Significantly, much of the activity of Citrus flavonoids appears to impact blood and microvascular endothelial cells, and it is not surprising that the two main areas of research on the biological actions of Citrus flavonoids have been inflammation and cancer. Epidemiological and animal studies point to a possible protective effect of flavonoids against cardiovascular diseases and some types of cancer. Although flavonoids have been studied for about 50 years, the cellular mechanisms involved in their biological action are still not completely known. Many of the pharmacological properties of Citrus flavonoids can be linked to the abilities of these compounds to inhibit enzymes involved in cell activation. Attempts to control cancer involve a variety of means, including the use of suppressing, blocking, and transforming agents. Suppressing agents prevent the formation of new cancers from procarcinogens, and blocking agents prevent carcinogenic compounds from reaching critical initiation sites, while transformation agents act to facilitate the metabolism of carcinogenic components into less toxic materials or prevent their biological actions. Flavonoids can act as all three types of agent. Many epidemiological studies have shown that regular flavonoid intake is associated with a reduced risk of cardiovascular diseases. In coronary heart disease, the protective effects of flavonoids include mainly antithrombotic, anti-ischemic, anti-oxidant, and vasorelaxant. It is suggested that flavonoids decrease the risk of coronary heart disease by three major actions: improving coronary vasodilatation, decreasing the ability of platelets in the blood to clot, and preventing low-density lipoproteins (LDLs) from oxidizing. The anti-inflammatory properties of the Citrus flavonoids have also been studied. Several key studies have shown that the anti-inflammatory properties of Citrus flavonoids are due to its inhibition of the synthesis and biological activities of different pro-inflammatory mediators, mainly the arachidonic acid derivatives, prostaglandins E 2, F 2, and thromboxane A 2. The anti-oxidant and anti-inflammatory properties of Citrus flavonoids can play a key role in their activity against several degenerative diseases and particularly brain diseases. The most abundant Citrus flavonoids are flavanones, such as hesperidin, naringin, or neohesperidin. However, generally, the flavones, such as diosmin, apigenin, or luteolin, exhibit higher biological activity, even though they occur in much lower concentrations. Diosmin and rutin have a demonstrated activity as a venotonic agent and are present in several pharmaceutical products. Apigenin and their glucosides have been shown a good anti-inflammatory activity without the side effects of other anti-inflammatory products. In this paper, we discuss the relation between each structural factor of Citrus flavonoids and the anticancer, anti-inflammatory, and cardiovascular protection activity of Citrus flavonoids and their role in degenerative diseases.
Flavonoids are a widely distributed group of polyphenolic compounds with health-related properties, which are based in their antioxidant activity. These properties have been found to include anticancer, antiviral, antiinflammatory activities, effects on capillary fragility, and an ability to inhibit human platelet aggregation. The antioxidant capacity of any flavonoid will be determined by a combination of the O-dihydroxy structure in the B-ring, the 2,3-double bond in conjugation with a 4-oxo function and the presence of both hydroxyl groups in positions 3 and 5. Flavanones, flavones, and flavonols are the flavonoids present in Citrus, and although flavones and flavonols have been found in low concentrations in Citrus tissues, in relationship to flavanones, these types of compounds have been show to be powerful antioxidants and free radical scavengers. Some Citrus flavonoids can be used directly as repellents or toxins or be used in plant improvement programs to obtain more resistant crops. In addition, some Citrus flavonoids and their derivates, in the field of food technology, are principally known for their ability to provide a bitter or sweet taste and as bitterness inhibitor. Keywords: Free radicals, antioxidant; anticarcinogenic; antiinflammatory; platelet aggregation; antiallergic; analgesic; antimicrobial; food additives
Previous studies have demonstrated that certain flavonoids can have an inhibitory effect on angiotensin-converting enzyme (ACE) activity, which plays a key role in the regulation of arterial blood pressure. In the present study, 17 flavonoids belonging to five structural subtypes were evaluated in vitro for their ability to inhibit ACE in order to establish the structural basis of their bioactivity. The ACE inhibitory (ACEI) activity of these 17 flavonoids was determined by fluorimetric method at two concentrations (500 µM and 100 µM). Their inhibitory potencies ranged from 17 to 95% at 500 µM and from 0 to 57% at 100 µM. In both cases, the highest ACEI activity was obtained for luteolin. Following the determination of ACEI activity, the flavonoids with higher ACEI activity (i.e., ACEI >60% at 500 µM) were selected for further IC50 determination. The IC50 values for luteolin, quercetin, rutin, kaempferol, rhoifolin and apigenin K were 23, 43, 64, 178, 183 and 196 µM, respectively. Our results suggest that flavonoids are an excellent source of functional antihypertensive products. Furthermore, our structure-activity relationship studies show that the combination of sub-structures on the flavonoid skeleton that increase ACEI activity is made up of the following elements: (a) the catechol group in the B-ring, (b) the double bond between C2 and C3 at the C-ring, and (c) the cetone group in C4 at the C-ring. Protein-ligand docking studies are used to understand the molecular basis for these results.
Nowadays, there is an interest in the consumption of food without synthetic additives and rather with the use of natural preservatives. In this regard, natural extracts of the Lamiaceae family, such as rosemary, have been studied because of its bioactive properties. Several studies have reported that rosemary extracts show biological bioactivities such as hepatoprotective, antifungal, insecticide, antioxidant and antibacterial. It is well known that the biological properties in rosemary are mainly due to phenolic compounds. However, it is essential to take into account that these biological properties depend on different aspects. Their use in foods is limited because of their odour, colour and taste. For that reason, commercial methods have been developed for the preparation of odourless and colourless antioxidant compounds from rosemary. Owing to the new applications of natural extracts in preservatives, this review gives a view on the use of natural extract from rosemary in foods and its effect on preservative activities. Specifically, the relationship between the structure and activity (antimicrobial and antioxidant) of the active components in rosemary are being reviewed.
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