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Fast Quantification of Phenylethyl Alcohol in Rose Water and Chemical Profiles of Rose Water and Oil of Rosa damascena and Rosa rugosa from Southeast China

Gaoming Lei,Longhu Wang,Xuesong Liu,Anyun Zhang

A new and effective high performance liquid chromatography (HPLC) method was developed for fast quantification of phenylethyl alcohol in rose water. Chemical profiles of rose water and oil of Rosa damascena and Rosa rugosa from Southeast China were investigated by gas chromatography (GC) and gas chromatography–mass spectrometry (GC–MS). Fast HPLC was achieved by rapid sample preparation and fast elution using acetonitrile–water (35:65, v/v) on Zorbax SB-C18. It was validated and applied to rapid analysis of different rose water samples, in which the contents of phenylethyl alcohol ranged from 454.6 to 526.7 µg/mL. GC and GC–MS revealed that rose water volatiles of R. damascena and R. rugosa mainly consisted of phenylethyl alcohol (90.2% and 78.7%, respectively) and citronellol (4.5% and 13.5%, respectively). This is the first report on fast HPLC quantification of phenylethyl alcohol in rose water and chemical profiles of rose water volatiles of R. damascena and R. rugosa from Southeast China. The developed HPLC method can serve as a fast quality control during rose water production.

Characterization and potential bioactivity of polyphenols of Rosa rugosa

Lan Wei,Jingjing Li,Yun Yang,Mei Zhu,Mengke Zhao,Jianhua Yang,Zhiyun Yang,Luyao Zhou,Shenyue Zhou,Jiajia Gong,Xiaogang Jiang,Jiangyun Liu,Yali Li,Jian Zhang

Rosa rugosa is widely cultivated in China, and the blossom of R. rugosa is used to extract rose essential oil or directly make into various foods, such as mei gui hua cake, mei gui hua sauce. Rose dregs are mostly used as fertilizer after extracting essential oil and the polar part has not been fully utilized. There is still much to be done in the products and deep processing of rose. In this study the content of total flavonol glycosides , the extractable polyphenols, the non-extractable polyphenols, the total phenolic and the total anthocyanins in R. rugosa from five major production areas in China was analyzed; the biological activities of the total extract, the polyphenols fraction, the flavonol glycosides fraction and the isolated compounds of R. rugosa were evaluated, including antioxidant, anti-ultraviolet, inhibitory activities of α -glucosidase, lipase , alveolar epithelial cell senescence and tyrosinase , together with regulating activities on intestinal flora . The components content of R. rugosa in different producing areas was significantly different. The total flavonol glycosides in Yunnan, the extractable polyphenols and the total phenolics in Shandong, the non-extractable polyphenols in Xinjiang, the total anthocyanins in Gansu was the higher than other areas. The polyphenols fraction showed antioxidant and anti-ultraviolet properties, inhibition of alveolar epithelial cell senescence, lipase and tyrosinase activities, and regulation of intestinal flora. The flavonol glycosides fraction showed α -glucosidase inhibitory activity. The results showed the polyphenols fraction and the flavonol glycosides fraction of R. rugosa could be used as skin care products and healthy food ingredient.

Preparation and in vitro Immunoreactivity of Rosa rugosa Polysaccharide Liposomes

Qinfang He,Riqing Cheng,Jiahao Shi,Ta Na,Qiherima Wang,Sarangowa Ochir

Background Rosa rugosa polysaccharides (RRP), a principal active component derived from R. rugosa Thunb., exert immunomodulatory effects. However, their therapeutic application is limited by rapid metabolism, short duration of action, and low bioavailability. Objectives To optimize the preparation process of Rosa rugosa polysaccharide liposomes (RRPL) and evaluate their immune cell activation in vitro. Methods The RRPL were prepared using the reverse-phase evaporation method, with encapsulation efficiency (EE) as the primary evaluation criterion. An orthogonal test was employed to optimize the preparation parameters. Various characteristics of RRPL were assessed, including morphology, particle size, Polydispersity Index (PDI), zeta potential, cumulative release rate in vitro, and stability. The immunological effects of RRPL were evaluated through cellular assays involving mouse spleen lymphocytes, peritoneal macrophages, and bone marrow-derived dendritic cells (BMDCs). Results The RRPL demonstrated an EE of approximately 81.96%, an average drug loading (DL) capacity of 13.86%, a particle size of 124.00 nm, a PDI of 0.23, and a zeta potential of -12.97 mV. The formulated RRPL exhibited high EE and DL capacity, alongside favorable slow-release properties and stability. These enhancements led to improved drug bioavailability and prolonged duration of action. Furthermore, RRPL significantly promoted the proliferation of spleen lymphocytes; enhanced the phagocytic activity of peritoneal macrophages; increased the secretion of interleukin (IL)-6, IL-1β, and interferon (IFN)-γ; activated immature BMDCs; and induced the maturation of BMDCs, resulting in increased production of IL-12p70 and tumor necrosis factor (TNF)-α. Conclusions This study successfully developed RRPL that markedly enhance immune cell activation compared with RRP. These findings provide a theoretical foundation for further exploration and development of these liposomal formulations.

Biosynthesis of Selenium Nanoparticles from Rosa rugosa Extract: Mechanisms and Applications for Sustainable Crop Protection

Le Song,Man Liang,Yingxiu Wang,Yanli Bian

Selenium nanoparticles (SeNPs) show great potential for sustainable agriculture, but their green synthesis and practical application still need further optimization. This study established a green synthesis method for SeNPs using lyophilized rose (Rosa rugosaThunb.) powder as both a reducing and stabilizing agent to reduce sodium selenite (Na2SeO3), key parameters, including template concentration, Na2SeO3/VC ratio, and reaction temperature were systematically optimized. This process yielded stable, spherical SeNPs with optimal properties, exhibiting a diameter of 90 nm and a zeta potential of −35 mV. Structural characterization confirmed that selenium forms chelation complexes through carboxyl and hydroxyl oxygen-binding sites. The SeNPs exhibited exceptional stability (retained 426 days at 25 °C) and pH tolerance (pH 4–10), though divalent cations (Ca2+) triggered aggregation. In agricultural application tests, 5 mg/L SeNPs increased tomato plant biomass by 84% and antioxidant capacity by 152% compared to controls, and the biosynthesis pathways of salicylic acid and jasmonic acid were upregulated. Moreover, the SeNPs exhibited strong concentration-dependent antifungal activity against several major pathogens. Among these pathogens, tomato gray mold (Botrytis cinerea) was the most sensitive, as evidenced by its low EC50(4.86 mg/L) and sustained high inhibition rates, which remained substantial even at 1 mg/L and reached 94% at 10 mg/L. These findings highlight SeNPs as a friendly alternative for minimizing agrochemical use in sustainable agriculture.

Untargeted metabolomics analysis revealed metabolite dynamics during the development and processing of Rosa rugosa flowers

Xi Cheng,Xin Li,Dongliang Chen,Qiong Wang,Hongli Wang,Kang Gao,Yanchao Luo,Yanni Sun,Conglin Huang

Rosa rugosa , which originated in China, is an important industrial plant, which have been used for landscaping, while its components have been included in foods, pharmaceuticals, and beauty and skin care products. As a potential available oil rose variety, the limited comprehensive understanding of R. rugosa ‘Han Xiang’ has hindered their development and utilization. In this study, UPLC-MS/MS and GC-MS techniques were applied to analyze metabolite dynamics during the development and processing of R. rugosa flowers. In total, 1816 non-volatile metabolites and 1029 volatile metabolites were identified in the development and processing of R. rugosa flowers. Significant differences in the non-volatile and volatile metabolites were detected in the petals and hydrosol. The differentially regulated non-volatile metabolite contents were highest in the bud stage petals, the differentially regulated volatile metabolite contents were highest in the full-bloom stage petals. Some key metabolites affect the presentation of rose color, flavor, and taste, as well as the efficacy of the product. The aim of this article is to provide a comprehensive understanding of R. rugosa ‘Han Xiang’ and to serve as a basis for further research and development. This study provides useful data for assessing rose flower quality as well as new insights into R. rugosa development and utility.

Bee Pollen Polysaccharide From Rosa rugosa Thunb. (Rosaceae) Promotes Pancreatic β-Cell Proliferation and Insulin Secretion

Yang Siwen,Qu Yunhe,Chen Jiyu,Chen Si,Sun Lin,Zhou Yifa,Fan Yuying

Insufficient pancreatic β-cell or insulin-producing β-cell are implicated in all types of diabetes mellitus. Our previous studies showed bee pollen polysaccharide RBPP-P improves insulin resistance in type 2 diabetic mice by inhibiting liver fat deposition. However, its potential of regulating β-cell function and integrity is not fully known. Herein, we observed that β-cell proliferation (n = 10), insulin synthesis (n = 5, p = 0.01684) and insulin incretion (n = 5, p = 0.02115) were intensely activated in MIN6 cells when treatment with RBPP-P. In alloxan-induced diabetic mice, oral administration of RBPP-P (n = 10) effectively decreased the blood glucose (p = 0.0326), drink intake (p < 0.001) and urine (p < 0.001). It directly stimulated phosphorylation of p38 (p = 0.00439), ERK (p = 0.02951) and AKT (p = 0.0072) to maintain the islet function and mass. Thus, our data suggest that RBPP-P is a natural compound to regulate β-cell proliferation and function, indicating it might have therapeutic potential against type 1 diabetes.

Therapeutic potential of Rosa rugosa polysaccharide and its nanofiber membrane in psoriasis via PI3K-AKT/mTOR pathway inhibition

Mengxiang Chen,Yi Peng,Rongtao Zhu,Xiaoting Luo,Xuemin Yang,Jiazhi Chen,Haiyan Chen,Wei Zhou,Zhiyun Du

Psoriasis is a chronic inflammatory skin disease with significant impacts on quality of life. Current treatments face challenges like high costs and side effects. This study explores the therapeutic potential of Rosa rugosa polysaccharide (RRPS) and its nanofiber membrane in psoriasis treatment. RRPS was extracted using a yeast fermentation enzyme-assisted method and characterized. In vitro studies on RAW264.7 macrophages showed that RRPS significantly reduced nitric oxide (NO) production, indicating anti-inflammatory effects. The nanofiber membrane, fabricated via electrospinning, has high porosity and sustained-release properties, enhancing drug delivery and skin barrier repair. In vivo studies using an imiquimod-induced psoriasis mouse model demonstrated that both RRPS and its nanofiber membrane improved psoriasis symptoms, reduced transepidermal water loss (TEWL), and inhibited pro-inflammatory cytokines (e.g., TNF-α, IL-6, IL-17A). Mechanistically, they suppressed the PI3K-AKT/mTOR pathway. The nanofiber membrane showed superior efficacy compared to RRPS alone, highlighting the benefits of electrospinning. This study suggests that Rosa rugosa polysaccharide and its nanofiber membrane could be a novel, effective, and safe alternative for psoriasis treatment by targeting the PI3K-AKT/mTOR pathway.

Degradation kinetic of anthocyanins from rose (Rosa rugosa) as prepared by microencapsulation in freeze-drying and spray-drying

Yajing Yu,Yuanping Lv

Anti-Obesity Effects of Rosa rugosa Thunb. Flower Bud Extracts on Lipid Metabolism Regulation in 3T3-L1 Adipocytes and Sprague Dawley Rats

Jung Min Kim,Kyoung Kon Kim,Hye Rim Lee,Jae Cheon Im,Tae Woo Kim

In modern society, obesity and its associated complications have emerged as serious public health concerns, primarily stemming from sedentary lifestyles and carbohydrate-rich diets. Due to the severe side effects often associated with pharmacological anti-obesity agents, emerging global efforts focus on preventive strategies, e.g., dietary modifications and weight gain-suppressing functional foods. In this context, plant-derived metabolites are extensively investigated for their beneficial anti-obesity effects. In this study, we evaluated how Rosa rugosa Thunb. flower bud extract affects fat metabolism in 3T3-L1 preadipocyte cells. The extract significantly inhibited adipocyte differentiation and intracellular triglyceride accumulation in 3T3-L1 cells, enhanced lipolysis, suppressed lipogenesis, and promoted energy metabolism in differentiated adipocytes. In vivo, it reduced body and organ weights and fat mass in high-fat diet-induced obese rats, along with marked adipocyte size and hepatic lipid accumulation reductions. In the epididymal adipose tissue, the extract similarly enhanced lipolytic activity, suppressed lipogenic enzyme expression, and stimulated energy expenditure. Taken together, our results demonstrate the potential of R. rugosa Thunb. flower bud extract in reducing fat accumulation through lipid metabolism modulation both in cellular and animal models. Further studies are warranted to identify the active constituents and evaluate the safety and efficacy of the extract in clinical applications.

Metabolomics, network pharmacology, and molecular docking reveal the anti-melanogenic efficacy and mechanism of gallocatechin in Rosa rugosa ‘Dian hong’ ethanol-water extracts

Yanxia Tao,Guanglian Hu,Qianqian Li,Wenjing Zhang,Xiaomi Yang,Xiaofei Li,Xuhong Zhou

First integrated network pharmacology and metabolomics study to elucidate the skin-whitening mechanism of Rosa rugosa ‘Dianhong’ (DH rose), a variety whose bioactive constituents and anti-melanogenic effects have not been previously characterized. • DH rose extracts demonstrated significant inhibition of tyrosinase activity and melanin production in both cellular and zebrafish models. • Gallocatechin was identified as a novel anti-melanogenic compound, expanding the current repertoire of natural tyrosinase inhibitors, with strong binding affinities to core targets (AKT1, TP53) confirmed by molecular docking. • Multi-target mechanism involving regulation of Rap1, PI3K-Akt, and MAPK signaling pathways, with core targets including EGFR, AKT1, SRC, and PTGS2. This study employed an integrated approach combining network pharmacology and metabolomics to systematically evaluate the anti-melanogenic potential of Rosa rugosa ‘Dianhong’ (DH rose) extracts, while also utilizing correlation analysis and molecular docking to predict novel anti-melanogenic compounds. The chemical constituents of DH rose extracts were identified using UPLC-MS/MS, followed by network pharmacology screening of active component targets, which were mapped against known anti-melanogenic targets to construct a compound-target-pathway network for identifying core targets and key signaling pathways. The inhibitory effects of the extracts on melanogenesis were subsequently validated in both cellular and zebrafish models, demonstrating that DH rose extracts significantly inhibited tyrosinase activity and melanin production. Integrated metabolomics and network pharmacology analyses suggested that the anti-melanogenic effect is mediated through the regulation of core targets such as EGFR, AKT1, SRC, and PTGS2, and pathways including Rap1, PI3K-Akt, and MAPK. Correlation analysis identified gallocatechin as a key bioactive compound, which significantly suppressed tyrosinase activity and reduced melanin levels in an α-MSH-induced zebrafish model, while molecular docking further confirmed strong binding affinities between gallocatechin and core targets. In conclusion, to our knowledge, this study applies an integrated network pharmacology and metabolomics strategy to elucidate the multi-target anti-melanogenic mechanism of DH rose, a specific variety whose bioactive constituents and anti-melanogenic effects have not been previously characterized. Notably, gallocatechin was identified as a rarely reported, candidate new anti-melanogenic compound, provide new insights into the current repertoire of natural tyrosinase inhibitors. These findings position DH rose as a promising candidate for cosmetic anti-melanogenic applications and highlight gallocatechin as a valuable lead compound for further development.

Ethanol Extract of Rosa rugosa Ameliorates Acetaminophen-Induced Liver Injury via Upregulating Sirt1 and Subsequent Potentiation of LKB1/AMPK/Nrf2 Cascade in Hepatocytes

Yecheng Lei,Xiao Lei,Anqi Zhu,Shijie Xie,Tiantian Zhang,Chuo Wang,Anning Song,Xiaoming Wang,Guangwen Shu,Xukun Deng

Acetaminophen (APAP)-induced liver injury is a common hepatic disease resulting from drug abuse. Few targeted treatments are available clinically nowadays. The flower bud ofRosa rugosahas a wide range of biological activities. However, it is unclear whether it alleviates liver injury caused by APAP. Here, we prepared an ethanol extract ofRosa rugosa(ERS) and analyzed its chemical profile. Furthermore, we revealed that ERS significantly ameliorated APAP-induced apoptosis and ferroptosis in AML-12 hepatocytes and dampened APAP-mediated cytotoxicity. In AML-12 cells, ERS elevated Sirt1 expression, boosted the LKB1/AMPK/Nrf2 axis, and thereby crippled APAP-induced intracellular oxidative stress. Both EX527 and NAM, which are chemically unrelated inhibitors of Sirt1, blocked ERS-induced activation of LKB1/AMPK/Nrf2 signaling. The protection of ERS against APAP-triggered toxicity in AML-12 cells was subsequently abolished. As expression of LKB1 was knocked down, ERS still upregulated Sirt1 but failed to activate AMPK/Nrf2 cascade or suppress cytotoxicity provoked by APAP. Results of in vivo experiments showed that ERS attenuated APAP-caused hepatocyte apoptosis and ferroptosis and improved liver injury and inflammation. Consistently, ERS boosted Sirt1 expression, increased phosphorylations of LKB1 and AMPK, and promoted Nrf2 nuclear translocation in the livers of APAP-intoxicated mice. Hepatic transcriptions of HO-1 and GCLC, which are downstream antioxidant genes of Nrf2, were also significantly increased in response to ERS. Our results collectively indicated that ERS effectively attenuates APAP-induced liver injury by activating LKB1/AMPK/Nrf2 cascade. Upregulated expression of Sirt1 plays a crucial role in ERS-mediated activation of LKB1.Keywords:extract ofRosa rugosa;acetaminophen;liver injury;Sirt1;Nrf2

A comparative study on chemical compositions and biological activities of four essential oils: Cymbopogon citratus (DC.) Stapf, Cinnamomum cassia (L.) Presl, Salvia japonica Thunb. and Rosa rugosa Thunb.

Chunlian Li,Yijie Luo,Weicheng Zhang,Qiuyang Cai,Xianyi Wu,Zekai Tan,Rui Chen,Zehao Chen,Shimin Wang,Lanyue Zhang

Ethnopharmacological relevance Essential oils (EOs) are important active ingredients in Chinese herbal medicine. Cymbopogon citratus (DC.) Stapf, Cinnamomum cassia (L.) Presl, Salvia japonica Thunb., and Rosa rugosa Thunb. are used in local and traditional medicine to treat inflammation-related diseases. While the constituents and bioactivities of EOs of the above four Chinese herbals have been reported previously, but their anti-inflammatory and antioxidant activities have not been systematically evaluated. Aim of the study The purpose of this study was to research the chemical constituents, anti-inflammatory activities, and antioxidant activities of EOs of four Chinese herbal medicines. Materials and methods Fresh plant materials were collected both in August 2018. The compositions of EOs were determined by the gas chromatography-mass spectrometry (GC-MS) method. TPA (12-O-tetradecylphophenol-13-acetate)-induced mouse ear model was evaluated the anti-inflammatory activities of EOs. The reduction of tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6), cyclooxygenase-2 (COX-2) and RelA protein of the nuclear factor kappa-B (NF-κB) in the signal pathway (P65) were measured. The antioxidant activities of EOs from four plants were determined by using 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging method. Results A total of 217 compounds were separated and identified from four EOs, mainly including trans-cinnamylaldehyde (68.75%), citronellal (38.16%), linalool (1.02–33.73%), geraniol (19.39%) and citronellol (17.18%). All four EOs reduced the damage of the ear tissue and had certain anti-inflammatory effects, and the EOs of C. citratus (CyCEOs) and S. japonica (SJEOs) had the best anti-inflammatory activities among others, even better than ibuprofen . The four EOs exhibited different DPPH radical-scavenging activities (IC 50 , 0.101–1.017%), where most of them were much lower than that of EOs of C. citratus (CiCEOs) (IC 50 , 0.101%) and EOs of R. rugosa (RREOs) (IC 50 , 0.142%). Conclusions The main components determine diverse propertise of these four EOs, our results suggested that four EOs presented anti-inflammatory and antioxidant effect via reducing the expression of TNF-a, IL-6, COX-2, and NF-κB p65, which may provide a new approach for development of new anti-inflammatory drugs.