Water Decoction Research Articles

Mechanism of Euodiae Fructus stir-fried with water decoction of Coptidis Rhizoma in treatment of chronic colitis based on UPLC-Q-TOF-MS, network pharmacology and experimental verification

To elucidate the mechanism of Euodiae Fructus stir-fried with water decoction of Coptidis Rhizoma in the treatment of chronic colitis, this study employed ultra performance liquid chromatography-quadrupole time-of-flight mass spectrometry(UPLC-Q-TOF-MS), network pharmacology, and experimental verification to predict the involved targets and signaling pathways. The chronic colitis mouse model was constructed to verify the core targets. A total of 48 compounds in the herbal medicine were identified by UPLC-Q-TOF-MS. SwissTargetPrediction was used to screen the potential active components and drug targets. GeneCards, OMIM, PharmGKB, and TDD were used to search for the disease targets. A total of 31 active ingredients, 453 targets of the herbal medicine, and 3 960 targets of chronic colitis were obtained. The common targets shared by the herbal medicine and chronic colitis were introduced into STRING to construct the protein-protein interaction(PPI) network, and CytoNCA plug-in was used to screen the key targets. A total of 90 key targets were obtained, and the key active components included isorhamnetin, quercetin, limonin, and oxyberberine. GO annotation and KEGG pathway enrichment for the key targets were carried out via DAVID. The targets were mainly involved in the positive regulation of protein phosphorylation, positive regulation of nitric oxide biosynthetic process, and negative regulation of apoptotic process. The medicine may treat chronic colitis through PI3 K-Akt, VEGF, HIF-1, and TNF signaling pathways. A mouse model of chronic colitis was established and then treated with Euodiae Fructus stir-fried with the water decoction of Coptidis Rhizoma. The experimental results demonstrated that the medicine can alleviate the pathological damage of colon, significantly reduce the levels of IL-1β, IL-6, and TNF-α, inhibit the activation of PI3 K/Akt pathway, and down-regulate the expression of VEGFA in the treatment of chronic colitis.

Investigation of the potential curative effects of Gui-Zhi-Jia-Ge-Gen decoction on wind-cold type of common cold using multidimensional analysis

Ethnopharmacological relevanceGui-Zhi-Jia-Ge-Gen decoction (GJGD) is a classical Chinese medicine prescription that has been widely used in clinical practice for centuries. In recent times, TCM has received considerable attention for its potential efficacy in treating a wind-cold type of common cold. However, the effect of the Gui-Zhi-Jia-Ge-Gen decoction on the wind-cold type of common cold is still not fully understood, which presents challenges for both quality control, research and development. Furthermore, the identification of potential pharmacodynamic ingredients (PPIs) is important for developing quality control procedures for industrial and large-scale production. Aim of the studyThe aim of this study was to investigate the potential curative effect of Gui-Zhi-Jia-Ge-Gen decoction on wind-type of common cold using multidimensional qualitative analysis that combined water-decoction spectrums, in vivo plasma spectrums, and molecular docking to identify key constituents of GJGD. Materials and methodsWater-based GJGDs were formulated according to the clinical usage documented in ancient medical texts. Ultra-high-performance liquid chromatography-quadrupole-time of flight mass spectrometry (UHPLC-Q-TOF-MS) was combined with computer-aided modeling screening to identify GJGD PPIs in rats following oral administration. Molecular docking experiments were carried out to predict the binding affinity of the PPIs to tumor necrosis factor α (TNF-α), interleukin 6 (IL-6), and interleukin-1β (IL-1β). Finally, the active ingredients of GJGD were further validated through pharmacodynamic experiments by assessing their efficacy in treating a wind-cold type of common cold in rats. ResultsA total of 61 compounds were identified in the GJGD, 8 of which were detected in rat blood samples, providing stronger evidence for PPIs. Molecular docking also confirmed that these 8 compounds had a better affinity for TNF-α, IL-6, and IL-1β. In animal studies, various doses of the GJGD groups and the positive control groups caused significant elevations (P < 0.05) in the levels of white blood cell count and lymphocyte ratio and caused a significant decrease (P < 0.05) in the monocyte ratio and neutrophilic granulocyte ratio compared to the model group. Organ indexes of the GJGD treated groups were higher than the model group (P < 0.05). Significant neutrophil infiltration, hemorrhage, compensatory vacuole, and interstitium proliferation were observed in the lung tissue of the model group. However, the lung tissues of the various dose groups that received GJGD showed a near normal appearance, except for slight thickening, interstitium proliferation, and compensatory vacuole in some areas. The GJGD was found to be effective against a cold-wind type of common cold, which is in accordance with molecular docking studies suggesting that GJGD may be effective against a cold-wind type of common cold. Finally, based on multidimensional analysis, 8 potential compounds in GJGD were identified as PPIs (puerarin, 3′-hydroxy puerarin, 3′- methoxy puerarin, daidzin, cinnamic acid, paeoniflorin, liquiritin, and glycyrrhizic acid). ConclusionThe present study combined water decoction spectral analysis, molecular docking, and in vivo blood plasma spectrum analysis to develop a multidimensional qualitative approach for the development of GJGD and to assess its effectiveness in a wind type of common cold in Sprague Dawley rats. Meanwhile, 8 compounds in the GJGD were identified as PPIs in this study, which may be useful in developing quality standards for complex TCM prescriptions.

Integrated metabolism, network pharmacology, and pharmacokinetics to explore the exposure differences of the pharmacodynamic material basis in vivo caused by different extraction methods for Saussurea involucrata

Ethnopharmacological relevanceSaussurea involucrata Kar.et Kir. (S.I.) has long been used as a precious national medicine and clinically proven to be an effective treatment for rheumatoid arthritis (RA) and cardiovascular diseases. In clinical practice, two extraction methods of S.I., including water decoction and alcohol extraction, are prescribed to treat the same conditions. Nevertheless, no study has been performed on the exposure differences of the pharmacodynamic material basis in vivo caused by different extraction methods. Aim of the studyBased on the integrated strategy of metabolism, network pharmacology, and pharmacokinetics, we aimed to reveal exposure differences in pharmacodynamic substances caused by different extraction methods. Materials and methodsUltra-high-performance liquid chromatography-high-resolution mass spectrometry (UPLC-HRMS) was employed to identify the chemical constituents of S.I. extracts and the metabolites in vivo after administration. Based on the analysis of prototype components in vivo, the major exposure active constituents, potential therapeutic targets and possible pharmacological mechanisms in RA treatment were investigated using network pharmacological analysis. Seven critical active components, including quercetin, hispidulin, apigenin, chlorogenic acid, arctigenin, syringin, and umbelliferone, were quantitatively compared between the alcohol, and aqueous extraction methods, which had been confirmed by the reference substance. ResultsThe chemical comparison demonstrated that the types of chemicals in the two extracts were identical, mainly flavonoids, phenylpropanoids, coumarins, lignins, sesquiterpene lactones, and others, but the contents of the primary constituents in the aqueous extract were lower than those of the alcohol extract. A total of 30 prototype components and 174 metabolites were analyzed and identified in rat plasma, urine, fecal, and bile samples. Twenty-three prototype components were analyzed by network pharmacology, and seven critical active components were selected as representative markers for the pharmacokinetic study. Pharmacokinetic studies had shown that the Tmax values of apigenin, hispidulin, chlorogenic acid, arctigenin, and syringin after the oral administration of the alcohol extract were lower than those after the oral administration of the aqueous extract, and the above components in the alcohol extract could increase the absorption. Compared with the aqueous extract group, the Tmax and T1/2 of quercetin and umbelliferone were longer; it was suggested that alcohol extraction might have a slow-release and long-term effect on these two components. The relative bioavailability of apigenin, hispidulin, quercetin, chlorogenic acid, and umbelliferone in the alcohol extract group were higher than those in the aqueous extract group, which was consistent with the traditional clinical experience that alcohol extract could improve the efficacy of S.I. ConclusionsThe major exposure active constituents in vivo were screened. The representative components that could be used in pharmacokinetics were determined by integrating network pharmacology and metabolism studies. The critical active compounds were quantitatively compared between the alcohol and aqueous extraction methods. This study clarified that flavonoids, coumarin, and phenylpropanoids might be the primary material basis that caused the exposure differences between aqueous and alcoholic extracts from S.I.. This research aimed to provide the basis of metabolism in vivo for further studying these pharmacodynamic differences.

Integrated systematic pharmacology analysis and experimental validation to reveal the mechanism of action of Semen aesculi on inflammatory bowel diseases

Background and ethnopharmacological relevanceSemen aesculi (SA), a traditional Chinese herb, has been used in the treatment of gastrointestinal disease for thousands of years. The escin was the main components of SA. A growing number of research showed that escin has a wide range of pharmacological activities in intestinal barrier dysfunction. Aim of the studyInflammatory bowel diseases (IBD) are an idiopathic disease of the intestinal tract with the hallmark features of mucosal inflammation and loss of barrier function. The theory of traditional Chinese medicine (TCM) suggests that SA plays a potential role in protecting the gastrointestinal diseases. The present study aimed to explore the effects of SA on the intestinal barrier under existing inflammatory conditions and elucidate underlying mechanisms. Materials and methodsThe bioactive components of SA and their predicted biological targets were combined to develop a compound target pathway network. It is used to predict the bioactive components, molecular targets, and molecular pathways of SA in improving IBD. The ingredients of SA were extracted by decoction either in water and ethanol and separated into four fractions (AE, EE, PEE and PCE). The effects of extractions were evaluated in the lipopolysaccharide (LPS)-induced RAW264.7 macrophages cell model, LPS-induced intestinal barrier injury model and imodium-induced constipation model. The high-performance liquid chromatography (HPLC) analysis was performed to identify the bioactive components. ResultsThe compound-target pathway network was identified with 10 bioactive compounds, 166 IBD-related targets, and 52 IBD-related pathways. In LPS-induced RAW264.7 cells, PEE and PCE significantly decreased nitric oxide (NO) production and TNF-α level. In mice, PEE and PCE administration improved intestinal barrier damage, increased intestinal motility, reduced levels of TNF-α and diamine oxidase (DAO). Furthermore, PEE and PCE administration not only decreased expression of p-Akt, p-IκBα, nuclear p-p65, and TNF-α level, but also increased expression of the zonula occludin-1 (ZO-1) in LPS-induced intestinal barrier injury model. The escin content of AE, EE, PEE and PCE gradually increased with an increase of the bioactivity. ConclusionsEscin was the main bioactive components of SA. The effects of SA on IBD were mediated by repairing the intestinal barrier and promoting intestinal motility. The mechanism of action of SA is related to inhibiting the Akt/NF-κB signaling pathway in intestinal tissue, at least, in part. Our results provide a scientific basis for further exploring the mechanisms involved in the beneficial effects of SA in IBD.

Influence of coexisting components in Coptidis Rhizoma on excretion of magnoflorine in rat bile, urine, and feces

Magnoflorine is an important aporphine alkaloid in Coptidis Rhizoma. As reported previously, coexisting components in Coptidis Rhizoma can change the pharmacokinetic characteristics of magnoflorine. To illustrate the interactional links of magnoflorine with its coexisting components in Coptidis Rhizoma, the present study investigated the influence of coexisting components in Coptidis Rhizoma on the excretion of magnoflorine in rat bile, urine, and feces. The rats were dosed with magnoflorine(30 mg·kg~(-1)) and water decoction of Coptidis Rhizoma(equivalent to 30 mg·kg~(-1) magnoflorine) via intragastric administration, and magnoflorine(10 mg·kg~(-1)) by intravenous administration, respectively, and the excretion of magnoflorine in rat bile, urine, and feces in 24 h was observed. The excretion rates of magnoflorine in bile and urine in 24 h were 0.90% and 37.11% respectively after intravenous administration of magnoflorine, which suggested that urination was the main excretive way of magnoflorine. The excretion rates of magnoflorine in feces were 8.77% and 6.18% respectively after intragastric administration of magnoflorine and water decoction of Coptidis Rhizoma, which indicated that defecation was the main excretion route of magnoflorine. The cumulative excretion rates of magnoflorine in the bile, urine, and feces in the Coptidis Rhizoma water decoction group were 77.78%, 79.44%, and 70.47% of those in the magnoflorine group. The results showed that the cumulative excretion rates of magnoflorine in rat bile, urine, and feces were not high, suggesting that magnoflorine was metabolized significantly in rats. The coexisting components of Coptidis Rhizoma could inhibit the excretion of magnoflorine in rat bile, urine, and feces, which was consistent with the decrease in the elimination rate of magnoflorine in the pharmacokinetics of Coptidis Rhizoma water decoction. It indicated interactions between drugs. This study is expected to provide references for the development of magnoflorine-containing new drugs and rational clinical medication of Coptidis Rhizoma.

Agarotetrol as an index for evaluating agarwood in crude drug products.

Agarotetrol in agarwood has been detected in water extracts or decoctions from medical use agarwood but the detection of agarotetrol has not been reported from other crude drugs. Agarwood generates the sedative benzylacetone upon heating. In this study, crude drug products containing many kinds of crude drugs in addition to agarwood were analyzed. Agarotetrol was detected and quantified, demonstrating that agarotetrol is useful for the quality evaluation of agarwood in complex prescriptions. High-performance liquid chromatography conditions to clearly separate agarotetrol from crude drug products were established and agarotetrol from Kampo decoctions was detected and quantified. Agarotetrol was also detected even from small crude drug product samples. These results suggest that agarotetrol is a useful component for the quality evaluation of agarwood in crude drug products.

Effect of extraction process on phytochemical composition and antioxidant properties of Rosmarius officinalis and Globularia alypum extracts

Rosmarinus officinalis and Globularia alypum are well known and commonly used in Algeria as species and medicinal plants. The composition and the biological activities of plants depend on several factors. We investigated the influence of one factor: the extraction process. Water and methanol (80%) were used as solvent in the extraction by infusion, decoction and cold maceration. The extracts were evaluated regarding yields, thin layer chromatography, phenolic content and antioxidant activity. Results showed that temperature increase plants extraction biomass efficiency (15.90% for rosemary and 28.10% for globular). Phytochemical screening of extracts revealed the presence of several phenolic classes, including flavonoids and tannins. In addition, G. alypum contains irridiods. Thin layer chromatography showed the presence of some phenolic compounds, particularly flavonoids, of which methanolic extracts gave the highest separation. Levels of total phenolics, flavonoïds and tannins were highly influenced by method and solvent system applied. Methanolic extracts were richest in flavonoïds (39.90 mg QE/g for rosmary and 17.97mg QE/g for globular). While, for both plants, higher concentrations of tannins were noted for aqueous extracts prepared by decoction (15.9 mg CE/g and 28.10 mg CE/g respectively). Regarding the antioxidant activity, the antiradical effect of the extracts against the DPPH radical was interesting with an IC50 between 0.024 and 0.33 mg/ml, noting that R. officinalis methanol extract was the most powerful. However, G. alypum extracts, presented a higher reductive power than rosemary. Aqueous extracts, were the most active, reaching optical densities of 1.41 for water infusion extract and 1.53 for water decoction extract.

Ethnopharmacological Study of the Medicinal Plants Used in the Treatment of Sickle Cell Anemia in the West Region of Cameroon.

Background Sickle cell anemia (SCA) or sickle cell disease (SCD) is a genetic disease associated with increased morbidity and mortality in Africa and other developing nations. Therefore, modern and traditional remedies are being introduced for use in the treatment and management of this disease. This is because safe, effective, and inexpensive therapeutic agents are urgently needed for the treatment of this disease in Africa and other developing nations. Objective The purpose of this study is to identify medicinal plant species commonly used by traditional healers in the treatment of sickle cell patients across some localities in the west region of Cameroon. Material and Methods. The ethnopharmacological survey was carried out in several districts within some localities of the western region of Cameroon. The survey was based on a semistructured questionnaire that was administered to 17 traditional healers and 62 sickle cell patients. It took place between November 2018 and March 2019. Personal information of participants and plant therapy data were gathered. Plants were identified at the National Herbarium of Cameroon. Literature review determined pharmacological effects and phytochemical compounds of the identified plants. Data were generally analysed using Epi Info 7 software for Windows. Results Twelve medicinal plant species belonging to 10 families are being used in the treatment of sickle cell anemia across the study sites. Euphorbiaceae is the dominant family with three plant species. Bark (39.3%) and seeds (35.7%) are the most used plant parts, which get administered through maceration, decoction, and chewing in water. According to the literature review, the identified plants have pharmacological effects and phytochemical compounds (especially polyphenols and alkaloids) that signify the presence of antioxidant compounds, which may possess an antisickling activity. There is therefore a need to conduct another study to scientifically validate (in vitro) antisickling properties of these plants. Conclusion This study has revealed promising medicinal plants that are currently applied in the traditional treatment of sickle cell anemia. Although still inconclusive, the association of pharmacological effects and phytochemical compounds with these medicinal plants justifies their use in traditional pharmacopoeia.

Current state of populations, resources, and biological activity Pulsatilla patens (Ranunculaceae) in Northern Kazakhstan

Abstract. Aidarkhanova GS, Kubentayev SA, Kukhar YV, Urazalina AS. 2022. Current state of populations, resources, and biological activity Pulsatilla patens (Ranunculaceae) in Northern Kazakhstan. Biodiversitas 23: 2311-2320. Pulsatilla (Ranunculaceae Juss.) is one of the complex groups in systematic and nomenclature terms, which has more than 30 taxa. Pulsatilla species are widely used against many pathologies. Anti-inflammatory, antibacterial, antifungal, antimicrobial, antimalarial, and antitumor properties of these plants are known. The object of our research was Pulsatilla patens (L.) Mill. (Ranunculaceae) from the allopathic complex P. patens with yellow flower color in the Northern regions of Kazakhstan. The article provides detailed information on environmental and biological features, morphology, geographical distribution, phylogenetic characteristics, and raw materials of P. patens in Northern Kazakhstan. In addition to these studies, the antimicrobial and fungicidal activity of extracts from leaves and roots of the species is shown. It was established that the species grows in 6 administrative regions of Central and Northern Kazakhstan and 7 floristic regions. In the studied region, P. patens are often found along rocky foothill terraces (mainly on the southern slopes), forest edges, along the southern slopes and tops of the hills of steppes, and among shrubs. Data on the study of P. patens biomorphology showed that quantitative parameters are characterized by the greatest intra- and inter-population variability CV (number of individuals per 1 m2 (38-69%); the number of basal leaves (44-61%); the number of generative shoots per bush (32-53%). Metric parameters such as height during flowering (17-27%), height during fruiting (12-18%), flower diameter (14-24%), leaf blade diameter (11-26%) are characterized by low and medium variability, both within the population and at the inter-population level. In the phenological aspect, the species begins to grow in the first half of April. Blooms from mid-April to early May. Bears fruit from the second half of May to early June. The complete end of vegetation falls at the end of September. Analysis of biological activity of stem extracts and leaves of P. patens of Kazakhstan population showed that they have pronounced fungicidal properties in relation to conditionally pathogenic yeast Candida parapsilosis and molds Aspergillus niger. Water decoction P. patens was also active against Escherichia coli, indicating that it has antibacterial properties.

Co-administration of Saffron and Chamomile Give Additive Effects of Antidiabetic and Antioxidant Activity with In vivo Augmentation of Brain BDNF, Acetylcholine Levels and Cognitive Functions in Streptozotocininduced Diabetic Rats

Objectives:Co-administration of chamomile and saffron is effective against diabetes and related complications.Background:Diabetes mellitus refers to comorbidities associated with reduced release of the brain-derived neurotropic factor and disruption in the metabolism of neurotransmitters leading to depression and cognitive impairment. Allopathic medications are available for the treatment of diabetes, but there is no cure and multiple adverse effects adhere to it. The therapeutic effects of co-administered chamomile with saffron may reverse diabetes and its complications.Methods:The present study sought to test the hypothesis, conducted on eighty Sprague-Dawley rats randomly divided into eight groups (n=10), including healthy controls, diabetic controls, methanolic extract treatment groups and water decoction treatment groups with respective dosage once a day for two weeks. The dose of a single herb group in methanolic extract and water decoction was saffron 10 mg/kg and chamomile 30 mg/kg, while co-administered groups received both herbs in half doses, saffron 5 mg/kg and chamomile 15 mg/kg. Two widely used tests for the assessment of memory (elevated plus maze and novel object recognition) were used to assess the mood and memory (cognitive) performance after the treatment.Results:It was observed that all treatment groups exhibited antidiabetic effects with improved mood and enhanced memory, high antioxidant profile, increased brain-derived neurotropic factor and acetylcholine concentration. However, the effects were greater in the co-administered groups of saffron and chamomile, especially the combined water decoction group.Conclusion :The study provides the successful results of co-administration of chamomile and saffron to alleviate diabetes and related complications.

THE EFFECTIVENESS OF THE DECOCTION OF RED BETEL LEAVES (PIPER CROCANTUM) AGAINST THE REDUCED SYMPTOMS OF FLUOR ALBUS IN ADOLESCENT GIRLS

Background: Fluor albus is excessive fluid from vagina that is not menstruation. To reduce the symptoms of fluor albus, non-pharmacological treatment from the decoction water of red betel leaves (Piper crocantum) was used in the present study. These red betel leaves (Piper crocantum) contain alkaloids that the green betel leaves do not have, and the alkaloids play a role as an antimicrobial agent. Besides, the red betel leaves have antiseptic power that is twice higher than the green betel leaves. The red betel leaves (Piper crocantum) also contain carvakrol which is anti-fungal and disinfectant, and it that can be used as an antiseptic medicine to maintain oral cavity health, cure fluor albus disease, and alleviate bad odor. Purpose: The present study aims to discover the effectiveness of the decoction of red betel leaves in reducing the fluor albus symptoms. Method: This study uses quasi-experimental research design with one group undertaking pre- and post-tests. It involved 20 adolescent girls of Al-Adzkia Sentul Boarding School in which the sample was taken using purposive sampling techniques. Further, a closed ended questionnaire is used to collect data, then analyzed using paired t-test. Result: The results showed a meaningful difference before being given treatment for 13.40. After treatment the value became 8.27 with a p-value &lt; of α (0.005). Conclusion: The results this study indicated a decrease in symptoms of vaginal discharge after the use of red betel leaf decoction and recommended it to be used as a form of non-pharmacological therapy or traditional medicine in reducing fluor albus symptoms in adolescent girls.

Soursop Leaf Water Decoction Against Decreased Uric Acid Levels in Menopause

Menopausal women are 60% more likely to develop gout, this is caused by a decrease in levels of the hormone estrogen which causes uncontrolled uric acid disposal. Gout sufferers who continue to take analgesic drugs will cause side effects that are berbahaya so that nonpharmacological treatment is needed. One of the nonpharmacological treatments is the provision of soursop leaf water decoction. The purpose of this study was to find out the effect of giving soursop leaf water decoction on the decrease in uric acid levels in menopausal mothers in Limba B Village of Gorontalo City. This research method uses pre-experiments with the design of one group pre-test-post-test. With a study population of 35 people and a sample of 15 people taken using purposive sampling techniques. The results of the research analysis used the Paired Sample T-Test which showed that there was an effect of giving soursop leaf water decoction before and after being given soursop leaf water decoction. with a value of p = 0.000 (&lt;0.05) which means H0 is rejected and Ha is accepted. Based on the results of research it can be concluded that the decoction of soursop leaf water has an effect on the decrease in uric acid levels in menopause.

Green Betel Leaf Water with Pure Honey Against Healing Perineum's Wounds Mother Postpartum

Many postpartum mothers die from perineal injuries. Perineal infection can occur if the perineal wound is not treated correctly and correctly. This study was conducted to assess the effectiveness of healing wounds perineum postpartum mothers using green betel leaves and pure honey. This type of research is pre-experimental using one pretest group-posttest design. The number of 20 samples is determined by purposive sampling. Intervention is done using betel leaf decoction water to rinse perineal wounds for one week. Water is made from 5 sheets of betel leaves boiled with 1000 millilitres of water for 30 minutes to 600 millilitres. Data collection uses observation sheets filled in before and after the intervention. Analysis of data using the McNemar test obtained the result of the P-value 0.021 with the meaning &lt;0.05. The results showed an effect of giving green betel leaf water and consuming pure honey to heal perineal wounds in postpartum mothers, so it is recommended that postpartum mothers suffering from perineal wounds use a decoction of green betel leaf water to rinse the perineum and consumption. Pure honey because of the benefits and content obtained in green betel leaves and pure honey in healing perineal wounds.

Isoindolines and phthalides from the rhizomes of Ligusticum chuanxiong and their relaxant effects on the uterine smooth muscle

Three undescribed isoindoline alkaloids, (+)-(R)-3-butyl-3-ethoxyisoindolin-1-one, (+)-(3S,6S,7R)-3-butyl-6,7-dihydroxy-3-methoxy-4,5,6,7-tetrahydroisoindolin-1-one, and (−)-(3R,6S,7R)-3-butyl-6,7-dihydroxy-3-methoxy-4,5,6,7-tetrahydroisoindolin-1-one, along with nine known phthalides were isolated from a water decoction of the rhizomes of Ligusticum chuanxiong using chromatographic methods. Their structures and absolute configurations were determined by extensive spectroscopic analyses and ECD data calculations. The relaxant effects of the isolated compounds on uterine contractions induced by oxytocin were investigated using a rat uterine smooth muscle contraction model. Furthermore, the effects of riligustilide on extracellular Ca2+ influx and intracellular Ca2+ release were assessed using high-KCl solution-induced and oxytocin-induced uterine smooth muscle contraction in a Ca2+-free balanced salt solution. The results showed that all the tested phthalides had inhibitory effects on oxytocin-induced uterine smooth muscle contraction. Riligustilide, a phthalide dimer, was the most active. Further examinations indicated that riligustilide reduced uterine smooth muscle contraction by inhibiting extracellular Ca2+ influx and intracellular Ca2+ release.

Protective effects of Ligularia fischeri root extracts against ulcerative colitis in mice through activation of Bcl-2/Bax signalings

BackgroundUlcerative colitis (UC) is a chronic inflammatory bowel disease characterized by high levels of proinflammatory cytokines and epithelial barrier dysfunction. The root of Ligularia fischeri (Ledeb.) Turcz. is a traditional Chinese medicinal herb with diverse therapeutic properties, which has been successfully used to treat inflammation-related diseases. However, little is known about its effect and mechanism against UC. PurposeTo investigate the efficacy and mechanism of L. fischeri root extracts against UC. MethodsL. fischeri root samples were prepared using the alcohol extraction method and liquid-liquid extraction method. A dextran sodium sulfate-induced UC mouse model and a lipopolysaccharide (LPS)-induced inflammatory cell model were employed in the present study. Cell apoptosis was detected by TUNEL staining, and an enzyme-linked immunosorbent assay was used to quantify the abundance of inflammatory factors in tissues. Hematoxylin and eosin staining and Masson staining were employed to analyze drug toxicity to the liver and kidney. A myeloperoxidase (MPO) assay kit was used to detect neutrophil infiltration in colon tissues. RT-qPCR was then employed to quantify the transcriptional levels of proinflammatory and apoptotic-related genes, while tight junction and apoptosis-related proteins were quantified via western blotting. Gas Chromatography/Mass Spectrometry analysis was then performed to identify the natural compounds in L. fischeri root extracts. ResultsThe water decoction extract, methanol extract, and especially the chloroform extract (CE) exerted potent therapeutic effects in UC mice. Similar to the positive control group (5-aminosalicylic acid), oral administration of CE (30, 60, and 90 mg/kg/d) elicited distinct therapeutic effects on UC mice in the medium- and high-dose groups. CE decreased disease activity index, histopathological score, and MPO level significantly, and effectively retained the colon length. Furthermore, CE significantly reduced the levels of proinflammatory cytokines, including interleukin (IL)-1β, IL-6, and tumor necrosis factor-α and enhanced the expression of tight junction proteins, such as zonula occludens (ZO)-1, ZO-2, claudin-1, and occludin, as well as the transcriptional levels of mucins, such as MUC-1 and MUC-2, in UC mice. Notably, CE prevented apoptosis of colonic epithelial cells by up-regulating Bcl-2 and down-regulating Bax. Also, CE inhibited the secretion of pro-inflammatory cytokines and apoptosis in LPS-induced RAW264.7 macrophages via the activation of Bcl-2/Bax signals. ConclusionsCollectively, L. fischeri root extracts, especially CE, have obvious therapeutic effects against UC. CE reduces inflammation and protects the intestinal epithelial cells and intestinal epithelial barrier via activation of the Bcl-2/Bax signaling pathway, and may be a promising therapeutic agent for UC treatment.

Optimisation of enzyme-assisted extraction of Erythronium sibiricum bulb polysaccharide and its effects on immunomodulation.

In this study, polysaccharides of Erythronium sibiricum bulb were extracted using enzyme-assisted extraction technology and then optimised by response surface methodology. The characteristics and immunomodulatory activities of the polysaccharide (E1P) were investigated. Setting the yield of polysaccharides as the index, the effects of amylase content, zymolytic time, extraction pH and zymolytic temperature were investigated. The optimal extraction conditions for polysaccharides were as follows: amylase content, 1% weight of pre-treated powder; zymolytic time, 2h; extraction pH, 7.5; and zymolytic temperature, 55°C. The yield was predicted to be 61.10%, which agreed with the value obtained in confirmatory experiments (59.71% ± 2.72%). Further research indicated that the primary component of E1P is glucose; however, it also contains a small quantity of galactose and arabinose. In vitro assays showed that E1P and ESBP (another kind of E. sibiricum bulb polysaccharide extracted by water decoction in our previous study) could significantly promote the cellular viability and phagocytosis of RAW264.7 cells without cytotoxicity. Moreover, they could enhance the ability to secrete nitric oxide and cytokines such as TNF-α and IL-1β. However, the immunomodulatory activities of E1P were better than those of ESBP. According to the results of this study, enzyme-assisted extraction represents a new strategy for extracting E. sibiricum bulb polysaccharides with higher yield and better immune activity.

Purification and characterization of a novel thermostable anticoagulant protein from medicinal leech Whitmania pigra Whitman

Ethnopharmacological relevanceThe prevalence of cardiovascular disease (CVD) is increasing worldwide. Despite significant improvements in novel targeted treatment agents, natural products purified from medicinal animals with minimal side effects have attracted much attention. Several native proteins explored from suck-blood leeches, such as non-thermostable hirudin and its variants, revealed potent anticoagulant activity. Traditional Chinese medicine clinics have proved that non-suck-blood leech Whitmania pigra Whitman (W. pigra) also played notable roles in CVD treatments even after decoction. However, only a few natural proteins and peptides have been identified from the fresh material of this medicinal species. Aim of the studyWe aimed to purify and characterize thermostable anticoagulant proteins from W. pigra for further development of a therapeutic agent for thrombosis. Materials and methodsW. pigra crude extract was prepared by decoction in water. Anticoagulant proteins were purified by DEAE cellulose DE-52, Sephadex G-75, and reversed-phase liquid chromatography sequentially and analyzed by SDS-PAGE and LC-MS/MS for structural information. In addition, we conducted in vitro anticoagulant experiments, including plasma recalcification time (PRT) assay, fibrinolytic assay, activated partial thromboplastin time (APTT), prothrombin time (PT), thrombin time (TT), fibrinogen (Fib) assay, and cell viability assays. Furthermore, a carrageenan-induced chronic thromboembolism model was employed in ICR mice, and four coagulation factors (APTT, PT, TT, and Fib) activities were determined after intragastric administration. ResultsThe anticoagulant protein WP-77 has a relative molecular weight of ca. 20.8 kDa. It was effective over a broad temperature range from 20 °C to 100 °C and a pH 2–8 condition. The anticoagulant activity of WP-77 was retained after incubation with pepsin but was greatly inhibited by trypsin (P < 0.01). It significantly prolonged APTT and TT (P < 0.05) but had little effect on PT and Fib in vitro. Furthermore, WP-77 of a low concentration resulted in the recovery of injured EA.hy926 by thrombin. The protein also significantly prolonged APTT and TT (P < 0.01) and inhibited thrombus formation in carrageenan-induced thrombosis mice, demonstrating its antithrombotic effect in vivo. ConclusionOur results suggest that WP-77 from W. pigra plays a distinct role in treating thrombotic diseases, and it is an essential substance of anticoagulant activity of non-suck-blood medicinal leeches. This thermostable anticoagulant protein could be a promising candidate for the development of clinical antithrombosis medicines.

Gas Chromatography-Mass Spectrometry-based Phytochemical Analysis and In-Vitro Anti-Lipid Peroxidation, Cyclooxygenase Inhibition Activities of Saudi Eruca sativa Leaves

Eruca sativa is a wholesome yearly shrubbery herb in Saudi Arabia. Eruca sativa leaves are a conventional food and are consumed raw in salads. The present research reports the phytochemical analysis, in-vitro anti-lipid peroxidation, total anti-oxidant capability, cyclooxygenase-1, and -2 (COX1 and COX2) inhibition activities of Saudi Eruca sativa leaves water decoction (EWD). Gas chromatography-mass spectrometry (GC-MS) of EWD revealed seventeen constituents of six different chemical groups: phenolics (23.60%), aromatic and aliphatic esters (16.97%), terpenoids (31.91%), heterocyclics (14.83%), sulfur containing organics (11.25%), and silyl compounds (1.44%). The presence of Astaxanthin (1.96%), Clionasterol (12.81%), Ingol-12-acetate (4.77%), and Phytol (12.37%) in EWD indicated that the decoction technique was effective in extracting thermostable terpenoids. This research is the first report on Eruca sativa unraveling the thermostable phytochemicals. The EWD exhibited a straight-line relationship between liver lipid peroxidation inhibition and 150 to 400 μg/ml concentrations. The % anti-lipid peroxidation effect produced by EWD and Quercetin was statistically significant. At the highest 400 μg/ml dose, EWD exhibits 68.46 and#177; 0.01% anti-lipid peroxidation activity. The demonstrated IC50 of EWD and Ascorbic acid concerning the total anti-oxidant capability is 217.90 μg/ml and 74.91 μg/ml. The in-vitro assay protocols delineated the modes of inhibition of the biological oxidation processes by Eruca sativa, indicating transfer of hydrogen ion and metal ions reduction. The COX inhibitory potential was screened using Ellmannand#39;s reagent. The IC50 values for COX1 and COX2 inhibitions were 152.31μg/ml and 146.4 μg/ml, respectively, indicating that EWD has a potent COX inhibitory potential compared to Indomethacin. The COX2/COX1 ratio of inhibition, less than one, suggested that EWD phytochemicals would be preferential inhibitors of COX2. The current investigation justifies Eruca sativa leaves as a beneficial health food by establishing the chemical composition of water decoction that contributed to the anti-oxidant and COX inhibition activity.

&amp;lt;i&amp;gt;Quassia undulata&amp;lt;/i&amp;gt; Oil Exploitation: Extraction’s Yield, Phytochemical Profile of Seeds and Oilcake Nutritional Value

Quassia undulata is a plant that belongs to the Simaroubaceae family. In Africa, it occurs in the wooded savannah from Senegal in the west to the Central African Republic in the east. The seeds from the plant are very rich in oil. The traditional extraction of this oil involves a phase of boiling the powder from the seeds in a decoction of Piliostigma thonningii leaves. Thus, the aim of this study is to determine the impact of Piliostigma thonningii leaves on the extraction yield, to assess the phytochemical profile of seeds and oilcake and, to determine the nutritional value of the cakes obtained after extraction. Thus, the traditional extraction of oil was carried out in the laboratory and physico-chemical and phytochemical analyses were carried out on the water decoction, the oil and, the oilcake. The results showed that the traditional extraction gives a low extraction yield (5.18% with PD and 6.12% without PD) compared to the Soxhlet extraction (56.9%). On the other hand, it was found that oil obtained by traditional extraction in the presence of Piliostigma thonningii leaves was of better physicochemical quality. Finally, oilcake very rich in proteins (36.71% - 42.69%) and mineral elements (110.9 - 152.33 mg/100g of calcium, 544.75 - 620.77 mg/100g of Potassium and 331.11 - 459.68 mg/100g of Magnesium) justify their use in human food. However, investigations should point to the impact of this traditional technique on the elimination of quassinoids, toxins and antihelminth compounds present in the seeds.

Efficacy of medicinal herbs in the management of depression prodromal to dementia: A translational study from murine models to humans

Depression is a prodromal sign of dementia and may worsen with metabolic disorders like diabetes mellitus. The present study was done to evaluate efficacy of saffron (Saf) and chamomile (Cham) against diabetes associated depression and memory impairment in murine model and through clinical trial in human volunteers visiting psychiatry clinics at the Aga Khan University Hospital, Karachi, Pakistan. In murine study, 50 old diabetic albino wistar rats divided into 5 groups as healthy control (HC), diabetic control (DC), Saf water decoction (WD) 10mg/kg, Cham water decoction (CWD) 30mg/kg and Saf+Cham WD 5mg/kg+15mg/kg for two weeks. The behavioral analysis was done through forced swim (FST) and novel object recognition tests (NOR). Afterwards, animals were sacrificed for blood and brain samples collection. In second phase, 100 depressed patients were given Saf+Cham tea (20mg+1mg) as an adjuvant therapy for depression, assessed through PHQ9 scale. in animals, treatment of Saf and Cham significantly reduced glucose (F4, 45 =9.847, p<0.05) and cholesterol levels (F4, 45 = 20.595, p<0.05). likewise, neurotransmitters dopamine (F4, 45 = 189.593, p<0.05) and acetylcholine (F4, 45 = 69995.098, p<0.05) were also increased along with enhancement in brain derived neurotrophic factor (BDNF) in the hippocampus (F4, 45 = 116.200; p<0.05) with improved FST (F4, 45 = 24.612, p<0.05) and NOR performance (F4, 45 = 55.718, p<0.05). The clinical trial also revealed significant improvement in PHQ 9 scale (F3, 80 = 20.036, p<0.05) with maintenance of normoglycemia (F3, 80 = 10.07, p<0.05) and cholesterol (F3, 80 = 8.89, p<0.05) of test volunteers. The study was validated through animals showing saffron and chamomile augment BDNF level and neurotransmitters with alleviation of metabolic alterations by regulating glucose and lipid metabolism. The clinical trial also showed strong modulating effects of herbal tea on metabolic profile with alleviation of depression a prodromal sign of dementia.