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Rosa × damascena Herrm., known as damask rose, is a bushy shrub that is found abundantly in Fars province, Iran. This species has been used in Iranian traditional practices for the treatment of abdominal pain and constipation, as gastrointestinal diseases. Brown sugar (Saccharum officinarum L.) has also shown laxative effects in pediatric patients with functional constipation.This study aimed to compare the effects of Polyethylene Glycol (PEG) and a syrup made of R. damascena and brown sugar on the treatment of functional constipation in children aged above 12 months.This double-blind randomized clinical trial was performed on 100 patients. One group received PEG and the other received an herbal syrup containing the decocted extract of 0.1 g R. damascena petals mixed with 0.85 g brown sugar per 1 mL. The patients were followed up for two and four weeks and their progresses were recorded.The cure rate was 100% in the R. damascena group and 91.7% in the control group. R. damascena and brown sugar syrup had an odds ratio of 1.09 in the treatment of functional constipation compared to PEG, but the difference was not statistically significant. The only adverse effect detected in the R. damascena group after four weeks was the bad taste of the medication that was too sweet. Nonetheless, this could be solved during the pharmaceutical processes.The R. damascena extract and brown sugar syrup can be used as an effective, safe, and inexpensive agent in the treatment of functional constipation.

Ethnopharmacological relevance Rosa odorata Sweet var. gigantea (Coll. et Hemsl.) Rehd. et Wils (Rosaceae), is also known as “GU-GONG-GUO”, the root of which has been recognized as common ethnodrug from the Yi nationality for treating inflammatory bowel disease. The aim of the present study was to investigate the preventive and curative effects of extract from the fruits of Rosa odorata Sweet var. gigantea (Coll.et Hemsl.) Rehd. et Wils (FOE) in vitro and in vivo as well as elucidate the potential mechanisms of the action involved. Materials and methods Male Wistar rats were applied to ethanol-induced gastric ulcer model. They were divided into six groups: control, model (GU), positive (Magnesium aluminate chewable tablets, 125 mg/kg), FOE low (125 mg/kg), middle (250 mg/kg) and high (500 mg/kg) doses groups. Histopathology observation of gastric tissues was detected by hematoxylin and eosin (H&E) staining. The expression of Nrf2, HO-1, Keap1, NF-κB p65 and IKKα/β in gastric tissues were evaluated by immunohistochemistry (IHC). The levels of cytokines in serum and tissues were measured by Enzyme-linked immunosorbent assay (ELISA). The expression of Nrf2, HO-1, Keap1, NF-κB p65, IKKα/β, PCNA and COX2 proteins were ulteriorly assessed by Western blotting to elucidate the molecular mechanism of FOE's protective effect on gastric ulcer. Results MTT detection showed that LPS reduced RAW264.7 cell survival, and FOE blocked the inhibition of RAW264.7 cell growth induced by LPS. When RAW264.7 cells were treated with both FOE (100 μg mL−1) and LPS (5 μg mL−1) for 24 h, compared with the model group, the level of NO, TNF-α, IL-6, IL-1β and MDA significantly decreased, and the activity of SOD was significantly reduced. Obvious pathological injuries in the GU model group were observed, which was improved after treatments with FOE. The contents of pro-inflammatory factors in serum and tissues were decreased by 25% whereas prostaglandin E2 (PGE2) and epidermal growth factor (EGF) were increased by 30% in a dose-dependent manner after FOE (500 mg/kg) treatments. In addition to the promotion effects of superoxide dismutase (SOD), FOE (500 mg/kg) also attenuated the levels of nitric oxide (NO) and malondialdehyde (MDA) by 20%. Likewise, the expression of NF-κB p65, IKKα/β and Keap1 were suppressed after treatments with FOE whereas Nrf2 and HO-1 showed the opposite trend, which mechanisms were found to be associated with Nrf2/NF-κB signaling pathways. Conclusion The study demonstrated that FOE is able to protect against GU via inhibiting NF-κB signaling pathway and activating Nrf2 signaling pathway, which might provide a stronger theoretical basis for the treatment of GU.

Ethnopharmacological relevance: Rosa rugosa Thunb is a traditional Uygur medicine that has been used in the treatment of diabetes in Uygur ancient recipe for hundreds of years. However, the mechanism of Rosa rugosa Thunb activity is still unclear. This study was designed to address this issue by studying the polyphenols enriched extract (RPE) of Rosa rugosa Thunb in diabetic rats. Materials and methods: RPE were tested in the inhibition of a-glucosidase and oxidative stress in vitro. RPE was administrated at dosages of 37.5, 75 and 150 mg/kg body weight in the type 2 diabetic rats, which were made by high fat diet feeding plus a low dose of STZ injection (30 mg/kg). The therapeutic effect was evaluated four weeks later. Oral glucose tolerance test (OGTT), insulin tolerance test (ITT) and insulin signal pathway (PI3K/AKT) were examined to determine insulin sensitivity. Blood glucose levels and body weight were measured weekly in the study. Results: In vitro, RPE exhibited an activity in the inhibition of a-glucosidase and had an excellent antioxidant activity in the liver of diabetic rats. RPE significantly decreased the fasting blood glucose, improved insulin sensitivity (HOMA-IR), OGTT, ITT and blood lipid profile. The glycogen synthesis and hexokinase activity were increased together with the improved signaling activity of insulin as indicated by p-IRS, p-IR, p-AKT, and p-GSK-3 beta. Conclusions: The results suggest that RPE reduced blood glucose in type 2 diabetic rats by improvement of insulin sensitivity. The effect is likely achieved by inhibition of oxidative stress and a-glucosidase.

Ethnopharmacological relevance The root of Rosa roxburghii Tratt (Ci Li Gen) is a kind of Chinese ethnomedicine in Gui Zhou province, used for the treatment of abdominal pain, acute bacillary dysentery, gastroenteritis and other diseases in human and livestock. Aim of the study The aim of this study was to isolate and identify the effective antimicrobial components from the ethyl acetate extract of the Ci Li Gen and to investigate its antimicrobial mechanism afterwards. Materials and methods The effective antimicrobial components in the ethyl acetate extract from the Ci Li Gen were isolated by high-performance liquid chromatography (HPLC) and identified by high-resolution mass spectrometry (HRMS) and nuclear magnetic resonance (NMR). The antibacterial activity was evaluated by the minimum inhibition concentration (MIC) measured by microdilution technique. The antibacterial mechanism was investigated by the time-kill curve, sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE) combined with NanoLC-ESI-MS/MS, intracellular esterase activity detected by Flow cytometry, and the ultrastructural changes of the Escherichia coli ATCC 25922 observed by scanning electron microscope (SEM). Results The effective antimicrobial component (peak 4) was identified as strictinin isomers by HRMS and NMR. The MIC of strictinin isomers against E. coli was 0.125 mg/mL. With respect to the negative control group, the results of SDS-PAGE and NanoLC-ESI-MS/MS showed that the up-regulated proteins of the strictinin isomers treated group were Metal-binding protein ZinT, 30S ribosomal protein S4 and 50S ribosomal protein L4, while the down-regulated protein was hydroperoxide reductase subunit C. Moreover, in the strictinin isomers treated group, the esterase activity in the E. coli cells was reduced and the bacteria E. coli became atrophied, pitted and contorted, and the surface of E. coli was rough and blurred. Conclusions According to the above results, the antimicrobial mechanism of strictinin isomers against E. coli were oxidative stress and protein synthesis disorder, which inhibited the activity of the enzymes required for bacterial growth and metabolism. These findings reflected the pleiotropic effects of strictinin isomers, making it a promising antimicrobial agent for pharmaceutical research.

Ethnopharmacological relevance As documented in the Chinese Materia Medica Grand Dictionary (中藥大辭典), a herbal formula (RL) consisting of Rosae Multiflorae Fructus (multiflora rose hips) and Lonicerae Japonicae Flos (Japanese honeysuckle flowers) has traditionally been used in treating inflammatory disorders. RL was previously reported to inhibit the expression of various inflammatory mediators regulated by NF-κB and MAPKs that are components of the TLR4 signalling pathways. Aim of the study This study aims to provide further justification for clinical application of RL in treating inflammatory disorders by further delineating the involvement of the TLR4 signalling cascades in the effects of RL on inflammatory mediators. Materials and methods RL consisting of Rosae Multiflorae Fructus and Lonicerae Japonicae Flos (in 5:3 ratio) was extracted using absolute ethanol. We investigated the effect of RL on the production of cytokines and chemokines that are regulated by three key transcription factors of the TLR4 signalling pathways AP-1, NF-κB and IRF3 in LPS-stimulated RAW264.7 cells using the multiplex biometric immunoassay. Phosphorylation of AP-1, NF-κB, IRF3, IκB-α, IKKα/β, Akt, TAK1, TBK1, IRAK-1 and IRAK-4 were examined in LPS-stimulated RAW264.7 cells and THP-1 cells using Western blotting. Nuclear localizations of AP-1, NF-κB and IRF3 were also examined using Western blotting. Results RL reduced the secretion of various pro-inflammatory cytokines and chemokines regulated by transcription factors AP-1, NF-κB and IRF3. Phosphorylation and nuclear protein levels of these transcription factors were decreased by RL treatment. Moreover, RL inhibited the activation/phosphorylation of IκB-α, IKKα/β, TAK1, TBK1 and IRAK-1. Conclusions Suppression of the IRAK-1/TAK1 and TBK1/IRF3 signalling pathways was associated with the effect of RL on inflammatory mediators in LPS-stimulated RAW264.7 and THP-1 cells. This provides further pharmacological basis for the clinical application of RL in the treatment of inflammatory disorders.

Ethnopharmacological relevance Rosa rugosa Thunb. is a traditional Chinese medicine that was used in the treatment of cardiovascular diseases and relative risk factors such as diabetes, hyperlipidemia, hypertension, and inflammation. Rosa rugosa flavonoids (RRFs) are the main components in Rosa rugosa Thunb. Several studies have demonstrated that RRFs can regulate plasma lipid contents, but the related mechanism of which has not yet been elucidated clearly. Aim of the study The goal of this study was to clarify the effects of RRFs on triglyceride metabolism and its related mechanisms. Materials and methods RRFs were obtained by ethanol extraction from Rosa rugosa Thunb.. Transgenic mice expressing human Apolipoprotein C3 (ApoC3) were used as a mouse model of hypertriglyceridemia. Fenofibrate (FNB), a PPARα agonist, was used as a positive control drug of decreasing high triglyceride. FNB (100 mg/kg) or RRFs (300 mg/kg) were given to the mice by gavage daily. Two weeks later, the changes of plasma lipid levels in the mice were measured by commercial kits, the clearance of triglyceride was evaluated by oral fat load test, and expression of the genes related to lipid β-oxidation and synthesis was detected in the mice livers by real time PCR. Results RRFs, as well as FNB, were found to significantly reduce plasma triglyceride (TG) levels in ApoC3 transgenic mice after administration of the drug for two weeks. Plasma lipid clearance rate was increased and lipid content in the mice livers was reduced after administration of RRF. Treatment with RRFs up-regulated mRNA expression of PPARα and its downstream gene of ACOX, while down-regulated mRNA expression of the genes related to fatty acid synthesis (FASN, SREBP-1c, and ACC1). The expression of LPL was raised, while the expression of ApoC3 was decreased, and Foxo1 was inhibited by RRFs in the mice livers. Conclusion RRFs can reduce plasma TG levels by repressing the expression of ApoC3 and inducing the expression of LPL in liver. RRFs could also reduce triglyceride in hepatocytes through increasing β-oxidation and decreasing synthesis of the lipids. These findings show the potency of further clinical application of RRFs as a hypolipidemic drug for treatment of cardiovascular diseases.

Ethnopharmacological relevance Rosa rugosa Thunb.'s flowers have been used for medicinal and food purposes for hundreds years in China. They have been used in Traditional Chinese Medicine (TCM) to effectively help in expansion of blood vessels and improvement of microcirculation. Current high prevalence of hypertension, and the associated side effects of synthetic Angiotensin I converting enzyme inhibitors usually prescribed for this condition, led us to the investigation of possible inhibitory activity of the Rosa rugosa Thunb. flower extracts on Angiotensin I converting enzyme (ACE). Materials and methods Two different extraction preparation: (1) powdered materials were extracted with water (RW) and then with water (RWW), ethyl acetate (RWE) and 95% ethanol (RWE95); (2) powdered materials were extracted with 95% ethanol (RE95) and then with water (RE95W), ethyl acetate (RE95E) and 95% ethanol (RE95E95). The inhibition activity was determined using in vitro the inhibitory effect on Angiotensin I converting enzyme (ACE), and using the acute response and chronic response on blood pressure which measured in spontaneously hypertensive rats (SHRs). Results Both RE95E95 and RWW had highest ACE inhibitor activities. The higher inhibitor activity of RE95E95 was also evaluated in SHRs by oral administration for antihypertensive effect. In acute experiment, the decrease in systolic blood pressure (SBP) and the increase in heart rate (HR) was observed at 2 h after administration at high (40 g/kg) and low (20 g/kg) dose; such reductions in SBP were maintained for 12 h. Low dose had reduced SBP significantly more than high dose. In multiple oral administration chronic experiment, a SBP reduction of 17.5 mmHg was observed after 6d administration at low dose, and such reductions were maintained for the next 8 days. Conclusions The experimental results demonstrated the antihypertensive effect of Rosa rugosa Thunb. flowers, which was attributed to inhibition of Angiotensin I converting enzyme.

Ethnopharmacological relevance: Rosa rugosa Thunb. (Rosaceae) has been traditionally used for treatments of diabetes, chronic inflammatory diseases, pain, and anticancer in Korea. Aim of study: We investigate the inhibitory effect of histone acetyltransferase activity from the methanol extract of stems of Rosa rugosa on androgen receptor-mediated transcriptional regulation. Materials and methods: For the present study, Rosa rugosa methanol extract (RRME) was obtained from stem part of Rosa rugosa using methanol extraction. Histone acetyltransferase assay were performed to measure the inhibitory effect on acetylation, reporter assay, real-time PCR and ChIP assay were performed to measure androgen receptor-mediated transcriptional regulation, and MTT test were performed to measure cell viability. Results: RRME inhibited both p300 and CBP (60–70% at 100g/ml) activity. We show RRME mediates agonist-dependent androgen receptor (AR) activation and suppresses antagonist-dependent inhibition. RRME treatment also decreased transcription of AR regulated genes and also reduced histone H3 and AR acetylation in the promoters of prostate-specific antigen (PSA) and -2-microglobulin (B2M). Finally, RRME treatment reduced the growth of LNCaP, a human prostate cancer cell line. Conclusion: These results demonstrate RRME is a potent HAT inhibitor, which reduced AR and histone acetylation leading to decreased AR-mediated transcription and reduced LNCaP cell growth. © 2008 Elsevier Ireland Ltd. All rights reserved.

The anti-inflammatory activities of Piper cubeba (fruit), Physalis angulata (flower) and Rosa hybrida (flower) were determined by carrageenan-induced paw edema, arachidonic acid-induced ear edema and formaldehyde-induced arthritis in mice. The anti-allergic and analgesic activities of these plants were also studied by using 2,4-dinitrofluorobenzene (DNFB)-induced contact hypersensitivity reaction (type IV) and hot plate test in mice, respectively. These plant extracts clearly exhibited inhibitory effects against acute and subacute inflammation by oral administration (200 mg/kg). Also, administration (200 mg/kg, p.o.) of plant extracts for 1 week significantly inhibited type IV allergic reaction in mice (P

Selvi, Selami/0000-0002-9959-6945 WOS: 000339035900008 PubMed: 24793217 Ethnopharmacological relevance: This study has identified not only the wild plants collected for medical purposes by local people of Elazig Province in the Eastern Anatolia Region, but also the uses and local names of these plants. These resources are usually regarded as part of a culture's traditional knowledge. Therefore, the aim of this study is to collect information from local population concerning the use of medicinal plants of the Elazig region; identify the most important medicinal plants used; determine the relative importance of the species surveyed and calculate the informant consensus factor (FIC) in relation to medicinal plant use. Materials and methods: A field study had been carried out for a period of approximately 2 years (2012-2013). A questionnaire was administered to the local people, through face-to-face interviews (Appendix A). Demographic characteristics of participants, names of the local plants, their utilized parts and preparation methods were investigated and recorded. The plant species were collected within the scope of the study; herbarium materials were prepared; and the specimens were entitled. The collected data were used to calculate the FTC and the plant use values. Results: 74 Plants were found to be used for medical purposes before in the literature analysis of the plants used in our study, while 6 plants were found to have no literature records. Our results showed that the highest use values were recorded for the species Unica dioica L (0.46) and Rosa canina L (0.42), while the highest FIC was cited for skin diseases (0.60). Conclusion: Data obtained showed that in the studied area the folk use of plants is alive and still derives from daily practice. Evaluation of pharmacological activity for the promising medicinal plants is suggested. (C) 2014 Elsevier Ireland Ltd. All rights reserved.

The hip of Rosa multiflora Thunb. has been traditionally used as a dietary supplement and a herbal remedy for the treatment of various diseases including cold, flu, inflammation, osteoarthritis, rheumatoid arthritis and chronic pain in China.To explore the anti-inflammatory ingredient of the hip of R. multiflora Thunb. and its mechanism of action.The ethanol extract of the hip of R. multiflora Thunb. was fractioned with petroleum ether, ethyl acetate and water, and each fraction was screened for anti-inflammatory activity in xylene-induced mouse ear edema model. Three more models, acetic acid-induced mouse vascular permeation, cotton pellet-induced rat granuloma, and carrageenan-induced rat hind paw edema were also employed to verify the anti-inflammatory effect of the identified fraction. To explore the mechanism of action, the activity of inducible nitric oxide synthase (iNOS) and the level of nitric oxide (NO) in sera, as well as mRNA expression level of cyclo-oxygenase-2 (COX-2) in inflammatory tissues of rats with carrageenan-induced hind paw edema were measured. GC-MS technology was applied to identify the active components in the active fraction.The petroleum ether fraction (PEF) was identified to be the active fraction in inflammation animal models (i.e., oral administration of PEF (168.48, 42.12 and 10.53 mg/kg) evoked a significantly (P0.001) dose-dependent inhibition of the xylene-induced mice ear edema). Down-regulating COX-2 expression (P0.001) and reducing NO production (P0.05) through inhibiting iNOS activity (P0.001) may be the partial mechanism of action of PEF. GC-MS analysis indicated that unsaturated fatty acids are enriched in PEF and may be responsible for the anti-inflammatory activity of PEF and this herb. The results of this study provide pharmacological and chemical basis for the application of the hip of R. multiflora Thunb. in inflammatory disorders.

Ethnopharmacological relevance Rosa canina L. is a medicinal plant largely used in traditional folk medicine. Several compounds from rose hip extracts were reported to display in vitro anti-inflammatory activities. Aim of the study The in vivo effects of Rosa canina extracts are still poorly investigated. In the present study the anti-inflammatory and the gastroprotective effects of a hydroalcoholic crude extract of Rosa canina fruits were tested in rat. Materials and methods The anti-inflammatory activity of the extract was tested on the carrageenin-induced rat paw edema assay. The gastroprotective effect was investigated on the ethanol-induced gastric damage model. The in vitro antioxidant activity of this extract was also quantified using the Briggs–Rauscher oscillating reaction, the Trolox Equivalent Antioxidant Capacity method, and the Total Phenolic Content. Results Data show that the Rosa canina extract inhibits the development of carrageenin-induced edema; the anti-inflammatory power is similar to that of indomethacin. The antiedema effect was more significant using a higher dose of the extract. The total score expressing gastric damage was lower in Rosa canina pre-treated stomachs with respect to unpre-treated ones, although the antiulcerogenic effectiveness was not statistically significant. The antiulcerogenic effectiveness was not statistically detectable, even if the total score expressing gastric damage was lower in Rosa canina stomachs from pre-treated rats with respect to unpre-treated ones. Chemical analysis revealed that the extract owns a good antioxidant activity that may also contribute to the anti-inflammatory effects observed in vivo. Conclusions Altogether, the present data demonstrate the anti-inflammatory property of Rosa canina suggesting its potential role as adjuvant therapeutic tool for the management of inflammatory-related diseases.

This study aimed to assess the anti-inflammatory and analgesic effects of Fructus Rosae Multiflorae (FRM, hips of Rosa multiflora Thunb.). FRM was extracted with 75% ethanol and the dried extract (FRME) was administered intragastrically (i.g.) at 100, 200 and 400 mg/kg. The anti-inflammatory effect was evaluated in four experimental animal models and analgesic effect in two animal models. Pretreatment with a single dose of FRME produced significant dose-dependent anti-inflammatory effects on carrageenin-induced rat hind paw edema, xylene-induced mouse ear edema and acetic acid-induced mouse vascular permeation. In a 7-day study, daily administration of FRME suppressed cotton pellet-induced rat granuloma formation. Pretreatment with a single dose of FRME also produced dose-dependent anti-nociceptive effects in thermally- and chemically induced mouse pain models. In addition, a single dose of FRME at 2.4 g/kg body weight (equivalent to 87.6 g of dried hips per kg body weight) produced no observable acute toxicity in mice within seven days. These results demonstrate that FRME possesses anti-inflammatory and analgesic effects and has no obvious acute toxicity, which advanced our understanding of the folk use of FRM in treating various inflammatory disorders.

Several therapeutic effects including hypnotic, antispasmodic, treatment of abdominal and chest pain and strengthening the heart have been described for the flowers of Rosa damascena. Therefore in the present study, the relaxant effects of ethanolic extract and essential oils of Rosa damascena on tracheal chains of guinea pigs were examined. The relaxant effects of four cumulative concentrations of ethanolic extract (0.25, 0.5, 0.75, and 1.0g%) and essential oils (0.25, 0.5, 0.75, and 1.0vol.%) in comparison with saline as negative control and four cumulative concentrations of theophylline (0.25, 0.5, 0.75, and 1.0mM) were examined by their relaxant effects on precontracted tracheal chains of guinea pig by 60mM KCl (group 1, n=5) and 10microM methacholine in two different conditions including: non-incubated tissues (group 2, n=8) and incubated tissues with 1microM propranolol and 1microM chlorpheniramine (group 3, n=5). In group 1 experiments two final concentrations of essential oil and theophylline and only final concentration of ethanolic extract showed relaxant effects compared to that of saline (p