China
Africa
Explore chapters and articles related to this topic
Chemistry and Pharmacology of Naturally Occurring Flavoalkaloids
Published in Namrita Lall, Medicinal Plants for Cosmetics, Health and Diseases, 2022
Rashmi Gaur, Jyoti Gaur, Nikhilesh Kumar
The natural products containing a flavonoid skeleton with one or more nitrogen atoms are known as flavoalkaloid, isoflavoalkaloid or neoflavoalkaloid, based upon the skeleton of the flavonoid component. These flavoalkaloids are known for their numerous medicinal properties (Ilkei et al., 2018). The chromone alkaloid’s isolation and synthesis have previously been reviewed by Houghton. Later, he reviewed the isolation and bioactivity in 2012. Blair et al. (2017) reviewed the occurrence and synthesis of flavoalkaloids, while Ilkei et al. (2018) reviewed the occurrence and skeletal description of flavoalkaloids. However, no one has covered the biological activity of these flavoalkaloids in depth. Furthermore, after 2018, more flavoalkaloids were identified (Gaur et al., 2020). This chapter will include all the flavoalkaloids that are currently known up until early 2020, describing their isolation and bioactivity.
Rhinitis
Published in Pudupakkam K Vedanthan, Harold S Nelson, Shripad N Agashe, PA Mahesh, Rohit Katial, Textbook of Allergy for the Clinician, 2021
Vinay Mehta, Srinivasan Ramanuja, Pramod S Kelkar
Cromolyn sodium is a mast cell stabilizer (Table 8.8), which prevents mast cells from releasing histamine. It has no serious side effects and is available over-the-counter as a nasal spray. However, most studies show it to be less effective than intranasal corticosteroids, intranasal antihistamines and even second-generation oral antihistamines. In addition, compliance is hampered by its short duration of action, which necessitates topical administration up to six times daily. Studies of intranasal chromones in the treatment of nonallergic rhinitis are lacking.
Pharmacological treatment of asthma-related issues in athletes
Published in John W. Dickinson, James H. Hull, Complete Guide to Respiratory Care in Athletes, 2020
Mast cell stabilisers, disodium cromoglycate and nedocromil sodium, attenuate both asthma and EIB when inhaled shortly before exercise. These agents have been shown to inhibit inflammatory mediator release and to reduce bronchoconstriction. However, the degree of broncho-protection afforded by cromones is lower than inhaled β2-agonists (~50 versus ~66%, respectively) and their duration of action is relatively short (1–2 h).
Chromone-based monoamine oxidase B inhibitor with potential iron-chelating activity for the treatment of Alzheimer’s disease
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2023
Changjun Zhang, Yujia Zhang, Yangjing Lv, Jianan Guo, Bianbian Gao, Yi Lu, Anjie Zang, Xi Zhu, Tao Zhou, Yuanyuan Xie
Subsequently, the MAOs inhibitory activity of the compounds was measured, as shown in Tables 2 and 3. As detailed below, generally, hybrids with C–N bond linkers were more potent than those amide bond-linked compounds, with most of them having inhibition rates over 40%. Chromones bearing substituents in position C-7 of chromone exhibited better MAO-B inhibitory activity with IC50 values ranging from micromolar concentration to nanomolar concentration. Furthermore, when the benzyloxy group was inserted into the C-7 of chromone, the inclusion of electron-withdrawing substituents (F, Cl) in the benzyloxy counterposition demonstrated higher activity than interposition replacement. The most promising chromone derivatives, on the other hand, are changed by alkyl groups at C-6 or C-7 of chromone nuclear (compounds 17a–e and IC50 values range from 67 to 88 nM). Among them, compound 17d showed the best inhibitory activity compared with the reference drug (Pargyline).
Evolution of chromone-like compounds as potential antileishmanial agents, through the 21st century
Published in Expert Opinion on Drug Discovery, 2020
Carlos F. M. Silva, Diana C. G. A. Pinto, Pedro A. Fernandes, Artur M. S. Silva
Finally, even though there is no evidence of any chromone-type compound being further developed as pre-clinical or clinical candidates, the authors believe that some of the described compounds may have demonstrated suitable preliminary results to be considered appropriately. For instance, several compounds were depicted as presenting IC50 levels lower than 1 µM, with low levels of macrophage toxicity simultaneously, which proves that these compounds might be able to treat leishmaniasis without affecting the human host. Furthermore, the authors firmly believe that this review might also be able to constitute a starting point for the development of further studies, such as quantitative structure-activity relationship (QSAR), molecular docking, or ADMET studies. These studies might not only allow us to predict some promising antileishmanial candidates against numerous potential targets but also assess the candidates’ pharmacokinetics’ profiles through the prediction of some parameters like absorption, metabolism, or even bioavailability.
Chromones: privileged scaffolds for the production of multi-target-directed-ligand agents for the treatment of Alzheimer’s disease
Published in Expert Opinion on Drug Discovery, 2018
Carlos F. M. Silva, Diana C. G. A. Pinto, Artur M. S. Silva
As mentioned earlier, chromones are widely known for their huge number of biological activities emphasizing their anti-inflammatory activity, with two compounds already marketed as anti-inflammatory drugs for the treatment of asthma, namely sodium cromoglicate and nedocromil sodium [11]. However, these compounds are also emerging as potential MTDLs for the treatment of AD, since they have been associated to several beneficial effects toward different molecular hallmarks of the AD, such as the decrease of the cholinergic levels, the formation, and aggregation of Aβ, metal levels regulation, among others. Therefore, the understanding of the chromones’ optimal structural characteristics related to their beneficial effects would constitute crucial progress for further synthesis.