Bioavailability Of Active Components Research Articles

Therapeutic implications of flaxseed peptides and bioactive components against various diseases

Flaxseed (Linum usitatissimum L.) is nutritionally loaded with alpha-linolenic acid, lignans, Secoisolariciresinol diglucoside, soluble fiber, proteins, and bioactive peptides that implicate numerous therapeutic and health-boosting effects. The current review article aimed to comprehensively summarize the essential components of flaxseed along with their therapeutic role against different physiological disorders. Flaxseed is used in different forms including oil, powder, extract and whole seed where polyunsaturated fatty acids such as alpha-linolenic acid are significantly abundant in flaxseed oil. Most of the fiber in flaxseed comes from the hull, which contains 9 % insoluble fiber and 20 % soluble fiber. Soluble fibers contain neutral glucose and acidic polysaccharides, while insoluble fibers consist of lignin, cellulose, and acid detergent fiber. Bioactive peptides present in flaxseeds have gained acceptance as health-promoting medicines due to their useful amino acid profile. Studies revealed that flaxseed is rich in 40 % protein and bioactive peptides which are made up of 20 amino acids and two (dipeptides) residues with a molecular mass of 0.4–2 kDa. Enzymatic hydrolysis is a successful process for producing and releasing bioactive peptides which are obtained from the wastes of flaxseed oil after extraction. Peptide fractions (1 kDa) obtained after ultrafiltration of alcalde-hydrolyzed flaxseed are used in various applications, including as a food source and nutraceutical. Flaxseed has become a well-acknowledged functional food due to its physiological properties, such as anti-diabetic, antibacterial, angiotensin-converting enzyme inhibition, and antioxidant capacity owing to the presence of peptides, SDG, lignin, ALA and fiber. In addition, these bioactive fractions of flaxseed in various forms tend to reduce and prevent arthritis, hyperlipidaemias, cardiovascular diseases, osteoporosis, neurological disorders, and cancers of many types. Hence, flaxseed is evident to be a versatile functional food that elicits several physiological disorders and ailments due to its mechanically active compounds. Further research is required about the bioavailability of active components and their broad spectrum application in humans for health promotion and disease prevention.

Optimization of green extraction process with natural deep eutectic solvent and comparative in vivo pharmacokinetics of bioactive compounds from Astragalus-Safflower pair

IntroductionNatural deep eutectic solvents (NaDESs) are promising not only in componential extraction, but also in drug delivery system due to their green and safe features. In this work, NaDESs were applied to extract bioactive components from Astragalus-Safflower pair, a classic traditional Chinese medicine combination. Furthermore, ready-to-use crude extracts were administrated to SD rats. MethodsTotal 9 NaDESs composed of food grade ingredients were screened for the extraction of representative 9 components (hydroxysafflor yellow A, anhydrosafflor yellow B, eleutheroside B, calycosin-7-O-glucoside, kaempferol-3-O-rutinoside, ononin, calycosin, astraganoside, and carthamin) from Astragalus-Safflower pair. Afterwards, genetic artificial neural network (GNN) was adopted for optimizing the ultrasound-assisted extraction process. After SD rats were orally administrated with the ready-to-use crude extracts extracted under the optimized conditions, the in vivo pharmacokinetic characteristics of 5 components were evaluated comprehensively from weight, gender, solvent and modeling surgery, under a well-established UPLC-MS/MS method. ResultsBetaine-Lactic acid (Bet-Lac) was eventually determined as the optimal extraction solvent for subsequent experiments. The optimal ultrasound assisted extraction process was as follows: 90 min of extraction time, 65 °C of temperature, 80% of Bet-Lac content and 50 mg/ml of solid-liquid ratio. Bet-Lac enhanced to varying degrees the bioavailability of analytes in normal and cerebral ischemia/reperfusion injured (CI/RI) rats in contrast with corresponding rats administrated with water extract groups (p < 0.05). Besides, the bioavailability of active components in CI/RI rat plasma was significantly lower than that in normal rats (p < 0.05), indicating pathological damage of CI/R had a significant impact on pharmacokinetic profile of compounds in rats. However, gender and body weight had no significant effects on the pharmacokinetic profile of bioactive components. ConclusionsNaDESs exhibited higher extraction efficiency than conventional solvents. And GNN is reliable to optimize the ultrasound assisted extraction process. This study supported the potential of non-toxic NaDESs as solvents for extraction process and drug delivery systems at the same time.

Review on drug delivery system for phytomedicine through mechanism of encapsulation

Natural products have limitation in the bioavailability of active components because of numbers of reasons which includes poor solubility of the ingredient, poor stability due to gastric and colonic acidity, poor metabolism by the effect of gut microflora, poor absorption across the intestinal wall, poor active efflux mechanism and first-pass metabolic effects these factors make the failure of clinical trials and efficacy of natural phytochemicals used for human consumption both in cell culture and preclinical animal model systems is distinctly addressed by various researchers. Over the past decades, extraordinary advances have been made successfully on the development of novel drug delivery systems for encapsulation of plant active metabolites including organic, inorganic and hybrid nanoparticles .Various nanosystems and advanced biotechnology systems have been introduced to improve the therapeutic efficacy, safety and market appeal of nutraceuticals and phytochemicals, including liposomes, polymeric micelles, nanoparticles, and phytosomes. The advanced formulas are confirmed to have extraordinary benefits over conventional and previously used systems in the manner of solubility, bioavailability, toxicity, pharmacological activity, stability, distribution, sustained delivery, and both physical and chemical degradation.

Comparison with Pharmacokinetic Characteristics of Aconitines after Compatibility with Fuzi and Ginseng

The herb-pair Gingseng-Fuzi (the root of Aconitum carmichaelii ) is named as Shenfu prescriptions and is popular in traditional Chinese medicine for treatment of heart failure, and even shock with severe-stage COVID-19. However, a narrow therapeutic window of Fuzi may cause significant regional loss of property and life in clinics. Therefore, systemic elucidation of compatibility mechanism using in vivo comparative exposure is particularly crucial to improve the safety dose window of Shenfu prescriptions. A high performance liquid chromatography-mass spectrometry method was developed for quantification of 11 aconitines in SD rat plasma within 9 min, and a systemic comparison with their pharmacokinetic characteristics after oral administration of a safe dosage of 2 g/Kg of Fuzi and Ginseng-Fuzi decoction for 24 h was conducted. Nine representative diester, monoester, and non-ester aconitines and two new active components ( e . g . songorine and indaconitine) were all adopted to elucidation of the differences of the contents in decoction and the pharmacokinetic parameters in vivo , including the terminal elimination half-life (T1/2), area under the concentration-time curve, mean residence time, time to achieve maximum concentration (Cmax), and maximum plasma concentration. It was found that the compatibility with Fuzi and gingseng could significantly increase their bioavailability of active components. Moreover, the in vivo exposure and the T1/2 of diester aconitines (aconitine and mesaconitine) and the monoester aconitines (benzoylaconitine, benzoylmesaconitine, and benzoylhypaconitine) were all increased significantly, indicating the efficacy was increased simultaneously. Songorine shown the largest Cmax with a potential decardiotoxicity ability. This study provided a solid pharmacokinetic parameters for development of safe and effective new Shenfu oral prescriptions.

Phospholipids: a novel adjuvant in herbal drug delivery systems.

Phytoconstituents have been used extensively in modern science because of their various pharmacological actions with few side effects. Regardless of their excellent therapeutic activity, several phytoconstituents have shown poor bioavailability in vivo. Phytoconstituents possess properties such as poor lipid solubility, large molecular size, and degradation in the gut due to the acidic environment. Gastric enzymes always limit their use. Phospholipids seem to be a major carrier for plant active molecules, which not only interact with the plant constituents on a molecular level but also protect the active components of the plant from degradation and increase the bioavailability of the active components by imparting lipid solubility to them. Complexation techniques enable researchers to convert the phytophospholipids into various dosage forms, including tablets and capsules. In the cosmetic industry, however, these complexes have acquired wider applicability in the form of gels and emulsions. Complexation of phospholipids with active components of plants improves their bioavailability and is being extensively studied by researchers, and further research in this regard is expected in the future. This review highlights the unique property of phospholipids in drug delivery, their health benefits, and their use in the herbal medicine systems to improve the bioavailability of active herbal components.

Effects of Tea Consumption on Nutrition and Health

Beneficial health effects of tea have been demonstrated in animal experiments and some human studies. The two most extensively investigated diseases are cancer and heart disease. Although mechanisms of protective activity of tea against these diseases have been proposed, there are inconsistencies in the relationship between tea consumption and the risk of these diseases in humans. The bioavailability of active components is beginning to be understood, but further research is required to determine whether the results from animal studies are applicable to humans. Also discussed are the possible effects of tea in increasing thermogenesis and bone density as well as decreasing risk of cataracts and arthritis. The potential health benefits of tea consumption warrant further investigation.