scholarly journals Antimicrobial and Antileishmanial Activities of Hypocrellins A and B

2004 ◽  
Vol 48 (11) ◽  
pp. 4450-4452 ◽  
Author(s):  
Guoyi Ma ◽  
Shabana I. Khan ◽  
Melissa R. Jacob ◽  
Babu L. Tekwani ◽  
Zuqiang Li ◽  
...  
Keyword(s):  
Antimicrobial Activities ◽  
Antileishmanial Activity ◽  
In Vivo Studies ◽  
Moderate Activity ◽  
Structure Activity ◽  
Hypocrellin A ◽  
Hypocrellin B ◽  
Antileishmanial Activities

ABSTRACT Hypocrellins A and B were evaluated for in vitro antimicrobial and antileishmanial activities. Hypocrellin A exhibited promising activity against Candida albicans and moderate activity against Staphylococcus aureus, methicillin-resistant S. aureus, Pseudomonas aeruginosa, and Mycobacterium intracellulare. Hypocrellin B showed weak antimicrobial activities. Hypocrellin A exhibited potent antileishmanial activity, while hypocrellin B was only moderately active. These results of promising antifungal and antileishmanial activity of hypocrellin A may be useful for further structure-activity relationship and in vivo studies.

scholarly journals Efficacy of Synthetic Peptides RP-1 and AA-RP-1 against Leishmania SpeciesIn VitroandIn Vivo

2011 ◽  
Vol 56 (2) ◽  
pp. 658-665 ◽  
Author(s):  
Marie Crisel B. Erfe ◽  
Consuelo V. David ◽  
Cher Huang ◽  
Victoria Lu ◽  
Ana Claudia Maretti-Mira ◽  
...  
Keyword(s):  
Intravenous Administration ◽  
Synthetic Peptides ◽  
Antileishmanial Activity ◽  
Host Defense Peptides ◽  
Content Type ◽  
Causative Agents ◽  
Antileishmanial Activities ◽  
Conventional Antibiotics

ABSTRACTHost defense peptides are naturally occurring molecules that play essential roles in innate immunity to infection. Based on prior structure-function knowledge, we tested two synthetic peptides (RP-1 and AA-RP-1) modeled on the conserved, microbicidal α-helical domain of mammalian CXCL4 platelet kinocidins. These peptides were evaluated for efficacy againstLeishmaniaspecies, the causative agents of the group of diseases known as leishmaniasis.In vitroantileishmanial activity was assessed against three distinctLeishmaniastrains by measuring proliferation, metabolic activity and parasite viability after exposure to various concentrations of peptides. We demonstrate that micromolar concentrations of RP-1 and AA-RP-1 caused dose-dependent growth inhibition ofLeishmaniapromastigotes. This antileishmanial activity correlated with rapid membrane disruption, as well as with a loss of mitochondrial transmembrane potential. In addition, RP-1 and AA-RP-1 demonstrated distinct and significantin vivoantileishmanial activities in a mouse model of experimental visceral leishmaniasis after intravenous administration. These results establish efficacy of RP-1 lineage synthetic peptides againstLeishmaniaspeciesin vitroand after intravenous administrationin vivoand provide further validation of proof of concept for the development of these and related systemic anti-infective peptides targeting pathogens that are resistant to conventional antibiotics.

scholarly journals Insects as a source of phenolic compounds and potential health benefits

2021 ◽  
pp. 1-12
Author(s):  
M.C. Nino ◽  
L. Reddivari ◽  
C. Osorio ◽  
I. Kaplan ◽  
A.M. Liceaga
Keyword(s):  
Phenolic Compounds ◽  
De Novo ◽  
Health Benefits ◽  
Antimicrobial Activities ◽  
In Vivo Studies ◽  
Plant Phenolics ◽  
Potential Health ◽  
Bioactive Potential

The use of insects in traditional medicine and unveiling the chemical structure of the bright pigments in butterfly wings led to the discovery of bioactive phenolic compounds in the insect bodies. These metabolites have been found not only due to the insect absorption and metabolisation of the plant-derived phenolic present in their diet, but also from the ability of insects to synthesise phenolic compounds de novo through the sclerotisation process. Plant phenolics are secondary metabolites involved in the protection of tissues against UV radiation, herbivores, and pathogens, as well as pigmentation of fruits and flowers. These bioactive compounds exhibit antioxidant, anti-inflammatory, anticancer, and antimicrobial activities, demonstrated through in vitro and in vivo studies. This bioactive potential is thought to occur due to their chemical characteristics that allow them to stabilise reactive oxygen species (ROS), chelate prooxidant metal ions, interact with key enzymes and signal cascades involved in biological pathways. Bioactivity of plant phenolics and both in vitro, in vivo studies, suggest that the dietary compounds absorbed by the insect maintain their chemical and bioactive properties. Further characterisation of the phenolic composition in edible insects and evaluation of their bioactive capacity as well as their bioavailability, could result in discovering additional health benefits of entomophagy apart from macro-nutritional (e.g. protein) content.

scholarly journals Improvement of In Vitro and In Vivo Antileishmanial Activities of 2′,6′-Dihydroxy-4′-Methoxychalcone by Entrapment in Poly(d,l-Lactide) Nanoparticles

1999 ◽  
Vol 43 (7) ◽  
pp. 1776-1778 ◽  
Author(s):  
Eduardo Caio Torres-Santos ◽  
José M. Rodrigues ◽  
Davyson L. Moreira ◽  
Maria Auxiliadora C. Kaplan ◽  
Bartira Rossi-Bergmann
Keyword(s):  
Polymeric Nanoparticles ◽  
Leishmania Amazonensis ◽  
Antileishmanial Activity ◽  
Antileishmanial Activities ◽  
Piper Aduncum

ABSTRACT The inhibition of intracellular Leishmania amazonensisgrowth by 2′,6′-dihydroxy-4′-methoxychalcone (DMC) isolated fromPiper aduncum was further enhanced after encapsulation of DMC in polymeric nanoparticles. Encapsulated DMC also showed increased antileishmanial activity in infected BALB/c mice, as evidenced by significantly smaller lesions and fewer parasites in the lesions.

scholarly journals Antileishmanial Activity of Cassia fistula L., Morus nigra L. and Ziziphus jujuba Mill., Plant Extracts

2021 ◽  
pp. 466-471
Author(s):  
Kashif Iqbal ◽  
Eshwa Dar ◽  
Abdul Rashid Shaikh ◽  
Samar Akhtar ◽  
. Marvi
Keyword(s):  
Lesion Size ◽  
Negative Control ◽  
Antileishmanial Activity ◽  
In Vivo Studies ◽  
Cassia Fistula ◽  
Standard Drug ◽  
Morus Nigra ◽  
Ziziphus Jujuba ◽  
Antileishmanial Activities

Aim: To investigate the different antileishmanial activities of extracts of Cassia Fistula L., Morus Nigra L. and Ziziphus Jujuba Mill. Methodology: In this method, three (03) plants having concentrations between 500 – 2000 µg/mL were subjected to KWH23 strains of L. tropica in which Standard drug was Amphotericin B and have negative control for 24 – 48 hours. To check the in-vivo studies, plant extract was tested on BALB/c mice (Iqbal et al., 2016). Results: It showed that inhibition (mean) of KWH23 strains at 500, 1000, 1500, 2000 µg/mL after 48 hours were 92.1 ± 0.02, 95.00 ± 0.05, 97.09 ± 0.07 and 98.05 ± 0.05 % respectively. It decreased the lesion size (mean) from 0.8 ± 0.1 mm to 0.40 ± 0.2 mm having significance value p < 0.01 after 8th week, and cure at 200 mg/Kg against intracellular amastigotes in BALB/c mice was 90.00% (95% Cl = 80.05 – 97.00). Conclusion: The result shows that Ziziphus jujuba Mill. leaves possess significant antileishmanial activity.

scholarly journals Structure–Activity Relationship Study of Newly Synthesized Iridium-III Complexes as Potential Series for Treating Thrombotic Diseases

2018 ◽  
Vol 19 (11) ◽  
pp. 3641 ◽  
Author(s):  
Chih-Hao Yang ◽  
Chih-Wei Hsia ◽  
Thanasekaran Jayakumar ◽  
Joen-Rong Sheu ◽  
Chih-Hsuan Hsia ◽  
...  
Keyword(s):  
Phenyl Group ◽  
Chloride Ion ◽  
Adenosine Diphosphate ◽  
Structure Activity Relationship ◽  
In Vivo Studies ◽  
Activity Relationship ◽  
Structure Activity ◽  
Induced Aggregation

Platelets play a major role in hemostatic events and are associated with various pathological events, such as arterial thrombosis and atherosclerosis. Iridium (Ir) compounds are potential alternatives to platinum compounds, since they exert promising anticancer effects without cellular toxicity. Our recent studies found that Ir compounds show potent antiplatelet properties. In this study, we evaluated the in vitro antiplatelet, in vivo antithrombotic and structure–activity relationship (SAR) of newly synthesized Ir complexes, Ir-1, Ir-2 and Ir-4, in agonists-induced human platelets. Among the tested compounds, Ir-1 was active in inhibiting platelet aggregation induced by collagen; however, Ir-2 and Ir-4 had no effects even at their maximum concentrations of 50 μM against collagen and 500 μM against U46619-induced aggregation. Similarly, Ir-1 was potently inhibiting of adenosine triphosphate (ATP) release, calcium mobilization ([Ca2+]i) and P-selectin expression induced by collagen-induced without cytotoxicity. Likewise, Ir-1 expressively suppressed collagen-induced Akt, PKC, p38MAPKs and JNK phosphorylation. Interestingly, Ir-2 and Ir-4 had no effect on platelet function analyzer (PFA-100) collagen-adenosine diphosphate (C-ADP) and collagen-epinephrine (C-EPI) induced closure times in mice, but Ir-1 caused a significant increase when using C-ADP stimulation. Other in vivo studies revealed that Ir-1 significantly prolonged the platelet plug formation, increased tail bleeding times and reduced the mortality of adenosine diphosphate (ADP)-induced acute pulmonary thromboembolism in mice. Ir-1 has no substitution on its phenyl group, a water molecule (like cisplatin) can replace its chloride ion and, hence, the rate of hydrolysis might be tuned by the substituent on the ligand system. These features might have played a role for the observed effects of Ir-1. These results indicate that Ir-1 may be a lead compound to design new antiplatelet drugs for the treatment of thromboembolic diseases.

scholarly journals Antileishmanial Structure-Activity Relationships of Synthetic Phospholipids: In Vitro and In Vivo Activities of Selected Derivatives

2007 ◽  
Vol 51 (12) ◽  
pp. 4525-4528 ◽  
Author(s):  
Karin Seifert ◽  
Andreas Lemke ◽  
Simon L. Croft ◽  
Oliver Kayser
Keyword(s):  
Leishmania Donovani ◽  
Positive Contribution ◽  
Structure Activity Relationships ◽  
Bearing Ring ◽  
Mammalian Cell Lines ◽  
Structure Activity ◽  
Head Groups ◽  
Antileishmanial Activities

ABSTRACT Antileishmanial activities of 91 synthetic phospholipids against Leishmania donovani were evaluated in vitro and cytotoxicity assessed against two mammalian cell lines. Promising compounds were tested further in vivo. In vitro structure-activity relationships showed a positive contribution of head groups bearing ring systems (N-methylpiperidino and N-methylmorpholino) to antileishmanial activity.

scholarly journals Prospects of honey in fighting against COVID-19: pharmacological insights and therapeutic promises

2020 ◽  
Author(s):  
Khandkar Shaharina Hossain ◽  
Md. Golzar Hossain ◽  
Akhi Moni ◽  
Mahbubur Rahman ◽  
Umma Habiba Rahman ◽  
...  
Keyword(s):  
Immune System ◽  
Chronic Diseases ◽  
Fungal Infections ◽  
Antimicrobial Activities ◽  
In Vivo Studies ◽  
Therapeutic Effects ◽  
Host Immune System ◽  
Varicella Zoster

Honey and its various ingredients have been in limelight as an effective natural therapy capable of normalizing the situation by attenuating acute inflammation through encouraging immune response. Several studies have proved its potential healing capability against numerous chronic diseases/conditions, including pulmonary disorders, cardiac disorders, diabetes, hypertension, autophagy dysfunction, bacterial and fungal infections. More importantly, honey showed its virucidal effect on several enveloped viruses such as HIV, influenza virus, herpes simplex, and varicella zoster virus. Honey may be beneficial for patients with COVID-19 caused by an enveloped virus SARS-CoV-2 through simultaneously boosting the host immune system, improving comorbid conditions and antiviral activities. Moreover, a clinical trial of honey on COVID-19 patients has been undergoing. In this review, we summarized the potential benefits of honey and its ingredients in the context of antimicrobial activities, numerous chronic diseases, and host immune system and thereby tried to establish a relationship with honey for the treatment of COVID-19. This review will be helpful to reconsider the insights into the possible potential therapeutic effects of honey in the context of COVID-19 pandemic. However, the effects of honey on SARS-CoV-2 replication and/or host immune system need to be further investigated by in vitro and in vivo studies.

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