scholarly journals Scolicidal and Apoptotic Activities of 5-hydroxy-1, 4-naphthoquinone as a Potent Agent against Echinococcus granulosus Protoscoleces

2021 ◽  
Vol 14 (7) ◽  
pp. 623
Author(s):  
Masoud Moghadaszadeh ◽  
Mehdi Khayyati ◽  
Adel Spotin ◽  
Roghayeh Norouzi ◽  
Abdol Sattar Pagheh ◽  
...  
Keyword(s):  
Echinococcus Granulosus ◽  
Public Health Problem ◽  
In Vivo Studies ◽  
Cystic Hydatid Disease ◽  
Liposomal System ◽  
Physico Chemical ◽  
Apoptotic Effect ◽  
Apoptotic Activity

Cystic hydatid disease (CHD) is a zoonotic disease with different clinical stages caused by the larval stage of the cestode Echinococcus granulosus. It is important to highlight as a public health problem in various regions of the world. In the current study, the efficacy and apoptotic activity of the liposomal system containing juglone (5-hydroxy-1,4-naphthoquinone) were assessed against protoscoleces (PSCs) in vitro. To this aim, firstly, liposomal vesicles were prepared by the thin-film method. Their physico-chemical features were assessed using Zeta-Sizer and Scanning Electron Microscope (SEM). Subsequently, various concentrations (50, 100, 200, 400, and 800 μg/mL) of juglone nanoliposomes at different exposure times (15, 30, 60, and 120 min) were used against PSCs. Results showed that juglone nanoliposomes at all tested concentrations induced scolicidal effect, however, 800 μg/mL and 400 μg/mL of juglone nanoliposomes could reach 100% mortality in 60 and 120 min, respectively. Additionally, we found that caspase-3 mRNA expression was higher in PSCs treated with juglone nanoliposomes compared to control groups (p < 0.001). Therefore, juglone nanoliposomes are suggested to have a more potent apoptotic effect on PSCs. Generally, optimized doses of juglone nanoliposomes could display significant scolicidal effects. Moreover, further in vivo studies are required to evaluate the efficacy of this nanoliposome.

Medicinal Plants and Bioactive Compounds for Diabetes Management: Important Advances for Drug Discovery

2020 ◽  
Vol 26 ◽  
Author(s):  
Kondeti Ramudu Shanmugam ◽  
Bhasha Shanmugam ◽  
Gangigunta Venkatasubbaiah ◽  
Sahukari Ravi ◽  
Kesireddy Sathyavelu Reddy
Keyword(s):  
Herbal Medicine ◽  
Medicinal Plants ◽  
Bioactive Compounds ◽  
Diabetes Management ◽  
Therapeutic Potential ◽  
Public Health Problem ◽  
In Vivo Studies ◽  
Major Public Health Problem

Background : Diabetes is a major public health problem in the world. It affects each and every part of the human body and also leads to organ failure. Hence, great progress made in the field of herbal medicine and diabetic research. Objectives: Our review will focus on the effect of bioactive compounds of medicinal plants which are used to treat diabetes in India and other countries. Methods: Information regarding diabetes, oxidative stress, medicinal plants and bioactive compounds were collected from different search engines like Science direct, Springer, Wiley online library, Taylor and francis, Bentham Science, Pubmed and Google scholar. Data was analyzed and summarized in the review. Results and Conclusion: Anti-diabetic drugs that are in use have many side effects on vital organs like heart, liver, kidney and brain. There is an urgent need for alternative medicine to treat diabetes and their disorders. In India and other countries herbal medicine was used to treat diabetes. Many herbal plants have antidiabetic effects. The plants like ginger, phyllanthus, curcumin, aswagandha, aloe, hibiscus and curcuma showed significant anti-hyperglycemic activities in experimental models and humans. The bioactive compounds like Allicin, azadirachtin, cajanin, curcumin, querceitin, gingerol possesses anti-diabetic, antioxidant and other pharmacological properties. This review focuses on the role of bioactive compounds of medicinal plants in prevention and management of diabetes. Conclusion: Moreover, our review suggests that bioactive compounds have the potential therapeutic potential against diabetes. However, further in vitro and in vivo studies are needed to validate these findings.

scholarly journals In Vitro and In Vivo Activities of E5700 and ER-119884, Two Novel Orally Active Squalene Synthase Inhibitors, against Trypanosoma cruzi

2004 ◽  
Vol 48 (7) ◽  
pp. 2379-2387 ◽  
Author(s):  
Julio A. Urbina ◽  
Juan Luis Concepcion ◽  
Aura Caldera ◽  
Gilberto Payares ◽  
Cristina Sanoja ◽  
...  
Keyword(s):  
Trypanosoma Cruzi ◽  
Chagas Disease ◽  
Public Health Problem ◽  
Squalene Synthase ◽  
Host Cells ◽  
In Vivo Studies ◽  
Inorganic Pyrophosphate ◽  
Orally Active

ABSTRACT Chagas' disease is a serious public health problem in Latin America, and no treatment is available for the prevalent chronic stage. Its causative agent, Trypanosoma cruzi, requires specific endogenous sterols for survival, and we have recently demonstrated that squalene synthase (SQS) is a promising target for antiparasitic chemotherapy. E5700 and ER-119884 are quinuclidine-based inhibitors of mammalian SQS that are currently in development as cholesterol- and triglyceride-lowering agents in humans. These compounds were found to be potent noncompetitive or mixed-type inhibitors of T. cruzi SQS with K i values in the low nanomolar to subnanomolar range in the absence or presence of 20 μM inorganic pyrophosphate. The antiproliferative 50% inhibitory concentrations of the compounds against extracellular epimastigotes and intracellular amastigotes were ca. 10 nM and 0.4 to 1.6 nM, respectively, with no effects on host cells. When treated with these compounds at the MIC, all of the parasite's sterols disappeared from the parasite cells. In vivo studies indicated that E5700 was able to provide full protection against death and completely arrested the development of parasitemia when given at a concentration of 50 mg/kg of body weight/day for 30 days, while ER-119884 provided only partial protection. This is the first report of an orally active SQS inhibitor that is capable of providing complete protection against fulminant, acute Chagas' disease.

scholarly journals Scrophulariae Radix: An Overview of Its Biological Activities and Nutraceutical and Pharmaceutical Applications

Molecules ◽  
2021 ◽  
Vol 26 (17) ◽  
pp. 5250
Author(s):  
Hae-Jin Lee ◽  
Hae-Lim Kim ◽  
Dong-Ryung Lee ◽  
Bong-Keun Choi ◽  
Seung-Hwan Yang
Keyword(s):  
Biological Activities ◽  
Neuroprotective Effect ◽  
In Vivo Studies ◽  
Amnesic Effect ◽  
In Vivo Experiments ◽  
Toxicological Studies ◽  
Apoptotic Effect ◽  
Pharmaceutical Industries

Scrophulariae Radix (SR) has an important role as a medicinal plant, the roots of which are recorded used to cure fever, swelling, constipation, pharyngitis, laryngitis, neuritis, sore throat, rheumatism, and arthritis in Asia for more than two thousand years. In this paper, the studies published on Scrophularia buergeriana (SB) and Scrophularia ningpoensis (SN) in the latest 20 years were reviewed, and the biological activities of SB and SN were evaluated based on in vitro and in vivo studies. SB presented anti-inflammatory activities, immune-enhancing effects, bone disorder prevention activity, neuroprotective effect, anti-amnesic effect, and anti-allergic effect; SN showed a neuroprotective effect, anti-apoptotic effect, anti-amnesic effect, and anti-depressant effect; and SR exhibited an immune-enhancing effect and cardioprotective effects through in vitro and in vivo experiments. SB and SN are both known to exert neuroprotective and anti-amensice effects. This review investigated their applicability in the nutraceutical, functional foods, and pharmaceutical industries. Further studies, such as toxicological studies and clinical trials, on the efficacy and safety of SR, including SB and SN, need to be conducted.

scholarly journals Evaluation of Leishmania infantum 30x biotherapy effects in the prevention and treatment of visceral leishmaniasis: in vivo and in vitro studies

2021 ◽  
Vol 15 (4) ◽  
pp. 26-29
Author(s):  
Ana Paula Bacellar Cajueiro ◽  
Gleyce Moreno Barbosa ◽  
Fortune Homsani ◽  
Ana Paula dos Santos Matos ◽  
Igor Almeida Rodrigues ◽  
...  
Keyword(s):  
Leishmania Infantum ◽  
Therapeutic Potential ◽  
Public Health Problem ◽  
In Vivo Studies ◽  
In Vitro Assays ◽  
Serum Samples ◽  
Hydropic Degeneration ◽  
No Release

Background: Leishmaniasis is a serious public health problem especially in developing countries [1]. The therapeutic potential of biotherapics against several microorganism has been described in vitro [2,3] and in vivo studies [4,5,6,7,8,9]. Considering the resistance of leishmaniasis to conventional treatment as well as previous studies with biotherapic, we evaluated the effects of Leishmania infantum 30x (BioLi30x) biotherapy. Aim: evaluate the antileishmanial effects of BioLi30x in in vivo and in vitro models. Methodology: The in vivo experiments were performed using BALB/c mice (n=138), divided into 8 groups: G1-healthy, G2-infected with L. infantum, G3-BioLi30x pre-treated, G4-BioLi30x pre/post-treated, G5-BioLi30x post-treated, G6-H2O30x post-treated, G7-Antimonium crudum 30x post-treated and G8-Glucantime® post-treated. After 49 days of treatment, the animals were submitted to euthanasia (ethical approval ECUA/UFRJ/066/14). Liver and spleen histological changes were evaluated, and serum samples were aliquoted and storage at -20°C for cytokine assays. The in vitro assays were performed using RAW 264.7 macrophages treated with BioLi30x and infected with L. infantum. The morphological aspects were evaluated by scanning electron microscopy (SEM), and the nitric oxide (NO) release was quantified in the supernatant of infected macrophages. Results: The histological analysis from 4 independent experiments showed livers with normal appearance (G1); periportal chronic hepatitis (G2,G4,G5,G8); discreet (G3,G7), moderate (G4,G5,G6), and severe (G2,G8) vacuolar hydropic degeneration; congestion and neutrophilic inflammation (G2,G4,G5,G6,G8), and possible amastigotes within macrophages (G2-G8). Spleens presented healthy appearance only in G1. All treated animals presented histological alterations, with different lesions severity, which involved spleen pulp hyperplasia with moderate disruption (G2,G8), as well as megakaryocytes and macrophages proliferation (G2- G8). SEM analyses showed BioLi30x treatments induced significant protozoan morphology alterations when compared to H2O30x. Besides, a 19% increase in the NO release was detected in RAW supernatants, when compared to H2O30x. Conclusions: BioLi30x and Antimonium crudum 30x modified the infection animal process, involving several cellular mechanisms as well as different histological damage. The in vitro experiments will be repeated in order to confirm these preliminary results.

scholarly journals Protection of pancreatic islets using theranostic silencing nanoparticles in a baboon model of islet transplantation

2020 ◽  
Author(s):  
Ada Admin ◽  
Thomas Pomposelli ◽  
Ping Wang ◽  
Kazuhiro Takeuchi ◽  
Katsunori Miyake ◽  
...  
Keyword(s):  
Islet Transplantation ◽  
In Vivo Studies ◽  
Pancreatic Islet Transplantation ◽  
Insulin Requirements ◽  
Novel Approach ◽  
Apoptotic Effect ◽  
Novel Strategy ◽  
Interfering Rna

The long-term success of pancreatic islet transplantation (Tx) as a cure for type 1 diabetes remains limited. Islet loss after Tx related to apoptosis, inflammation and other factors continues to limit its efficacy. In this project we demonstrate a novel approach aimed at protection of islets prior to Tx in non-human primates (NHP, baboons) by silencing a gene (caspase 3) responsible for induction of apoptosis. This was done using small interfering RNA (siRNA, siCas-3) conjugated to magnetic nanoparticles (MN). In addition to serving as carriers for siCas-3 these nanoparticles also act as reporters for magnetic resonance imaging so islets labeled with MN-siCas-3 can be monitored in vivo after Tx. In vitro studies showed the anti-apoptotic effect of MN-siCas-3 on islets in culture resulting in a minimal islet loss. For in vivo studies donor baboon islets were labeled with MN-siCas-3 and infused into recipient diabetic subjects. A dramatic reduction in insulin requirements was observed in animals transplanted even with a marginal number of labeled islets compared to controls. By demonstrating the protective effect of MN-siCas-3 in the challenging NHP model, this study proposes a novel strategy to minimize the number of donor islets required from either cadaver or living donor.

scholarly journals Effects of Isorhamnetin on Diabetes and Its Associated Complications: A Review of In Vitro and In Vivo Studies and a Post Hoc Transcriptome Analysis of Involved Molecular Pathways

2022 ◽  
Vol 23 (2) ◽  
pp. 704
Author(s):  
Feten Zar Kalai ◽  
Mondher Boulaaba ◽  
Farhana Ferdousi ◽  
Hiroko Isoda
Keyword(s):  
Transcriptome Analysis ◽  
Biological Activities ◽  
Public Health Problem ◽  
In Vivo Studies ◽  
Major Public Health Problem ◽  
Glucose Levels ◽  
Oxidative Damages ◽  
Post Hoc

Diabetes mellitus, especially type 2 (T2DM), is a major public health problem globally. DM is characterized by high levels of glycemia and insulinemia due to impaired insulin secretion and insulin sensitivity of the cells, known as insulin resistance. T2DM causes multiple and severe complications such as nephropathy, neuropathy, and retinopathy causing cell oxidative damages in different internal tissues, particularly the pancreas, heart, adipose tissue, liver, and kidneys. Plant extracts and their bioactive phytochemicals are gaining interest as new therapeutic and preventive alternatives for T2DM and its associated complications. In this regard, isorhamnetin, a plant flavonoid, has long been studied for its potential anti-diabetic effects. This review describes its impact on reducing diabetes-related disorders by decreasing glucose levels, ameliorating the oxidative status, alleviating inflammation, and modulating lipid metabolism and adipocyte differentiation by regulating involved signaling pathways reported in the in vitro and in vivo studies. Additionally, we include a post hoc whole-genome transcriptome analysis of biological activities of isorhamnetin using a stem cell-based tool.

scholarly journals Dextran-Curcumin Nanosystems Inhibit Cell Growth and Migration Regulating the Epithelial to Mesenchymal Transition in Prostate Cancer Cells

2021 ◽  
Vol 22 (13) ◽  
pp. 7013
Author(s):  
Emilia Bevacqua ◽  
Manuela Curcio ◽  
Federica Saletta ◽  
Orazio Vittorio ◽  
Giuseppe Cirillo ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Epithelial To Mesenchymal Transition ◽  
In Vivo Studies ◽  
Ros Production ◽  
Cell Growth And Migration ◽  
Mesenchymal Transition ◽  
Curcumin Nanoparticles ◽  
Apoptotic Effect

Functional nanocarriers which are able to simultaneously vectorize drugs to the site of interest and exert their own cytotoxic activity represent a significant breakthrough in the search for effective anticancer strategies with fewer side effects than conventional chemotherapeutics. Here, we propose previously developed, self-assembling dextran-curcumin nanoparticles for the treatment of prostate cancer in combination therapy with Doxorubicin (DOXO). Biological effectiveness was investigated by evaluating the cell viability in either cancer and normal cells, reactive oxygen species (ROS) production, apoptotic effect, interference with the cell cycle, and the ability to inhibit cell migration and reverse the epithelial to mesenchymal transition (EMT). The results proved a significant enhancement of curcumin efficiency upon immobilization in nanoparticles: IC50 reduced by a half, induction of apoptotic effect, and improved ROS production (from 67 to 134%) at low concentrations. Nanoparticles guaranteed a pH-dependent DOXO release, with a more efficient release in acidic environments. Finally, a synergistic effect between nanoparticles and Doxorubicin was demonstrated, with the free curcumin showing additive activity. Although in vivo studies are required to support the findings of this study, these preliminary in vitro data can be considered a proof of principle for the design of an effective therapy for prostate cancer treatment.

scholarly journals The Role of Chitosan Oligosaccharide in Metabolic Syndrome: A Review of Possible Mechanisms

Marine Drugs ◽  
2021 ◽  
Vol 19 (9) ◽  
pp. 501
Author(s):  
Wenjing Tao ◽  
Geng Wang ◽  
Jintao Wei
Keyword(s):  
Metabolic Syndrome ◽  
Biological Activities ◽  
Public Health Problem ◽  
In Vivo Studies ◽  
Chitosan Oligosaccharide ◽  
Major Public Health Problem ◽  
Beneficial Effects

Metabolic syndrome, a cluster of metabolic disorders including central obesity, insulin resistance, hyperglycemia, dyslipidemia, and hypertension, has become a major public health problem worldwide. It is of great significance to develop natural products to prevent and treat metabolic syndrome. Chitosan oligosaccharide (COS) is an oligomer of chitosan prepared by the deacetylation of chitin, which is the second most abundant polymer in nature. In recent years, COS has received widespread attention due to its various biological activities. The present review will summarize the evidence from both in vitro and in vivo studies of the beneficial effects of COS on obesity, dyslipidemia, diabetes mellitus, hyperglycemia, and hypertension, and focus attention on possible mechanisms of the prevention and treatment of metabolic syndrome by COS.

scholarly journals Protection of pancreatic islets using theranostic silencing nanoparticles in a baboon model of islet transplantation

2020 ◽  
Author(s):  
Ada Admin ◽  
Thomas Pomposelli ◽  
Ping Wang ◽  
Kazuhiro Takeuchi ◽  
Katsunori Miyake ◽  
...  
Keyword(s):  
Islet Transplantation ◽  
In Vivo Studies ◽  
Pancreatic Islet Transplantation ◽  
Insulin Requirements ◽  
Novel Approach ◽  
Apoptotic Effect ◽  
Novel Strategy ◽  
Interfering Rna

The long-term success of pancreatic islet transplantation (Tx) as a cure for type 1 diabetes remains limited. Islet loss after Tx related to apoptosis, inflammation and other factors continues to limit its efficacy. In this project we demonstrate a novel approach aimed at protection of islets prior to Tx in non-human primates (NHP, baboons) by silencing a gene (caspase 3) responsible for induction of apoptosis. This was done using small interfering RNA (siRNA, siCas-3) conjugated to magnetic nanoparticles (MN). In addition to serving as carriers for siCas-3 these nanoparticles also act as reporters for magnetic resonance imaging so islets labeled with MN-siCas-3 can be monitored in vivo after Tx. In vitro studies showed the anti-apoptotic effect of MN-siCas-3 on islets in culture resulting in a minimal islet loss. For in vivo studies donor baboon islets were labeled with MN-siCas-3 and infused into recipient diabetic subjects. A dramatic reduction in insulin requirements was observed in animals transplanted even with a marginal number of labeled islets compared to controls. By demonstrating the protective effect of MN-siCas-3 in the challenging NHP model, this study proposes a novel strategy to minimize the number of donor islets required from either cadaver or living donor.

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