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Marine Fungi-Derived Secondary Metabolites: Potential as Future Drugs for Health Care
Published in Hafiz Ansar Rasul Suleria, Megh R. Goyal, Health Benefits of Secondary Phytocompounds from Plant and Marine Sources, 2021
Syed Shams Ul Hassan, Hui-Zi Jin, Abdur Rauf, Saud Bawazeer, Hafiz Ansar Rasul Suleria
Three isocoumarins (penicillisocoumarin A (image 87 in Figure 8.7), penicillisocoumarin B (image 88 in Figure 8.7) and penicillisocoumarin D (image 89 in Figure 8.7)) were examined for their cytotoxic and antibacterial activities. However, all these three compounds only exhibited potent antibacterial activity against E. coli with MIC value of 32 μg/ml [45].
Affinity Labeling
Published in Roger L. Lundblad, Chemical Reagents for Protein Modification, 2020
Suicide inhibitors of enzymes30,31 can be considered a class of affinity labeling reagents.4 In general, however, these reagents are used more frequently as probes of enzyme mechanisms rather than for the site-specific modification of proteins. Some recent elegant examples of this approach include the studies on isocoumarin derivatives by Powers and co-workers32 and substituted benzoxaxinones by Abeles and co-workers.33 In the former study,32 3,4-dichloroisocoumarin was found to be an effective inhibitor of serine proteases such as human leukocyte elastase and chymotrypsin but had no effect on a related sulfydryl protease such as papain. Isocoumarin alone had no effect and the 3-chloroisocoumarin was much less effective. In the latter study, the catalysis-dependent inactivation of chymotrypsin with the formation of an ortho-substituted benzoyl-chymotrypsin. This inactive derivative slowly reactivates with the release of benzoyleneurea.
Catalog of Herbs
Published in James A. Duke, Handbook of Medicinal Herbs, 2018
Herb contains about 0.3% essential oil composed of methyl chavicol (60 to 70%) and some p-methoxycinnamic aldehyde, a bitter substance. The following are reported in tarragon oil: alpha-pinene, beta-pinene, camphene, limonene, cis-ocimene, trans-ocimene, methyl chavicol, p-methoxy cinnamaldehyde, delta-4-carene, alpha-phellandrene, and linalool. The oil contains limonene, cis- and trans- oeimene, cis- and trans-alloocimene, linalool, butyric acid, methyl chavicol (major constituent), geraniol, 1,2-dimethoxy-4-allyl benzene, and eugenol. Recently the isocoumarin artemedinol has been discovered. Tarragon herbage contains rutin, which was first isolated from rue and is best known for its ability to decrease capillary permeability and fragility. It is also said to be a cancer-preventative, i.e., inhibiting tumor formation on mouse skin by the carcinogen benzopyrene, and protective against irradiation damage. Rutin is also useful to counteract edema, atherogenesis, thrombogenesis, inflammation, spasms, and hypertension. It was once official in the U.S. for arteriosclerosis, hypertension, diabetes, and allergic manifestations. It is suggested that it may be useful for stroke prevention.29
Isocoumarins: a new class of selective carbonic anhydrase IX and XII inhibitors
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2022
Mehmet Onyılmaz, Murat Koca, Alessandro Bonardi, Mustafa Degirmenci, Claudiu T. Supuran
The structurally diverse isocoumarin derivatives X(1–20) were synthesised according to the general synthetic route shown in Scheme 1. 3-Acetylisocoumarin-substituted compounds B were synthesised as previously described by some of us15. The hydrazone derivatives X(1–5) were obtained by reacting B with substituted hydrazines16. The aldehydes X(6–10) were synthesised in high yields by using the Vilsmeier-Haack procedure17. These aldehydes were condensed with barbituric acid/2-thiobarbituric acid under acid condition at reflux to produce the final derivatives X(10–20). The chemical structures of the novel isocoumarin-substituted derivatives reported here were confirmed by analytical and spectral data (see Materials and methods for details).
The role of kallikreins in inflammatory skin disorders and their potential as therapeutic targets
Published in Critical Reviews in Clinical Laboratory Sciences, 2021
Caitlin T. Di Paolo, Eleftherios P. Diamandis, Ioannis Prassas
Naturally derived compounds have also been identified as KLK inhibitors. Isocoumarins, which are a class of natural polyphenolic compounds, display inhibitor effects toward KLK5 and KLK7 [157]. Based on this finding, isomannide rigid scaffolds were used to devise isomannide-based peptidomimetic derivatives that improved inhibition constant (Ki) values to the submicromolar range for KLK5 [158,159]. More recently, another plant polyphenol called Brazilin was also identified with comparable Ki values to what was initially reported with the original isocoumarin compounds [160]. Fukugetin is a natural plant flavanone-flavone biflavonoid compound that also displays inhibitory activity toward the KLKs, but is unique in that it presents a mixed-type mechanism of inhibition that makes it useful for the development of an exosite-type inhibitor [161]. It is capable of binding both the free enzyme and the enzyme–substrate complex with two different affinity constants. Small natural plant-extracts called terterpenoids were also found to be selective toward only the trypsin-like KLKs [162]. 3-Acyltetramic acids are naturally occurring metabolites of terrestrial and marine organisms that exhibit a variety of biological properties such as antibacterial, antiviral, antifungal, and antihumoral activities [163]. They were found to be novel inhibitors of KLK5 and KLK7, with the nature and length of the acyl chain being crucial to the KLK5, KLK7, and trypsin inhibition activities [163].