Identification Data of secondary metabolites and Antibacterial Action of leaf extract of Lantana camara L. on multidrug-resistant microorganisms.

Tentative identification of secondary metabolites in Lantana camara L. leaves was done. This plant belongs to the verbenaceae family and is used for several treatments in folk medicine. The data was acquired by collecting leaves and their stems of L. camara manually, in Nampula city, during the flowering period around 4pm. Then, the plant material collected was washed with water to remove impurities, and it was covered by paper and dried in the sun for a week. After the drying process, it was crushed and sieved, and 200 g of homogeneous powder was obtained. The method of preparation of the leaf extract of L. camara was cold maceration, mixing 200 g of powder leaves with 2 L of 90 % ethanol, in the proportion of 1 g/10 mL, and it was stored in favourable conditions and stirred occasionally during a week. Then it was filtrated and divided into two parts so as to be dried in an oven at 80 °C for 8 h and another part was dried in a rotary evaporator at 42 °C for 6 h. Before drying the ethanolic extract, the yield of the dry extract was determined. The class of alkaloids, tannins, saponins, phenolic compounds and quinone were identified using general and specific chemical reagents. In addition, antibacterial action against Escherichia coli and Staphylococus aureus was evaluated using a disc diffusion method, according to Kirby-Bauer. These data provide helpful leads for pharmacological intervention from the extraction of the raw form of the metabolites, which is responsible for the antibacterial action specifically for the eradication of multidrug-resistant bacteria.

Bioaccessibility of Rosmarinic Acid and Basil (Ocimum basilicum L.) Co-Compounds in a Simulated Digestion Model-The Influence of the Endogenous Plant Matrix, Dose of Administration and Physicochemical and Biochemical Digestion Environment.

The objective of this study is to determine the effect of endogenous plant matrix components, dose and digestion-related factors on the bioaccessibility of rosmarinic acid and basil co-compounds in in vitro digestion conditions. Different forms of administration, i.e., basil raw plant material, dry extract, and isolated rosmarinic acid at various doses, were applied for the digestion experiment. To evaluate the contribution of biochemical and physicochemical digestion factors, samples were subjected to a full digestion process or treated only with a digestion fluid electrolyte composition without using biochemical components (i.e., digestion enzymes and bile salts), and bioaccessibility was monitored at the gastric and intestinal steps of digestion. The results showed that the components of the endogenous raw plant matrix significantly limited the bioaccessibility of rosmarinic acid and basil co-compounds, especially at the gastric stage of digestion. Physicochemical digestion factors were mainly responsible for the bioaccessibility of basil phytochemicals. Higher doses allowed maintenance of bioaccessibility at a relatively similar level, whereas the most negative changes in bioaccessibility were induced by the lowest doses. In conclusion, the determination of the bioaccessibility of bioactive phytochemicals from basil and factors influencing bioaccessibility may help in better prediction of the pro-health potential of this plant.

Analysis on Determination and Quantity Transfer of Standard Decoction of Ginseng Radix et Rhizoma by Fresh and Traditional Cutting / 中国实验方剂学杂志

ObjectiveTo analyze the quantity-quality transfer of standard decoction of Ginseng Radix et Rhizoma（GRR） decoction pieces produced by fresh and traditional cutting， and to provide reference for quality control and application development of the decoction pieces produced by fresh cutting. MethodTen batches of representative GRR decoction pieces produced by fresh and traditional cutting and their standard decoctions were prepared by standard process， and high performance liquid chromatography（HPLC） fingerprint of the standard decoction was established and performed on an Agilent EC-C18 column（4.6 mm×150 mm， 2.7 μm） with acetonitrile（A）-0.1% phosphoric acid aqueous solution（B） as the mobile phase for gradient elution（0-23 min， 18%-21%A； 23-35 min， 21%-28%A； 35-80 min， 28%-32%A）， and the detection wavelength was 203 nm. Then similarity evaluation， principal component analysis（PCA） and partial least squares-discriminant analysis（PLS-DA） of fingerprint of the standard decoction were performed to screen the differential components with variable importance in the projection（VIP） value>1. Quantitative analysis was carried out on the screened known differential components， and combined with the indicators of the dry extract rate and the transfer rate， to explore the differences in the quantity-quality transfer between the standard decoction of GRR decoction pieces produced by fresh and traditional cutting. ResultThe fingerprint similarity of the standard decoction of GRR decoction pieces produced by fresh and traditional cutting was more than 0.950， and 18 common peaks were identified， including 9 identified common peaks. The results of PCA and PLS-DA showed that there were some differences in the contents of index components between the two standard decoctions. The contents of ginsenoside Rg1， Re and Ro in GRR decoction pieces produced by fresh cutting were higher than those in traditional decoction pieces， while the contents of ginsenoside Rb1， Rc ， Rb2 and Rd were lower than those in traditional decoction pieces. The contents of ginsenoside Rg1， Re， Rb1 and Ro in the standard decoction of GRR decoction pieces produced by fresh cutting were higher than those in the standard decoction of traditional decoction pieces， while the contents of ginsenoside Rc ， Rb2 and Rd were comparable between the two standard decoctions. Compared with the standard decoction of the traditional decoction pieces， the average transfer rates of ginsenoside Rg1， Rb1， Rc， Rb2 and dry extract rate of the standard decoction of GRR decoction pieces produced by fresh cutting were significantly increased（P<0.05）， and the average transfer rate of ginsenoside Re and Rd also increased， but the difference was not statistically significant. ConclusionThe dry extract rate， content and transfer rate of index components of standard decoction of GRR decoction pieces produced by fresh cutting are better than those of the standard decoction of traditional decoction pieces， which can provides data support for the subsequent clinical application of fresh cutting products.

Analysis on Determination and Quantity Transfer of Standard Decoction of Ginseng Radix et Rhizoma by Fresh and Traditional Cutting / 中国实验方剂学杂志

ObjectiveTo analyze the quantity-quality transfer of standard decoction of Ginseng Radix et Rhizoma（GRR） decoction pieces produced by fresh and traditional cutting， and to provide reference for quality control and application development of the decoction pieces produced by fresh cutting. MethodTen batches of representative GRR decoction pieces produced by fresh and traditional cutting and their standard decoctions were prepared by standard process， and high performance liquid chromatography（HPLC） fingerprint of the standard decoction was established and performed on an Agilent EC-C18 column（4.6 mm×150 mm， 2.7 μm） with acetonitrile（A）-0.1% phosphoric acid aqueous solution（B） as the mobile phase for gradient elution（0-23 min， 18%-21%A； 23-35 min， 21%-28%A； 35-80 min， 28%-32%A）， and the detection wavelength was 203 nm. Then similarity evaluation， principal component analysis（PCA） and partial least squares-discriminant analysis（PLS-DA） of fingerprint of the standard decoction were performed to screen the differential components with variable importance in the projection（VIP） value>1. Quantitative analysis was carried out on the screened known differential components， and combined with the indicators of the dry extract rate and the transfer rate， to explore the differences in the quantity-quality transfer between the standard decoction of GRR decoction pieces produced by fresh and traditional cutting. ResultThe fingerprint similarity of the standard decoction of GRR decoction pieces produced by fresh and traditional cutting was more than 0.950， and 18 common peaks were identified， including 9 identified common peaks. The results of PCA and PLS-DA showed that there were some differences in the contents of index components between the two standard decoctions. The contents of ginsenoside Rg1， Re and Ro in GRR decoction pieces produced by fresh cutting were higher than those in traditional decoction pieces， while the contents of ginsenoside Rb1， Rc ， Rb2 and Rd were lower than those in traditional decoction pieces. The contents of ginsenoside Rg1， Re， Rb1 and Ro in the standard decoction of GRR decoction pieces produced by fresh cutting were higher than those in the standard decoction of traditional decoction pieces， while the contents of ginsenoside Rc ， Rb2 and Rd were comparable between the two standard decoctions. Compared with the standard decoction of the traditional decoction pieces， the average transfer rates of ginsenoside Rg1， Rb1， Rc， Rb2 and dry extract rate of the standard decoction of GRR decoction pieces produced by fresh cutting were significantly increased（P<0.05）， and the average transfer rate of ginsenoside Re and Rd also increased， but the difference was not statistically significant. ConclusionThe dry extract rate， content and transfer rate of index components of standard decoction of GRR decoction pieces produced by fresh cutting are better than those of the standard decoction of traditional decoction pieces， which can provides data support for the subsequent clinical application of fresh cutting products.

Ivy Leaf Dry Extract EA 575® Has an Inhibitory Effect on the Signalling Cascade of Adenosine Receptor A2B.

Ivy leaf dry extract EA 575® is used to improve complaints of chronic inflammatory bronchial diseases and acute inflammation of the respiratory tract accompanied by coughing. Its mechanism of action has so far been explained by influencing ß2-adrenergic signal transduction. In the present study, we investigated a possible influence on adenosine receptor A2B (A2BAR) signalling, as it has been described to play a significant and detrimental role in chronic inflammatory airway diseases. The influence of EA 575® on A2BAR signalling was assessed with measurements of dynamic mass redistribution. Subsequently, the effects on A2BAR-mediated second messenger cAMP levels, ß-arrestin 2 recruitment, and cAMP response element (CRE) activation were examined using luciferase-based HEK293 reporter cell lines. Lastly, the impact on A2BAR-mediated IL-6 release in Calu-3 epithelial lung cells was investigated via the Lumit™ Immunoassay. Additionally, the adenosine receptor subtype mediating these effects was specified, and A2BAR was found to be responsible. The present study demonstrates an inhibitory influence of EA 575® on A2BAR-mediated general cellular response, cAMP levels, ß-arrestin 2 recruitment, CRE activation, and IL-6 release. Since these EA 575®-mediated effects occur within a time frame of several hours of incubation, its mode of action can be described as indirect. The present data are the first to describe an inhibitory effect of EA 575® on A2BAR signalling. This may offer an explanation for the beneficial clinical effects of the extract in adjuvant asthma therapy.

Development and Characterization of New Green Propolis Extract Formulations as Promising Candidates to Substitute for Green Propolis Hydroalcoholic Extract.

The technologies used to produce the different dosage forms of propolis can selectively affect the original propolis compounds and their biological activities. The most common type of propolis extract is hydroethanolic. However, there is considerable demand for ethanol-free propolis presentations, including stable powder forms. Three propolis extract formulations were developed and investigated for chemical composition and antioxidant and antimicrobial activity: polar propolis fraction (PPF), soluble propolis dry extract (PSDE), and microencapsulated propolis extract (MPE). The different technologies used to produce the extracts affected their physical appearance, chemical profile, and biological activity. PPF was found to contain mainly caffeic and p-Coumaric acid, while PSDE and MPE showed a chemical fingerprint closer to the original green propolis hydroalcoholic extract used. MPE, a fine powder (40% propolis in gum Arabic), was readily dispersible in water, and had less intense flavor, taste, and color than PSDE. PSDE, a fine powder (80% propolis) in maltodextrin as a carrier, was perfectly water-soluble and could be used in liquid formulations; it is transparent and has a strong bitter taste. PPF, a purified solid with large amounts of caffeic and p-Coumaric acids, had the highest antioxidant and antimicrobial activity, and therefore merits further study. PSDE and MPE had antioxidant and antimicrobial properties and could be used in products tailored to specific needs.

Micronized Palmitoylethanolamide, Hempseed Oil, and Maritime Pine Bark Dry Extract (Pelvipea®) for Pelvic Pain: An In Vitro Study for Urothelial Inflammation Treatment.

Urothelial inflammation plays a key role in the pathogenesis of chronic pelvic pain due to its origin in the bladder. The aim of this study was to evaluate the efficacy of a patent-pending formulation (Pelvipea®) composed of micronized palmitoylethanolamide (PEA), hempseed oil, and maritime pine bark dry extract in reducing urothelial inflammation, as well as the effect of each ingredient individually, in order to define the synergistic effect of the three ingredients. An in vitro bladder urothelium model composed of the T24 cell line was exposed to a conditioned media obtained by treating macrophage-differentiated THP-1 cells with different concentrations of the functional ingredients and a mixture of them in the presence of the pro-inflammatory stimulus of Escherichia coli. Cells exposed only to the inflammatory stimulus in the absence of pre-treatment were considered as a positive control for inflammation. The impact of each functional ingredient and their mixture on inflammation was evaluated by the determination of transcription factor NF-kB and of pro-inflammatory cytokine expression. Statistical analysis was performed using the t-test, comparing the mixture and the single ingredients for every condition tested. All results were reported as fold change (mean ± standard deviation), the ratio between the values obtained from the respective treatments for inflammation control. The three functional ingredients did not induce negative effects on THP-1 cell vitality. The levels of NF-kB were reduced following treatment with hempseed oil, maritime pine bark dry extract, and the mixture at all tested concentrations, and with micronized PEA from 25 to 200 µg/mL. Treatment with the mixture resulted in the lowest expression levels of interleukins (IL)-1ß, IL-6, and IL-8 compared to the single functional ingredients at a concentration of 230 µg/mL, with values of 0.08 (±0.00), 0.01 (±0.00), and 0.32 (±0.01), respectively. The mixture of micronized PEA, hempseed oil, and maritime pine bark dry extract (Pelvipea®) at 230 µg/mL showed the best efficacy in urothelial IL-1ß, IL-6, and IL-8 reduction compared with the singular components. This formulation may represent a promising therapeutic option to relieve painful symptoms originating in the bladder. However, in vivo studies are needed to confirm these results.

Olive juice dry extract containing hydroxytyrosol, as a nontoxic and safe substance: Results from pre-clinical studies and review of toxicological studies.

Products derived from olives, such as the raw fruit and oils, are widely consumed due to their taste, and purported nutritional/health benefits. Phenolic compounds, especially hydroxytyrosol (HT), have been proposed as one of the key substances involved in these effects. An olive juice extract, standardized to contain 20% HT ("OE20HT"), was produced to investigate its health benefits. The aim of this study was to demonstrate the genotoxic safety of this ingredient based on in vitro Ames assay and in vitro micronucleus assay. Results indicated that OE20HT was not mutagenic at concentrations of up to 5000 µg/plate, with or without metabolic activation, and was neither aneugenic nor clastogenic after 3-hour exposure at concentrations of up to 60 µg/mL with or without metabolic activation, or after 24-hour exposure at concentrations of up to 40 µg/mL. To further substantiate the safety of OE20HT following ingestion without conducting additional animal studies, a comprehensive literature review was conducted. No safety concerns were identified based on acute or sub-chronic studies in animals, including reproductive and developmental studies. These results were supported by clinical studies demonstrating the absence of adverse effects after oral supplementation with olive extracts or HT. Based on in vitro data and the literature review, the OE20HT extract is therefore considered as safe for human consumption at doses up to 2.5 mg/kg body weight/day.

Hypoglycemic effect of the dry leaf extract of Myrcia multiflora in streptozotocin-induced diabetic mice.

ETHNOPHARMACOLOGICAL RELEVANCE: Myrcia multiflora (Lam) DC. is a medicinal plant used in folk medicine for diabetes control, mainly in the Brazilian Amazon. The leaves of this species has already demonstrated antidiabetic properties; however, in mice with type 2 diabetes (DM2), the cumulative effect of the consumption of the dry extract of M. multiflora leaves (Mm) has not yet been reported. AIM OF THE STUDY: To investigate the effect of the dry extract obtained from the infusion of the dried leaves of M. multiflora on the blood glucose levels of diabetic mice. MATERIALS AND METHODS: DM2 was induced in Swiss male mice by a single intraperitoneal injection of streptozotocin [150 mg/kg body weight (bw)]. The animals were divided into two control groups (healthy and diabetic without treatment) and three sample groups that received Mm (25 and 50 mg/kg bw) and acarbose (200 mg/kg bw) by gavage once daily for 28 days (D28). Additionally, biochemical parameters, thiobarbituric acid reactive species (TBARS) levels in the liver, and histopathological analyses of the kidneys and liver were performed. RESULTS: On the seventh day of treatment, a 74.7% reduction in glucose levels were observed in the group of diabetic animals treated with Mm (50 mg/kg bw) when compared to the beginning of the treatment. At D28, the hypoglycemic effect was maintained. The results of the biochemical and histopathological parameters and the TBARS levels suggest that this dry extract exerts nephro- and hepatoprotective effects. CONCLUSIONS: The findings demonstrate the potential that this extract has to inhibit the α-glucosidase enzyme, and it acts similarly to the positive control acarbose. Furthermore, this extract is nephro- and hepatoprotective. Therefore, this dry extract has the potential to be an adjuvant for DM2, which corroborates its use in folk medicine.

Analysis of Formulation and Characteristics of Provincial Standards for Traditional Chinese Medicine Dispensing Granules / 中国实验方剂学杂志

In order to standardize the quality control of traditional Chinese medicine（TCM） dispensing granules， the Chinese Pharmacopoeia Commission has promulgated and implemented 200 national drug standards for TCM dispensing granules， but there are still varieties of TCM dispensing granules without unified standards. Many provinces have actively invested in the formulation of provincial standards for TCM dispensing granules to make up for the gaps in standards for varieties of traditional Chinese medicine dispensing granules other than the national standards. By the end of July 2022， 29 provincial-level administrative regions have successively promulgated and implemented a total of 5 602 provincial standards for TCM dispensing granules， involving more than 400 varieties. In order to better understand the formulation and characteristics of provincial standards， this study took 105 provincial standards that have been promulgated and implemented in Henan province as an example， and comprehensively analyzed the formulation and characteristics through quality control indicators such as dry extract rate of raw materials， contents of index components and their transfer rates， specifications and so on. The formulation and characteristics of the same TCM dispensing granules in the provincial standards of different provinces were further analyzed， in order to provide reference for the formulation of provincial standards of TCM dispensing granules and the implementation of national standards.

EFFECT OF DRY EXTRACT FROM REISHI MUSHROOMS ON THE STATE OF ANTIOXIDANT SYSTEM IN RATS WITH DMH-INDUCED COLON CARCINOGENESIS.

OBJECTIVE: The aim: To study pro- and antioxidant systems indicators in rats with chemically induced colon carcinogenesis on the background of the reishi mushrooms dry extract use. PATIENTS AND METHODS: Materials and methods: The study was performed on 120 white male rats. Chronic oncogenic intoxication was modeled by administering 1,2-dimethyl¬hydrazine (DMH) hydrochloride for 30 weeks (1 time per week). A dry extract from the reishi mushrooms was administered intragastrically daily at a dose of 100 mg/kg of the animal's body weight. Blood and liver samples were taken for research monthly. The state of the pro- and antioxidant systems was studied by the content of oxidative modification of proteins products, superoxide dismutase and catalase activity, contents of reduced glutathione and ceruloplasmin. RESULTS: Results: An increase in the activity of free radical oxidation processes after DMH-induced colon carcinogenesis in rats is evidenced by a decrease in the super-oxide dismutase activity, catalase activity, content of reduced glutathione, an increase in the content of ceruloplasmin and products of oxidative modification of proteins in the blood serum and liver of animals. The effectiveness of the dry extract of reishi mushrooms and its positive effect on the state of pro- and antioxidant systems was experimentally proved. CONCLUSION: Conclusions: The use of the dry extract of reishi mushrooms under conditions of DMH-induced colon carcinogenesis in rats led to normalization of the anti¬oxidant protection system state and the reduction of oxidative stress.

A new direct compression mechanism of structural transition in Poria cocos extract composite particles.

The structural transition to generate amorphous translucent grains in Poria cocos dry extract (PCE) composite particles was found and studied as a new direct compression mechanism. The pressure and displacement sensing techniques were used to obtained stress-strain profiles during compression. The Exponential function, Kawakita model, Shapiro model and Heckel model were used to analysis mechanical properties of powders. 12 parameters derived from compression models and powder physical properties were applied to partial least squares method (PLS) for analyzing powder compression mechanism. It was found that only the oven-dried PCE composite particles undergoes the structural transition and generate translucent grains scattered and embedded in tablet, and these tablets have excellent mechanical stability. The structural transition in plant dry extract as the PCE composite particles could be exploited to improve powder compression and tabletability.

Hypoglycemic effect and toxicity of the dry extract of Eugenia biflora (L.) DC. leaves.

ETHNOPHARMACOLOGICAL RELEVANCE: The leaves of Eugenia biflora (Myrtaceae) are traditionally used by Amazonian populations for the control of diabetes. However, their chemical composition has not yet been described and pharmacological evidence has not been reported. OBJECTIVE: This study aimed to identify the chemical constituents and evaluate the hypoglycemic and toxic effect of the dry extract of the E. biflora leaves (DEEB). MATERIALS AND METHODS: DEEB, obtained by infusion, was analyzed using LC-HRMS and NMR, whose the catechin flavonoid was quantified using NMR. The antidiabetic effect of DEEB was evaluated according to its inhibition of the enzymes α-amylase and α-glucosidase, as well as the content of total phenols, free radical scavengingand antiglycation activities, and its in vitro cell viability. Oral maltose tolerance and chronic multiple dose tests (28 days) in streptozotocin-induced diabetic mice (STZ) were performed. The hypoglycemic effect and toxicity of this extract were evaluated in the multiple dose assay. Biochemical parameters, hemolysis, and levels of the thiobarbituric acid reactive species in the liver were investigated and histopathological analyses of the kidneys and liver were performed. RESULTS: Eight phenolic compounds were identified, with catechin (15.5 ± 1.7 mg g-1) being the majority compound and a possible chemical marker of DEEB. The extract showed inhibition activity of the enzyme α-glucosidase. Chronic administration of DEEB (50 mg/kg of body weight) reduced glucose levels in diabetic animals, similar to acarbose; however, DEEB (100 and 200 mg/kg bw) caused premature death of mice by D22 of the treatment. Our data indicate that one of the mechanisms of toxicity in DEEB may be related to the aggravation of oxidative stress in the liver. This histopathological study indicated that DEEB failed to minimize the progression of the toxicity of diabetes caused by STZ. CONCLUSIONS: This study demonstrated the hypoglycemic potential of E. biflora leaves. However, the prolonged use of this tea can be harmful to its users due to its considerable toxicity, which needs to be better investigated.

Association between ivy leaves dry extract EA 575 prescriptions and antibiotic use, sick leave duration, and repeated infections in adult patients.

OBJECTIVES: The present study aimed to analyze the association between the prescription of ivy leaf dry extract EA 575 (licensed under the trade name Prospan® in Germany) and the incidence of antibiotic use, incident bacterial complications, and days of sick leave in adult patients with cold diseases. METHODS: This retrospective cohort study was based on the IQVIA Disease Analyzer database and included adult patients from 1032 general practices in Germany with a documentation of common cold between 2017 and 2020 (index date) and prescription of either EA 575 or an antibiotic drug within 3 days after index date. 1:1 propensity score matching based on age, sex, index month, physician, health insurance status, and the Charlson Comorbidity Index was carried out. Univariable regression models were used to investigate the association between EA 575 prescription and defined outcomes. RESULTS: Data of 7034 patients treated with EA 575 and 7034 matched patients receiving an antibiotic were available. EA 575 prescription was associated with significantly lower odds of an antibiotic prescription in the time periods of 4-30 days (OR: 0.83; 95% CI: 0.72-0.96) and 31-365 days (OR: 0.44; 95% CI: 0.40-0.48) after the index date. EA 575 prescription was significantly associated with a lower rate of sick leave of more than 7 days (33.0% vs. 37.7%, OR: 0.81; 95% CI: 0.73-0.90) in patients with any sick leave, as well as with lower odds of a new cough diagnosis (OR: 0.91, 95% CI: 0.85-0.98) when compared to antibiotic prescription. CONCLUSION: Our study provides further evidence that the use of phytopharmaceuticals, in particular ivy leaf dry extract EA 575, could contribute to a reduction in the number of inappropriate antibiotic prescriptions for respiratory infection with cough symptoms.

Ivy leaves dry extract EA 575® mediates biased ß2-adrenergic receptor signaling.

BACKGROUND: ß2-adrenergic receptor (ß2-AR) stimulation activates the G protein/cAMP pathway, which is opposed by the GRK2/ß-arrestin 2 pathway. The latter is undesirable in the treatment of respiratory diseases. HYPOTHESIS/PURPOSE: EA 575® is capable of mediating a biased ß2-adrenergic signaling pathway. METHODS: The impact of the ivy leaves dry extract EA 575® on ß2-adrenergic signaling was tested in a dynamic mass redistribution assay in HEK wild-type and in HEK ß-arrestin knock-out cells. cAMP formation and recruitment of ß-arrestin 2 were investigated using GloSensor™ and PathHunter® assays, respectively. NFκB transcriptional activity was determined in both HEK wild-type as well as HEK ß-arrestin knock-out cells. RESULTS: EA 575® inhibits the recruitment of ß-arrestin 2 and thereby enhances G protein/cAMP signaling under ß2-stimulating conditions, as evidenced by a corresponding increase in cAMP formation. While ß2-AR-mediated inhibition of NFκB transcriptional activity is ß-arrestin-dependent, EA 575® leads to significant inhibition of NFκB transcriptional activity in ß-arrestin knock-out cells and thus via a ß-arrestin-independent signaling pathway. CONCLUSION: EA 575® is the first active phytopharmaceutical ingredient for which biased ß2-adrenergic activation has been described. This shift towards G protein/cAMP signaling provides the molecular basis for the clinically proven efficacy of EA 575® in the treatment of lower respiratory tract diseases. In this light, EA 575® could potentially reduce ß-arrestin-mediated adverse effects in new combinatorial therapeutic approaches.

Safety and efficacy of a feed additive consisting of a dried extract from the roots of Panax ginseng C.A. Meyer (P. ginseng dry extract) for use in cats and dogs (C.I.A.M.).

Following a request from the European Commission, the EFSA Panel on Additives and Products or Substances used in Animal Feed (FEEDAP) was asked to deliver a scientific opinion on the safety and efficacy of a dried extract prepared from the roots of Panax ginseng C.A. Meyer (P. ginseng dry extract) when used as a sensory additive in feed for cats and dogs. P. ginseng dry extract is specified to contain at least 27-30% total ginsenosides (as ginsenosides RG1). Since uncertainty remains concerning the nature of up to 73% of the extract, the FEEDAP Panel was unable to conclude on the safety of the additive at the proposed use levels of up to 20 mg/kg complete feed for cats and dogs. In the absence of data, no conclusions can be drawn on the safety for the user. Since ginseng and its extracts are recognised to flavour food and their function in feed would be essentially the same as that in food, no further demonstration of efficacy is considered necessary.

Safety and efficacy of a feed additive consisting of a dried extract from the leaves of Ginkgo biloba L. (G. biloba dry extract) for use in cats and dogs (C.I.A.M.).

Following a request from the European Commission, the EFSA Panel on Additives and Products or Substances used in Animal Feed (FEEDAP) was asked to deliver a scientific opinion on the safety and efficacy of a dried extract prepared from the leaves of Ginkgo biloba L. (G. biloba dry extract) when used as a sensory additive in feed for cats and dogs. G. biloba dry extract is specified to contain at least 24% flavonol glycosides, at least 6% terpene lactones and less than 5 ppm ginkgolic acids. Since uncertainty remains concerning the nature of up to 75% of the extract, the additive is not sufficiently characterised to allow an assessment based on the individual components. In view of the indication of potential carcinogenicity from the results of studies by the National Toxicology Program of the USA, obtained with a G. biloba extract comparable with the additive under assessment, the FEEDAP Panel concludes that the additive cannot be considered safe for cats and dogs. In the absence of data, no conclusions can be drawn on the safety for the user. In the absence of evidence that the extract acts as a flavour in animal feed or has an effect on palatability, the FEEDAP Panel was unable to conclude on the efficacy of the additive.

Safety and efficacy of a feed additive consisting of a dried extract from the roots of Arctium lappa L. (A. lappa dry extract) for use in cats and dogs (C.I.A.M.).

Following a request from the European Commission, the EFSA Panel on Additives and Products or Substances used in Animal Feed (FEEDAP) was asked to deliver a scientific opinion on the safety and efficacy of a dried extract prepared from the roots of Arctium lappa L. (A. lappa dry extract) when used as a sensory additive (flavouring compound) in feed for cats and dogs. A. lappa dry extract is specified to contain at least 2% inulin. Since uncertainty remains concerning the nature of up to 77% of the additive, the FEEDAP Panel was unable to conclude on the safety of the extract at the proposed use levels of up to 40 mg/kg complete feed for cats and dogs. In the absence of data, no conclusions can be drawn on the safety for the user. In the absence of convincing evidence that the extract acts as a flavour in animal feed or has an effect on palatability, the FEEDAP Panel was unable to conclude on the efficacy of the additive.

Phytochemical and Psychotropic Research of Motherwort (Leonurus cardiaca L.) Modified Dry Extracts.

The prospect of creating a new medicine with psychotropic activity is shown as a result of studying the chemical composition and pharmacological activity of modified dry extracts of motherwort (Leonurus cardiaca L.) tincture. The most promising substances were the dry extracts, modified by adding small amounts of arginine, valine, phenylalanine, glycine, lysine, and alanine. A total of 15 main phenolic substances were found in the extracts, and eight of them were identified. There were also 10 hydroxycinnamic acids in these extracts, three of which were identified (chlorogenic, caffeic, and rosmarinic acids). The dominant hydroxycinnamic acids were chlorogenic and caffeic acids. Among flavonoids, catechin, hyperoside, and rutin were identified. It should be noted that the extracts had a significant content of ellagic acid. On the basis of the results of the phytochemical analysis of the extracts, it can be concluded that the composition of phenolic compounds does not differ significantly, and the main differences are related to amino acids, which obviously have an impact on the overall pharmacological effect. The results obtained indicate the presence of anxiolytic activity in the motherwort extracts studied in complex with amino acids. The extracts with glycine, valine, and arginine were more effective in reducing anxiety in animals.

Analysis on Quality Transmitting of Substance Benchmarks of Yihuangtang / 中国实验方剂学杂志

Objective:To explore the quality transmitting relationship between decoction pieces and substance benchmarks with the fingerprint， index component content and dry extract rate as evaluation indexes， and investigate the key quality attributes of 15 batches of substance benchmarks of Yihuangtang， and establish the quality standard of this substance benchmarks. Method:Fifteen batches of Yihuangtang substance benchmarks freeze-dried powder samples were prepared， the fingerprint and index component content of 15 batches of decoction pieces and substance benchmarks were determined by high performance liquid chromatography （HPLC）， the mobile phase was acetonitrile （A）-0.1% phosphoric acid aqueous solution （B） for gradient elution （0-6 min， 97%B； 6-12 min， 97%-92%B； 12-25 min， 92%-90%B； 25-35 min， 90%-89%B； 35-50 min， 89%-82%B； 50-75 min， 82%-72%B； 75-85 min， 72%-35%B）， the detection wavelength was set at 230 nm， combined the dry extract rate to clarify the attribution of characteristic peaks and the range of similarity with the control chromatogram， the content range and transfer rate range of geniposidic acid and berberine hydrochloride， the dry extract rate range and the variation range of the substance benchmarks. Result:The established HPLC fingerprint had good precision， repeatability and stability， and could be used for the simultaneous determination of decoction pieces and substance benchmarks of Yihuangtang. The similarities between the control chromatogram and fingerprint of substance benchmarks were >0.99. A total of 15 characteristic peaks were assigned， and 8 characteristic peaks were identified by the reference substances， of which 6 were from Phellodendri Chinensis Cortex processed with salt， 1 was from Plantaginis Semen processed with wine， and 1 was from stir-fried Dioscoreae Rhizoma. The content ranges of geniposidic acid and berberine hydrochloride in 15 batches of substance benchmarks of Yihuangtang were 0.10%-0.16% and 0.63%-1.05%， the transfer rate ranges of them were 20.91%-32.65% and 19.60%-29.59%， respectively. The dry extract rate range of the substance benchmarks was 8.45%-9.92%. Conclusion:The quality standard of Yihuangtang substance benchmarks can be preliminarily formulated by the combination of fingerprint， dry extract rate and determination of index component， which can provide the basis for the quality control of Yihuangtang and the development of related preparations.