Therapeutic evaluation of RDP-58 and cold plasma in vivo in combination with 5 amino salicylic acid: a study in mice

2021 ◽  
Author(s):  
Kalyan Chakravarthy Lnu
Keyword(s):  
Salicylic Acid ◽  
Cold Plasma ◽  
Therapeutic Evaluation ◽  
Amino Salicylic Acid

scholarly journals Characterization of 22 Antituberculosis Drugs for Inhibitory Interaction Potential on Organic Anionic Transporter Polypeptide (OATP)-Mediated Uptake

2016 ◽  
Vol 60 (5) ◽  
pp. 3096-3105 ◽  
Author(s):  
M. Masud Parvez ◽  
Jin Ah Jung ◽  
Ho Jung Shin ◽  
Dong Hyun Kim ◽  
Jae-Gook Shin
Keyword(s):  
Salicylic Acid ◽  
Interaction Potential ◽  
Organic Anion ◽  
Inhibitory Interaction ◽  
Content Type ◽  
Organic Anion Transporting Polypeptide ◽  
Amino Salicylic Acid ◽  
Inhibitory Potential

ABSTRACTWe investigated the inhibitory interaction potential of 22 currently marketed antituberculosis (TB) drugs on organic anion-transporting polypeptide 1B1 (OATP1B1)-, OATP2B1-, and OATP1B3-mediated uptake usingin vitroXenopusoocytes and HEK cells. Rifabutin, ethambutol, amoxicillin, linezolid,p-amino salicylic acid, and rifapentine exhibited mild to moderate inhibitory effects on OATP-mediated uptake of estrone-3 sulfate, estradiol 17β-d-glucuronide, and rosuvastatin. The 50% inhibitory concentration (IC50) values of rifabutin, amoxicillin, ethambutol,p-amino salicylic acid, and linezolid were 35.4, 36.2, 57.6, 72.6, and 65.9 μM, respectively, for uptake mediated by organic anionic transporter polypeptide 1B1 (OATP1B1) and 28.8, 28.9, 53.9, 31.5, and 61.0 μM, respectively, for uptake mediated by organic anionic transporter polypeptide 1B3 (OATP1B3). Streptomycin and linezolid showed greater inhibition of organic anionic transporter polypeptide 2B1 (OATP2B1)-mediated uptake, with IC50values of 33.2 and 35.6 μM, respectively, along with mild inhibition of other drugs. Furthermore, rifabutin, amoxicillin, and rifapentine significantly inhibited OATP1B1-mediated rosuvastatin uptake, with IC50values of 12.3, 13.0, and 11.0 μM, respectively, which showed a similar profile to estrone-3 sulfate uptake. The calculatedRvalues ([I]u inlet,max/Ki, where [I]u inlet,maxrepresents the maximum estimated inhibitor concentration inlet to the liver andKiis the inhibition constant) as the drug-drug interaction (DDI) indexes of PAS, ethambutol, and amoxicillin were 26.1, 6.5, and 4.3 for OATP1B1 and 52.0, 8.0, and 4.6 for OATP1B3, and those for streptomycin, amikacin, and linezolid were 5.0, 4.2, and 4.4 for OATP2B1, respectively, suggesting a higher possibility ofin vivoDDIs. This study is the first comprehensive report to show the novel inhibitory potential of 22 marketed anti-TB drugs on OATP-mediated uptake, providing evidence for futurein vivoclinical DDI studies.

Synthesis and Characterization of New Zinc Phthalocyanine - Dodecenyl Succinic Anhydride Benzoic Groups

2020 ◽  
Vol 17 (6) ◽  
pp. 488-495
Author(s):  
Hussein Ali Al-Bahrani ◽  
Mohanad Mousa Kareem ◽  
Abdul Amir Kadhum ◽  
Nour A. Alrazzak
Keyword(s):  
Salicylic Acid ◽  
Succinic Anhydride ◽  
Zinc Phthalocyanine ◽  
Central Metal ◽  
Target Compound ◽  
Compound I ◽  
Metal Phthalocyanines ◽  
Metal Atoms ◽  
Amino Salicylic Acid

Background: The phthalocyanines a series of compounds involves four iso-indole units linked by aza nitrogen atoms bonded with metal atoms that are normally located in the center a phthalocyanines ring. Some of the central metal-phthalocyanines can be excited by ultraviolet light and emit a fluorescence in far-red region. Objective: To synthesize a derivative of phthalocyanines namely 4,4',4' '-tri-(dodecenyl succinic anhydride)- 4' ' '-(5-amino salicylic acid) zinc phthalocyanine with a zinc central metal. Materials and Methods: The reaction of 4- nitro Phthalonitrile and 4- amino Phthalonitrile with ZnCl2 in the presence of dimethyl amino ethanol afforded 4,4',4' '-triamino-4' ' '-nitro zinc phthalocyanine. This product reacted with 5-amino salicylic acid to yield tetra-(5-amino salicylic acid) zinc phthalocyanine. A dodecenyl succinic anhydride was added on the amine group of benzoic rings to afford 4,4',4' '-tri-(dodecenyl succinic anhydride)-4' ' '-(5-amino salicylic acid) zinc phthalocyanine(I), the target compound. Results and Discussion: Compound I is successfully synthesized with a yield of 72% from tetra-(5-amino salicylic acid) zinc phthalocyanine with dodecenyl succinic anhydride. Conclusion: The newly synthesized molecule of 4,4',4' '-tri-(dodecenyl succinic anhydride)-4' ' '-(5-amino salicylic acid) zinc phthalocyanine (I), tetra-(5-amino salicylic acid) zinc phthalocyanine(E) and 4,4',4' '- triamino-4' ' '-nitro zinc phthalocyanine (S). The reaction of 4- nitro Phthalonitrile and 4- amino and the structure of compound I is confirmed and its formation was proven.

Cold Plasma Treatment Promotes Full-thickness Healing of Skin Wounds in Murine Models

2021 ◽  
pp. 153473462110021
Author(s):  
Joon M. Jung ◽  
Hae K. Yoon ◽  
Chang J. Jung ◽  
Soo Y. Jo ◽  
Sang G. Hwang ◽  
...  
Keyword(s):  
Wound Healing ◽  
Plasma Treatment ◽  
Cold Plasma ◽  
Smooth Muscle Actin ◽  
Treated Group ◽  
Control Group ◽  
Alpha Smooth Muscle Actin ◽  
Skin Wound Healing

Cold plasma can be beneficial for promoting skin wound healing and has a high potential of being effectively used in treating various wounds. Our aim was to verify the effect of cold plasma in accelerating wound healing and investigate its underlying mechanism in vitro and in vivo. For the in vivo experiments, 2 full-thickness dermal wounds were created in each mouse (n = 30). While one wound was exposed to 2 daily plasma treatments for 3 min, the other wound served as a control. The wounds were evaluated by imaging and histological analyses at 4, 7, and 11 days post the wound infliction process. Immunohistochemical studies were also performed at the same time points. In vitro proliferation and scratch assay using HaCaT keratinocytes and fibroblasts were performed. The expression levels of wound healing–related genes were analyzed by real-time polymerase chain reaction and western blot analysis. On day 7, the wound healing rates were 53.94% and 63.58% for the control group and the plasma-treated group, respectively. On day 11, these rates were 76.05% and 93.44% for the control and plasma-treated groups, respectively, and the difference between them was significant ( P = .039). Histological analysis demonstrated that plasma treatment promotes the formation of epidermal keratin and granular layers. Immunohistochemical studies also revealed that collagen 1, collagen 3, and alpha-smooth muscle actin appeared more abundantly in the plasma-treated group than in the control group. In vitro, the proliferation of keratinocytes was promoted by plasma exposure. Scratch assay showed that fibroblast exposure to plasma increased their migration. The expression levels of collagen 1, collagen 3, and alpha-smooth muscle actin were elevated upon plasma treatment. In conclusion, cold plasma can accelerate skin wound healing and is well tolerated.

scholarly journals Improving the Biocontrol Potential of Bacterial Antagonists with Salicylic Acid against Brown Rot Disease and Impact on Nectarine Fruits Quality

Agronomy ◽  
2021 ◽  
Vol 11 (2) ◽  
pp. 209
Author(s):  
Nadia Lyousfi ◽  
Rachid Lahlali ◽  
Chaimaa Letrib ◽  
Zineb Belabess ◽  
Rachida Ouaabou ◽  
...  
Keyword(s):  
Salicylic Acid ◽  
Disease Severity ◽  
Mycelial Growth ◽  
Brown Rot ◽  
Antagonistic Bacteria ◽  
Biological Treatments ◽  
Rot Disease ◽  
The Impact

The main objective of this study was to evaluate the ability of both antagonistic bacteria Bacillus amyloliquefaciens (SF14) and Alcaligenes faecalis (ACBC1) used in combination with salicylic acid (SA) to effectively control brown rot disease caused by Monilinia fructigena. Four concentrations of salicylic acid (0.5%, 2%, 3.5%, and 5%) were tested under in vitro and in vivo conditions. Furthermore, the impact of biological treatments on nectarine fruit parameters’ quality, in particular, weight loss, titratable acidity, and soluble solids content, was evaluated. Regardless of the bacterium, the results indicated that all combined treatments displayed a strong inhibitory effect on the mycelial growth of M. fructigena and disease severity. Interestingly, all SA concentrations significantly improved the biocontrol activity of each antagonist. The mycelial growth inhibition rate ranged from 9.79% to 88.02% with the highest reduction rate recorded for bacterial antagonists in combination with SA at both concentrations of 0.5% and 3.5%. The in vivo results confirmed the in vitro results with a disease severity varying from 0.00% to 51.91%. A significant biocontrol improvement was obtained with both antagonistic bacteria when used in combination with SA at concentrations of 0.5% and 2%. The lowest disease severity observed with ACBC1 compared with SF14 is likely due to a rapid adaptation and increase of antagonistic bacteria population in wounded sites. The impact of all biological treatments revealed moderate significant changes in the fruit quality parameters with weight loss for several treatments. These results suggest that the improved disease control of both antagonistic bacteria was more likely directly linked to both the inhibitory effects of SA on pathogen growth and induced fruit resistance.

Crystals and molecular structure ofp-amino-salicylic acid

1954 ◽  
Vol 7 (12) ◽  
pp. 808-812 ◽  
Author(s):  
F. Bertinotti ◽  
C. Giacomello ◽  
A. M. Liquori
Keyword(s):  
Molecular Structure ◽  
Salicylic Acid ◽  
Amino Salicylic Acid

Interactions of gallic acid, resveratrol, quercetin and aspirin at the platelet cyclooxygenase-1 level Functional and modelling studies

2009 ◽  
Vol 102 (08) ◽  
pp. 336-346 ◽  
Author(s):  
Marilena Crescente ◽  
Gisela Jessen ◽  
Stefania Momi ◽  
Hans-Dieter Höltje ◽  
Paolo Gresele ◽  
...  
Keyword(s):  
Salicylic Acid ◽  
Platelet Aggregation ◽  
Gallic Acid ◽  
Molecular Modelling ◽  
In Silico Docking ◽  
Cyclooxygenase 1 ◽  
Modelling Studies ◽  
Cox 1

SummaryWhile resveratrol and quercetin possess antiplatelet activity, little is known on the effect of gallic acid on platelets.We studied the interactions of these three different polyphenols among themselves and with aspirin, at the level of platelet cyclooxygenase-1 (COX-1). Both functional (in vitro and in vivo) and molecular modelling approaches were used. All three polyphenols showed comparable antioxidant activity (arachidonic acid [AA]-induced intraplatelet ROS production); however, resveratrol and quercetin, but not gallic acid, inhibited AA-induced platelet aggregation. Gallic acid, similarly to salicylic acid, the major aspirin metabolite, prevented inhibition of AA-induced platelet function by aspirin but, at variance with salicylic acid, also prevented inhibition by the other two polyphenols. Molecular modelling studies, performed by in silico docking the polyphenols into the crystal structure of COX-1, suggested that all compounds form stable complexes into the COX-1 channel, with slightly different but functionally relevant interaction geometries. Experiments in mice showed that gallic acid administered before aspirin, resveratrol or quercetin fully prevented their inhibitory effect on serum TxB2. Finally, a mixture of resveratrol, quercetin and gallic acid, at relative concentrations similar to those contained in most red wines, did not inhibit platelet aggregation, but potentiated sub-inhibitory concentrations of aspirin. Gallic acid interactions with other polyphenols or aspirin at the level of platelet COX-1 might partly explain the complex,and possibly contrasting, effects of wine and other components of the Mediterranean diet on platelets and on the pharmacologic effect of lowdose aspirin.

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