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Phototherapy Using Nanomaterials
Published in D. Sakthi Kumar, Aswathy Ravindran Girija, Bionanotechnology in Cancer, 2023
A. N. Resmi, V. Nair Resmi, C. R. Rekha, V. Nair Lakshmi, Shaiju S. Nazeer, Ramapurath S. Jayasree
Functionalized fullerenes, which are composed of 60 or 70 carbon atoms, have attracted wide interest in the research field of PDT. They can be very effective in photo inactivation of cancer cells, depending on the functional groups introduced into the molecule and can generate ROSs upon illumination [202]. The first in vitro study of capability of fullerenes to create ROSs and catalyze the phototoxic reaction upon photo excitation was demonstrated on thymocytes and Ehrlich ascites cells [203]. In this work, the aqueous solution of fullerenes C60 was irradiated with visible light to these cell suspensions for short interval of time and increased rate of ROS was demonstrated. One of the major drawbacks, which limit the applications of fullerenes in biological system, is its poor water solubility. This may be overcome by introducing substituents, which are water soluble, mixing with water-soluble polymers or lipid membranes, and reduction to water-soluble anions. The comparison of the photodynamic activity of six functionalized fullerenes with 1, 2, or 3 hydrophilic or 1, 2, or 3 cationic groups was detailed in another work. Here, they considered three mouse cancer cell lines viz. J774, LLC, and CT26, which were incubated for 24 h with fullerenes and illuminated with white light. It was found that the photodynamic activity of the functionalized fullerenes was inversely proportional to the degree of substitution of the fullerene nucleus for both the neutral and the cationic series. They further inferred that photo toxicity can be mediated both by superoxide and 1O2 [202, 204].
Antibiotics: The Need for Innovation
Published in Nathan Keighley, Miraculous Medicines and the Chemistry of Drug Design, 2020
A single fluorine atom at position 6 greatly increased activity as well as uptake into the bacterial cell. Addition of a piperazine ring on position 7 is beneficial; improved oral adsorption, tissue distribution, metabolic stability, as well as improving the level and spectrum of activity are among the advantages. Presumably, the ability for the basic substituent to form a zwitterion with the carboxyl group is the reason for these improved drug properties. Further modifications include addition of an isopropyl ring to nitrogen 1, and replacement of pyridine with benzene. This leads to the development of ciprofloxacin, which is regarded as one of the most active broad spectrum antibiotics available. Furthermore, bacteria are slow to develop resistance to it, unlike nalidixic acid.
Pharmacognostic Studies on Ormocarpum sennoides (Willd.) DC.
Published in Parimelazhagan Thangaraj, Phytomedicine, 2020
M. M. Sudheer Mohammed, A. Narayanasamy, S. Mahadevan
Historically, plants have yielded some of our most important drugs (Heinrich et al. 2012), but many of them are used without standardization, which in turn leads to adulteration. Substitute or counterfeit herbal materials often found in the market is a major problem in the herbal industry. Standardization of a crude drug is essential to avoid and identify the adulterants or substituents (Kumar et al. 2012). Standardization is performed by stepwise pharmacognostic and phytochemical studies.
Transdermal delivery of inflammatory factors regulated drugs for rheumatoid arthritis
Published in Drug Delivery, 2022
Yanyan Zhang, Zhaoju Gao, Shushu Chao, Wenjuan Lu, Pingping Zhang
NSAIDs are widely used to reduce the symptoms of RA, which are a class of anti-inflammatory drugs that do not contain steroidal skeletons. Most of NSAIDs have the basic structure of aromatic acid with pKa values of 3–5 (Badri et al., 2016). According to different aryl structures and substituents, the hydrophilic and lipophilic properties of drugs will be different (Miranda et al., 2021). For example, the partition coefficient values (logP) for NSAIDs ketoprofen, celecoxib, indomethacin, flurbiprofen, and diclofenac are 0.97, 3.53, 3.8, 4.16 and 4.51, respectively (Subongkot & Sirirak, 2020; Arunprasert et al., 2021; Miranda et al., 2021). NSAIDs have antipyretic, analgesic, and anti-inflammatory effects, which can inhibit the conversion of arachidonic acid to prostaglandin by inhibiting COX-2, and then reducing the production of pain-causing prostaglandin (Bazan et al., 2002; Abbasi et al., 2019). In addition, the decrease of prostaglandin can inhibit the activation of inflammatory T helper lymphocytes 17, then inhibiting the transformation of T cells into an inflammatory state, and further reducing the secretion of inflammatory factors (Jia et al., 2014; Samuels et al., 2018).
A patent review of MAT2a inhibitors (2018–2021)
Published in Expert Opinion on Therapeutic Patents, 2022
Stephen J. Atkinson, Laura Evans, James S. Scott
A final composition of matter filing from Agios on MAT2a inhibitors published in December 2020 [20]. This application followed the same format as previously, with data once again binned against the same assays. This patent claims a regioisomeric pyridone core to those illustrated in the 2019 filings, whereby the pyridone nitrogen is now between the carbonyl and the second heteroaryl ring (cf. Figure 4). There are 190 compounds, with 68 compounds with the optimal profile and 12 compounds where preparation is described in full. Example 119 (13, Figure 6) is a representative example of the equity, although there are additional examples described with further aza-functionality added to either ring of the 6,6-core (e.g. Figure 5, X or Y = N). Once again the preferred substituents show similarity with the previous filings, suggesting these groups are close to optimal for this pharmacophore.
Is it possible to design a clinically viable heroin vaccine? The progress and pitfalls
Published in Expert Opinion on Drug Discovery, 2022
Therese J. Ziaks, Candy S. Hwang
The selection of the heroin hapten is the lynchpin of the vaccine. A heroin hapten can be referred to as dynamic if it stimulates antibodies for 1, 5, and 6. The benefit of this strategy is that it generates serum antibodies for all three psychoactive compounds to create a more efficacious vaccine. Preclinical studies demonstrate that serum antibodies exhibit specificity for heroin and its metabolites, with the highest affinity toward 5. However, the drawback is controlling the uniformity of these immunoconjugates during scale-up manufacturing as the hapten may exhibit batch variation due to rapid hydrolysis from 1 to 5. During a long-term stability study with the heroin vaccine in liquid formation, a higher titer and affinity for 6 was not observed. Interestingly, this would have been expected under prolonged aqueous conditions if the acetate moieties on heroin underwent hydrolysis [21]. Alternatively, replacing acetyl groups with other substituents may remove the inconsistency from a dynamic hapten, but may generate antibodies with less specificity to heroin and its metabolites. An additional option is a morphine-based hapten (11) [17,18], which entirely avoids the potential challenge of manufacturing a heroin-based hapten under good manufacturing practice (GMP), as heroin is the requisite precursor and a Schedule I drug regulated by the Drug Enforcement Administration.