Anti-cancer effect of Rumex obtusifolius in combination with arginase/nitric oxide synthase inhibitors via downregulation of oxidative stress, inflammation, and polyamine synthesis.

Cancer continues to be a leading cause of death worldwide, making the development of new treatment methods crucial in the fight against it. With cancer incidence rates increasing worldwide, ongoing research must focus on identifying new and effective ways to prevent and treat the disease. The combination of herbal extracts with chemotherapeutic agents has gained much interest as a novel strategy to combat cancer. Rumex obtusifolius L. is a wild plant known for its medicinal properties and is widely distributed worldwide. Our preclinical evaluations suggested that R. obtusifolius seed extracts possessed cancer-inhibiting properties and we also evaluated the beneficial effects of the arginase inhibitor NG-hydroxy-nor-L-arginine and nitric oxide inhibitor NG-nitro-L-arginine methyl ester in the treatment of breast cancer. The current study aimed to combine these observations and evaluate the antioxidant and antitumor properties of R. obtusifolius extracts alone and in combination with the arginase and nitric oxide synthase inhibitors. Metabolic characterization of the plant extract using a liquid chromatography/high-resolution mass spectrometry advanced system revealed the presence of 240 phenolic compounds many of which possess anticancer properties, according to the literature. In vitro studies revealed a significant cytotoxic effect of the R. obtusifolius extracts on the human colon (HT29) and breast cancer (MCF-7) cell lines. Thus, a new treatment approach of combining R. obtusifolius bioactive phytochemicals with the arginase and nitric oxide synthase inhibitors NG-nitro-L-arginine methyl ester and/or NG-hydroxy-nor-L-arginine, respectively, was proposed and could potentially be an effective way to treat breast cancer. Indeed, these combinations showed immunostimulatory, antiproliferative, antioxidant, anti-inflammatory, and antiangiogenic properties in a rat breast cancer model.

Antiulcer Activity of Anthraquinone-Flavonoid Complex of Rumex tianschanicus Losinsk.

The composition of an ethanol extract from the roots of Rumex tianschanicus Losinsk of the Trans-Ili Alatau wild flora was studied in order to determine its antiulcer activity. The phytochemical composition of the anthraquinone-flavonoid complex from (AFC) R. tianschanicus revealed the presence of numerous polyphenolic compounds, the most abundant of which are anthraquinones (1.77%), flavonoids (6.95%), and tannins (13.39%). The use of column chromatography (CC) and thin-layer chromatography (TLC) in conjunction with UV, IR, NMR spectroscopy, and mass spectrometry data allowed the researchers to isolate and identify the major components of the anthraquinone-flavonoid complex's polyphenol fraction: physcion, chrysophanol, emodin, isorhamnetin, quercetin, and myricetin. The gastroprotective effect of the polyphenolic fraction of the anthraquinone-flavonoid complex (AFC) of R. tianschanicus roots was examined in an experimental model of rat gastric ulcer induced by indomethacin. The preventive and therapeutic effect of the anthraquinone-flavonoid complex at a dose of 100 mg/kg was analyzed using intragastric administration per day for 1 to 10 days, followed by a histological examination of stomach tissues. It has been demonstrated that prophylactic and prolonged use of the AFC R. tianschanicus in laboratory animals resulted in significantly less pronounced hemodynamic and desquamative changes in the epithelium of gastric tissues. The acquired results thus offer fresh insight into the anthraquinone and flavonoid metabolite component composition of R. tianschanicus roots, and they imply that the examined extract can be used to develop herbal medicines with antiulcer activity.

Isolation and characterisation of pharmaceutically versatile molecules from Rumex dentatus and evaluation of their cytotoxic activity against human cancer cell lines.

The disclosed study reveals isolation, characterization and anticancer evaluation of Rumex dentatus. The extracts and isolated compounds were used for cytotoxic activity against (lung (A549), pancreatic (MIAPaCa), colon (HCT-116), breast (MDA-MB-231) and breast (MDA-MB-468) cell lines. The extracts were screened for cytotoxicity using MTT colorimetric assay. Out of all extracts, methanolic (30) %: chloroform fraction (TAW6) with 75.01% inhibition at a concentration 100 µg/mL was observed. The selected extracts were further processed for column chromatography and led to isolation of seven compounds (A to G). The structural determination of isolated compounds was carried out using 1HNMR, 13CNMR, IR and HRMS. All the isolates were tested for cytotoxic activity and compound B was found most active with IC50 values 11.29 µg against HCT-116 (Colon). The compound B was then used for detailed study via transwell invasion assay and wound healing assay. Thus the significant anticancer activity particularly against colon cancerous cell lines recommends that the (Rumex dentatus) could act as a potential drug candidate for cancer, more particularly for colon cancer.

Antibacterial constituents of Rumex nepalensis spreng and its emodin derivatives.

The CH2Cl2-MeOH (1:1) extract of roots of Rumex nepalensis (Polygonaceae) displayed significant antibacterial activity against five bacterial strains with MICs (62.5-31.2 µg.mL-1). The EtOAc soluble fraction displayed a significant activity against the same strains with MICs (31.2-3.9 µg.mL-1). The purification of the EtOAc fraction yielded one new phenylisobenzofuranone derivative, berquaertiide (1), along with 19 known compounds (2-20). Their structures were elucidated based on the analysis of their NMR and MS data. All the isolated compounds were assessed for their antibacterial activity. Compound 2 was the most active against all the tested strains (15.7 to 1.9 µg.mL-1), while compounds 3-7 displayed good activities on at least one of the tested strains. In addition, seven analogues (21-27) of compound 2 were prepared and further assessed for their antibacterial activity. Compounds 26 and 27 were most active than 2 against Salmonella enterica and Klebsiella pneumoniae with MIC (125 and 15.6 µg.mL-1, respectively).

Pharmacological Basis of Rumex hastatus D. Don in Gastrointestinal Diseases with Focusing Effects on H+/K+-ATPase, Calcium Channels Inhibition and PDE Mediated Signaling: Toxicological Evaluation on Vital Organs.

This present study aimed to delineate Rumex hastatus D. Don crude extract (Rh.Cr), n-Hexane, ethyl acetate, aqueous fractions (Rh.n-Hex, Rh.ETAC, Rh.Aq) and rutin for antidiarrheal, antisecretory effects, anti-spasmodic, gastrointestinal transient time, anti H. pylori, antiulcer effects, and toxicology. The preliminary phytochemical analysis of Rumex hastatus showed different phytoconstituents and shows different peaks in GC-MC chromatogram. Rumex hastatus crude extract (Rh.Cr), fractions, and rutin attributed dose-dependent (50-300 mg/kg) protection (0-100%) against castor oil-induced diarrhea and dose-dependently inhibited intestinal fluid secretions in mice. They decreased the distance traversed by charcoal in the gastrointestinal transit model in rats. In rabbit jejunum preparations, Rh.Cr and Rh.ETAC caused a concentration-dependent relaxation of both spontaneous and K+ (80 mM)-induced contractions at a similar concentration range, whereas Rh.n-Hex, rutin, and verapamil were relatively potent against K+-induced contractions and shifted the Ca2+ concentration-response curves (CRCs) to the right, Rh.Cr (0.3-1 mg/mL) and Rh.ETAC (0.1-0.3 mg/mL) shifted the isoprenaline-induced inhibitory CRCs to the left. Rh.n-Hex, Rh.ETAC and rutin showed anti-H. pylori effect, also shows an inhibitory effect against H+/K+-ATPase. Rumex hastatus showed gastroprotective and antioxidant effects. Histopathological evaluation showed improvement in cellular architecture and a decrease in the expression of inflammatory markers such as, cyclooxygenase (COX-2), tumor necrosis factor (TN,F-α) and phosphorylated nuclear factor kappa B (p-NFƙB), validated through immunohistochemistry and ELISA techniques. In RT-PCR it decreases H+/K+-ATPase mRNA levels. Rumex hastatus was found to be safe to consume up to a dose of 2000 mg/kg in a comprehensive toxicity profile. Docking studies revealed that rutin against H+/K+-ATPase pump and voltage-gated L-type calcium channel showed E-values of -8.7 and -9.4 Kcal/mol, respectively. MD simulations Molecular Mechanics Poisson Boltzmann surface area and molecular mechanics Generalized Born surface area (MMPBSA/GBSA) findings are consistent with the in-vitro, in-vivo and docking results.

Study on HPLC Fingerprint, Network Pharmacology, and Antifungal Activity of Rumex japonicus Houtt.

BACKGROUND: Rumex japonicus Houtt (R. japonicus) is used mainly to treat various skin diseases in Southeast Asia. However, there are few studies on its quality evaluation methods and antifungal activity. OBJECTIVE: To establish the quality control criteria for the effective parts from R. japonicus against psoriasis. METHODS: High-performance liquid chromatography (HPLC) was established for its fingerprint, and the similarity evaluation, cluster analysis (CA) and principal component analysis (PCA) were used to reveal the differences of those fingerprints among the tested R. japonicus. Network pharmacology analyzed the relationship between the components and psoriasis, revealing the potential targets of R. japonicus. Oxford cup anti-C. albicans experiment was used to verify the antifungal activity of R. japonicus. RESULTS: HPLC was developed for the R. japonicus fingerprint by optimizing for 10 batches of quinquennial R. japonicus from different habitats; the 18 common peaks were identified with 10 characteristic peaks such as rutin, quercetin, aloe-emodin, nepodin, emodin, musizin-8-O-ß-D-glucoside, chrysophanol, emodin-8-O-ß-D-glucopyranoside, chrysophanol-8-O-ß-D-glucopyranoside, and aloin, respectively. The network pharmacology-based analysis showed a high correlation between R. japonicus and psoriasis, revealing the potential targets of R. japonicus. The oxford cup anti-Candida albicans experiment displayed a significant activity response to emodin-8-O-ß-D-glucopyranoside and the ethyl acetate fraction of R. japonicus acidic aqueous extract. CONCLUSIONS: A new and optimized HPLC method was created, and the research provides an experimental basis for the development of effective drugs related to C. albicans. HIGHLIGHTS: The fingerprint of R. japonicus was organically combined with network pharmacology to further clarify its criteria for quality control.

Investigation and Biological Assessment of Rumex vesicarius L. Extract: Characterization of the Chemical Components and Antioxidant, Antimicrobial, Cytotoxic, and Anti-Dengue Vector Activity.

The objective of this study was to assess the biological potency and chemical composition of Rumex vesicarius aboveground parts using GC-MS. In this approach, 44 components were investigated, comprising 99.99% of the total volatile compounds. The major components were classified as fatty acids and lipids (51.36%), oxygenated hydrocarbons (33.59%), amines (7.35%), carbohydrates (6.06%), steroids (1.21%), and alkaloids (0.42%). The major components were interpreted as 1,3-dihydroxypropan-2-yl oleate (oxygenated hydrocarbons, 18.96%), ethyl 2-hydroxycyclohexane-1-carboxylate (ester of fatty acid, 17.56%), and 2-propyltetrahydro-2H-pyran-3-ol (oxygenated hydrocarbons, 11.18%). The DPPH antioxidant activity of the extracted components of R. vesicarius verified that the shoot extract was the most potent with IC50 = 28.89 mg/L, with the percentages of radical scavenging activity at 74.28% ± 3.51%. The extracted plant, on the other hand, showed substantial antibacterial activity against the diverse bacterial species, namely, Salmonella typhi (23.46 ± 1.69), Bacillus cereus (22.91 ± 0.96), E. coli (21.07 ± 0.80), and Staphylococcus aureus (17.83 ± 0.67). In addition, the extracted plant was in vitro assessed as a considerable anticancer agent on HepG2 cells, in which MTT, cell proliferation cycle, and DNA fragmentation assessments were applied on culture and treated cells. The larvicidal efficacy of the extracted plant was also evaluated against Aedes aegypti, the dengue disease vector. As a result, we may infer that R. vesicarius extract increased cytocompatibility and cell migratory capabilities, and that it may be effective in mosquito control without causing harm.

Rumex nervosus could alleviate streptozotocin-induced diabetic nephropathy in rats by activating Nrf2 signaling.

This study tested the protective effect of Rumex nervous (R. nervosus) methanol extract against streptozotocin (STZ)-mediated type 1 diabetes mellitus (T1DM)-induced nephropathy in rats and examined if this protection involves activating the nuclear factor erythroid 2 related factor-2 (Nrf2). Rats were divided into control, R. nervous (300 mg), STZ (T1DM), STZ + R. nervosus (100, 200, or 300 mg/kg), and STZ + R. nervosus (300 mg/kg) + brusatol (an Nrf2 inhibitor). With no effect on fasting glucose and insulin levels, R. nervosus methanol extract preserved kidney histological structure and alterations kidney function markers (e.g. albumin, creatinine, and urine volume) in the STZ-diabetic rats. R. nervosus also reduced levels of reactive oxygen species (ROS), malondialdehyde (MDA), tumor necrosis factor-α (TNF-α), and interleukine-6 (IL-6), nuclear levels of the nuclear factor kappa beta (NF-κB), and mRNA of caspase-3 and Bax in the kidneys of these diabetic rats. Concomitantly, it stimulated renal mRNA levels of Bcl2 and Nrf2, cytoplasmic and nuclear levels of Nrf2, and levels of glutathione (GSH), catalase (CAT), and superoxide dismutase (SOD). All these effects were dose-dependent, with the maximum effect seen with the 300 mg/kg dose, all prevented by brusatol. Also, these effects occurred without any alteration in the transcription of the Kelch-like ECH-associated protein 1 (keap-1). Similar effects on levels of GSH, SOD, CAT, and NF-κB, as well as expression of Nrf2, were also observed in the kidney of control + R. nervous-treated rats. In conclusion, R. nervosus prevents diabetic nephropathy in rats by upregulating and activating Nrf2.

Effects of indirect plant-plant interaction via root exudate on growth and leaf chemical contents in Rumex obtusifolius.

Belowground plant-plant interactions can affect the concentrations of leaf chemicals, but the mechanism is not clear. Here, we investigated the effects of intra- and interspecific root exudates on the growth and leaf chemical content of Rumex obtusifolius. Seedlings of R. obtusifolius were grown with exposure to root exudates collected from other R. obtusifolius plants or from Trifolium repens, Festuca ovina, or Plantago asiatica plants, and the total phenolic, condensed tannin, dry biomass, and chlorophyll contents of the leaves were examined. The root exudates from conspecific plants had no effect on the total phenolic, condensed tannin, and chlorophyll contents of the leaves but did significantly reduce the dry leaf biomass. Root exudates from heterospecific plants had different effects depending on the species. These results were different from the results of a previous study that examined the effects of direct plant-plant interaction in R. obtusifolius. Thus, indirect interaction via root exudates induces different effects in leaves from direct interaction.

Overview of the Biological Activity of Anthraquinons and Flavanoids of the Plant Rumex Species.

Rumex confertus belongs to the genus Rumex and is classified as an invasive parasitic plant in agriculture. Despite other Rumex species being widely used in herbal medicine due to their antimicrobial, antioxidant, antitumor, and anti-inflammatory effects, there are almost no information about the potential of Rumex confertus for the treatment of various diseases. In this review we analyzed scientific articles revealing properties of Rumex plant's substances against cancer, diabetes, pathogenic bacterial invasions, viruses, inflammation, and oxidative stress for the past 20 years. Compounds dominating in each composition of solvents for extraction were discussed, and common thin layer chromatography(TLC) and high performance liquid chromatography(HPLC) methods for efficient separation of the plant's extract are included. Physico-chemical properties such as solubility, hydrophobicity (Log P), pKa of flavonoids, anthraquinones, and other derivatives are very important for modeling of pharmacokinetic and pharmacodynamics. An overview of clinical studies for abounded selected substances of Rumex species is presented.

Identification of Antibacterial Components in the Methanol-Phase Extract from Edible Herbaceous Plant Rumex madaio Makino and Their Antibacterial Action Modes.

Outbreaks and prevalence of infectious diseases worldwide are some of the major contributors to morbidity and morbidity in humans. Pharmacophageous plants are the best source for searching antibacterial compounds with low toxicity to humans. In this study, we identified, for the first time, antibacterial components and action modes of methanol-phase extract from such one edible herbaceous plant Rumex madaio Makino. The bacteriostatic rate of the extract was 75% against 23 species of common pathogenic bacteria. The extract was further purified using the preparative high-performance liquid chromatography (Prep-HPLC) technique, and five separated componential complexes (CC) were obtained. Among these, the CC 1 significantly increased cell surface hydrophobicity and membrane permeability and decreased membrane fluidity, which damaged cell structure integrity of Gram-positive and -negative pathogens tested. A total of 58 different compounds in the extract were identified using ultra-HPLC and mass spectrometry (UHPLC-MS) techniques. Comparative transcriptomic analyses revealed a number of differentially expressed genes and various changed metabolic pathways mediated by the CC1 action, such as down-regulated carbohydrate transport and/or utilization and energy metabolism in four pathogenic strains tested. Overall, the results in this study demonstrated that the CC1 from R. madaio Makino are promising candidates for antibacterial medicine and human health care products.

More Than Just a Weed: An Exploration of the Antimicrobial Activity of Rumex crispus using a Multivariate Data Analysis Approach.

Plants have a long history of use for their medicinal properties. The complexity of botanical extracts presents unique challenges and necessitates the application of innovative approaches to correctly identify and quantify bioactive compounds. For this study, we used untargeted metabolomics to explore the antimicrobial activity of Rumex crispus (yellow dock), a member of the Polygonaceae family used as an herbal remedy for bacterial infections. Ultra-performance liquid chromatography coupled with high resolution mass-spectrometry (UPLC-MS) was used to identify and quantify the known antimicrobial compound emodin. In addition, we used biochemometric approaches to integrate data measuring antimicrobial activity from R. crispus root starting material and fractions against methicillin-resistant Staphylococcus aureus (MRSA) with UPLC-MS data. Our results support the hypothesis that multiple constituents, including the anthraquinone emodin, contribute to the antimicrobial activity of R. crispus against MRSA.

The impact of aqueous and N-hexane extracts of three Fabaceae species on seed germination and seedling growth of some broadleaved weed species.

Weed infestation is a persistent problem for centuries and continues to be major yield reducing issue in modern agriculture. Chemical weed control through herbicides results in numerous ecological, environmental, and health-related issues. Moreover, numerous herbicides have evolved resistance against available herbicides. Plant extracts are regarded as an alternative to herbicides and a good weed management option. The use of plant extracts is environmentally safe and could solve the problem of herbicide resistance. Therefore, laboratory and wire house experiments were conducted to evaluate the phytotoxic potential of three Fabaceae species, i.e., Cassia occidentalis L. (Coffee senna), Sesbania sesban (L.) Merr. (Common sesban) and Melilotus alba Medik. (White sweetclover) against seed germination and seedling growth of some broadleaved weed species. Firstly, N-hexane and aqueous extracts of these species were assessed for their phytotoxic effect against lettuce (Lactuca sativa L.). The extracts found more potent were further tested against germination and seedling growth of four broadleaved weed species, i.e., Parthenium hysterophorus L. (Santa-Maria), Trianthema portulacastrum L. (Pigweed), Melilotus indica L (Indian sweetclover). and Rumex dentatus L. (Toothed dock) in Petri dish and pot experiments. Aqueous extracts of all species were more toxic than their N-hexane forms for seed germination and seedling growth of lettuce; therefore, aqueous extracts were assessed for their phytotoxic potential against four broadleaved weed species. Aqueous extracts of all species proved phytotoxic against T. portulacastrum, P. hysterophorus, M. indica and R. dentatus and retarder their germination by 57, 90, 100 and 58%, respectively. Nevertheless, foliar spray of C. occidentalis extract was the most effective against T. portulacastrum as it reduced its dry biomass by 72%, while M. alba was effective against P. hysterophorus, R. dentatus and M. indica and reduced their dry biomass by 55, 68 and 81%, respectively. It is concluded that aqueous extracts of M. alba, S. sesban and C. occidentalis could be used to retard seed germination of T. portulacastrum, P. hysterophorus, M. indica and R. dentatus. Similarly, aqueous extracts of C. occidentalis can be used to suppress dry biomass of T. portulacastrum, and those of M. alba against P. hysterophorus, R. dentatus. However, use of these extracts needs their thorough testing under field conditions.

Phenolic Compounds of Rumex roseus L. Extracts and Their Effect as Antioxidant and Cytotoxic Activities.

Rumex roseus L. (R. roseus) is acknowledged as an aromatic plant. For its excellent biological properties, it was used as a traditional medicine. The aim of the present study is to evaluate the chemical components and their effect as the biological activities of Tunisian extracts of R. roseus. Consecutive extractions by cold maceration of the aerial part with solvents of increasing polarity (cyclohexane (CYH), dichloromethane (DCM), and methanol (MeOH)) were performed, and the different chemical groups (phenolics, flavonoids, tannins, anthocyanins, etc.) were identified. In addition, the volatile compounds of the obtained extracts were identified before and after derivatization. Moreover, their antioxidant and anticancer activities were evaluated. The analysis of HPLC-DAD revealed the identification of 18 components from organic extracts, among them are, for example, chlorogenic acid and shikonin, while GC-MS analysis allowed the detection of 34 volatile compounds. Some of those compounds were identified for the first time in plant extracts such as pyrazolo[3,4-d] pyrimidine-3,4(2H,5H)-dione (1); L-proline (16); 2-amino-3-hydroxybutanoic acid (19); L-(-)-arabitol (23); D-(-)-fructopyranose (25); and D-(+)-talopyranose (27). DPPH tests revealed that the most important antioxidant activity was found in the methanolic extract with 75.2% inhibition at 50 mg/L and that the highest cytotoxic activity against HCT-116 and MCF-7 was recorded in the dichloromethane extract with 62.1 and 80.0% inhibition at 50 mg/L, respectively. The biological activities were fully correlated with the chemical composition of the different extracts. So, we can suggest that R. roseus is a source of bioactive molecules that could be considered potential alternatives for use in dietary supplements for the prevention or treatment of diseases.

Evaluation of phytochemical, anti-oxidant and cardiac depressant effect of Rumex dentatus by using Langendorff's isolated heart apparatus.

Rumex dentatus has been used traditionally for ailment of cardiovascular diseases. The aim of the present study was to assess cardiovascular effects in isolated perfused rabbit heart. Aqueous and n-butanolic fractions were assessed for their effect on perfusion pressure (PP), force of contraction (FC) and heart rate (HR) of rabbit heart using Langendorff's method. The possible mechanisms of action of extracts/fraction were assessed with and without application of different agonist/antagonist. Phytochemical, toxicity and anti-oxidant activities were also determined. Both extracts at 1mg/mL dose produced a highly significant decrease in FC and HR but PP remained unchanged. Moreover, aqueous fraction of Rumex dentatus at 0.001mg/mL dose produced a highly significant decrease in FC and HR but no significant change in PP was observed. Atropine 10-5 M did not inhibit the cardiac depressant response of both fractions. Furthermore, both fractions blocked the positive ionotropic and chronotropic effects of adrenaline and calcium chloride. Phytochemical studies have shown the presence of some phytochemicals. Acute and sub-chronic toxicity studies demonstrated that test extracts are safe and produced no significant changes in haematological and biochemical parameters. Crude extract showed significant antioxidant activity like ascorbic acid. This study revealed that this plant have good cardiac depressant effect.

Antibacterial, antifungal and antioxidant activities of whole plant chemical constituents of Rumex abyssinicus.

BACKGROUND: Antibiotic resistance has contributed to the burden of infectious diseases both in the hospital and community setting, and represents a great threat to public health. Previous studies have revealed the role of reactive oxygen species as intermediate mediators of tissue damage, following antibiotherapies, indicating the need of associating antioxidants to these treatments. Therefore, the present work was designed to study the antibacterial, antifungal and antioxidant activities of extracts and compounds from Rumex abyssinicus Jacq. (Polygonaceae), as well as to investigate the antibacterial mechanisms of action of the most effective agents. METHODS: The plant extracts were prepared by maceration in organic solvents followed by column chromatography of the EtOAc fraction and purification of different fractions which led to the isolation and characterization of pure compounds. The antimicrobial activities of the extracts/compounds and their combinations with ciprofloxacin and fluconazole were evaluated using the broth microdilution method by determining the minimum inhibitory concentration (MIC) and minimum microbicidal concentration (MMC). The effects of the extracts on the bacterial cell membrane and microbial respiratory chain dehydrogenase enzyme activity were determined by spectrophotometric methods. Antioxidant activity was evaluated using 1,1-diphenyl-2-picrylhydrazyl (DPPH) and gallic acid equivalent antioxidant capacity (GAEAC) assays. RESULTS: Chrysophanol (1), physcion (2), Ergosta-6,22-diene-3,5,8-triol (3), emodin (4), 6-hydroxyemodin (citreorosein) (5), chrysophanein (6) and physcionin (7) were isolated from EtOAc fraction of R. abyssinicus and displayed different degrees of antimicrobial activities (MIC = 8-256 µg/mL). The MeOH extract and compounds 2 and 4 exhibited synergistic effects with ciprofloxacin and fluconazole. Compounds 1, 2 and the combined mixture of 6 + 7 displayed the highest antioxidant activity (GAEAC = 83.38-106.03 µg/mL). CONCLUSION: R. abyssinicus is a potential source of antibacterial, antifungal and antioxidant agents. The antibacterial mechanisms of action of the MeOH extract and compound 2 are due to disruption of the cytoplasmic membrane and inhibition of the microbial respiratory chain dehydrogenase enzyme activity. To the best of our knowledge, this is the first report of test samples and ciprofloxacin / fluconazole association against MDR strains. The observed activity of the isolated compounds against bacteria and fungi including MDR strains deserves further exploration.

Phytochemical analysis, in-vitro anti-proliferative, anti-oxidant, anti-diabetic, and anti-obesity activities of Rumex rothschildianus Aarons. extracts.

BACKGROUND: Rumex rothschildianus is the sole member of a unique section of the genus Rumex, in the family Polygonaceae. This species is a very rare small dioecious annual, endemic to Palestine that is traditionally used as food and for the treatment of various diseases. Therefore, the current investigation aimed to screen the chemical constituents, antioxidants, anti-α-amylase, anti-α-glucosidase, antilipase, and cytotoxic effects of four solvents fractions of R. rothschildianus leaves. METHODS: Dried powder of R. rothschildianus leaves was extracted in four solvents with different polarities. Several qualitative and quantitative phytochemical tests were performed to determine the components of the extracts. The colorimetric analysis was used for the quantitative determination of phenols, flavonoids, and tannins. In-vitro assays were performed to evaluate the extracts for antioxidant, anti-α-amylase, anti-α-glucosidase, and antilipase inhibitory activities, as well as cytotoxicity by MTS assay against cervical carcinoma cells line (HeLa) and breast cancer cell line (MCF7). RESULTS: The acetone fraction of R. rothschildianus leaves showed the most significant antioxidant activity, due to having the highest content of flavonoids and phenolics, with an IC50 value of 6.3 ± 0.4 µg/ml, compared to 3.1 ± 0.9 µg/ml for Trolox, and regarding lipase inhibition activity the acetone fraction showed the most potent activity with an IC50 value of 26.3 ± 0.6 µg/ml, in comparison with orlistat positive control IC50 12.3 µg/ml. The same extract was the most potent inhibitor of α-amylase and α-glucosidase, with IC50 values of 19.1 ± 0.7 µg/ml and 54.9 ± 0.3 µg/ml, respectively, compared to 28.8, 37.1 ± 0.3 µg/ml of acarbose, respectively. The hexane fraction showed 99.9% inhibition of HeLa cells and 97.4% inhibition for MCF7 cells. CONCLUSION: The acetone fraction of R. rothschildianus leaves might provide a source of bioactive compounds for the treatment of oxidative stress. Similarly, the hexane fraction indicates the promising antitumor potential of R. rothschildianus. Clearly, these initial indications need further purification of potentially active compounds, and ultimately, in-vivo studies to determine their effectiveness.

Comparison of Phytochemical Profile and Bioproperties of Methanolic Extracts from Different Parts of Tunisian Rumex roseus.

The genus Rumex (Polygonaceae) is distributed worldwide and the different species belonging to it are used in traditional medicine. The present study aimed at the evaluation of the phytochemical profile and the biochemical properties of methanolic extracts from different parts (roots, stems, and leaves) of Rumex roseus, a wild local Tunisian plant traditionally used as food. The phytochemical analysis on the extracts was performed using standard colorimetric procedures, HPLC-DAD, and HPLC-DAD-ESI-MS; then, several in vitro cell-free assays have been used to estimate their antioxidant/free radical scavenging capability (TAC-PM, DPPH, TEAC, FRAP, ORAC, SOD-like activity, and HOCl-induced albumin degradation). Additionally, anti-inflammatory effect of these extracts was evaluated in an in vitro model of acute intestinal inflammation in differentiated Caco-2 cells. The results showed that the methanolic extracts from stems and, especially, leaves contain substantial amounts of flavones (apigenin and luteolin, together with their derivatives), while the extract from roots is characterized by the presence of tannins and quinic acid derivatives. All the extracts appeared endowed with excellent antioxidant/free radical scavenging properties. In particular, the extract from roots was characterized by a remarkable activity, probably due to its different and peculiar polyphenolic composition. Furthermore, both Rumex roseus roots and stems extracts demonstrated an anti-inflammatory effect in intestinal epithelial cells, reducing TNF-α-induced gene expression of IL-6 and IL-8. In conclusion, R. roseus methanolic extracts have shown to be potential sources of bioactive compounds to be used in the prevention and treatment of pathologies related to oxidative stress and inflammation.

Inhibition of Jurkat T Cell Proliferation by Active Components of Rumex japonicus Roots Via Induced Mitochondrial Damage and Apoptosis Promotion.

Rumex japonicus Houtt (RJH) is a valuable plant used in traditional medicine to treat several diseases, such as scabies and jaundice. In this study, Jurkat cell growth inhibitory extracts of R. japonicus roots were subjected to bioassay-guided fractionation, resulting in the isolation of three naphthalene derivatives (3-5) along with one anthraquinone (6) and two phenolic compounds (1 and 2). Among these compounds, 2-methoxystypandrone (5) exhibited potent anti-proliferative effects on Jurkat cells. Analysis by flow cytometry confirmed that 2-methoxystypandrone (5) could significantly reduce mitochondrial membrane potential and promote increased levels of mitochondrial reactive oxygen species (ROS), suggesting a strong mitochondrial depolarization effect. Real-time quantitative polymerase chain reaction (qPCR) analysis was also performed, and the results revealed that the accumulation of ROS was caused by reduced mRNA expression levels of heme oxygenase (HO-1), catalase (CAT), glutathione peroxidase (GPx), and superoxide dismutase (SOD). In addition, 2-methoxystypandrone (5) triggered strong apoptosis that was mediated by the arrest of the G0/G1 phase of the cell cycle. Furthermore, 2-methoxystypandrone (5) downregulated p-IκB-α, p-NF-κB p65, Bcl2, and Bcl-xl and upregulated BAX proteins. Taken together, these findings revealed that 2-methoxystypandrone (5) isolated from RJH could potentially serve as an early lead compound for leukemia treatment involving intracellular signaling by increasing mitochondrial ROS and exerting anti-proliferative effects.

Phytochemical and Biological Characterization of Methanolic Extracts from Rumex algeriensis and Rumex tunetanus.

The present study is aimed at the evaluation of the phytochemical profile and the biochemical properties of methanolic extracts obtained from different parts of Rumex algeriensis and Rumex tunetanus, two relict species limited to the North Africa. Phytochemical analyses of these extracts were performed using standard colorimetric procedures, HPLC-DAD, and HPLC-DAD-ESI/MS, and their antioxidant/free radical scavenging capability was estimated through several in vitro cell-free assays. Moreover, the anti-inflammatory potential of these extracts was demonstrated in an in vitro model of acute intestinal inflammation using differentiated Caco-2 cells. The results showed that all the extracts appeared endowed with excellent antioxidant/free radical scavenging properties. In particular, the extracts from both R. algeriensis and R. tunetanus flowers, and that from R. algeriensis stems were characterized by a remarkable SOD-like and NO-scavenging activity, as well as by the capability to protect albumin against HClO-induced degradation. Furthermore, the extracts from flowers of both Rumex species, as well as R. algeriensis stems, showed an anti-inflammatory effect in intestinal epithelial cells, as demonstrated by the inhibition of TNF-α-induced gene expression of IL-6 and IL-8. In conclusion, R. algeriensis and R. tunetanus have shown to be potential sources of bioactive products to be used in the prevention and treatment of pathologies related to oxidative stress and inflammation.