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Rosmarinic acid (RA) is a highly valued natural phenolic compound that is very commonly found in plants of the families Lamiaceae and Boraginaceae, including Coleus blumei, Heliotropium foertherianum, Rosmarinus officinalis, Perilla frutescens, and Salvia officinalis. RA is also found in other members of higher plant families and in some fern and h...
Citations
... The phenolic compound rosmarinic acid also showed good docking scores against the targeted S. cervi DEPs. Rosmarinic acid is an anticancer, antiangiogenic, anti-inflammatory, and antimicrobial agent [66]. We observed that rosmarinic acid could bind strongly to several proteins, such as ADK, enolase, GAPDH, HSP 70, and PGK. ...
Lymphatic filariasis (LF) continues to impact 657 million individuals worldwide, resulting in lifelong and chronic impairment. The prevalent anti-filarial medications—DEC, albendazole, and ivermectin—exhibit limited adulticidal efficacy. Despite ongoing LF eradication programs, novel therapeutic strategies are essential for effective control. This study examines the mechanism of action of Ocimum sanctum on the filarial parasites Setaria cervi via a synergistic biochemical and proteomics methodology. The ethanolic extract of Ocimum sanctum (EOS) demonstrated potential anti-filarial action in the MTT reduction experiment, with an LC50 value of 197.24 µg/mL. After EOS treatment, an elevation in lipid peroxidation (51.92%), protein carbonylation (48.99%), and NADPH oxidase (88.88%) activity, along with a reduction in glutathione (GSH) (−39.23%), glutathione reductase (GR) (−60.17%), and glutathione S transferase (GST) (−50.48%) activity, was observed. The 2D gel electrophoresis identified 20 decreased and 11 increased protein spots in the EOS-treated parasites relative to the control group. Additionally, in drug docking analysis, the EOS bioactive substances ursolic acid, rutin, and rosmarinic acid show a significant binding affinity with the principal differentially expressed proteins. This paper demonstrates, for the first time, that the anti-filarial efficacy of EOS is primarily facilitated by its impact on energy metabolism, antioxidant mechanisms, and stress response systems of the parasites.
... The caffeic acid and 3,4-dihydroxyphenyllactic acid found in these plants occur as RA derivatives [22]. There are many studies on the numerous effects of RA, such as antitumor, anti-inflammatory, and antioxidant, and there are reports on its pharmacological effects [23]. Its inhibitory properties have been described in cancers such as skin, pancreatic, and breast cancer [24]. ...
Background/Objectives: Ovarian cancer has the highest mortality rate in the world. Treatment methods are listed as surgery, chemotherapy, and radiotherapy, depending on the stage of cancer, but developing resistance to chemotherapy increases the need for alternative agents that act on the same pathways. The effects of rosmarinic acid (RA) and doxorubicin (DX) on the activation of FOXP3, an important tumor suppressor gene, in OVCAR3 cells were examined. Materials and Methods: In this study, a human ovarian adenocarcinoma cell line was used. MTT analysis was performed to reveal the result of RA and DX on ovarian cancer cell proliferation. Expression levels of FOXP3 for cell proliferation and Capase-3 for apoptosis were determined by RT-qPCR. The wound healing model was applied to determine cell migration rates. The results were evaluated with one-way ANOVA in an SPSS 20.0 program as p ≤ 0.05. Results: It was determined that RA and DX alone and in combination inhibited the proliferation of OVCAR3 cells in different doses for 24, 48, and 72 h, and caused the cells to die by causing them to undergo apoptosis. Caspase-3 expression increased approximately tenfold in OVCAR3 cells, while FOXP3 expression was upregulated only in RA treatment and was downregulated in DX and RA + DX treatments. Conclusions: According to the results of our study, it was determined that the FOXP3 signaling pathway related to apoptosis, and proliferation was affected by the combination treatment of RA and DX in the OVCAR3 cancer cell line. This shows that RA will gain an important place in cancer treatment with more comprehensive study.
... The presence of numerous phytoconstituents in the investigated leaf extract of the herb [6] and, in particular, the high content of the polyphenolic compounds rosmarinic acid (RA) and ferulic acid (FA), as well as the iridoid glycoside epideoxyloganic acid, could be a cause of the established antiproliferative and anti-clonogenic effect of N. nuda. Available data confirm that RA possesses various pharmacological effects such as antioxidant, antiinflammatory, antimutagenic, colony-inhibitory, anticancer, etc. [32][33][34][35][36][37][38]. In particular, in colon carcinoma cell lines, CT26 and HCT116, the antimetastatic, antiproliferative, anti-invasive, and anti-migratory activities of RA are mediated by the activation of AMPactivated protein kinase, induction of caspase-3, -8, and -9, as well as reduction of the MMP-2, MMP-9, cyclin D1, CDK4, ICAM-1, and integrin β1 expression [39]. ...
Despite significant efforts, cancer remains the second leading cause of mortality worldwide. The medicinal plant Nepeta nuda L. represents a valuable source of biologically active compounds with pharmacological activities including antioxidant, anti-inflammatory, antimicrobial, and antiviral. This study aimed to assess the antiproliferative potential and mechanisms of action of aqueous extract from the leaves of wild-grown N. nuda. Cancer cell lines, MDA-MB-231, MCF7 (breast), HT29, Colon 26 (colon), and HepG2 (liver cancer), and a non-cancerous skin cell line, BJ, were assessed for antiproliferative activity by MTT assay and observation of cell morphological alterations. The cancer cell line that was most sensitive to the extract was further studied for apoptotic alterations by Annexin V/propidium iodide staining, colony-forming assay, and qRT-PCR analysis. The results revealed that the plant extract inhibited the proliferation of all investigated cancer cell lines with the strongest cytostatic effect on Colon 26 cells with a half maximal inhibitory concentration (IC50) value of 380.2 μg/mL and a selectivity index (SI) of 3.5. The extract significantly inhibited the ability of cells to form colonies, exhibited considerable proapoptotic potential involving the participation of the CASP8 gene, and increased the expression levels of ATG3 and the BECN1 gene, which suggests a role of autophagic cell death in the antitumor action.
... Rosmarinic acid (ROS), a natural polyphenolic compound, has garnered attention for its potential as an anticancer agent [12]. Studies indicate that it demonstrates anticancer properties by modulating signaling pathways involved in cancer cell growth [13,14]. Nevertheless, a challenge in utilizing ROS for cancer therapy lies in its limited water solubility [15]. ...
Background: Rosmarinic acid (ROS) has gained notable attention for its anticancer potential; however, its limited aqueous solubility hinders its effective delivery and application in pharmaceutical formulations. Methods: To overcome this limitation, an inclusion complex of ROS with β-cyclodextrin (β-CD) was prepared using the recrystallization method. The resultant ROS–β-CD complex was comprehensively characterized by powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FT-IR), and scanning electron microscopy (SEM). Results: The ROS–β-CD complex showed a significant improvement in the solubility and dissolution profile of ROS, underscoring its potential for enhanced bioavailability and therapeutic efficacy in pharmaceutical applications. In vitro assays were performed to assess the effects on cell viability, proliferation, apoptotic pathways, and 3D spheroid tumor models. Conclusions: The results demonstrated that ROS–β-CD exhibited superior anticancer properties compared to free ROS, effectively reducing the viability and proliferation of the MD-MBA-231 cell line and inducing apoptosis. This research signifies a substantial advancement in developing therapeutic strategies for TNBC, leveraging the distinct properties of the ROS–β-CD inclusion complex.
... However, comparing the antioxidant properties of cooked garlic samples with other studies in the literature is challenging because the results obtained vary depending on various parameters such as the composition of garlic, cooking technique, processing time, temperature, and extraction technique, as well as units used for giving the results. In one study, Alide et al. [17] reported that the amount of total remarkable biological properties of this phenolic acid have been demonstrated, such as hepatoprotective [74], antiinflammatory [71,75], anticancer [76] and neuroprotective activity [77]. It has found a place as a valuable antioxidant in the food industry thanks to its properties of free radical scavenging, chelating pro-oxidant ions, and inhibiting lipid peroxidation [78][79][80]. ...
This study determined the effects of cooking Taşköprü garlic, which is grown with a geographical indication in Turkiye, in three cooking materials (unbleached parchment paper (UP), bleached parchment paper (BP), and oven bag (OB)) and four vegetable oils (sunflower oil (SO), hazelnut oil (HO), corn oil (CO), and olive oil (OO)) on total phenolic content, antioxidant activity, phenolic compound profile, and chemical compound profile. The effects of cooking material (CM) and oil type (OT) on garlic samples’ TPC were found to be insignificant (p > 0.05). However, cooking material (CM) and oil type (OT) impacted antioxidant activity. According to cooking material, statistically, the highest antioxidant activity with the DPPH method was identified in garlic cooked using UP and BP, while the highest antioxidant activity with the ABTS method was found in garlic cooked with BP and OB. The garlic samples roasted with the mentioned oils and cooking materials were analyzed by LC-MS/MS in terms of thirty-five phenolic compounds. However, only five of these compounds (quinic acid, fumaric acid, hesperidin, ferulic acid, and rosmarinic acid) were detected in the samples. The chemical components of the cooked garlic samples primarily consist of terpenoids (β–sitosterol and squalene). The use of cooking material affected the amount of squalene compound in all garlic samples cooked with olive oil. Among these samples, the lowest squalene rate (52.11%) was found in only roasted garlic. In addition, according to GC-MS results, we can say that the use of hazelnut oil and unbleached parchment paper in the roasting process has a protective effect on the cis-vaccenic acid compound, which is known to show anticancer properties.
Graphical Abstract
... It is a widespread phenolic chemical that may be found in over 30 different plant families and is involved in a wide variety of fascinating biological and pharmacological processes. [45] RA has two catechol groups throughout its structure which have exhibited diverse biological-related properties-anti-inflammation, antibacterial, antiviral, antitumor, neuroprotective effects, photoprotective, and wound healing. [46] Because of these properties, it has been the subject of research and development in pharmaceutical studies as a natural chemical with potential biomedical applications. ...
Various wound dressings have been developed so far for wound healing, but most of them are ineffective in properly reestablishing the skin's structure, which increases infection risks and dehydration. Electrospun membranes are particularly interesting for wound dressing applications because they mimic the extracellular matrix of healthy skin. In this study, a potential wound healing platform capable of inducing synergistic antibacterial and antioxidation activities was developed by incorporating bio‐active rosmarinic acid‐hydroxyapatite hybrid (HAP‐RA) with different contents (0.5, 1, and 1.5 wt.%) into the electrospun polyamide 6 (PA6) nanofibers. Then, polyethylene glycol (PEG) was introduced to the nanofibrous composite to improve the biocompatibility and biodegradability of the dressing. The results indicated that the hydrophilicity, water uptake, biodegradability, and mechanical properties of the obtained PA6/PEG/HAP‐RA nanofibrous composite enhanced at 1 wt.% of HAP‐RA. The nanofibrous composite had excellent antibacterial activity. The antioxidation potential of the samples was assessed in vitro. The MTT assay performed on the L929 cell line confirmed the positive effects of the nanofibrous scaffold on cell viability and proliferation. According to the results, the PA6/PEG/HAP‐RA nanofibrous composite showed the desirable physiochemical and biological properties besides antibacterial and antioxidative capabilities, making it a promising candidate for further studies in wound healing applications.
... Among them, rosmarinic acid has been studied more. In industry, rosmarinic acid can be manufactured via esterification concerning 3,4-dihydroxyphenyllactic acid and caffeic acid [43], which has been proven to have a strong anti-tumor role [44]. The structural formula of the active components of P. vulgaris is shown in Figure 3. consisting of three cyclohexane rings and one cyclopentane ring was found at the C5-6 position. ...
... Among them, rosmarinic acid has been studied more. In industry, rosmarinic acid can be manufactured via esterification concerning 3,4-dihydroxyphenyllactic acid and caffeic acid [43], which has been proven to have a strong anti-tumor role [44]. The structural formula of the active components of P. vulgaris is shown in Figure 3. ...
Purpose: To investigate and systematically describe the mechanism of action of Prunella vulgaris (P. vulgaris) against digestive system tumors and related toxicity reduction. Methods: This study briefly describes the history of medicinal food and the pharmacological effects of P. vulgaris, focusing on the review of the anti-digestive tumor effects of the active ingredients of P. vulgaris and the mechanism of its toxicity reduction. Results: The active ingredients of P. vulgaris may exert anti-tumor effects by inducing the apoptosis of cancer cells, inhibiting angiogenesis, inhibiting the migration and invasion of tumor cells, and inhibiting autophagy. In addition, P. vulgaris active ingredients inhibit the release of inflammatory factors and macrophages and increase the level of indicators of oxidative stress through the modulation of target genes in the pathway to achieve the effect of toxicity reduction. Conclusion: The active ingredients in the medicine food homology plant P. vulgaris not only treat digestive system tumors through different mechanisms but also reduce the toxic effects. P. vulgaris is worthy of being explored more deeply.
... Z. capitata contains rosmarinic acid (top concentration), a phenolic compound with antitumor, antimicrobial, anti-inflammatory, antioxidant, and antidepressant properties. (Swamy et al. 2018;Nadeem et al. 2019). Quercetin and its glycosides are types of flavonoid, have been demonstrated in vitro to have strong biological activity and to prevent the proliferation of prostate cancer cells (Gouda et al. 2022;Jakimiuk et al. 2022). ...
Abstract
Ziziphora capitata (Lamiaceae family) aerial parts extract contains 57 metabolites, including flavonoids, phenolic acids, anthocyanins, and coumarins, as assessed by UPLC-QTOF-MS/MS. Successive extracts (hexane, chloroform, ethyl acetate, ethanol 95%, and water) were tested in vitro cytotoxic activity against HepG-2, MCF-7, HCT-116, A549, and PC3 cell lines. The results revealed that hexane extract exhibited the most potent cytotoxic activity among PC3 and A549 cell lines, IC50 = 47.1 ± 1.75 and 49.2 ± 1.08 µg/mL compared to Vinblastine IC50 = 42.47 ± 1.95 and 24.64 ± 1.18 µg/mL, respectively, and had a moderate impact on the remaining cell lines. Moreover, the chloroform and ethyl acetate extracts exhibited moderate affinity among all tested cell lines. Furthermore, the total phenolic and flavonoid contents were assessed. The molecular docking simulation was performed inside the effective sites of VEGFR-2 and TS as anticancer targets for the top ten phytochemicals. The results showed higher binding energy values for VEGFR-2 than for TS compared to vinblastine and co-crystallized ligands.
... A plethora of pharmacological properties has been attributed to Rosmarinic Acid, including antiviral, antibacterial, astringent, antimutagenic, anti-inflammatory, antiallergic, and antioxidant activities, with the latter two being the most widely known and extensively studied [50,63,70,72,77,82,83]. Studies have shown that Rosmarinic Acid also acts as an immunomodulatory and neuroprotective factor [83]. Rosmarinic Acid's contribution to the reduction in tumor development has been noticed in many cancer types, including colon, breast, liver, stomach, and lung, as well as melanoma and leukemia [77,84]. ...
Breast cancer is the most frequent type of cancer in women. Oncogenic transcription factors promote the overproduction of cellular adhesion molecules and inflammatory cytokines during cancer development. Cancer cells exhibit significant upregulation of antiapoptotic proteins, resulting in increased cell survival, tumor growth, and metastasis. Research on the cell cycle-mediated apoptosis pathway for drug discovery and therapy has shown promising results. In fact, dietary phytoconstituents have been extensively researched for anticancer activity, providing indirect protection by activating endogenous defense systems. The role of polyphenols in key cancer signaling pathways could shed light on the underlying mechanisms of action. For instance, Rosmarinic Acid, a polyphenol constituent of many culinary herbs, has shown potent chemoprotective properties. In this review, we present recent progress in the investigation of natural products as potent anticancer agents, with a focus on the effect of Rosmarinic Acid on triple-negative BC cell lines resistant to hormone therapy. We highlight a variety of integrated chemical biology approaches aimed at utilizing relevant mechanisms of action that could lead to significant clinical advances in BC treatment.
... Rosmarinic acid, a caffeic acid ester with a molecular weight of 360 Da, belongs to the hydroxyl cinnamic acids family. It is formed by the esterification of 3,4-dihydroxycinnamic acid (caffeic acid) and 3,4-dihydroxyphenyllactic acid (DHPL) (39)(40)(41). This compound possesses a hydroxylated cinnamic acid moiety at the ortho-, meta-, or para-position of the benzene ring. ...
The Salvia genus, a member of the Lamiaceae family, exhibits a rich array of secondary metabolites, including di- and triterpenoids, phenols, polyphenols, and essential oil compounds. These constituents contribute to valuable pharmacological activities such as antibacterial, antiviral, anti-inflammatory, and antioxidant properties. Among these metabolites, rosmarinic acid stands out as a particularly promising compound, deriving from the precursors phenylalanine and tyrosine. It belongs to the phenolic compound class and acts as an ester of caffeic acid, showcasing diverse therapeutic potentials like antifungal, antibacterial, antiviral, antioxidant, anticancer, anti-ageing, anti-inflammatory, and anti-diabetic effects. To facilitate the production of such secondary metabolites, plant tissue culture techniques have played a pivotal role, with hairy root cultures being one of the preferred methods. This review provides an extensive examination of the biosynthetic pathway of rosmarinic acid and its successful generation using hairy root cultures. Additionally, the review highlights the utilization of genetic modification tools and various biotic and abiotic elicitors, including yeast extract, methyl jasmonate, and silver ion (Ag+), in hairy root cultures of diverse Salvia species to enhance the production of rosmarinic acid.
