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Pharmacological Treatment of Lymph Stasis
Published in Waldemar L. Olszewski, Lymph Stasis: Pathophysiology, Diagnosis and Treatment, 2019
The benzopyrones represent a very effective pharmacological means of treating acute and chronic forms of high protein edema including primary and secondary forms of lymphedema. Their effectiveness is not only related to the dose but also to the type of benzopyrone used. The most efficacious benzopyrone investigated to date has been coumarin administered as 200 mg/d. Under such a regimen a patient with a long-standing lymphostatic disorder can expect subjective improvements in bursting pains, tightness, tension, heaviness, and mobility of the extremity within 4 weeks. There will be a softening of the tissues (assessed by tonometry) which can be objectively measured within 8 weeks and a reduction in the circumference and volume of edema fluid of the limb within 6 months. All of these mean a better quality of survival for the patient. For patients with acute lymphostatic disorders through thermal wounding, traumatic damage, or surgical intervention, there can be a reduction in the amount of edema fluid accumulation and associated pain. While the necessary detailed clinical trials have not been pursued, experimental work indicates the benzopyrones to be very useful prophylactically when surgical intervention of any type is anticipated.
Interstitium and Lymphatics
Published in John H. Barker, Gary L. Anderson, Michael D. Menger, Clinically Applied Microcirculation Research, 2019
Tissue proteolysis, while not strictly speaking part of the microcirculation, is intimately related to it. A number of cells in the tissues lyse proteins, e.g., macrophages, basal epithelial cells, fibroblasts, etc.9,25 The macrophages in particular have a very important role in reducing chronic high-protein edemas by this mechanism. This is, of course, only their physiological role; in inflammation and other pathological conditions, they act both in an immunological way and in the lysis of excess proteins, dead cells, and bacteria, etc. These cells are normally very numerous in the tissues.13 Very approximate calculations5 indicated that macrophages may remove about 30% of the protein that reaches the tissues from the blood capillaries. However, a model implies their normal role may be much less than this (Table 5), while they have a considerable effect in limiting high-protein edemas.8 This activity can be much increased by the benzopyrone drugs.
Lower limb
Published in Tor Wo Chiu, Stone’s Plastic Surgery Facts, 2018
Benzopyrone (a class of drug originally used in patients with vascular disease, e.g. coumarin) can induce phagocytosis by binding to interstitial proteins, but clinical results have been mixed. Overuse with coumarin can cause hepatotoxicity; Paroven (an oxerutin) is supposedly less hepatotoxic. Daflon (a bioflavinoid) is similar, and a 500 mg twice daily dose has been shown to be more effective than placebo; but, in general, poor quality data prevent its recommendation (Badger C, Cochrane Database Syst, 2004).
A role for flavonoids in the prevention and/or treatment of cognitive dysfunction, learning, and memory deficits: a review of preclinical and clinical studies
Published in Nutritional Neuroscience, 2023
Matin Ramezani, Arman Zeinaddini Meymand, Fariba Khodagholi, Hamed Mohammadi Kamsorkh, Ehsan Asadi, Mitra Noori, Kimia Rahimian, Ali Saberi Shahrbabaki, Aisa Talebi, Hanieh Parsaiyan, Sepideh Shiravand, Niloufar Darbandi
Flavonoids as plant secondary metabolites are an important class of natural products extensively found in colorful fruits and vegetables. Flavonoids are of interest because of a broad spectrum of health-promoting effects which apply not only to the nutraceutical, pharmaceutical, and medicinal purposes but also to cosmetic applications. Their anti-oxidative, anti-inflammatory, anti-mutagenic and anti-carcinogenic features can modulate essential cellular enzyme functions. They are synthesized by plants and can be extracted from different parts. An abundant number of them are located in the nucleus of mesophyll cells. They have a defense mechanism against infections, stress, and pressure imposed on the plant and are classified as the low-molecular-weight phenolic compounds having a benzopyrone structure [10–12].
Assessment of Antihyperlipidemic and Antitumor Effect of Isolated Active Phytoconstituents from Apium graveolens L. through Bioassay-Guided Procedures
Published in Journal of Dietary Supplements, 2019
This article also deals with the isolation and characterization of coumarin derivatives. Coumarin is a fragrant organic chemical compound in the benzopyrone chemical class. Dietary exposure to benzopyrones is quite significant as these compounds are found in vegetables, fruits, seeds, nuts, coffee, tea, and wine. Coumarins are important compounds that contribute to the adaptation of plants to biotic or abiotic stresses. Coumarin and its derivatives are considered phenylpropanoids. Coumarins are reported to exhibit anticonvulsant (Luszczki, Andres-Mach, & Glensk, 2010), antihyperglycemic (Ramesh & Pugalendi, 2006), antimyotoxic (Toyama Dde, Diz Filho, & Cavada, 2011), antiinflammatory, and antiviral activities (Selim & Ouf, 2012).
Synthesis, computational studies and assessment of in vitro inhibitory activity of umbelliferon-based compounds against tumour-associated carbonic anhydrase isoforms IX and XII
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2020
Francesca Mancuso, Laura De Luca, Andrea Angeli, Sonia Del Prete, Clemente Capasso, Claudiu T. Supuran, Rosaria Gitto
Coumarin (2H-chromen-2-one 1, Figure 1) is classified as a member of a large class of phenolic chemotypes occurring in higher plants, bacteria and fungi. Apart from natural coumarins, a wide collection of (semi)synthetic coumarins are endowed by various pharmacological properties such as anticancer, anticoagulant, anti-inflammatory, and antimicrobial activities1. From a structural point of view, the coumarins are classified in different chemical classes (simple coumarins, fused polycyclic coumarins, phenylcoumarins, biscoumarins, and so on)1,2. The existence of an extensive library of coumarins from (semi)synthetic source has been triggered by the high versatility of benzo-α-pyrone system to be an excellent scaffold to perform structural modifications3–6. Moreover, the chemical diversity of the coumarin system implies that they might play an important role in medicinal chemistry for drug discovery processes, so that many coumarins are used currently in drug development as vitamin K antagonists, choleretic and antibacterial and antiviral agents7–11. It has been suggested that the benzopyrone structure enables its derivatives to readily interact with biological molecular targets through a network of non-covalent interactions such as hydrophobic, π–π stacking, and cation–π interactions as well as hydrogen and coordination bond interactions. Specifically, coumarin-based compounds interact with human carbonic anhydrases (CAs, EC 4.2.1.1), which possess significant esterase activity and induce the opening of lactone ring; due to the formation of the corresponding carboxylic derivative, non-classical CA inhibitory effects have been evidenced for coumarin-derived compounds (vide infra)12–14.