Displaying publications 21 - 40 of 132 in total

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  1. Kassim M, Achoui M, Mansor M, Yusoff KM
    Fitoterapia, 2010 Dec;81(8):1196-201.
    PMID: 20708657 DOI: 10.1016/j.fitote.2010.07.024
    We investigated the effects of honey and its methanol and ethyl acetate extracts on inflammation in animal models. Rats' paws were induced with carrageenan in the non-immune inflammatory and nociceptive model, and lipopolysaccharide (LPS) in the immune inflammatory model. Honey and its extracts were able to inhibit edema and pain in inflammatory tissues as well as showing potent inhibitory activities against NO and PGE(2) in both models. The decrease in edema and pain correlates with the inhibition of NO and PGE(2). Phenolic compounds have been implicated in the inhibitory activities. Honey is potentially useful in the treatment of inflammatory conditions.
    Matched MeSH terms: Inflammation/drug therapy*
  2. Zakaria ZA, Wen LY, Abdul Rahman NI, Abdul Ayub AH, Sulaiman MR, Gopalan HK
    Med Princ Pract, 2007;16(6):443-9.
    PMID: 17917444
    The present study was carried out to determine the antinociceptive, anti-inflammatory and antipyretic activities of the aqueous extract of Bauhinia purpurea leaves using animal models.
    Matched MeSH terms: Inflammation/drug therapy*
  3. Leong CF, Soo PY, Fadilah SAW, Cheong SK
    Med J Malaysia, 2003 Mar;58(1):131-4.
    PMID: 14556340
    A 49 year-old Indian housewife was diagnosed with Hodgkin's disease in 1995. She was given combination chemotherapy comprising Chlorambucil, Vincristine, Procarbazine and Prednisolone. Unfortunately she defaulted after two courses of chemotherapy. One year later, she developed progressive right knee swelling and pain, associated with loss of appetite, loss of weight, intermittent fever, night sweats and pruritus. The right knee swelling measured 15 cm x 20 cm and was warm and tender. A plain radiograph of the right knee revealed osteolytic lesions at the distal end of the right femur and the proximal ends of the right tibia and fibula, associated with gross periosteal reaction and soft tissue swelling. Apart from left cervical lymphoadenopathy, examination of other systems was unremarkable. Pelvic bone marrow biopsy was inconclusive. An open biopsy of the lower end of the right femur was consistent with Hodgkin's disease. She was given salvage combination therapy comprising Chlorambucil, Vincristine, Procarbazine, Prednisolone, Doxorubicin, Bleomycin and Vinblastine. She tolerated the treatment well and responded with significant reduction in the swelling and pain of the right knee. Unfortunately, she again defaulted treatment after 2 courses of chemotherapy. This case illustrates an unusual presentation of Hodgkin's disease in relapse.
    Matched MeSH terms: Inflammation/drug therapy*
  4. Wong SK, Chin KY, Ima-Nirwana S
    Int J Med Sci, 2020;17(11):1625-1638.
    PMID: 32669965 DOI: 10.7150/ijms.47103
    Oxidative stress and inflammation are two interlinked events that exist simultaneously in metabolic syndrome (MetS) and its related complications. These pathophysiological processes can be easily triggered by each other. This review summarizes the current evidence from animal and human studies on the effects of vitamin C in managing MetS. In vivo studies showed promising effects of vitamin C, but most of the interventions used were in combination with other compounds. The direct effects of vitamin C remain to be elucidated. In humans, the current state of evidence revealed that lower vitamin C intake and circulating concentration were found in MetS subjects. A negative relationship was observed between vitamin C intake / concentration and the risk of MetS. Oral supplementation of vitamin C also improved MetS conditions. It has been postulated that the positive outcomes of vitamin C may be in part mediated through its anti-oxidative and anti-inflammatory properties. These observations suggest the importance of MetS patients to have an adequate intake of vitamin C through food, beverages or supplements in order to maintain its concentration in the systemic circulation and potentially reverse MetS.
    Matched MeSH terms: Inflammation/drug therapy
  5. Elsayed EA, El Enshasy H, Wadaan MA, Aziz R
    Mediators Inflamm, 2014;2014:805841.
    PMID: 25505823 DOI: 10.1155/2014/805841
    For centuries, macrofungi have been used as food and medicine in different parts of the world. This is mainly attributed to their nutritional value as a potential source of carbohydrates, proteins, amino acids, and minerals. In addition, they also include many bioactive metabolites which make mushrooms and truffles common components in folk medicine, especially in Africa, the Middle East, China, and Japan. The reported medicinal effects of mushrooms include anti-inflammatory effects, with anti-inflammatory compounds of mushrooms comprising a highly diversified group in terms of their chemical structure. They include polysaccharides, terpenoids, phenolic compounds, and many other low molecular weight molecules. The aims of this review are to report the different types of bioactive metabolites and their relevant producers, as well as the different mechanisms of action of mushroom compounds as potent anti-inflammatory agents.
    Matched MeSH terms: Inflammation/drug therapy*
  6. Tew XN, Xin Lau NJ, Chellappan DK, Madheswaran T, Zeeshan F, Tambuwala MM, et al.
    Chem Biol Interact, 2020 Feb 01;317:108947.
    PMID: 31968208 DOI: 10.1016/j.cbi.2020.108947
    Inflammatory responses play a remarkable role in the mechanisms of acute and chronic respiratory diseases such as chronic obstructive pulmonary disease (COPD), asthma, pulmonary fibrosis and lung cancer. Currently, there is a resurgence in the use of drugs from natural sources for various ailments as potent therapeutics. Berberine, an alkaloid prominent in the Chinese traditional system of medicine has been reported to exert therapeutic properties in various diseases. Nevertheless, the number of studies focusing on the curative potential of berberine in inflammatory diseases involving the respiratory system is limited. In this review, we have attempted to discuss the reported anti-inflammatory properties of berberine that function through several pathways such as, the NF-κB, ERK1/2 and p38 MAPK pathways which affect several pro-inflammatory cytokines in the pathophysiological processes involved in chronic respiratory diseases. This review would serve to provide valuable information to researchers who work in this field and a new direction in the field of drug discovery with respect to respiratory diseases.
    Matched MeSH terms: Inflammation/drug therapy*
  7. Ilori NTO, Liew CX, Fang CM
    Mol Biol Rep, 2020 Dec;47(12):9883-9894.
    PMID: 33244664 DOI: 10.1007/s11033-020-06025-x
    This appraisal is comprised of the inflammatory studies that have been conducted on Clinacanthus nutans, Acanthus ebracteatus, and Barleria lupulina. The review aims to provide a comprehensive evaluation of the supporting and contradictory evidence on each plants' anti-inflammatory properties, whilst addressing the gaps in the current literature. The databases used to obtain relevant studies were Google Scholar, ResearchGate, PubMed and Nusearch (University of Nottingham). A total of 13 articles were selected for this review. A. ebracteatus was found to suppress neutrophil migration and weakly inhibits chronic inflammatory cytokines. Furthermore, B. lupulina and C. nutans were shown to possess very similar anti-inflammatory properties. The studies on C. nutans indicated that its anti-inflammatory effect is strongly related to the inhibition of toll-like receptor 4 (TLR4). Moreover, several phytoconstituents isolated from B. lupulina were shown to activate the anti-inflammatory Nrf2 pathway. Overall, all the studies have provided evidence to support the use of these plants as anti-inflammatory herbal remedies. However, their exact mechanism of action and the responsible phytoconstituents are yet to be established.
    Matched MeSH terms: Inflammation/drug therapy*
  8. Khalatbari-Soltani S, Tabibi H
    Clin Exp Nephrol, 2015 Jun;19(3):331-5.
    PMID: 25446285 DOI: 10.1007/s10157-014-1061-3
    Inflammation is a common complication in hemodialysis (HD) patients with no valid treatment strategy. In addition, carnitine deficiency occurs frequently in HD patients because of intradialytic loss of carnitine, impaired de novo carnitine renal synthesis, and reduced dietary intake. It appears that carnitine deficiency is related to inflammation in HD patients. A few clinical trials have investigated the effect of L-carnitine supplement on inflammatory markers in HD patients. All studies in this field, except one, showed that L-carnitine could significantly reduce C-reactive protein and serum amyloid A, as two systemic inflammation markers, in HD patients. Therefore, considering high prevalence of inflammation and carnitine deficiency in HD patients, L-carnitine therapy is a reasonable approach for reducing systemic inflammation and its complications in these patients.
    Matched MeSH terms: Inflammation/drug therapy*
  9. Rehman K, Aluwi MF, Rullah K, Wai LK, Mohd Amin MC, Zulfakar MH
    Int J Pharm, 2015 Jul 25;490(1-2):131-41.
    PMID: 26003416 DOI: 10.1016/j.ijpharm.2015.05.045
    Imiquimod is a chemotherapeutic agent for many skin-associated diseases, but it has also been associated with inflammatory side effects. The aim of this study was to prevent the inflammatory effect of commercial imiquimod (Aldara(®)) by controlled release of imiquimod through a hydrogel/oleogel colloidal mixture (CA bigel) containing fish oil as an anti-inflammatory agent. Imiquimod permeability from Aldara® cream and bigel through mice skin was evaluated, and the drug content residing in the skin via the tape stripping technique was quantified. The fish oil fatty acid content in skin along with its lipophilic environment was also determined. An inflammation study was conducted using animal models, and Aldara(®) cream was found to potentially cause psoriasis-like inflammation, which could be owing to prolonged application and excessive drug permeation. Controlled release of imiquimod along with fish oil through CA bigel may have caused reduced imiquimod inflammation. NMR studies and computerized molecular modeling were also conducted to observe whether the fish oil and imiquimod formed a complex that was responsible for improving imiquimod transport and reducing its side effects. NMR spectra showed dose-dependent chemical shifts and molecular modeling revealed π-σ interaction between EPA and imiquimod, which could help reduce imiquimod inflammation.
    Matched MeSH terms: Inflammation/drug therapy
  10. Arulselvan P, Fard MT, Tan WS, Gothai S, Fakurazi S, Norhaizan ME, et al.
    Oxid Med Cell Longev, 2016;2016:5276130.
    PMID: 27803762
    Inflammation is a comprehensive array of physiological response to a foreign organism, including human pathogens, dust particles, and viruses. Inflammations are mainly divided into acute and chronic inflammation depending on various inflammatory processes and cellular mechanisms. Recent investigations have clarified that inflammation is a major factor for the progression of various chronic diseases/disorders, including diabetes, cancer, cardiovascular diseases, eye disorders, arthritis, obesity, autoimmune diseases, and inflammatory bowel disease. Free radical productions from different biological and environmental sources are due to an imbalance of natural antioxidants which further leads to various inflammatory associated diseases. In this review article, we have outlined the inflammatory process and its cellular mechanisms involved in the progression of various chronic modern human diseases. In addition, we have discussed the role of free radicals-induced tissue damage, antioxidant defence, and molecular mechanisms in chronic inflammatory diseases/disorders. The systematic knowledge regarding the role of inflammation and its associated adverse effects can provide a clear understanding in the development of innovative therapeutic targets from natural sources that are intended for suppression of various chronic inflammations associated diseases.
    Matched MeSH terms: Inflammation/drug therapy*
  11. Dar MJ, Ali H, Khan A, Khan GM
    J Drug Target, 2017 Aug;25(7):582-596.
    PMID: 28277824 DOI: 10.1080/1061186X.2017.1298601
    Colon-specific drug delivery has found important applications in the wide array of diseases affecting the lower intestinal tract. Recent developments and advancements in the polymer-based colonic delivery ensure targeted therapeutics with reduced systemic adverse effects. Latest progress in the understanding of polymer science has decorated a polymer-based formulation with a number of special features, which may prove effective in the localized drug targeting at specific sites of the intestine. Upon oral administration, polymeric vehicles or polymer-coated formulations serve to protect the drug from premature release and degradation in the upper gastrointestinal tract. Moreover, it also facilitates the selective accumulation and controlled release of the drug at inflamed sites of the colon. This review article focuses on a wide coverage of major polymers, their modifications, pros and cons, mechanism of colon targeting and applications as a vehicle system for colonic drug delivery, with a special emphasis on the inflammatory bowel disease.
    Matched MeSH terms: Inflammation/drug therapy*
  12. Chen LH, Xue JF, Zheng ZY, Shuhaidi M, Thu HE, Hussain Z
    Int J Biol Macromol, 2018 Sep;116:572-584.
    PMID: 29772338 DOI: 10.1016/j.ijbiomac.2018.05.068
    Hyaluronic acid (HA) plays multifaceted role in regulating various biological processes and maintaining homeostasis into the body. Numerous researches evidenced the biomedical implications of HA in skin repairmen, cancer prognosis, wound healing, tissue regeneration, anti-inflammatory, immunomodulation. The present review was aimed to summarize and critically appraise the recent developments and efficacy of HA for treatment of inflammatory skin and joint diseases. A thorough analysis of the literature revealed that HA based formulations (i.e., gels, creams, autologous graft, thin sheets, soaked gauze, gauze pad, tincture, injection) have shown remarkable efficacy in treating a wide range of inflammatory skin diseases. The safety, tolerability, and efficacy of HA (as intra-articular injection) have also been well-documented for treatment of various types of joint disease including knee osteoarthritic, joint osteoarthritis, canine osteoarthritis, and meniscal swelling. Intra-articular injection of HA produces remarkable reduction in joint pain, synovial inflammation, and articular swelling. A remarkable improvement in chondrocyte density, territorial matrix appearance, reconstitution of superficial amorphous layer of the cartilage, collagen remodelling, and regeneration of meniscus have also been evident in patients treated with HA. Conclusively, we validate that the application/administration of HA is a promising pharmacotherapeutic regimen for treatment of inflammatory skin and joint diseases.
    Matched MeSH terms: Inflammation/drug therapy
  13. Harikrishnan H, Jantan I, Alagan A, Haque MA
    Inflammopharmacology, 2020 Feb;28(1):1-18.
    PMID: 31792765 DOI: 10.1007/s10787-019-00671-9
    The causal and functional connection between inflammation and cancer has become a subject of much research interest. Modulation of cell signaling pathways, such as those involving mitogen activated protein kinases (MAPKs), nuclear factor kappa β (NF-κB), phosphatidylinositol 3-kinase and protein kinase B (PI3K/Akt), and Wnt, and their outcomes play a fundamental role in inflammation and cancer. Activation of these cell signaling pathways can lead to various aspects of cancer-related inflammation. Hence, compounds able to modulate inflammation-related molecular targets are sought after in anticancer drug development programs. In recent years, plant extracts and their metabolites have been documented with potential in the prevention and treatment of cancer and inflammatory ailments. Plants possessing anticancer and anti-inflammatory properties due to their bioactive constituents have been reported to modulate the molecular and cellular pathways which are related to inflammation and cancer. In this review we focus on the flavonoids (astragalin, kaempferol, quercetin, rutin), lignans (phyllanthin, hypophyllanthin, and niranthin), tannins (corilagin, geraniin, ellagic acid, gallic acid), and triterpenes (lupeol, oleanolic acid, ursolic acid) of Phyllanthus amarus, which exert various anticancer and anti-inflammatory activities via perturbation of the NF-κB, MAPKs, PI3K/Akt, and Wnt signaling networks. Understanding the underlying mechanisms involved may help future research to develop drug candidates for prevention and new treatment for cancer and inflammatory diseases.
    Matched MeSH terms: Inflammation/drug therapy*
  14. Sukocheva OA, Furuya H, Ng ML, Friedemann M, Menschikowski M, Tarasov VV, et al.
    Pharmacol Ther, 2020 03;207:107464.
    PMID: 31863815 DOI: 10.1016/j.pharmthera.2019.107464
    Inflammatory gastrointestinal (GI) diseases and malignancies are associated with growing morbidity and cancer-related mortality worldwide. GI tumor and inflammatory cells contain activated sphingolipid-metabolizing enzymes, including sphingosine kinase 1 (SphK1) and SphK2, that generate sphingosine-1-phosphate (S1P), a highly bioactive compound. Many inflammatory responses, including lymphocyte trafficking, are directed by circulatory S1P, present in high concentrations in both the plasma and the lymph of cancer patients. High fat and sugar diet, disbalanced intestinal flora, and obesity have recently been linked to activation of inflammation and SphK/S1P/S1P receptor (S1PR) signaling in various GI pathologies, including cancer. SphK1 overexpression and activation facilitate and enhance the development and progression of esophageal, gastric, and colon cancers. SphK/S1P axis, a mediator of inflammation in the tumor microenvironment, has recently been defined as a target for the treatment of GI disease states, including inflammatory bowel disease and colitis. Several SphK1 inhibitors and S1PR antagonists have been developed as novel anti-inflammatory and anticancer agents. In this review, we analyze the mechanisms of SphK/S1P signaling in GI tissues and critically appraise recent studies on the role of SphK/S1P/S1PR in inflammatory GI disorders and cancers. The potential role of SphK/S1PR inhibitors in the prevention and treatment of inflammation-mediated GI diseases, including GI cancer, is also evaluated.
    Matched MeSH terms: Inflammation/drug therapy*
  15. Ranneh Y, Mahmoud AM, Fadel A, Albujja M, Akim AM, Hamid HA, et al.
    PMID: 32957878 DOI: 10.2174/1386207323999200918152111
    BACKGROUND: Systemic acute inflammation is the hallmark of sepsis and is associated with multiple organ dysfunction.

    OBJECTIVE: This study investigated the potential of Stingless Bee Honey (SBH) to suppress lipopolysaccharide (LPS)-induced systemic acute inflammation in rats and to reveal the probable mechanism of action.

    METHODS: Rats received 4.6 and 9.2 g/kg SBH for 7 days followed by a single injection of LPS after which blood samples were taken 6h later.

    RESULTS: LPS induced liver, kidney, heart, and lung injury, were manifested by increased serum transaminases, alkaline phosphatase, creatine kinase, creatinine, and urea, along with multiple histological alterations, particularly leukocyte infiltration. Pro-inflammatory cytokines were elevated in the serum, and NF-κB p65, p38 MAPK, and HMGB-1 were significantly increased in different tissues of LPS-challenged rats. SBH prevented tissue injury, ameliorated pro-inflammatory cytokines, and suppressed NF-κB p65, p38 MAPK, and HMGB-1 in rats that had received LPS. In addition, SBH diminished reactive oxygen species (ROS) production, lipid peroxidation, and oxidative DNA damage, and enhanced glutathione and Nrf2 in LPS-treated rats.

    CONCLUSION: SBH prevents systemic acute inflammation by suppressing NF-κB, p38 MAPK, HMGB-1, oxidative stress, and tissue injury in rats. Thus, SBH may represent an effective anti-inflammatory nutraceutical, pending further mechanistic studies.

    Matched MeSH terms: Inflammation/drug therapy*
  16. Prasher P, Sharma M, R Wich P, Jha NK, Singh SK, Chellappan DK, et al.
    Future Med Chem, 2021 12;13(23):2027-2031.
    PMID: 34596425 DOI: 10.4155/fmc-2021-0218
    Matched MeSH terms: Inflammation/drug therapy*
  17. Aamir K, Khan HU, Hossain CF, Afrin MR, Jusuf PR, Waheed I, et al.
    Life Sci, 2022 Jan 15;289:120232.
    PMID: 34919901 DOI: 10.1016/j.lfs.2021.120232
    BACKGROUND: Type 2 diabetes mellitus (T2DM) is a worldwide health issue primarily due to failure of pancreatic β-cells to release sufficient insulin.

    PURPOSE: The present work aimed to assess the antidiabetic potential of arjunolic acid (AA) isolated from Terminalia arjuna in type 2 diabetic rats.

    STUDY DESIGN: After extraction, isolation and purification, AA was orally administered to type 2 diabetic Sprague Dawley rats to investigate antidiabetic effect of AA.

    METHOD: T2DM was induced via single intraperitoneal injection of streptozotocin-nicotinamide (STZ-NIC) in adult male rats. After 10 days, fasting and random blood glucose (FBG and RBG), body weight (BW), food and water intake, serum C-peptide, insulin and glycated hemoglobin (HbA1c) was measured to confirm T2DM development. Dose dependent effects of orally administered AA (25 and 50 mg/kg/day) for 4 weeks was investigated by measuring BW variation, fasting and postprandial hyperglycemia, oral glucose tolerance test (OGTT), and levels of serum HbA1c, serum total cholesterol (TC), triglyceride (TG), low density lipoprotein (LDL), high density lipoprotein (HDL), serum and pancreatic C-peptide, insulin, growth differentiation factor 15 (GDF-15), serum and pancreatic inflammatory cytokines.

    RESULTS: The oral administration of AA in preclinical model of T2DM significantly normalized FBG and RBG, restored BW, controlled polyphagia, polydipsia and glucose tolerance. In addition, AA notably reduced serum HbA1c, TC, TG, LDL with non-significant increase in HDL. On the other hand, significant increase in serum and pancreatic C-peptide and insulin was observed with AA treatment, while serum and pancreatic GDF-15 were non-significantly altered in AA treated diabetic rats. Moreover, AA showed dose dependent reduction in serum and pancreatic proinflammatory cytokines including TNF-α, IL-1β and IL-6.

    CONCLUSION: For the first time our findings highlighted AA as a potential candidate in type 2 diabetic conditions.

    Matched MeSH terms: Inflammation/drug therapy
  18. Oo MMT, Oo PH, Saddki N
    Int J Dent Hyg, 2023 Feb;21(1):195-202.
    PMID: 35946123 DOI: 10.1111/idh.12614
    OBJECTIVES: This study determined the efficacy of alcohol-free 0.05% cetylpyridinium chloride (CPC) mouthwash as an adjunct to twice-daily toothbrushing in comparison with 0.12% chlorhexidine gluconate (CHX) mouthwash and a placebo in reducing plaque accumulation and gingival inflammation. The side effects of the mouthwashes were also determined.

    MATERIALS AND METHODS: A double-blind, parallel, randomized control trial was conducted with 219 university students who were divided into three trial groups using block randomization: CPC, CHX and placebo groups. Clinical oral examinations to assess dental plaque accumulation (modified Quigley-Hein Plaque Index), gingival health (Löe and Silness Gingival Index) and tooth staining (modified Lobene Stain Index) were performed at baseline and at 6 weeks.

    RESULTS: Plaque and gingivitis scores were not significantly different among participants at baseline. After 6 weeks, plaque and gingivitis scores between the CPC and placebo groups and between the CHX and placebo groups were found to be significantly different. However, there was no significant difference between the CPC and CHX groups. The staining scores of participants in the CPC group were lower than those in the CHX group, but the difference was not significant. Taste alteration and numbness were more common among participants in the CHX group than in the CPC group. No significant difference in the perception of a burning sensation was observed.

    CONCLUSIONS: The 0.05% CPC mouthwash was as efficient as 0.12% CHX mouthwash in reducing dental plaque accumulation and gingival inflammation with fewer side effects, supporting its use as an adjunct to toothbrushing.

    Matched MeSH terms: Inflammation/drug therapy
  19. Bhatt S, Devadoss T, Jha NK, Baidya M, Gupta G, Chellappan DK, et al.
    Metab Brain Dis, 2023 Jan;38(1):45-59.
    PMID: 36239867 DOI: 10.1007/s11011-022-01095-1
    Major depressive disorder (MDD) or Depression is one of the serious neuropsychiatric disorders affecting over 280 million people worldwide. It is 4th important cause of disability, poor quality of life, and economic burden. Women are more affected with the depression as compared to men and severe depression can lead to suicide. Most of the antidepressants predominantly work through the modulation on the availability of monoaminergic neurotransmitter (NTs) levels in the synapse. Current antidepressants have limited efficacy and tolerability. Moreover, treatment resistant depression (TRD) is one of the main causes for failure of standard marketed antidepressants. Recently, inflammation has also emerged as a crucial factor in pathological progression of depression. Proinflammatory cytokine levels are increased in depressive patients. Antidepressant treatment may attenuate depression via modulation of pathways of inflammation, transformation in structure of brain, and synaptic plasticity. Hence, targeting inflammation may be emerged as an effective approach for the treatment of depression. The present review article will focus on the preclinical and clinical studies that targets inflammation. In addition, it also concentrates on the therapeutic approaches' that targets depression via influence on the inflammatory signaling pathways. Graphical abstract demonstrate the role of various factors in the progression and neuroinflammation, oxidative stress. It also exhibits the association of neuroinflammation, oxidative stress with depression.
    Matched MeSH terms: Inflammation/drug therapy
  20. Boidin L, Moinard M, Moussaron A, Merlier M, Moralès O, Grolez GP, et al.
    J Control Release, 2024 Jul;371:351-370.
    PMID: 38789088 DOI: 10.1016/j.jconrel.2024.05.033
    Ovarian cancer (OC) is one of the most lethal cancers among women. Frequent recurrence in the peritoneum due to the presence of microscopic tumor residues justifies the development of new therapies. Indeed, our main objective is to develop a targeted photodynamic therapy (PDT) treatment of peritoneal carcinomatosis from OC to improve the life expectancy of cancer patients. Herein, we propose a targeted-PDT using a vectorized photosensitizer (PS) coupled with a newly folic acid analog (FAA), named PSFAA, in order to target folate receptor alpha (FRα) overexpressed on peritoneal metastasis. This PSFAA was the result of the coupling of pyropheophorbide-a (Pyro-a), as the PS, to a newly synthesized FAA via a polyethylene glycol (PEG) spacer. The selectivity and the PDT efficacy of PSFAA was evaluated on two human OC cell lines overexpressing FRα compared to fibrosarcoma cells underexpressing FRα. Final PSFAA, including the synthesis of a newly FAA and its conjugation to Pyro-a, was obtained after 10 synthesis steps, with an overall yield of 19%. Photophysical properties of PSFAA in EtOH were performed and showed similarity with those of free Pyro-a, such as the fluorescence and singlet oxygen quantum yields (Φf = 0.39 and ΦΔ = 0.53 for free Pyro-a, and Φf = 0.26 and ΦΔ = 0.41 for PSFAA). Any toxicity of PSFAA was noticed. After light illumination, a dose-dependent effect on PS concentration and light dose was shown. Furthermore, a PDT efficacy of PSFAA on OC cell secretome was detected inducing a decrease of a pro-inflammatory cytokine secretion (IL-6). This new PSFAA has shown promising biological properties highlighting the selectivity of the therapy opening new perspectives in the treatment of a cancer in a therapeutic impasse.
    Matched MeSH terms: Inflammation/drug therapy
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