2 Non-Steroidal Anti-Inflammatory Drugs

Adams, S. S.; Cobb, Ronald R.

doi:10.1016/s0079-6468(08)70442-9

Cited by 30 publications

(10 citation statements)

References 290 publications

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“…e . 2-(phenylamino)benzoic acid 6 were chosen as suitable initial candidates for the screen due to similarities in structure to anthranilic acid and also their prolific record as agents used in the treatment of numerous inflammatory diseases [ 28 , 29 , 30 ]. Both NSAIDs readily conjugated to the chlorin scaffold in a controlled and predictable fashion and altering the reaction time and equivalents of reagents used could maximize the degree of functionalization and achieve conjugates 9a , 9b , 10a and 10b in good yields as per the Fig 2 .…”

Section: Resultsmentioning

confidence: 99%

Lead Structures for Applications in Photodynamic Therapy. 6. Temoporfin Anti-Inflammatory Conjugates to Target the Tumor Microenvironment for In Vitro PDT

et al. 2015

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Due to the ongoing development of clinical photodynamic therapy (PDT), the search continues for optimized photosensitizers that can overcome some of the side effects associated with this type of treatment modality. The main protagonists being: post-treatment photosensitivity, due to only limited cellular selectivity and post-treatment tumor regrowth, due to the up-regulation of pro-inflammatory agents within the tumor microenvironment. A photosensitizer that could overcome one or both of these drawbacks would be highly attractive to those engaged in clinical PDT. Certain non-steroidal anti-inflammatory drugs (NSAIDs) when used in combination with PDT have shown to increase the cytotoxicity of the treatment modality by targeting the tumor microenvironment. Temoporfin (m-THPC), the gold standard chlorin-based photosensitizer (PS) since its discovery in the 1980’s, has successfully been conjugated to non-steroidal anti-inflammatory compounds, in an attempt to address the issue of post-treatment tumor regrowth. Using a modified Steglich esterification reaction, a library of “iPorphyrins” was successfully synthesized and evaluated for their PDT efficacy.

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Section: Resultsmentioning

confidence: 99%

Lead Structures for Applications in Photodynamic Therapy. 6. Temoporfin Anti-Inflammatory Conjugates to Target the Tumor Microenvironment for In Vitro PDT

et al. 2015

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“…(S) naproxen, a known nonsteroidal anti inflammatory drug [28] and a derivatizing agent to assess the optical purity and kinetic resolution of racemates of optically active amines of various classes [29][30][31][32][33][34], was selected by us due to its unique spectral characteristics. It contains a strong chromophore group (the molecular extinction coefficient ε = 100000 at λ = 230 nm) and has fluores cent properties, which is why it can accurately be detected by UV spectroscopy.…”

Section: Resultsmentioning

confidence: 99%

Surface modification of Fe3O4 magnetic nanoparticles with (S)-naproxen

et al. 2012

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Fe 3 O 4 magnetic nanoparticles (MNPs) were obtained using the gas condensation method. These MNPs were modified with 3 aminopropylsilane (APS) through covalent bonding. The methods of qualitative and quantitative analysis of the modified MNPs were developed using UV and IR spectroscopy and induc tively coupled plasma emission spectrometry (ICP ES). It was established that the maximum loading level of APS on the surface of Fe 3 O 4 MNPs was 0.91 mmol/g MNP. The study of the activity of the surface amino groups of the nanocomposites was carried out by the example of their modification with (S) naproxen. The optimum conditions for coupling reaction were found. It was shown that the reaction proceeded most effi ciently when using 1 ethyl 3 (3 dimethylaminopropyl)carbodiimide (EDC) as coupling agent in the pres ence of 1 hydroxy 1H benzotriazole (HOBt). The maximum immobilization level of (S) naproxen on the Fe 3 O 4 MNP surface was 0.55 mmol/g MNP. Thus, the high reactivity of amino groups of the obtained nano composites was shown, making it possible to further modify them.

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“…In order to evaluate the possible anti-inflammatory activity of tomatine and tomatidine on the later stages of inflammation, the widely used carrageenan impregnated cotton pellet granuloma test was selected. Granulation tissue formation has been shown to be depressed by nearly all anti-inflammatory drugs, but the steroids are most active while phenylbutazone and salicylates show poor activity and chloroquine is almost inactive (Whitehouse, 1965; Adams & Cobb, 1967). The effect of tomatine in suppressing granulation tissue formation seems to be similar to that of steroids, since the inhibition of the granuloma formation was directly proportional to the dose of tomatine used.…”

Section: Discussionmentioning

confidence: 99%

Anti‐inflammatory activity of the steroid alkaloid glycoside, tomatine

Filderman

Kovács

1969

British J Pharmacology

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. Tomatine, isolated from extracts of crown gall‐infected tomato plants or obtained commercially, was tested for anti‐inflammatory activity using three different methods. . Tomatine administered to intact rats intramuscularly in a dose range of 1–10 mg/kg or orally in doses of 15–30 mg/kg exerted a significant dose dependent inhibition of carrageenan induced paw oedema. The inhibitory effect of tomatine when given in a dose of 10 mg/kg intramuscularly to intact rats lasted more than 24 hr. . In adrenalectomized rats significant dose‐related inhibition of paw oedema was obtained with tomatine and the inhibition at each dose level (0·5–10 mg/kg) was found to be greater than that found in intact animals. . Tomatine administered subcutaneously to intact rats daily for 7 days in doses of 5 or 10 mg/kg exerted a significant, dose dependent inhibition of granulation tissue formation induced by the subcutaneous implantation of carrageenan impregnated cotton pellets. . Tomatine administered to intact mice in a dose of 10 mg/kg subcutaneously 1 hr before the intraperitoneal injection of acidified saline and intravenous pontamine sky blue significantly decreased the leakage of the protein bound dye into the peritoneal cavity. . Tomatidine, the aglycone of tomatine, was not effective at dose levels of 10–20 mg/kg in any of the three tests.

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2 Non-Steroidal Anti-Inflammatory Drugs

Cited by 30 publications

References 290 publications

Lead Structures for Applications in Photodynamic Therapy. 6. Temoporfin Anti-Inflammatory Conjugates to Target the Tumor Microenvironment for In Vitro PDT

Lead Structures for Applications in Photodynamic Therapy. 6. Temoporfin Anti-Inflammatory Conjugates to Target the Tumor Microenvironment for In Vitro PDT

Surface modification of Fe3O4 magnetic nanoparticles with (S)-naproxen

Anti‐inflammatory activity of the steroid alkaloid glycoside, tomatine

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