Ytterbium triflate hydrate catalyzed Michael addition and cyclocondensation of α,β-unsaturated ketones with active methylene compounds

Catalyzed by ytterbium（III） triflate hydrate [Yb（OTf）3.xH20], the Michael addition and cyclocondensation of α,β-unsaturated ketones with active methylene compounds to afford the 1,4-adducts and benzo[b]pyran derivatives, respectively were studied.

THE SECONDARY REACTION IN THE CONDENSATION OF 1-METHYL-2-METHYLTHIO-IMIDAZOLINE WITH ACTIVE METHYLENE COMPOUNDS

Mono-substituted heterocyclic ketene aminals are formed by the reaction of 1-methyl-2-methylthio-imidazoline with active methylene compounds containinq an acetyl or benzoyl group by the elimination of both a methylthio and an acyl group.This is resulted by the secondary reactio of the produced methanethiol to attack the more active carbonyl group.

Bioactive compounds in Hericium erinaceus and their biological properties:a review

Hericium erinaceus is a nutritious edible and medicinal fungi,rich in a variety of functional active ingredients,with various physiological functions such as antioxidation,anticancer,and enhancing immunity.It is also effective in protecting the digestive system and preventing neurodegenerative diseases.In this review paper,we summarize the sources,structures and efficacies of the main active components in H.erinaceus fruiting body,mycelium,and culture media,and update the latest research progress on their biological activities and the related molecular mechanisms.Based on this information,we provide detailed challenges in current research,industrialization and information on the active ingredients of H.erinaceus.Perspectives for future studies and new applications of H.erinaceus are proposed.

Nutritional Composition and Bioactive Compounds of Bael (Aegle marmelos) and Development of Functional Food Products

Aegle marmelos, widely known as bael, belongs to the Rutaceae family. It is one of the most inexpensive and appealing fruits, considered to be an essential source of natural antioxidants and bioactive components. The major purpose of the research study was to investigate the nutritional composition and bioactive constituents of bael pulp, as well as to develop new value-added products that maintain the maximum quantity of nutrients. The developed food products were subjected to evaluate sensory attributes according to a nine-point hedonic scale. It was found that the moisture, protein, fat, crude fiber, and total ash content of bael fruit pulp were 61.20%, 2.48%, 0.47%, 3.04%, and 1.29%, respectively. When compared to the catechin standard, the antioxidant activity of such extract indicated good antioxidant capacity, with an IC50 value of 75.68 μg/ml for methanol extract. Vitamin C content was about 10.21 mg/100g. Besides, total flavonoid and phenolic contents were found as 140 mg of Quercetin Equivalent (QE)/g and 106.65 mg of Gallic Acid Equivalent (GAE)/g, respectively. Results of sensory attributes revealed that there was a significant difference (P ba and bael bar. The overall acceptability of bael murabba (6.7) and bael bar (7.1) is acceptable in quality, but their specific characteristics were found slightly different by the test panelists. These products might be applicable for the treatment of several diseases like atherosclerosis, diabetes, constipation, irritable bowel syndrome, peptic ulcer, tumor, and osteoporosis.

Potential Benefits of Bioactive Compounds of Traditional Rice Grown in South and Southeast Asia:A Review

Traditional rice varieties have been widely cultivated and popularly consumed by Asian people for a very long time and have recently garnered increased consumer concern.Traditional or indigenous rice varieties are known to be rich in a wide range of bioactive compounds,particularly phenolic compounds,flavonoids,tannins,anthocyanins,proanthocyanidins,phytic acids,andγ-oryzanol.We have identified 32 phenolic acids,including hydroxycinnamic acid derivatives,and 7 different flavonoids in rice varieties.These bioactive compounds have unique physiological effects on human health.Additionally,rice grains exhibit nutraceutical potential for antidiabetic,antiarthritic,anti-inflammatory,antibacterial,and antitumor activities.In this review,we critically analyzed the bioactive components of traditional rice and their nutraceutical potential in protecting against harmful microbial activities.To ensure that future generations have access to these beneficial substances,it is crucial to preserve traditional rice varieties.

Comparative Analysis of the Photosynthetic Characteristics and Active Compounds of Semiliquidambar cathayensis Chang Heteromorphic Leaves

In the present study,the variation patterns of leaf shape in different populations of individual Semiliquidambar cathayensis plants were analyzed to investigate the relationship among leaf shape variation,photosynthetic properties,and active compounds to understand the genetic characteristics of S.cathayensis and screen elite germplasms.The leaf shape of 18 offspring from three natural S.cathayensis populations was analyzed to investigate the level of diversity and variation patterns of leaf shape.Furthermore,photosynthetic pigment content,physiological parameters of photosynthesis,and the active compounds in leaves of different shapes were determined.Statistical analysis showed that the leaf shape variation in S.cathayensis indicated a high level of genetic diversity among and within the populations.Cluster analysis showed that the three natural populations formed two clusters,one whose offspring was dominated by entire leaves and another characterized by palmately trifoliate leaves.The differences in photosynthetic characteristics and active compounds of leaves of three different shapes were comprehensively evaluated using principal component analysis.Two principal components with a cumulative contribution rate of 92.768%were extracted,of which the highest comprehensive score was for asymmetrically lobed leaves.The leaf shape in different S.cathayensis germplasms exhibited distinct patterns,and there were some correlations between the photosynthetic properties and active compounds in leaves of different shapes.Thus,the leaf shape can be used to predict active compound content,and in turn,select varieties based on that purpose;it also provides a simple and effective method to classify S.cathayensis germplasms.

Effects of different thermal processing methods on bioactive components,phenolic compounds,and antioxidant activities of Qingke(highland hull-less barley)

Qingke(highland hull-less barley)is a grain replete with substantial nutrients and bioactive ingredients.In this study,we evaluated the effects of boiling(BO),steaming(ST),microwave baking(MB),far-infrared baking(FB),steam explosion(SE),and deep frying(DF)on bioactive components,phenolic compounds,and antioxidant activities of Qingke compared with the effects of traditional roast(TR).Results showed that the soluble dietary fiber,beta-glucan and water-extractable pentosans of Qingke in dry heat processes of TR,SE,MB and FB had a higher content compared with other thermal methods and had a better antioxidant activity of hydroxyl radical scavenging and a better reduction capacity,while those in wet heat processes of BO and ST had a better antioxidant activity of ABTS radical scavenging and a better Fe^(2+) chelating ability.DF-and SE-Qingke had a higher content of tocopherol,phenolic,and flavonoid.Overall,6 free phenolic compounds and 12 bound phenolic compounds of Qingke were identified,and free phenolic compounds suffered more damage during thermal processing.Principal component analysis showed that SE had more advantages in retaining and improving the main biological active ingredients of Qingke,and it may be the best method for treating Qingke.

Protective mechanism of quercetin compounds against acrylamide-induced hepatotoxicity

Quercetin compounds have antioxidant,anti-inflammatory and anticancer pharmacological functions.Longterm exposure to acrylamide(AA)can cause liver injury and endanger human health.However,whether quercetin compounds can attenuate AA-induced liver injury and the specific mechanism are not clear.Here,we studied the mechanism and structure-activity relationship of quercetin compounds in reducing AA-induced hepatotoxicity in vivo and in vitro.In vivo studies found that quercetin-like compounds protect against AAinduced liver injury by reducing oxidative stress levels,activating the Akt/m TOR signaling pathway to attenuate autophagy,and improving mitochondrial apoptosis and endoplasmic reticulum stress-mediated apoptosis.In vitro studies found that quercetin compounds protected Hep G2 cells from AA by attenuating the activation of AA-induced autophagy,lowering reactive oxygen species(ROS)levels by exerting antioxidant effects and thus attenuating oxidative stress,increasing mitochondrial membrane potential(MMP),and improving apoptosis-related proteins,thus attenuating AA-induced apoptosis.Furthermore,the conformational differences between quercetin compounds correlated with their protective capacity against AA-induced hepatotoxicity,with quercetin showing the best protective capacity due to its strongest antioxidant activity.In conclusion,quercetin compounds can protect against AA-induced liver injury through multiple pathways of oxidative stress,autophagy and apoptosis,and their protective capacity correlates with antioxidant activity.

Screening for Antioxidant Phenolic Compounds from Polygonum capitatum

[Objectives]To discover antioxidant natural products from the famous Hmong medicinal plant Polygonum capitatum.[Methods]The antioxidant activities of the isolated components were evaluated by ABTS and DPPH assays.[Results]A total of 27 free phenolics were isolated form P.capitatum.Then the in vitro antioxidant potential of these components was evaluated according to the DPPH and ABTS radical scavenging assays.Among them,five compounds(13,14,17,23,and 25)showed most significant ABTS radical-scavenging activity(IC 50 values of 3.81-15.09μg/mL).And 12 components(1,2,6,7,9,12,13,14,16,17,23,and 25)showed notable radical scavenging activity against DPPH(inhibition rates>88%).[Conclusions]Most of the above bioactive compounds were reported for the first time.

Evaluation of Anti-Wrinkle, Relieving Effect and Safety of A Group of Hexapeptide Compounds

The anti-wrinkle,relieving effect and safety of a group of hexapeptide compounds(HCs)were evaluated by in vitro antioxidant test,hyaluronidase inhibition test and human clinical test.The results showed that HCs possess+high overall antioxidant activity,and the scavenging activity of ABTS•radical and DPPH radical by 4 mg/mL HCs solution were(92.23±1.15)%and(90.24±1.25)%.The scavenging activity of PTIO radical by 80 mg/mL HCs solution was(80.29±2.41)%.The inhibition rate of 80 mg/mL HCs on hyaluronidase was(75.00±6.13)%.The test of clinical results showed that the HCs have good anti-wrinkle and relieving effect,and no case of grade 1 or above skin adverse reactions occurred,indicating that HCs have good safety.

Bioactive Compounds and Insecticidal Activity of Hysterionica pinifolia, a Native South American Plant

Phytochemical investigation of the purified fractions of the active dichloromethane extract of Hysterionica pinifolia (Poir.) Baker led to the identification of five compounds. New acetylenic alcohol (E)-undec-3-en-5,7-diyne-1-ol (1) and three other compounds (3), (4), and (5) were reported for the first time in this species. Furthermore, forty-six components from the volatile fraction of H. pinifolia were identified. These compounds were elucidated using 1D and 2D NMR spectroscopy as well as MS-ESI and GC-FID-MS experiments. The dichloromethane extract, its fractions, and the methanolic extract were tested for insecticidal activity against Tribolium castaneum under laboratory conditions. The dichloromethane extract and the fraction F2 were found to be active, showing high larval mortality. The dichloromethane extract was also active against T. castaneum adults. The results have shown that H. pinifolia could be considered, in a near future, as a potential source for the development of a botanical insecticide for pest control.

Lipase-catalyzed Knoevenagel condensation between α,β-unsaturated aldehydes and active methylene compounds

A simple and efficient Knoevenagel condensation between a b-unsaturated aldehydes and active methylene compounds is reported.Notably,this condensation can be catalyzed by PPL（lipase from porcine pancreas） with satisfied yields（49%–92%）.Moreover,PPL induces moderate Z/E selectivity in the Knoevenagel condensation.

Bioactive compounds of sea cucumbers and their therapeutic effects

Abstract Sea cucumbers belong to the Class Holothuroidea of marine invertebrates. They are commercially valuable and prized as a food and folk medicine in Asia. Nutritionally, sea cucumbers have an impressive profile of valuable nutrients such as vitamins, minerals and amino acids. A number of unique biological and pharmacological activities/properties, including anticancer, anticoagulant/antithrombotic, antimicrobial, antioxidant, antihyperlipidemic, antihyperglycemic, anti-inflammatory, antihypertension and radioprotective, have been ascribed to various compounds isolated from sea cucumbers. The therapeutic properties and medicinal benefits of sea cucumbers can be linked to the presence of a wide array ofbioactives, especially triterpene glycosides, acid mucopolysaccharide, sphingoid bases, glycolipids, fucosylated chondroitin sulfate, polysaccharides, phospholipids, cerebrosides, phosphatidylcholines, and other extracts and hydrolysates. This review highlights the valuable bioactive components as well as the multiple therapeutic properties of sea cucumbers with a view to exploring their potential uses as functional foods and a natural source of new multifunctional drugs.

The Condensation of Aromatic Aldehydes with Acidic Methylene Compounds in Water

The condensation of aromatic aldehydes with acidic methylene compounds such as malononitrile, methyl cyanoacetate, cyanoacetamide, 5,5-dimethyl-1,3-cyclohexanedione, bartbituric acid and 2-thiobarbituric acid proceeded very efficiently in water in the presence of triethylbenzylammonium chloride (TEBA) and the products were isolated simply by filtration.

Degradation of Organic Compounds by Active Species Sprayed in a Dielectric Barrier Corona Discharge System

Investigation was made into the degradation of organic compounds by a dielectric barrier corona discharge （DBCD） system. The DBCD, consisting of a quartz tube, a concentric high voltage electrode and a net wrapped to the external wall （used as ground electrode）, was introduced to generate active species which were sprayed into the organic solution through an aerator fixed on the bottom of the tube. The effect of four factors-the discharge voltage, gas flow rate, solution conductivity, and pH of wastewater, on the degradation efficiency of phenol was assessed. The obtained results demonstrated that this process was an effective method for phenol degradation. The degradation rate was enhanced with the increase in power supplied. The degradation efficiency in alkaline conditions was higher than those in acid and neutral conditions. The optimal gas flow rate for phenol degradation in the system was 1.6 L/min, while the solution conductivity had little effect on the degradation.

Variation in Antioxidants, Bioactive Compounds and Antioxidant Capacity in Germinated and Ungerminated Grains of Ten Rice Cultivars

Present study was conducted to characterise ten rice(Oryza sativa L.) cultivars viz. IET-23466, Dhan-201, IET-23448, MAS-946, IET-23445, IET-23463, IET-23455, PR-123, PR-115 and IET-23449 based on antioxidants(total phenolics, flavonols and tannins), bioactive compounds(phytic acid, gamma amino butyric acid, tocopherol and reduced ascorbate) and antioxidant activity(1,1-diphenyl-2-picrylhydrazyl radical scavenging activity, hydroxyl radical scavenging activity, free radical antioxidant power and total reducing power) with an aim to identify cultivars containing higher health promoting components after germination. Three cultivars IET-23466, IET-23463 and PR-123 performed better as revealed by higher level of antioxidants, bioactive compounds and antioxidant activity before and after germination. Three cultivars MAS-946, IET-23445 and IET-23449 had moderate level of antioxidants, bioactive compounds and antioxidant activity. Four cultivars Dhan-201, IET-23448, IET-23455 and PR-115 performed intermediately. Strong positive correlation was observed among total phenolics and the antioxidant activity. Phytic acid was found to be negatively correlated to the antioxidant activity. Our results highlighted that cultivars IET-23466, IET-23463 and PR-123 hold great potential after germination and would open up a useful opportunity for the functional food industry, and consumption of these cultivars after germination would afford health benefits to consumers since they contain higher level of antioxidants.

Structural Features and Biological Activities of Bioactive Compounds from Fortunella margarita(Lour.) Swingle：A Review

Fortunella margarita（Lour.） Swingle, commonly known as kumquat, is the smallest citrus fruit. It thrives in southeastern China and is widely cultivated and consumed in the world due to its multiple health benefits. It has been used as an important herbal medicine in traditional Chinese medicine and also as one of the most popular fruits. There are various kinds of bioactive compounds in F. margarita, such as polysaccharides, limonoids, essential oils, flavonoids, phenolic acids, vitamins, dietary fiber, etc. In addition, many studies have reported that these bioactive compounds can be used as antioxidant, antimicrobial, hypolipidemic, drosophila lure components in functional foods, pharmaceuticals and daily chemical products due to their biological activities. This review focuses on the structural features and biological activities of polysaccharides, limonoids, essential oils and flavonoids and other bioactive substances from F. margarita and their potential applications in food, daily chemical and pharmaceutical industries.

African eggplant(Solanum anguivi Lam.)fruit with bioactive polyphenolic compounds exerts in vitro antioxidant properties and inhibits Ca^(2+)-induced mitochondrial swelling

Objective:To evaluate the antioxidant and radical scavenging activities of Solanum anguivi fruit(SAG)and its possible effect on mitochondrial permeability transition pore as well as mitochondrial membrane potential(△Ψ_m)isolated from rat liver.Methods:Antioxidant activity of SAG was assayed by using 2,2-diphenyl-1-picrylhydrazyl(DPPH),reducing power,iron chelation and ability to inhibit lipid peroxidation in both liver and brain homogenate of rats.Also,the effect of SAG on mitochondrial membrane potential and mitochondrial swelling were determined.Identification and quantification of bioactive polyphenolics was done by HPLC-DAD.Results:SAG exhibited potent and concentration dependent free radical-scavenging activity(IC_(50)/DPPH=275.03±7.8μg/mL).Reductive and iron chelation abilities also increase with increase in SAG concentration.SAG also inhibited peroxidation of cerebral and hepatic lipids subjected to iron oxidative assault.SAG protected against Ca^(2+)(110μmol/L)-induced mitochondrial swelling and maintained the△Ψ_m.HPLC analysis revealed the presence of gallic acid[(17.54±0.04)mg/g],chlorogenic acid(21.90±0.02 mg/g),caffeic acid(16.64±0.01 mg/g).rutin[(14.71±0.03)mg/g]and quercetin[(7.39±0.05)mg/g].Conclusions:These effects could be attributed to the bioactive polyphenolic compounds present in the extract.Our results suggest that SAG extract is a potential source of natural antioxidants that may be used not only in pharmaceutical and food industry but also in the treatment of diseases associated with oxidative stress.

Non-Nutritive Bioactive Compounds in Pulses and Their Impact on Human Health: An Overview

This review describes the non-nutritive biologically active components in grain legumes and discusses about the bioactivity of phenols, isoflavones, phytosterols, phytic acid, saponins, tannins, protease inhibitors and bioactive complex carbohydrates in different pulse grains. These bioactive components have wide ranging biological activities and conesquently many different targets and mechanism of action. The potential beneficial effect of these compounds especially their antioxidant properties and their role in the prevention of non-communicable chronic diseases such as coronary heart disease, stroke, cancer and diabetes has been discussed.

Antialgal and Antilarval Activities of Bioactive Compounds Extracted from the Marine Dinoflagellate Amphidinium carterae

Abstract With the global ban on the application of organotin-based marine coatings by the International Maritime Organization, the development of environmentally friendly, low-toxic and nontoxic antifouling compounds for marine industries has become an urgent need. Marine microorganisms have been considered as a potential source of natural antifoulants. In this study, the antifouling potential of marine dinoflagellate Amphidinium carterae, the toxic and red-tide microalgae, was investigated. We performed a series of operations to extract the bioactive substances from Amphidinium carterae and tested their antialgal and antilarval activities. The crude extract of Amphidinium carterae showed significant antialgal activity and the ECs0 value against Skeletonema costatum was 55.4 ~tg mL-1. After purification, the isolated bioactive substances （the organic extract C） exhibited much higher antialgal and antilar- val activities with ECso of 12.9μgmL-1 against Skeletonema costatum and LC50 of 15.1 μmL-1 against Amphibalanus amphitrite larvae. Subsequently, IR, Q-TOFMS, and GC-MS were utilized for the structural elucidation of the bioactive compounds, and a series of unsaturated and saturated 16- to 22-carbon fatty acids were detected. The data suggested the bioactive compounds isolated from Amphidinium carterae exhibited a significant inhibiting effect against the diatom Skeletonema costatum and Amphibalanus amphi- trite larvae, and could be substitutes for persistent, toxic antifouling compounds.