review

Author:
Singh, Ruby; Bhardwaj, Diksha; Saini, Munna Ram
Source:
RSC advances 2021 v.11 no.8 pp. 4760-4804
ISSN:
2046-2069
Subject:
drugs,   etc   ; carbon; quinoxalines;     Show all 3 Subjects
Abstract:
... The nitrogen-containing indeno[1,2-b]quinoxaline ring is a privileged structurally fused active system and has notable applications in various fields of chemistry. For the past several years, it has been recognized as an important building block in organic synthesis. This review summarizes the reactions of indeno[1,2-b]quinoxalinone as a key construction block for producing a variety of indeno[1,2 ...
DOI:
10.1039/d0ra09130h

14. GW4064 enhances the chemosensitivity of colorectal cancer to oxaliplatin by inducing pyroptosis

Author:
Guo, Jing; Zheng, Jianbao; Mu, Mingchao; Chen, Zilu; Xu, Zhengshui; Zhao, Chenye; Yang, Kui; Qin, Xiao; Sun, Xuejun; Yu, Junhui
Source:
Biochemical and biophysical research communications 2021 v.548 pp. 60-66
ISSN:
0006-291X
Subject:
drug resistance; drugs,   etc   ; cell growth; colorectal neoplasms; pyroptosis; research;     Show all 6 Subjects
Abstract:
... Repeated and long-term oxaliplatin therapy leads to drug resistance and severe adverse events, which limit its clinical use. These difficulties highlight the importance of identifying potent and specific drug combinations to enhance the antitumor effects of oxaliplatin. The farnesoid X receptor (FXR) deficiency in colorectal cancer (CRC) suggests that restoring FXR function might be a promising st ...
DOI:
10.1016/j.bbrc.2021.02.043

15. Controlled drug release: On the evolution of physically entrapped drug inside the electrospun poly(lactic-co-glycolic acid) matrix

Author:
Wu, Jiaen; Xu, Shanshan; Han, Charles C.; Yuan, Guangcui
Source:
Journal of controlled release 2021 v.331 pp. 472-479
ISSN:
0168-3659
Subject:
drug delivery systems; drugs,   etc   ; evolution; humidity; neutrons; polymers; temperature; transportation;     Show all 8 Subjects
Abstract:
... The drug loading and releasing properties of poly(lactic-co-glycolic acid) (PLGA) were approached with the application of neutron techniques. The neutron reflection (NR) study on the response of PLGA material to vapor and to bulk water revealed that the hydration of PLGA origins from the molecular compatibility between water and PLGA. Hydration is reversible with regard to the change in humidity a ...
DOI:
10.1016/j.jconrel.2021.01.038

16. Choices of chromatographic methods as stability indicating assays for pharmaceutical products: A review

Author:
Chew, Yik-Ling; Khor, Mei-Ann; Lim, Yau-Yan
Source:
Heliyon 2021 v.7 no.3 pp. e06553
ISSN:
2405-8440
Subject:
drug formulations; drugs,   etc   ; active pharmaceutical ingredients; chemical species; qualitative analysis;     Show all 5 Subjects
Abstract:
... Stability indicating assay describes a technique which is used to analyse the stability of drug substance or active pharmaceutical ingredient (API) in bulk drug and pharmaceutical products. Stability indicating assay must be properly validated as per ICH guidelines. The important components in a stability indicating assay include sensitivity, specificity, accuracy, reliability, reproducibility and ...
DOI:
10.1016/j.heliyon.2021.e06553

17. Smart stimuli-responsive drug delivery systems based on cyclodextrin: A review

Author:
Tian, Bingren; Liu, Yumei; Liu, Jiayue
Source:
Carbohydrate polymers 2021 v.251 pp. 116871
ISSN:
0144-8617
Subject:
drug delivery systems; drugs,   etc   ; cyclodextrins; enzymes; magnetic materials; pH; temperature;     Show all 7 Subjects
Abstract:
... Stimulated by researches in materials chemistry and medicine fields, drug delivery has entered a new stage of development. Drug delivery systems have been extensively studied according to the differences in the drug therapeutic environment such as pH, light, temperature, magnet, redox, enzymes, etc. Cyclodextrin is a smart tool that has been proven to be used in the preparation of drug delivery, a ...
DOI:
10.1016/j.carbpol.2020.116871

18. Current and emerging methods for treatment of hemoglobin related cutaneous discoloration: A literature review

Author:
Urakov, Aleksandr; Urakova, Natalia; Nikolenko, Vladimir; Belkharoeva, Rosa; Achkasov, Evgeny; Kochurova, Ekaterina; Gavryushova, Liliya; Sinelnikov, Mikhail
Source:
Heliyon 2021 v.7 no.1 pp. e05954
ISSN:
2405-8440
Subject:
drug therapy; drugs,   etc   ; bilirubin; blood; cosmetics; discoloration; hematoma; hemoglobin; patents;     Show all 9 Subjects
Abstract:
... Currently, there is no available medication for immediate correction of bruise discoloration. Instead, makeup, cosmetic powders, concealers, and various traditional herbal remedies are used to mask discoloration. These approaches have no influence on the pathology behind the discoloration. The purpose of this study was to explore existing methods and current trends in correction of hemoglobin rela ...
DOI:
10.1016/j.heliyon.2021.e05954

19. Depletion of glioma stem cells by synergistic inhibition of mTOR and c-Myc with a biological camouflaged cascade brain-targeting nanosystem

Author:
Ma, Yuying; Zhang, Jinnan; Rui, Yalan; Rolle, Janiqua; Xu, Tian; Qian, Zhiyu; Gu, Yueqing; Li, Siwen
Source:
Biomaterials 2021 v.268 pp. 120564
ISSN:
0142-9612
Subject:
drug resistance; drugs,   etc   ; biocompatible materials; camouflage; glioblastoma; longevity; therapeutics;     Show all 7 Subjects
Abstract:
... Glioma stem cells (GSCs), as a subpopulation of stem cell-like cells, have been proposed to play a crucial role in the progression of drug-resistance in glioblastoma (GBM). Therefore, the targeted eradication of GSCs can serve as a promising therapeutic strategy for the reversal of drug-resistance in GBM. Herein, the effects of silencing c-Myc and m-TOR on primary GBM cells extracted from patients ...
DOI:
10.1016/j.biomaterials.2020.120564

20. The guest polymer effect on the dissolution of drug–polymer crystalline inclusion complexes

Author:
Chen, Lu; Huang, Yanbin
Source:
RSC advances 2021 v.11 no.22 pp. 13091-13096
ISSN:
2046-2069
Subject:
drugs,   etc   ; crystal structure; hydrophilicity; hydrophobicity;     Show all 4 Subjects
Abstract:
... A drug–polymer crystalline inclusion complex (IC) is a novel solid form of drug, in which drug molecules form parallel channels, and linear polymer chains reside in these channels. In this study, we used carbamazepine (CBZ) as a model drug, and directly studied the effect of different types of guest polymers on the dissolution properties of drug–polymer ICs. We successfully prepared ICs formed fro ...
DOI:
10.1039/d1ra01926k