scholarly journals Cysteamine with In Vitro Antiviral Activity and Immunomodulatory Effects Has the Potential to Be a Repurposing Drug Candidate for COVID-19 Therapy

Cells ◽  
2021 ◽  
Vol 11 (1) ◽  
pp. 52
Author(s):  
Tonino Alonzi ◽  
Alessandra Aiello ◽  
Linda Petrone ◽  
Saeid Najafi Fard ◽  
Manuela D’Eletto ◽  
...  
Keyword(s):  
Treatment Time ◽  
Treatment Options ◽  
Drug Candidate ◽  
Immunomodulatory Effects ◽  
Novel Therapy ◽  
Blood Samples ◽  
Cytopathic Effects ◽  
Anti Inflammatory ◽  
Immune Response In Vitro

The ongoing pandemic of coronavirus disease-2019 (COVID-19), caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), needs better treatment options both at antiviral and anti-inflammatory levels. It has been demonstrated that the aminothiol cysteamine, an already human applied drug, and its disulfide product of oxidation, cystamine, have anti-infective properties targeting viruses, bacteria, and parasites. To determine whether these compounds exert antiviral effects against SARS-CoV-2, we used different in vitro viral infected cell-based assays. Moreover, since cysteamine has also immune-modulatory activity, we investigated its ability to modulate SARS-CoV-2-specific immune response in vitro in blood samples from COVID-19 patients. We found that cysteamine and cystamine decreased SARS-CoV-2-induced cytopathic effects (CPE) in Vero E6 cells. Interestingly, the antiviral action was independent of the treatment time respect to SARS-CoV-2 infection. Moreover, cysteamine and cystamine significantly decreased viral production in Vero E6 and Calu-3 cells. Finally, cysteamine and cystamine have an anti-inflammatory effect, as they significantly decrease the SARS-CoV-2 specific IFN-γ production in vitro in blood samples from COVID-19 patients. Overall, our findings suggest that cysteamine and cystamine exert direct antiviral actions against SARS-CoV-2 and have in vitro immunomodulatory effects, thus providing a rational to test these compounds as a novel therapy for COVID-19.

scholarly journals In Vitro Studies on the Immunomodulatory Effects of Pulicaria crispa Extract on Human THP-1 Monocytes

2020 ◽  
Vol 2020 ◽  
pp. 1-14
Author(s):  
Tarfa Albrahim ◽  
Moonerah M. Alnasser ◽  
Mashael R. Al-Anazi ◽  
Muneera D. ALKahtani ◽  
Saad Alkahtani ◽  
...  
Keyword(s):  
Staining Method ◽  
Inflammatory Diseases ◽  
Annexin V ◽  
Cytotoxic Activities ◽  
Immunomodulatory Effects ◽  
Macrophage Differentiation ◽  
Future Studies ◽  
Late Apoptosis ◽  
Anti Inflammatory

Background. Pulicaria crispa (P. crispa) is a plant from the Compositae family that exhibits antioxidant, anti-inflammatory, antibacterial, and cytotoxic activities. Objective. The current study aimed at investigating the immunomodulatory effects of P. crispa extract in lipopolysaccharide- (LPS-) stimulated human monocytic THP-1 cells. Methods. To induce macrophage differentiation, THP-1 cell lines were treated with phorbol-12-myristate 13-acetate, followed by exposure to LPS with or without 50 or 100 μg/ml of P. crispa extract. The following tests were employed to test the immunomodulatory effects of the extract: MTT assay, ELISA, Western blotting analysis, cell migration and phagocytosis assays, and Annexin V staining method. Results. Exposure to 100 μg/ml P. crispa extract significantly reduced THP-1 cell proliferation, migration, and phagocytosis (in LPS-stimulated cells, but not in unstimulated cells). Moreover, the extract alone significantly reduced the rate of THP-1 cell apoptosis, while it increased the rate of late apoptosis. Molecular investigations showed that treatment with P. crispa extract significantly upregulated the expression of ERK1, p-MAPK, P-P38, and Bcl2, while it significantly reduced the expression of ERK5, Bax, NF-κB, P-NF-κB, CCL1, CCL2, CCL5, CCL22, CXCL1, and CXCL10. Conclusion. Pulicaria crispa extract exhibited anti-inflammatory, antiproliferative, antimigratory, and antiphagocytic effects in LPS-stimulated THP-1 cells. Future studies should investigate these mechanisms in animal models with chronic inflammatory diseases.

scholarly journals In VitroandIn VivoEfficacies of Mefloquine-Based Treatment against Alveolar Echinococcosis

2010 ◽  
Vol 55 (2) ◽  
pp. 713-721 ◽  
Author(s):  
Tatiana Küster ◽  
Britta Stadelmann ◽  
Corina Hermann ◽  
Sabrina Scholl ◽  
Jennifer Keiser ◽  
...  
Keyword(s):  
Alveolar Echinococcosis ◽  
Severe Disease ◽  
Treatment Options ◽  
Drug Candidate ◽  
Combined Application ◽  
New Treatment ◽  
Complete Detachment ◽  
Laminated Layer

ABSTRACTAlveolar echinococcosis (AE) is caused by the metacestode stage of the fox tapewormEchinococcus multilocularisand causes severe disease in the human liver, and occasionally in other organs, that is fatal when treatment is unsuccessful. The present chemotherapy against AE is based on mebendazole and albendazole. Albendazole treatment has been found to be ineffective in some instances, is parasitostatic rather than parasiticidal, and usually involves the lifelong uptake of large doses of drugs. Thus, new treatment options are urgently needed. In this study we investigated thein vitroandin vivoefficacy of mefloquine againstE. multilocularismetacestodes. Treatment using mefloquine (20 μM) againstin vitrocultures of metacestodes resulted in rapid and complete detachment of large parts of the germinal layer from the inner surface of the laminated layer within a few hours. Thein vitroactivity of mefloquine was dependent on the dosage.In vitroculture of metacestodes in the presence of 24 μM mefloquine for a period of 10 days was parasiticidal, as determined by murine bioassays, while treatment with 12 μM was not. Oral application of mefloquine (25 mg/kg of body weight administered twice a week for a period of 8 weeks) inE. multilocularis-infected mice was ineffective in achieving any reduction of parasite weight, whereas treatment with albendazole (200 mg/kg/day) was highly effective. However, when the same mefloquine dosage was applied intraperitoneally, the reduction in parasite weight was similar to the reduction seen with oral albendazole application. Combined application of both drugs did not increase the treatment efficacy. In conclusion, mefloquine represents an interesting drug candidate for the treatment of AE, and these results should be followed up in appropriatein vivostudies.

scholarly journals Anti-Inflammatory and Immunomodulatory Effects of Barberry (Berberis vulgaris) and Its Main Compounds

2019 ◽  
Vol 2019 ◽  
pp. 1-10 ◽  
Author(s):  
Rasool Nasiri Kalmarzi ◽  
Seyyed Nima Naleini ◽  
Damoon Ashtary-Larky ◽  
Ilaria Peluso ◽  
Leila Jouybari ◽  
...  
Keyword(s):  
English Language ◽  
Cell Immune Response ◽  
Immunomodulatory Effects ◽  
Effector Cells ◽  
Berberis Vulgaris ◽  
Anti Inflammatory ◽  
Main Components ◽  
Whole Plants

Berberis vulgaris is a well-known herb in Iran that is widely used as a medicinal plant and a food additive. The aim of this study was to investigate the anti-inflammatory and immunomodulatory effects of Barberry and its main compounds. This narrative review was conducted by searching keywords such as B. vulgaris, Barberry, immunomodulatory, anti-inflammatory, medicinal herbs, plants, and extract, separately or combined in various databases, such as Web of Sciences, PubMed, and Scopus. According to the inclusion and exclusion criteria, just English language articles, which reported effective whole plants or herbal compounds, were included. 21 articles were reviewed in this study. In the in vivo models (mice, rats, and human cells) and in the in vitro models (some organ cells such as the spleen, kidney, blood, and brain), B. vulgaris and its main components showed anti-inflammatory effects in both models. The main mechanisms were the shift of cell immune response to Th2, T reg induction, inhibition of inflammatory cytokines (IL-1, TNF, and IFN-γ), and stimulation of IL-4 and IL-10. The induction of apoptosis in APCs and other effector cells was another important mechanism.

Genoprotective Effect of New Triazine Derivatives in Endosulfan Mediated Toxicity, an In vivo and In vitro Study

2018 ◽  
Vol 16 (1) ◽  
pp. 52-57
Author(s):  
Nima Naderi ◽  
Seyed Mostafa Ghasemi Najarkolaee ◽  
Mona Modanlookordi ◽  
Mohammad Shokrzadeh ◽  
Hamid Irannejad
Keyword(s):  
Neuroprotective Activity ◽  
Drug Candidate ◽  
Control Group ◽  
P Value ◽  
Amyloid Toxicity ◽  
Triazine Derivatives ◽  
Anti Inflammatory ◽  
Inflammatory Effect

Background: Recently, we reported synthesis and neuroprotective activity of some new 1,2,4-triazine derivatives against H2O2 and &#946;-amyloid toxicity in two neurotic cell lines, SHSY5Y and PC12. Methods: The promising results obtained prompted us to further study on these potent neuroprotective agents. In the current study, in vivo anti-inflammatory effect and also genoprotective activity of these compounds in endosulfan-mediated toxicity were investigated. Compounds RT and SMO exhibited high anti-inflammatory effect at 3 and 4 hours after injection in 20 mg/kg, and were even more effective than Indomethacin (20 mg/kg). Results: Interestingly, compound SMO in 200 &#181;M was the best compound in reducing micronuclei significantly (P value <0.0001) in lymphocytes treated with endosulfan compared to control group. Conclusion: Herein, we report SMO as a genoprotective agent and a new drug candidate for endosulfan mediated toxicity.

scholarly journals Immunomodulatory Activities of Selected Essential Oils

Biomolecules ◽  
2020 ◽  
Vol 10 (8) ◽  
pp. 1139 ◽  
Author(s):  
Georg Sandner ◽  
Mara Heckmann ◽  
Julian Weghuber
Keyword(s):  
Essential Oils ◽  
Study Data ◽  
In Vivo Studies ◽  
Immunomodulatory Effects ◽  
Regulatory Pathways ◽  
Cellular Effects ◽  
Anti Inflammatory ◽  
Toxic Potential

Recently, the application of herbal medicine for the prevention and treatment of diseases has gained increasing attention. Essential oils (EOs) are generally known to exert various pharmacological effects, such as antiallergic, anticancer, anti-inflammatory, and immunomodulatory effects. Current literature involving in vitro and in vivo studies indicates the potential of various herbal essential oils as suitable immunomodulators for the alternative treatment of infectious or immune diseases. This review highlights the cellular effects induced by EOs, as well as the molecular impacts of EOs on cytokines, immunoglobulins, or regulatory pathways. The results reviewed in this article revealed a significant reduction in relevant proinflammatory cytokines, as well as induction of anti-inflammatory markers. Remarkably, very little clinical study data involving the immunomodulatory effects of EOs are available. Furthermore, several studies led to contradictory results, emphasizing the need for a multiapproach system to better characterize EOs. While immunomodulatory effects were reported, the toxic potential of EOs must be clearly considered in order to secure future applications.

scholarly journals Anti-inflammatory and immunomodulatory effects of Aquaphilus dolomiae extract on in vitro models

2016 ◽  
Vol Volume 9 ◽  
pp. 421-434 ◽  
Author(s):  
Marie-Françoise Aries ◽  
Hélène Hernandez-Pigeon ◽  
Clémence Vaissière ◽  
Hélène Delga ◽  
Antony Caruana ◽  
...  
Keyword(s):  
In Vitro Models ◽  
Immunomodulatory Effects ◽  
Anti Inflammatory

scholarly journals Nicotinic Amidoxime Derivate BGP-15, Topical Dosage Formulation and Anti-Inflammatory Effect

Pharmaceutics ◽  
2021 ◽  
Vol 13 (12) ◽  
pp. 2037
Author(s):  
Ágota Pető ◽  
Dóra Kósa ◽  
Ádám Haimhoffer ◽  
Pálma Fehér ◽  
Zoltán Ujhelyi ◽  
...  
Keyword(s):  
Macrophage Activation ◽  
In Vitro Release ◽  
Antioxidant Effect ◽  
Penetration Enhancers ◽  
Drug Candidate ◽  
Uvb Radiation ◽  
Anti Inflammatory ◽  
Inflammatory Effect

BGP-15 is a Hungarian-developed drug candidate with numerous beneficial effects. Its potential anti-inflammatory effect is a common assumption, but it has not been investigated in topical formulations yet. The aim of our study was to formulate 10% BGP-15 creams with different penetration enhancers to ensure good drug delivery, improve bioavailability of the drug and investigate the potential anti-inflammatory effect of BGP-15 creams in vivo. Since the exact mechanism of the effect is still unknown, the antioxidant effect (tested with UVB radiation) and the ability of BGP-15 to decrease macrophage activation were evaluated. Biocompatibility investigations were carried out on HaCaT cells to make sure that the formulations and the selected excipients can be safely used. Dosage form studies were also completed with texture analysis and in vitro release with Franz diffusion chamber apparatus. Our results show that the ointments were able to reduce the extent of local inflammation in mice, but the exact mechanism of the effect remains unknown since BGP-15 did not show any antioxidant effect, nor was it able to decrease LPS-induced macrophage activation. Our results support the hypothesis that BGP-15 has a potential anti-inflammatory effect, even if it is topically applied, but the mechanism of the effect remains unclear and requires further pharmacological studies.

scholarly journals Anti-Inflammatory Activity and Quality Control of Erysimum cheiri (L.) Crantz

2021 ◽  
Vol 2021 ◽  
pp. 1-12
Author(s):  
Ghazaleh Mosleh ◽  
Amir Azadi ◽  
Sedigheh Khademian ◽  
Reza Heidari ◽  
Abdolali Mohagheghzadeh
Keyword(s):  
Quality Control ◽  
Diclofenac Sodium ◽  
Water Soluble ◽  
Inflammatory Activity ◽  
Drug Candidate ◽  
Aerial Parts ◽  
Stretching Vibration ◽  
Ft Ir ◽  
Anti Inflammatory

Wallflower (Erysimum cheiri) is employed as a popular herbal drug in traditional Persian medicine. Topical formulations including cerates, lotions, sitz baths, and poultices for inflammatory disorders such as arthritis, anal fissure, endometriosis, and mastitis are known. However, there is no monograph in current pharmacopoeia for the wallflower drug. The present study is aimed to screen in vitro anti-inflammatory activity of wallflower and perform quality control and characterization tests for different organs of the herb. In this regard, albumin denaturation activity, macroscopic and microscopic, phytochemical, HPTLC, and FT-IR characteristics were investigated. Wallflower showed strong anti-inflammatory activity compared to diclofenac sodium. The root (1.25, 2.5, and 5 mg/mL) and flower (10 mg/mL) extract exhibited higher anti-inflammatory activities than that of other plant organs at the same concentrations. Moreover, total ash was found higher in aerial parts ( 21.52 ± 0.06 % ) than flower ( 11.01 ± 0.03 % ), root ( 5.03 ± 0.03 % ), and seed ( 6.95 ± 0.06 % ), while water-soluble ash was higher in seed ( 34.89 ± 0.26 % ) than flower ( 5.00 ± 0.03 % ), aerial parts ( 7.16 ± 0.06 % ), and root ( 5.04 ± 0.01 % ). Acid-insoluble ash and sulphated ash were higher in root ( 9.50 ± 0.04 % ) and aerial part ( 28.37 ± 0.57 % ), respectively. In addition, loss on drying was ranged from 2.20 ± 0.20 % in flowers to 6.00 ± 0.10 % in aerial parts. On the other hand, HPTLC analysis verified cardenolide compounds in all organs of the herb, and quercetin was detected in the flavonoid fingerprint of acid hydrolysed flowers. According to FT-IR results, the observed spectral region at ~3500 cm-1 attributed to -OH stretching vibration. Also, C–H (~2900-2950 cm-1), isothiocyanate (~2340 cm-1), -C=O (~1740 cm-1), conjugated C=C of the aromatic ring (~1650 cm-1), and structure of the aromatic group (~1200-1000 cm-1) were monitored. This work is the first study to the best of our knowledge, suggesting wallflower as a potential drug candidate with the basis for a monograph in addition to initial in vitro anti-inflammatory data.

Leishmanicidal effect of Spiranthera odoratíssima (Rutaceae) and its isolated alkaloid skimmianine occurs by a nitric oxide dependent mechanism

Parasitology ◽  
2011 ◽  
Vol 138 (10) ◽  
pp. 1224-1233 ◽  
Author(s):  
ROGERIO ALEXANDRE NUNES DOS SANTOS ◽  
JOÃO BATISTA ◽  
SUELLEN IARA GUIRRA ROSA ◽  
HERON FERNANDES TORQUATO ◽  
CARMEN LÚCIA BASSI ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
In Silico ◽  
Negative Impact ◽  
Treatment Options ◽  
Interleukin 10 ◽  
Current Treatment ◽  
Drug Candidate ◽  
Immunomodulatory Activity ◽  
Neglected Diseases

SUMMARYLeishmaniasis is one of the neglected diseases. High cost, systemic toxicity, and diminished efficacy due to development of resistance by the parasites has a negative impact on the current treatment options. Thus, the search for a new, effective and safer anti-leishmanial drug becomes of paramount importance. Compounds derived from natural products may be a better and cheaper source in this regard. This study evaluated the in vitro anti-leishmanial activity of Spiranthera odoratíssima (Rutaceae) fractions and isolated compounds, using promastigote and amastigote forms of different Leishmania species. J774 A.1 macrophage was used as the parasite host cell for the in vitro assays. Evaluations of cytoxicity, nitric oxide (NO), interleukin-10 and in silico analysis were carried out. In vitro experiments showed that the fruit hexanic fraction (Fhf) and its alkaloid skimmianine (Skm) have a significant (P<0·001) effect against L. braziliensis. This anti-L. braziliensis activity of Fhf and Skm was due to increased production of NO and attenuation of IL-10 production in the macrophages at concentrations ranging from 1·6 to 40·0 μg/ml. The in silico assay demonstrated significant interaction between Skm and amino acid residues of NOS2. Skm is thus a promising drug candidate for L. braziliensis due to its potent immunomodulatory activity.

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