Anti-inflammatory Ingredients Research Articles

Design of an anti-inflammatory diet (ITIS diet) for patients with rheumatoid arthritis

BackgroundRheumatoid arthritis (RA) is a chronic systemic autoimmune disease that affects synovial joints, leading to inflammation, joint destruction, loss of function, and disability. Although recent pharmaceutical advances have improved treatment of RA, patients with RA often inquire about dietary interventions to improve RA symptoms, as they perceive rapid changes in their symptoms after consumption of certain foods. There is evidence that some ingredients have pro- or anti-inflammatory effects. In addition, recent literature has shown a link between diet and microbiome changes. Both diet and the gut microbiome are linked to circulating metabolites that may modulate inflammation. However, evidence of the effects of an anti-inflammatory and probiotic-rich diet in patients with RA is scarce. There is also a need for biological data to support its anti-inflammatory effects. MethodsThe main goal of this study is to delineate the design process for a diet tailored to our RA population. To achieve this goal, we collected information on diet, supplements, cooking methods, and intake of different ingredients for each patient. Different groups were interviewed, and their feedback was assessed to design a diet that incorporates suggested anti-inflammatory ingredients in a manner that was easy for patients to adopt based on their lifestyles and backgrounds. ResultsWe designed a diet that includes a high intake of potential anti-inflammatory ingredients. Feedback from highly motivated patients was critical in constructing an anti-inflammatory diet (ITIS diet) with elevated adherence. ConclusionIn order to tailor our diet, we surveyed our patients on several different parameters. We obtained important feedback on how feasible our ITIS diet is for RA patients. Using this feedback, we made minor improvements and finalized the design of the ITIS diet. This diet is being used in an on-going pilot study to determine their anti-inflammatory effect in pain and joint swelling in RA patients. Trial registrationNot applicable.

Study on Anti-Inflammatory Effect and Major Anti-Inflammatory Components of PSORI-CM02 by Zebrafish Model.

PSORI-CM02 is an optimization formula of PSORI-CM01, which is a clinical herbal formula for the treatment for psoriasis in the Guangdong Provincial Hospital of Chinese Medicine. Previous research indicates that it plays a critical role in anti-inflammation and immunoregulation. Rhizoma smilacis glabrae (RSG) is one herbal medicine of PSORI-CM02, whose effective anti-inflammatory component is astilbin. This study aims to test the anti-inflammatory and immunoregulation effects of astilbin as well as RSG in PSORI-CM02, and we, respectively, used the CuSO4-induced neutrophil-specific transgenic zebrafish model Tg(mpx: EGFP) and the melanin allele mutated Albino strain zebrafish model to visualize the effects of neutrophil recruitment and macrophage phagocytosis. Our data indicated that both PSORI-CM02 and astilbin had anti-inflammatory effects, leading to a reduction in the recruitment of neutrophils and promotion in macrophage phagocytosis. Nevertheless, the negative liquor of Rhizoma smilacis glabrae (PSORI-CM02 without RSG) also had anti-inflammatory and promoting macrophage phagocytosis effects. The results revealed the formula excluding RSG also had anti-inflammatory and immunoregulation effects, which demonstrated that RSG was not the major anti-inflammatory herbal medicine in PSORI-CM02. Similarly, astilbin was not the major anti-inflammatory active ingredient in the formula. The anti-inflammatory and the promotion of macrophage phagocytosis effect of PSORI-CM02 in vivo zebrafish were the results of multiple component interaction, which was the common characteristic of the Chinese medicine compound.

Anti-inflammatory mechanism and active ingredients of the Chinese tallow tree.

The leaf of the Chinese tallow tree (CTT, Sapium sebiferum (L.) Roxb) has been used in Traditional Chinese Medicine (TCM) to treat eczema, shingles, edema, swelling, ascites, scabs, and snakebites. The present work aimed to explore the antioxidant-related anti-inflammatory mechanisms of CTT leaf and to further investigate their possible active ingredients. The anti-inflammatory activities of different fractions were determined using a 12-O-tetradecanoylphorbol-13-acetate (TPA) induced model of acute edema in mouse ears. The SOD, CAT and GCL activities and the GSH content of the ear tissue were measured using kits, and the ratio of the treated and control ears was calculated. The anti-inflammatory activities of each single compound and those of a mixture of the compounds were also determined using the TPA-induced model. The anti-inflammatory effects of the three fractions were positively correlated with their increasing GSH capacities. Although the GSH levels decreased during TPA-induced acute edema, the CTT leaf extract could recover these levels by increasing the glutamate cysteine ligase activity. The mixture of ellagic acid, isoquercitrin and astragalin showed an anti-inflammatory effect similar to that of the CTT leaf extract. However, none of these three individual compounds showed comparable activity alone. These results demonstrated that increasing GSH is an antioxidant-related anti-inflammatory mechanism of CTT leaves. In addition, ellagic acid, isoquercitrin and astragalin were found to be jointly responsible for this bioactivity.

NOx-, IL-1β-, TNF-α-, and IL-6-Inhibiting Effects and Trypanocidal Activity of Banana (Musa acuminata) Bracts and Flowers: UPLC-HRESI-MS Detection of Phenylpropanoid Sucrose Esters.

Banana inflorescences are a byproduct of banana cultivation consumed in various regions of Brazil as a non-conventional food. This byproduct represents an alternative food supply that can contribute to the resolution of nutritional problems and hunger. This product is also used in Asia as a traditional remedy for the treatment of various illnesses such as bronchitis and dysentery. However, there is a lack of chemical and pharmacological data to support its consumption as a functional food. Therefore, this work aimed to study the anti-inflammatory action of Musa acuminata blossom by quantifying the cytokine levels (NOx, IL-1β, TNF-α, and IL-6) in peritoneal neutrophils, and to study its antiparasitic activities using the intracellular forms of T. cruzi, L. amazonensis, and L. infantum. This work also aimed to establish the chemical profile of the inflorescence using UPLC-ESI-MS analysis. Flowers and the crude bract extracts were partitioned in dichloromethane and n-butanol to afford four fractions (FDCM, FNBU, BDCM, and BNBU). FDCM showed moderate trypanocidal activity and promising anti-inflammatory properties by inhibiting IL-1β, TNF-α, and IL-6. BDCM significantly inhibited the secretion of TNF-α, while BNBU was active against IL-6 and NOx. LCMS data of these fractions revealed an unprecedented presence of arylpropanoid sucroses alongside flavonoids, triterpenes, benzofurans, stilbenes, and iridoids. The obtained results revealed that banana inflorescences could be used as an anti-inflammatory food ingredient to control inflammatory diseases.

Alleviation of infectious-bursal-disease-virus-induced bursal injury by betaine is associated with DNA methylation in IL-6 and interferon regulatory factor 7 promoter

Infectious bursal disease virus (IBDV) often infects young chickens and causes severe immunosuppression and inflammatory injury. Betaine is an antiviral and anti-inflammatory ingredient that may exert functions through epigenetic regulation. However, the effects of betaine on an IBDV-induced bursal injury and their underlying mechanisms have not been investigated. In this study, betaine was supplemented to the drinking water of newly hatched commercial broilers for 3 wk. Afterward, the chickens were infected with the IBDV. After 5 D of infection, the bursal lesions were examined. The mRNA expression levels of IBDV VP2 gene, pro-inflammatory cytokines, and interferons were detected. Furthermore, the 5-methylcytosine level of the CpG island in the promoter region of IL-6 and interferon regulatory factor 7 (IRF7) were determined. The IBDV induced the depletion of lymphocytes and inflammation in the bursal follicles. IBDV infection considerably elevated the mRNA levels of VP2, IL-6, types I (IFNα and IFNβ) and II (IFNγ) interferons, and IRF7. The CpG island methylation in the promoter regions of IL-6 and IRF7 were substantially decreased after IBDV infection. Betaine administration attenuated the IBDV-induced bursal lesions. Meanwhile, the IBDV-induced mRNA expression levels of IL-6, IFNβ, and IRF7 were suppressed by betaine consumption. Furthermore, the hypomethylation effects of IBDV infection to the promoter regions of IL-6 and IRF7 genes were eliminated and relieved by betaine administration. Our results indicated that the IBDV-induced expression levels of IL-6 and IRF7 genes are associated with the suppression of methylation in the promoter region. Betaine administration through drinking water may alleviate the IBDV-induced bursal injury via epigenetic regulation.

Investigation of metabolism of HN-1 isolated from Millettia pachyloba in vivo and in vitro

Ultra-fast performance liquid chromatography-mass spectrometry( UFLC-MS/MS) was used to study the anti-inflammatory active ingredient of Millettia pachyloba,6-methoxy-8,8-dimethyl-3-( 2,4,5-trimethoxyphenyl)-4 H,8 H-pyrano[2,3-f]chromen-4-one( HN-1),in liver microsomes of rats,mice,rhesus monkeys,Beagle dogs and humans metabolic stability,and compare the metabolic differences between different species. The metabolic phenotype in human liver microsomes was determined by chemical inhibitor method. Using UPLC-Q-TOF-MS/MS detection method,the in vitro metabolites of various liver microsomes were preliminarily inferred by comparing the samples incubated for 0 min and 60 min in vitro. The metabolites of HN-1 in SD rats were presumed by comparing feces,urine,plasma blanks and samples after administration. The results showed that the metabolism of HN-1 in various liver microsomes was stable,and the metabolic properties of dog and human liver microsomes were the closest. It is mainly catabolized by CYP1 A1,CYP2 D6 and CYP3 A4 isoenzymes in human liver microsomes. The metabolites of HN-1 in vitro and in vivo,including 3 in vitro metabolites and5 in vivo metabolites,were preliminarily estimated. The results laid the foundation for further pharmacological studies of HN-1.

Efficient Extraction of Anti-Inflammatory Active Ingredients from Schefflera octophylla Leaves Using Ionic Liquid-Based Ultrasonic-Assisted Extraction Coupled with HPLC.

Schefflera octophylla (Lour.) Harms, a kind of traditional Chinese medicine (TCM), is commonly used for anti-inflammatory, analgesic, rheumatism, fever, and hemostasis therapy. In our previous studies, two major triterpenoids were isolated and identified from leaves of S. octophylla, and evaluated for their inhibitory effects on lipopolysaccharide (LPS)-induced nitric oxide production in RAW264.7 cells; both of them displayed significant anti-inflammatory activities at their noncytotoxic concentrations. Therefore, it is very useful to establish an efficient and green extraction method to isolated the two major triterpenoids from leaves of S. octophylla. In this paper, ionic liquid based ultrasonic-assisted extraction (ILUAE) was successfully applied to extract the two major triterpenoids from leaves of S. octophylla. Four single factors (ionic liquids (ILs) concentration, solid–liquid ratio, centrifugal speed, mesh number), with a greater impact on extraction rate, were selected from a variety of influencing factors, and the optimal conditions were obtained by Box–Behnken response surface methodology (RSM). Under optimal conditions, the total extraction yield and extraction rate of two triterpenoids were 288.03 mg/g and 28.80%, respectively, which was 6.80% higher than that of 70% Ethanol (220 mg/g and 22%, respectively).

Topical Non-Pharmacological Treatment for Facial Seborrheic Dermatitis.

Facial seborrheic dermatitis (FSD) is a chronic and relapsing inflammatory skin disorder occurring in areas of the face rich in sebaceous glands. It clinically manifests as erythematous scaly macules or plaques, often associated with pruritus. Although the pathogenesis of seborrheic dermatitis is not yet fully understood, Malassezia yeast, hormones, sebum levels, and immune response are known to play important roles. Additional factors including drugs, cold temperatures, and stress may exacerbate the condition. Currently, the available treatments do not cure the disease but relieve symptoms. Various pharmacological treatments are available, including antifungal agents, keratolytics, topical low-potency steroids, and calcineurin inhibitors. All of them provide several benefits, but they also have potential side effects. Seborrheic dermatitis tends to have a chronic, recurrent course. To avoid the long-term use of drugs, topical non-pharmacological products such as cosmetics or medical devices may improve clinical outcomes. Products with antimicrobial and anti-inflammatory ingredients such as zinc, piroctone olamine, dihydroavenanthramide, biosaccharide gum-2, and stearyl glycyrrhetinate may speed FSD recovery and avoid flare-ups. Finally, the use of specific cleansers, moisturizers, and sunscreens formulated as light creams or gel/creams should be strongly recommended to all FSD patients. We provide a brief review of the most used non-pharmacological cleansers, topical gel/creams, and specific sunscreens in the management of FSD.

Bioactive Compounds Constituent and Anti-Inflammatory Activity of Natural Rice Bran Oil Produced from Colored and Non-Pigmented Rice in Northern Thailand

The aims of the study were to measure and compare the content of the bioactive compounds in natural rice bran oils (NRBOs) and investigate for anti-inflammatory activity through inhibition effect on nitric oxide (NO) and inducible nitric oxide synthase (iNOS) in RAW264.7 mouse macrophage cells.NRBOs were prepared from colored and non-pigmented rice in northern Thailand using the cold-press technique. The bioactive compound constituents in NRBOs, including tocotrienols, tocopherols, and γ-oryzanol were analyzed by reversed-phase HPLC. Then, anti-inflammatory activity was investigated through an inhibition effect on NO and iNOS production induced by combined lipopolysaccharide (LPS)-interferon-γ (IFN-γ) in RAW264.7 mouse macrophage cells. The results demonstrated that NRBOs prepared from purple rice, red rice and non-pigmented rice consist of δ, γ, and α-tocotrienol, δ, β, γ, and α-tocopherol, and γ-oryzanol. γ-Oryzanol, γ-tocotrienol, and γ-tocopherol were the major bioactive compounds in NRBOs. NRBOs prepared from purple rice bran exhibited higher concentrations of the bioactive compounds than red rice bran and non-pigmented rice bran, respectively. Khaoʹ′ GamLeum-Phua (KGLP) exhibited the highest amount of δ, γ and α-tocotrienol, δ, γ, β and α-tocopherol, and γ-oryzanol. Interestingly, all NRBOs inhibited NO and iNOS production by LPS/IFN-γ-stimulated RAW264.7 cells. Additionally, NRBO prepared from KGLP exhibited the highest inhibitory activity on NO and iNOS production. There may a potential use for pigmented NRBOs especially cultivated in mountainous areas which containing high amounts of tocotrienols, tocopherols, and γ-oryzanol, as a natural anti-inflammatory active ingredient in nutraceutical and cosmeceutical products.

Separation and Enrichment of Three Coumarins from Angelicae Pubescentis Radix by Macroporous Resin with Preparative HPLC and Evaluation of Their Anti-Inflammatory Activity.

In order to enrich and separate three coumarins (columbianetin acetate, osthole and columbianadin) from Angelicae Pubescentis Radix (APR), an efficient method was established by combining macroporous resins (MARs) with preparative high-performance liquid chromatography (PHPLC). Five different macroporous resins (D101, AB-8, DA-201, HP-20 and GDX-201) were used to assess the adsorption and desorption characteristics of three coumarins. The result demonstrated that HP-20 resin possessed the best adsorption and desorption capacities for these three coumarins. Moreover, the adsorption dynamics profiles of three coumarins were well fitted to the pseudo second order equation (R2 > 0.99) for the HP-20 resin. The adsorption process was described by the three isotherms models including Langmuir (R2 > 0.98, 0.046 ≤ RL ≤ 0.103), Freundlich (R2 > 0.99, 0.2748 ≤ 1/n ≤ 0.3103) and Dubinin Radushkevich (R2 > 0.97). The contents of columbianetin acetate, osthole and columbianadin in the product were increased 10.69-fold, 19.98-fold and 19.68-fold after enrichment, respectively. Three coumarins were further purified by PHPLC and the purities of them reached above 98%. Additionally, the anti-inflammatory effects of these three coumarins were assessed by Lipopolysaccharide (LPS)-induced RAW 264.7 cells. It was found that the production of NO and MCP-1 was obviously inhibited by three coumarins. Columbianetin acetate, osthole and columbianadin could be used as potentially natural anti-inflammatory ingredients in pharmaceutical products. It was concluded that the new method combining MARs with PHPLC was efficient and economical for enlarging scale separation and enrichment of columbianetin acetate, osthole and columbianadin with anti-inflammatory effect from the APR extract.

Bee Pollen Extracts Modulate Serum Metabolism in Lipopolysaccharide-Induced Acute Lung Injury Mice with Anti-Inflammatory Effects.

Bee pollen (BP) collected from different floras possesses various potential bioactivities, but the mechanism-related research on anti-inflammatory effects is limited. Here, three types of BP originating from Camellia sinensis L. (BP-Cs), Nelumbo nucifera Gaertn. (BP-Nn), and Brassica campestris L. (BP-Bc) were assessed using molecular and metabolomics methods to determine their anti-inflammatory effects. The differences in polyphenolic abundance of three types of BP extracts were determined by HPLC-DAD/Q-TOF-MS. In vitro anti-inflammatory effects of three BP extracts were evaluated in a lipopolysaccharide (LPS)-induced RAW 264.7 cells model. BP-Cs extract with the most abundant polyphenols was found to be the most effective in reducing inflammation by downregulating inflammatory-related genes expression and blocking the activation of MAPK and NF-κB signaling pathways. Polyphenol-rich BP-Cs was further evaluated for their in vivo anti-inflammatory effect in a LPS-induced acute lung injury mouse model. An UPLC-Q-TOF/MS-based metabolomics approach was applied to analyze metabolite changes in mouse serum. Weshowed that the pretreated BP-Cs extract alleviated inflammation and regulated glycerophospholipid metabolism significantly. Ourfindings provide a foundation for developing and justifying BP as a potential anti-inflammatory ingredient in functional foods or nutraceutical formulations.

Assessing Cheese Whey Components for Their Potential to Improve Intestinal Health (P06-097-19)

ObjectivesTo evaluate the potential of cheese whey bioactive components for intestinal health and barrier function in vitro. MethodsHT29-MTX intestinal globet cells were treated with whey protein isolate (WPI), glycomacropeptides (GMP) and a galacto-oligosacharide rich whey protein isolate (WPI-GOS) followed by challenge with lipopolysaccharides (LPS, 4 μg/ml). Reactive oxygen species (ROS) production was assessed using the 2,7 dichlorofluorescein diacetate (DCFH-DA) assay. Gene and protein expression of intestinal inflammation biomarkers were also assessed using standard analytical techniques. The effects of WPI, WPI-GOS and GMP on barrier function were assessed on a co-culture (Caco-2/HT29-MTX in a 75/25 ratio, respectively) cell model through the transepithelial electrical resistance (TEER) and apparent permeability (Papp) assays; whereas protein expression of tight junction biomarkers was assessed by Western Blots. ResultsWPI, GMP and WPI-GOS did not inhibit cell viability of colon cells within a dose range of 25–100 μg/ml. LPS induced ROS production in HT29-MTX cells up to 1.92 -fold of control and this effect was prevented by WPI, GMP and WPI-GOS (100 μg/ml) that maintained ROS down to levels that were similar to controls not challenged with LPS. GMP protected colon cells at a highest extent against the expression of inflammatory biomarkers (nuclear factor kappa β (NF-kβ), tumor necrosis factor (TNF-α) and toll-like receptor 4 (TLR-4)) on HT29-MTX cells challenged with LPS and maintained NF-kβ and TNF-α at levels similar to untreated control. In addition, GMP improved TEER (1.3-fold of untreated control) and decreased intestinal permeability by 64% in Caco-2/HT29-MTX co-cultures. Finally, these results were accompanied by the upregulation of tight junction proteins (Claudin-1, Claudin-3, Occludin and Zonulin-1) exerted by GMP and WPI at similar levels. ConclusionsWPI, GMP and WPI-GOS protected against ROS production at similar levels. However, GMP protected colon cells against LPS-induced inflammation and improved barrier function with higher potency than WPI and WPI-GOS. These results strongly suggest that cheese whey components may be used by the functional foods industry as ingredients to improve intestinal health with emphasis on GMP as anti-inflammatory ingredient. Funding SourcesBUILD Dairy Program.

Antioxidative oxygenated terpenoids with bioactivities against pro-inflammatory inducible enzymes from Indian squid, Uroteuthis (Photololigo) duvaucelii

Cephalopod squid, Uroteuthis (Photololigo) duvaucelii is consumed as culinary delicacy along the southwest part of Asian continent. Ethyl acetate:methanol extract of U. duvaucelii was chromatographically fractionated to yield C19 furano-norditerpenoid (1) along with irregular C15 sesquiterpenoid (2) and C20 diterpenoid compounds (3). In vitro anti-inflammatory and antioxidant analyses were utilised to evaluate their bio-potentials. The C19 furano-norditerpenoid was reported for significantly effective 2,2-diphenyl-1-picrylhydrazyl radical inhibition (IC50 0.60 mg/mL) than other compounds and α-tocopherol (IC50 ≥ 0.64 mg/mL). The 2,2’-azino-bis-3-ethylbenzothiozoline-6-sulfonic acid inhibition and ferrous ion chelating potentials were higher for compounds 1 and 2 (IC50 ∼ 0.69 and ∼0.84 mg/mL, respectively) compared to α-tocopherol (IC50 0.76–0.95 mg/mL). The studied compounds displayed comparable inhibitory activities with synthetic ibuprofen against pro-inflammatory inducible 5-lipoxygenase (IC50 ∼ 0.92 mg/mL). The lower hydrophobicity and steric variables were directly correlated with their antioxidative and anti-inflammatory properties. The studied compounds could be utilised as natural antioxidants and anti-inflammatory functional food ingredients.

Anti-inflammatory lindenane sesquiterpeniods and dimers from Sarcandra glabra and its upregulating AKT/Nrf2/HO-1 signaling mechanism

Sarcandra glabra (Thunb.) Nakai (Chloranthaceae), grown and cultivated evergreen shrub in south of China, has been used in traditional Chinese medicines (TCMs) to treat bruises, bone fractures and arthritis which were partly due to inflammation. Previous phytochemical and pharmacological researches indicated that flavonoids, coumarins, phenolic acids as its main anti-inflammatory ingredients related to its traditional efficacy. Our present research aimed to elucidate whether the fascinating and abundant lindenane-type sesquiterpeniods are also its anti-inflammatory components and uncover its anti-inflammatory mechanism. On the guidance of results of phytochemical fraction and anti-inflammatory activity evaluation, ten anti-inflammatory lindenane sesquiterpenes with half maximal inhibitory concentration (IC50) values from 8.13 ± 0.37 to 24.06 ± 0.60 μM, including seven dimmers (1-7) and three monomers (8-10) were discovered and characterized from the anti-inflammatory fraction of roots of title plant. Considering the activity and quantity, shizukaol D was selected as the target for further mechanism study. Firstly, shizukaol D could downregulate the expression of inducible nitric oxide synthase (iNOS) and suppress the protein level of nuclear factor kappa B (NF-κB) p65 as well as the nuclear translocation of NF-κB p65. Meanwhile, shizukaol D also decreased the level of reactive oxygen species (ROS) and enhanced the activities of phase II defense enzymes superoxide dismutase (SOD), glutathione (GSH) and glutathione peroxidase (GSH-px) by elevating the expression of heme oxygenase-1 (HO-1) and NAD(P)H: quinone oxidoreductase 1 (NQO1) via promoting nuclear factor E2-related factor 2 (Nrf2) activation as well as its nuclear translocation, and regulating the pathway of phosphoinositide 3-kinases (PI3K)/ protein kinase B (AKT) rather than mitogen-activated protein kinase (MAPK) to the activation of Nrf2/HO-1 signaling. Taken together, our research provided the phytochemical and pharmacological evidences for that the major sesquiterpenoid dimers can be defined as the anti-inflammatory ingredients of S.glabra and this kind of sesquiterpenoids, such as shizukaol D, can be as an attractive therapeutic candidate for inflammatory diseases.

Study on compatibility of active ingredients of Simiao Yongan Decoction in rats with in situ single-pass intestinal perfusion model

To study the compatibility rule of Simao Yongan Decoction,the rat single pass intestinal perfusion model in situ was used in this study. On the basis of early research,the five kinds of anti-inflammatory active ingredients,i.e. chlorogenic acid,liquiritin,hyperoside,angoroside C and isochlorogenic acid C in Simao Yongan Decoction were selected as research objects. The contents of the above five actives compounds with various compatibility combinations and in different intestinal segment perfusates were determined by using the method of ultra-performance liquid chromatography-mass spectrometry( UPLC-MSn). The kinetic parameters of intestinal absorption of the five anti-inflammatory active ingredients were calculated,which could be used to evaluate the intestinal absorption of each component in different combinations. The results showed that the absorption parameters of liquiritin in ileum were highest in Glycyrrhizae Radix et Rhizoma single herb,while the absorption parameters of other four components in ileum and duodenum were highest in the compatible combinations. Among them,the absorption parameters of chlorogenic acid in ileum and duodenum were highest in the whole prescription compatibility; ischlorogenic acid C showed higher absorption levels in the whole prescription and the herb compatibility of Lonicerae Japonicae Flos-Scrophulariae Radix-Glycyrrhizae Radix et Rhizoma. However,the absorption levels of hyperoside and angoroside C in different compatibilities were quite different in ileum and duodenum. In this study,the intestinal absorption of five anti-inflammatory active ingredients in Simiao Yongan Decoction with different compatibility combinations was investigated,revealing that the absorption of active ingredients varied with the different compatibility combinations and different intestinal segments. At the same time,the above research also indicated that the absorption of active ingredients could be obviously promoted by the compatibility of compound prescriptions,laying a foundation for the research on the compatibility rule of Simiao Yongan Detection from the biological point of view.

The identification and isolation of anti-inflammatory ingredients of ethno medicine Breynia fruticosa

Ethnopharmacological relevanceBreynia fruticosa is a folk medicine in China, traditionally used to treat gastroenteritis, sore throat, eczema and arthritis. However, the bioactive ingredients are unknown. Aim of the studyTo identify and isolate the anti-inflammatory ingredients of B. fruticosa. Materials and methodsB. fruticosa extracts were fractioned by Amberchrom CG161M and Toyopearl HW40C resins. Acetic acid-induced capillary permeability mice model was used to evaluate the anti-inflammation activities of fractions. The anti-inflammatory ingredients were identified by high performance liquid chromatography/mass spectroscopy (HPLC-MS). On-line two dimensional liquid chromatography system was constructed to remove the tannins and enrich the breynins. The breynins were purified by preparative HPLC and evaluated for their anti-arthritis activities using complete Freund's adjuvant (CFA) induced arthritis rats model. ResultsThe anti-inflammatory ingredients of B. fruticosa are sulfur containing sesquiterpenoids (breynins). The on-line two dimensional preparative liquid chromatography system can effectively remove the tannins and enrich the bioactive ingredients in large scale within 1 h. Four major breynins were purified, and their structures were elucidated by analysis of MS and NMR data. Breynins can significantly prevent the rats' arthritis deterioration, with inhibition ratio 50% at dose 0.2 mg kg−1, comparable with that of indomethacin at dose 2 mg kg−1. ConclusionThe breynins have strong anti-arthritis activities, which is responsible to the anti-inflammatory effects of B. fruticosa. However, breynins are also toxic components of B. fruticosa.

Rapid discovery and identification of the anti-inflammatory constituents in Zhi-Shi-Zhi-Zi-Chi-Tang.

The anti-inflammatory active ingredients of Zhi-Shi-Zhi-Zi-Chi-Tang (ZSZZCT), a traditional Chinese medicine formula, were predicted and identified using an approach based on activity index, LC-MS, semi-preparative LC and NMR. Firstly, the whole extract of ZSZZCT was analyzed using liquid chromatography-quadrupole time of flight-mass spectrometry (LC-Q-TOF-MS) and liquid chromatography - ion trap mass spectrometry (LC-IT-MS), 79 constituents were detected and 39 constituents were identified unambiguously or tentatively. Subsequently, the whole extract of the formula was separated into multiple components and the activity index method was used to calculate index values of the 79 constituents by integrating the chemical and pharmacological information of multiple components. Four polymethoxyl flavones were predicted as the major active constituents according to the activity index values. Furthermore, three polymethoxyl flavones were prepared using the strategy with semi-preparative LC guided by LC-MS, and their anti-inflammatory activities were validated. The results show that three polymethoxyl flavones with higher positive index values, i.e., 3, 5, 6, 7, 8, 3', 4'-heptamethoxyflavone, 3-hydroxynobiletein and tangeretin had significant anti-inflammatory effects. In conclusion, the predicted results indicated that the activity index method is feasible for the accurate prediction of active constituents in TCM formulae.

The Screening Research of NF-κB Inhibitors from Moutan Cortex Based on Bioactivity-Integrated UPLC-Q/TOF-MS.

Inflammation is a common and important pathological process, and nuclear factor-κB (NF-κB) is a key mediator of it. Moutan Cortex (MC), the dried root cortex of Paeonia suffruticosa Andr., is widely used as a remedy for the treatment of inflammatory diseases in Asian region. However, there are few studies on the systematic identification of NF-κB inhibitors of MC. In this study, the effect of inhibiting NF-κB activation of MC was assessed at the cellular level using a tumor necrosis factor-α (TNF-α) induced inflammatory model. Subsequently, ultra-performance liquid chromatography-quadrupole/time of flight-mass spectrometry (UPLC-Q/TOF-MS) combined with biological activity assay was established to screen and identify potential anti-inflammatory ingredients in MC. The results revealed that MC significantly inhibited the activation of NF-κB. Seven potential NF-κB inhibitors were screened from MC, including oxypaeoniflorin, paeoniflorin, galloylpaeoniflorin, benzoyloxypaeoniflorin, mudanpioside C, gallic acid, and paeonol. Among them, the NF-κB inhibitor activity of galloylpaeoniflorin, benzoyloxypaeoniflorin, and mudanpioside C is first reported here. In conclusion, the anti-inflammatory activity of MC was associated with the seven components mentioned above. And the bioactivity-integrated UPLC-Q/TOF which contains both chemical and bioactive details is suitable for screening active ingredients from natural medicines.

Autophagy Activation by Crepidiastrum Denticulatum Extract Attenuates Environmental Pollutant-Induced Damage in Dermal Fibroblasts.

Pollution-induced skin damage results in oxidative stress; cellular toxicity; inflammation; and, ultimately, premature skin aging. Previous studies suggest that the activation of autophagy can protect oxidation-induced cellular damage and aging-like changes in skin. In order to develop new anti-pollution ingredients, this study screened various kinds of natural extracts to measure their autophagy activation efficacy in cultured dermal fibroblast. The stimulation of autophagy flux by the selected extracts was further confirmed both by the expression of proteins associated with the autophagy signals and by electron microscope. Crepidiastrum denticulatum (CD) extract treated cells showed the highest autophagic vacuole formation in the non-cytotoxic range. The phosphorylation of adenosine monophosphate kinase (AMPK), but not the inhibition of mammalian target of rapamycin (mTOR), was observed by CD-extract treatment. Its anti-pollution effects were further evaluated with model compounds, benzo[a]pyrene (BaP) and cadmium chloride (CdCl2), and a CD extract treatment resulted in both the protection of cytotoxicity and a reduction of proinflammatory cytokines. These results suggest that the autophagy activators can be a new protection regimen for anti-pollution. Therefore, CD extract can be used for anti-inflammatory and anti-pollution cosmetic ingredients.

Wlasciwosci fizykochemiczne i funkcjonalne biokompozytow polimerowych

Biocomposite films based on chitosan (Chit) and sodium alginate (Alg) and containing anti-inflammatory (zinc sulfate) and antimicrobial (sulfanilamide) pharmaceutical ingredients were prepared. The effects of variable chitosan and alginate contents on the chemical structure and phase transition temperatures of biocomposites were studied using infrared spectroscopy (FT-IR), nuclear magnetic re­sonance (NMR) and differential scanning calorimetry (DSC). Thermal analysis showed that the addition of pharmaceuticals decreased the melting temperature and melting enthalpy of polymer biocomposites.