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A proton-coupled organic cation antiporter is involved in the blood-brain barrier transport of aconitum alkaloids
ConclusionsThese results demonstrate that a novel proton-coupled organic cation antiporter plays a predominant role in the blood to brain influx of AC, MA and HA at the BBB, and thus affect the safety of Aconitum species.Graphical abstract
Source: Journal of Ethnopharmacology - January 20, 2020 Category: Drugs & Pharmacology Source Type: research

Antifibrotic action of Yifei Sanjie formula enhanced autophagy via PI3K-AKT-mTOR signaling pathway in mouse model of pulmonary fibrosis
Publication date: October 2019Source: Biomedicine & Pharmacotherapy, Volume 118Author(s): Jing-Ze Yu, Yi Ying, Yang Liu, Chun-Bin Sun, Chen Dai, Shan Zhao, Shou-Zheng Tian, Jing Peng, Ni-Ping Han, Jia-Li Yuan, Jin-Yuan Yan, Zhong-Shan YangAbstractPulmonary fibrosis (PF) is a crippling disease characterized by progressive dyspnea and associated with a high mortality rate, but its origin is unknown and there is no effective treatment. Yifei Sanjie formula (YFSJF) is a Chinese medicine that is widely used for treatment of respiratory systems disease. However, the molecular basis for the function of YFSJF has not been determin...
Source: Biomedicine and Pharmacotherapy - August 9, 2019 Category: Drugs & Pharmacology Source Type: research

Plant-Derived Alkaloids: The Promising Disease-Modifying Agents for Inflammatory Bowel Disease
Conclusion This paper summarizes the current findings regarding the anti-colitis activity of plant-derived alkaloids and shows how these alkaloids exhibit significant and beneficial effects in alleviating colonic inflammation. These natural alkaloids are not only promising agents for IBD treatment but are also components for developing new wonder drugs. However, the underlying molecular mechanisms or toxicological evaluation of most plant-derived alkaloids still require much scientific research, and their actual efficacies for IBD patients have not been verified well in field research. Thus, further clinical trials to elu...
Source: Frontiers in Pharmacology - April 11, 2019 Category: Drugs & Pharmacology Source Type: research

The Mechanistic Links between Insulin and Human Organic Anion Transporter 4
In conclusion, our study demonstrated that insulin stimulates hOAT4 expression and transport activity by abrogating the inhibition effect of Nedd4-2 on the transporter. Moreover, insulin regulates hOAT4 by competing with sgk2 rather than through sgk2.Graphical abstract
Source: International Journal of Pharmaceutics - November 17, 2018 Category: Drugs & Pharmacology Source Type: research

Functionalized carbon nanotubes as emerging delivery system for the treatment of cancer
Publication date: Available online 8 July 2018Source: International Journal of PharmaceuticsAuthor(s): Shubhangi Mahajan, Abhimanyu Patharkar, Kaushik Kuche, Rahul Maheshwari, Pran Kishore Deb, Kiran Kalia, Rakesh K. TekadeAbstractIn recent time, carbon nanotubes (CNTs) have gained vital importance for pharmaceutical formulation scientist for delivering drugs and genes, owing to their excellent surface properties. For example, their aspect ratio is thought to be responsible for their excellent cell penetration aptitude; anisotropic conductivity/semi-conductivity along their axis is ideal for integration with nervous and mu...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Characterization of modified mesoporous silica nanoparticles as vectors for siRNA delivery
Publication date: Available online 21 February 2018Source: Asian Journal of Pharmaceutical SciencesAuthor(s): Anna Slita, Anna Egorova, Eudald Casals, Anton Kiselev, Jessica M. RosenholmAbstractGene therapy using siRNA molecules is nowadays considered as a promising approach. For successful therapy, development of a stable and reliable vector for siRNA is crucial. Non-viral and non-organic vectors like mesoporous silica nanoparticles (MSN) are associated with lack of most viral vector drawbacks, such as toxicity, immunogenicity, but also generally a low nucleic acid carrying capacity. To overcome this hurdle, we here modif...
Source: Asian Journal of Pharmaceutical Sciences - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Functionalized carbon nanotubes as emerging delivery system for the treatment of cancer
Publication date: Available online 8 July 2018Source: International Journal of PharmaceuticsAuthor(s): Shubhangi Mahajan, Abhimanyu Patharkar, Kaushik Kuche, Rahul Maheshwari, Pran Kishore Deb, Kiran Kalia, Rakesh K. TekadeAbstractIn recent time, carbon nanotubes (CNTs) have gained vital importance for pharmaceutical formulation scientist for delivering drugs and genes, owing to their excellent surface properties. For example, their aspect ratio is thought to be responsible for their excellent cell penetration aptitude; anisotropic conductivity/semi-conductivity along their axis is ideal for integration with nervous and mu...
Source: International Journal of Pharmaceutics - July 8, 2018 Category: Drugs & Pharmacology Source Type: research

Characterization of modified mesoporous silica nanoparticles as vectors for siRNA delivery
Publication date: Available online 21 February 2018Source: Asian Journal of Pharmaceutical SciencesAuthor(s): Anna Slita, Anna Egorova, Eudald Casals, Anton Kiselev, Jessica M. RosenholmAbstractGene therapy using siRNA molecules is nowadays considered as a promising approach. For successful therapy, development of a stable and reliable vector for siRNA is crucial. Non-viral and non-organic vectors like mesoporous silica nanoparticles (MSN) are associated with lack of most viral vector drawbacks, such as toxicity, immunogenicity, but also generally a low nucleic acid carrying capacity. To overcome this hurdle, we here modif...
Source: Asian Journal of Pharmaceutical Sciences - July 5, 2018 Category: Drugs & Pharmacology Source Type: research

Puerarin improves methotrexate-induced renal damage by up-regulating renal expression of Oat1 and Oat3 in vivo and in vitro
Publication date: July 2018 Source:Biomedicine & Pharmacotherapy, Volume 103 Author(s): Qi Liu, Zhihao Liu, Xiaokui Huo, Changyuan Wang, Qiang Meng, Huijun Sun, Pengyuan Sun, Jinyong Peng, Xiaodong Ma, Kexin Liu The regulation of renal transporters such as organic anion transporter (OATs) is a new target for treatment of acute renal failure. The purpose of this study was to investigate whether the effect of puerarin (Pur) on renal damage induced by methotrexate (MTX) is related to the expression of renal Oat1/3 in vivo and in vitro, and to explore the related mechanisms. Effect of Pur on the renal damage caused by...
Source: Biomedicine and Pharmacotherapy - April 25, 2018 Category: Drugs & Pharmacology Source Type: research

Characterization of modified mesoporous silica nanoparticles as vectors for siRNA delivery
Publication date: Available online 21 February 2018 Source:Asian Journal of Pharmaceutical Sciences Author(s): Anna Slita, Anna Egorova, Eudald Casals, Anton Kiselev, Jessica M. Rosenholm Gene therapy using siRNA molecules is nowadays considered as a promising approach. For successful therapy, development of a stable and reliable vector for siRNA is crucial. Non-viral and non-organic vectors like mesoporous silica nanoparticles (MSN) are associated with lack of most viral vector drawbacks, such as toxicity, immunogenicity, but also generally a low nucleic acid carrying capacity. To overcome this hurdle, we here modified t...
Source: Asian Journal of Pharmaceutical Sciences - April 14, 2018 Category: Drugs & Pharmacology Source Type: research

AG490, a JAK2-specific inhibitor, downregulates the expression and activity of organic anion transporter-3
Publication date: Available online 8 February 2018 Source:Journal of Pharmacological Sciences Author(s): Jinghui Zhang, Chenchang Liu, Guofeng You Human organic anion transporter-3 (hOAT3) is richly expressed in the kidney, where it plays critical roles in the secretion of clinically important drugs, including anti-viral therapeutics, anti-cancer drugs, antibiotics, antihypertensives, and anti-inflammatories. In the current study, we examined the role of AG490, a specific inhibitor of the Janus tyrosine kinase 2 (JAK2), in hOAT3 transport activity in the kidney COS-7 cells. AG490 induced a time- and concentration-depende...
Source: Journal of Pharmacological Sciences - February 15, 2018 Category: Drugs & Pharmacology Source Type: research

Shikonin upregulates the expression of drug-metabolizing enzymes and drug transporters in primary rat hepatocytes
Conclusions Shikonin effectively upregulates the transcription of CYP isozymes, phase II detoxification enzymes, and phase III membrane transporters and this function is at least partially through activation of AhR and Nrf2. Moreover, Nrf2 activation is dependent on mitogen-activated protein kinases. Graphical abstract
Source: Journal of Ethnopharmacology - February 4, 2018 Category: Drugs & Pharmacology Source Type: research

Recent Progress in Delivery of Therapeutic and Imaging Agents Utilizing Organic-inorganic Hybrid Nanoparticles.
Abstract Delivery of conventional small molecule drugs and currently evolving nucleic acid-based therapeutics, such as small interfering RNAs (siRNAs) and genes, and contrast agents for high resolution imaging, to the target site of action is highly demanding to increase the therapeutic and imaging efficacy while minimizing the off-target effects of the delivered molecules, as well as develop novel therapeutic and imaging approaches. Organic-inorganic hybrid nanoparticles offer a number of advantages by combining the unique properties of the organic and inorganic counterparts, thus improving the pharmacokinetic be...
Source: Current Drug Delivery - November 19, 2017 Category: Drugs & Pharmacology Authors: Tanzina HS, Chowdhury E Tags: Curr Drug Deliv Source Type: research

Folate appended cyclodextrins for drug, DNA, and siRNA delivery.
Abstract Drug, DNA, and siRNA delivery systems based on cyclodextrin (CD) core and connected with folate (FA) via various linkers are presented. They include simple mono-derivatized cyclodextrins as well as cyclodextrins with higher degree of substitution, both in their primary and secondary sides. Examples of simple polymers and dendrimers are also discussed. Such carriers possess properties inherent to both of their components. Cyclodextrin provides the ability to encapsulate organic molecules in its inner cavity, thus improving their solubility in water, bioavailability, and stability, while FA assures targetin...
Source: European Journal of Pharmaceutics and Biopharmaceutics - September 9, 2017 Category: Drugs & Pharmacology Authors: Ceborska M Tags: Eur J Pharm Biopharm Source Type: research

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