槲皮素:一种增压的抗炎、抗病毒、抗衰老药物等

 

 

 

 

 

什么是槲皮素?

 

槲皮素这个名字来自拉丁语“Quercetum”,意思是橡树林,属于人体不能产生的黄酮醇类。(资源)

 

槲皮素被认为是用于治疗代谢和炎症性疾病的最广泛使用的生物类黄酮之一,但是其水溶性差、化学不稳定性和口服生物利用度低显着限制了其应用。  (资源)

 

 

 

强效抗炎、抗病毒和抗衰老

 

槲皮素是一种强大的免疫调节剂,可增强免疫功能并中和体内的自由基以支持缓和的炎症反应。

 

它具有作为抗炎剂直接作用于细胞的独特能力,并具有在体内和体外证实的与预防心血管疾病一致的特性。  (资源)

 

“槲皮素具有很强的抗氧化、抗炎、免疫调节和抗病毒特性,它的特点是在动物和人类中都具有非常高的安全性。” (资源)

 

然而,槲皮素的生物利用度极低,其吸收会受到大量营养素的影响。  (资源)

 

 

 


 

吸收受到水不溶性的严重限制

 

在人体(例如,口腔、小肠、肝脏、肾脏)中消化的槲皮素会发生葡萄糖醛酸化、硫酸化或甲基化。

 

就其本身而言,槲皮素的有限吸收会抑制它穿透细胞膜进入细胞内部。  (资源)

 

“槲皮素由于其基本的化学结构,显示出显着的抗氧化活性,这可能有助于它通过建立共振稳定的苯氧基自由基来减少自由基。

 

槲皮素在胃肠道的吸收率低,在生物药剂学分类系统下,它被归类为 IV 类化合物(低溶解度、低渗透性)。

 

据信,结晶槲皮素作为纯物质的低生物利用度是其在消化道中的低溶解度的结果。

 

此外,槲皮素的生物利用度会受到食物的影响。  (资源)

 

为了克服这些问题,对槲皮素进行纳米封装可以显着提高其稳定性、功效和生物利用度。”  (资源)

 

 

 


 

脂质体槲皮素增加口服吸收 20 倍

 

 

 

 

 

To overcome this limitation, scientists developed liposomal quercetin to investigate its distribution in vivo.

 

Liposomes chauffeur active ingredients into the body via the gut and into your cells to be used.

 

A study published in June, 2021 showed promising results for liposomal quercetin for boosting immunity.

 

Quercetin in a delivery-food grade system with sunflower phospholipids increases its oral absorption up to 20-fold.”  (Source)

 

Liposomes can act as a suitable vesicle to enhance the solubility of hydrophobic bioactive compounds by encapsulating the compounds within the membrane bilayers.

 


 

Liposomal Quercetin provides sustained release

 

In vitro release experiments showed that the release rate of liposomal quercetin is much slower than that of free quercetin, and achieves a sustained release effect and improves the medicinal value of quercetin.  (Source)

 

“Based on in vitro characteristic results, we concluded that this nano-formulation was a stable nanoparticulate system with high quercetin loading.

After nano-encapsulation, compared with quercetin alone, much strong inhibition capabilities.”

 

 

 

 

 

This study found Liposomal Quercetin greatly suppressed the growth of solid tumors in mice and was much more effective than non-liposomal quercetin.

 

Researchers believe the increased effectiveness was due to increased bioavailability to cells.

 

The chart at right shows Liposomal Quercetin (Q-PEGL) was available in the plasma for 24 hours, vs 2 hours for standard Quercetin (FQ).

 

This is because Liposomes are composed of the same material as the cell membrane, so is not seen as a foriegn substance to be filtered out by the liver.

 

Our data indicated that peglyated liposomal quercetin can significantly improve the solubility and bioavailability of quercetin and can be a potential application in the treatment of tumor.” (Source)

 

Liposomes merge with cell membrane to deliver ingredients

 

 

 

 

 

Quercetin-loaded liposomes are able to penetrate the cell membrane bilayer, allowing the pure quercetin to be effectively ushered into the gut for ease of absorption.  (Source)

 


 

Liposomal Quercetin Promotes Immune Resilience

 

A 2021 study shows liposomal quercetin is an effective agent in combination with standard care, when used in early stage of viral infection. (Source)

 

Quercetin contributes to immune resilience through a few different pathways.  It has antiviral and anti-inflammatory properties to support the natural immune response.  (Source)

 


 

Quercetin Liposomes Have Very High Safety Profile

 

“Quercetin has strong antioxidant, anti-inflammatory, immunomodulatory, and antiviral properties, and it is characterized by a very high safety profile, exerted in animals and in humans.”  (Source)

 

 

 

 

 

Quercetin May Lower Inflammatory Biomarkers

 

Flavonoid quercetin is a semi-lipophilic molecule that is of great interest to researchers due to its nutritional value. This compound has been shown, in vitro, to be a strong antioxidant and is one of the most powerful scavengers of reactive oxygen species. The free radical-scavenging effect of quercetin is based on its ability to donate a proton.

 

Quercetin has been shown to reduce inflammatory pain via the inhibition of oxidative stress and cytokine production.  (Source)

 

One study published in the European Journal of Clinical Nutrition found that supplementing with quercetin helped lower levels of the inflammatory biomarker C-reactive protein (CRP).  (Source)

 

“Our findings showed a significant effect of quercetin supplementation on the C-reactive protein-especially at doses above 500 mg/day.”

 

Quercetin as a Natural Allergy Relief

 

 

 

 

 

Quercetin’s best-known mechanism of action involves its ability to stabilize mast cell membranes, which decreases the release of histamine into the cells—an inflammatory chemical involved in allergic symptoms such as sneezing and itching.  

 

In this way it provides nutritional support for individuals who occasionally suffer from allergies.

 

Quercetin has the unique ability to help block histamine release, the main trigger for respiratory and sinus health issues. (Source)

 

That’s why it’s a very popular phytonutrient for promoting respiratory health and sinus comfort.

 

“In conclusion, our results indicate that quercetin is more effective than cromolyn in inhibiting release of pro-inflammatory cytokines from human mast cells.”  (Source)

 


 

Quercetin Supports Optimal Blood Pressure and Cardiovascular Health

 

Quercetin also has impressive cardiovascular benefits: One meta‐analysis of randomized controlled trials found that supplementing with the plant powerhouse could help stabilize blood pressure.  (Source)

 

In a study done by Greek cardiologists on thirty men who already had coronary heart disease (CHD) on the consumption of red grape polyphenol extract rich in quercetin caused an increase in flow-mediated dilation of major arteries, a potent indicator of improved endothelial health. (Source)

 


 

Quercetin May Strengthen Blood Vessels

 

Quercetin may improve blood vessel cell health and blood flow through arteries in people with heart disease.  (Source)

 

According to a study by the American Heart and Stroke Association, taking quercetin supplements could be an effective way to reduce blood pressure.   (Source)

 

Other research showed that people who were overweight and took a quercetin supplement of 150 milligrams daily had lower levels of harmful cholesterol in their blood, as well as reduced systolic blood pressure, which measures the pressure in the blood vessels during a heartbeat.  (Source)

 


 

References

 

Endogenous and Exogenous Mediators of Quercetin Bioavailability

 

Towards an Understanding of the Low Bioavailability of Quercetin:  A Study of Its Interaction with Intestinal Lipids

 

Quercetin Reduces Systolic Blood Pressure and Plasma Oxidized Low-Density Lipoprotein Concentrations in Overweight Subjects with a High-Cardiovascular Disease Risk Phenotype:  A Double-blinded, Placebo-Controlled Cross-over Study

 

Quercetin Is More Effective than Cromolyn in Blocking Human Mast Cell Cytokine Release and Inhibits Contact Dermatitis and Photosensitivity in Humans

 

Overviews of Biological Importance of Quercetin: A Bioactive Flavonoid

 

Liposomal Quercetin Efficiently Suppresses Growth of Solid Tumors in Murine Models

 

Improved Therapeutic Efficacy of Quercetin-Loaded Polymeric Nanoparticles

 

Polyphenolic Compounds from Red Grapes Acutely Improve Endothelial Function in Patients with Coronary Heart Disease.

 

Review of the Biology of Quercetin and Related Bioflavonoids

 

Quercetin and Endurance Exercise Capacity

 

The Effects of Quercetin Supplementation on Body Composition, Exercise Performance and Muscle Damage in Athletes

 

Liposomes as Advanced Delivery Systems for Nutraceuticals

 

Effects of Quercetin on Blood Pressure: A Systematic Review and Meta‐Analysis of Randomized Controlled Trials

 

Quercetin, Inflammation and Immunity

 

Impact of Quercetin Encapsulation with Added Phytosterols on Bilayer Membrane and Photothermal-Alteration of Novel Mixed Soy Lecithin-Based Liposome

 

Quercetin-Loaded Nanomedicine as Nutritional Application

 

 

 

 

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LIPOSOMAL POWDER QUERCETIN CAPSULES