In vitro and in vivo antileishmanial activities of a Brazilian green propolis extract

Propolis is produced by honeybees from materials collected from plants they visit. It is a resinous material having mixtures of wax and bee enzymes. Propolis is also known as bee glue and used by bees as a building material in their hives, for blocking holes and cracks, repairing the combs and strengthening their thin borders. It has been extensively used since ancient times for different purposes in traditional human healthcare practices. The quality and composition of propolis depend on its geographic location, climatic zone and local flora. The New Zealand and Brazilian green propolis are the two main kinds that have been extensively studied in recent years. Their bioactive components have been found to possess a variety of therapeutic potentials. It was found that Brazilian green propolis improves the cognitive functions of mild cognitive impairments in patients living at high altitude and protects them from neurodegenerative damage through its antioxidant properties. It possesses artepillin C (ARC) as the key component, also known to possess anticancer potential. The New Zealand propolis contains caffeic acid phenethyl ester (CAPE) as the main bioactive with multiple therapeutic potentials. Our lab performed in vitro and in vivo assays on the extracts prepared from New Zealand and Brazilian propolis and their active ingredients. We provided experimental evidence that these extracts possess anticancer, antistress and hypoxia-modulating activities. Furthermore, their conjugation with γCD proved to be more effective. In the present review, we portray the experimental evidence showing that propolis has the potential to be a candidate drug for different ailments and improve the quality of life.

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Neuroprotection by Brazilian Green Propolis againstIn vitroandIn vivoIschemic Neuronal Damage

Evidence-based Complementary and Alternative Medicine ◽

10.1093/ecam/neh078 ◽

2005 ◽

Vol 2 (2) ◽

pp. 201-207 ◽

Cited By ~ 56

Author(s):

Masamitsu Shimazawa ◽

Satomi Chikamatsu ◽

Nobutaka Morimoto ◽

Satoshi Mishima ◽

Hiroichi Nagai ◽

...

Keyword(s):

Oxidative Stress ◽

Cerebral Ischemia ◽

Neuronal Damage ◽

Focal Cerebral Ischemia ◽

Brain Infarction ◽

Folk Medicine ◽

Neuroprotective Function ◽

Brazilian Green Propolis

We examined whether Brazilian green propolis, a widely used folk medicine, has a neuroprotective functionin vitroand/orin vivo.In vitro, propolis significantly inhibited neurotoxicity induced in neuronally differentiated PC12 cell cultures by either 24 h hydrogen peroxide (H2O2) exposure or 48 h serum deprivation. Regarding the possible underlying mechanism, propolis protected against oxidative stress (lipid peroxidation) in mouse forebrain homogenates and scavenged free radicals [induced by diphenyl-p-picrylhydrazyl (DPPH). In micein vivo, propolis [30 or 100 mg/kg; intraperitoneally administered four times (at 2 days, 1 day and 60 min before, and at 4 h after induction of focal cerebral ischemia by permanent middle cerebral artery occlusion)] reduced brain infarction at 24 h after the occlusion. Thus, a propolis-induced inhibition of oxidative stress may be partly responsible for its neuroprotective function againstin vitrocell death andin vivofocal cerebral ischemia.

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The Role of Propolis in Pulp Pain by Inhibiting Cyclooxygenase-2 Expression

Conservative Dentistry Journal ◽

10.20473/cdj.v11i1.2021.11-18 ◽

2021 ◽

Vol 11 (1) ◽

pp. 11

Author(s):

Ira Widjiastuti ◽

Widya Saraswati ◽

Annisa Rahma

Keyword(s):

Side Effects ◽

Pain Relief ◽

Inflammatory Pain ◽

Cyclooxygenase 2 ◽

Propolis Extract ◽

In Silico Studies ◽

Cox 2

Background: Inflammation of the pulp can lead to elicit pain. Pain in inflammation is induced by the cyclooxygenase-2 enzyme (COX-2) which induces prostaglandin E2 (PGE2) resulting in pain. Pain in the pulp can be relieved by eugenol. In its application, eugenol is toxic to pulp fibroblasts. Due to the side effect, it is worth considering other biocompatible materials with minimal side effects, such as propolis. Flavonoids and phenolic acids that contained in propolis can inhibit COX-2. Therefore, an analysis outlined in the literature review is needed to examine the results of research related to the role of propolis as pulp pain relief by inhibiting COX-2 expression. Purpose: To analyze the role of propolis in pulp pain by inhibiting COX-2 expression. Reviews: Propolis extract that extracted by ethanol, water, and hydroalcohol has pain relief properties in the pulp by inhibiting COX-2 by directly binding to the COX-2 receptors and by reducing the production of proinflammatory cytokines which are COX-2 inducers, proven through in vivo, in vitro, and in silico studies in various target cell organs. Conclusion: Propolis extract has high prospect as inflammatory pain inhibitor in the pulp by inhibit COX-2 expression.

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Brazilian Green Propolis Protects against Retinal Damage In Vitro and In Vivo

Evidence-based Complementary and Alternative Medicine ◽

10.1093/ecam/nek005 ◽

2006 ◽

Vol 3 (1) ◽

pp. 71-77 ◽

Cited By ~ 41

Author(s):

Yuta Inokuchi ◽

Masamitsu Shimazawa ◽

Yoshimi Nakajima ◽

Shinsuke Suemori ◽

Satoshi Mishima ◽

...

Keyword(s):

Oxidative Stress ◽

Retinal Ganglion Cells ◽

Ganglion Cells ◽

Water Soluble ◽

Retinal Damage ◽

Retinal Ganglion ◽

Neuroprotective Effects ◽

Brazilian Green Propolis

Propolis, a honeybee product, has gained popularity as a food and alternative medicine. Its constituents have been shown to exert pharmacological (anticancer, antimicrobial and anti-inflammatory) effects. We investigated whether Brazilian green propolis exerts neuroprotective effects in the retinain vitroand/orin vivo.In vitro, retinal damage was induced by 24 h hydrogen peroxide (H2O2) exposure, and cell viability was measured by Hoechst 33342 and YO-PRO-1 staining or by a resazurin–reduction assay. Propolis inhibited the neurotoxicity and apoptosis induced in cultured retinal ganglion cells (RGC-5, a rat ganglion cell line transformed using E1A virus) by 24 h H2O2 exposure. Propolis also inhibited the neurotoxicity induced in RGC-5 cultures by staurosporine. Regarding the possible underlying mechanism, in pig retina homogenates propolis protected against oxidative stress (lipid peroxidation), as also did trolox (water-soluble vitamin E). In micein vivo, propolis (100 mg kg−1; intraperitoneally administered four times) reduced the retinal damage (decrease in retinal ganglion cells and in thickness of inner plexiform layer) induced by intravitrealin vivo N-methyl-d-aspartate injection. These findings indicate that Brazilian green propolis has neuroprotective effects against retinal damage bothin vitroandin vivo, and that a propolis-induced inhibition of oxidative stress may be partly responsible for these neuroprotective effects.

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

Antimicrobial Agents and Chemotherapy ◽

10.1128/aac.05349-11 ◽

2011 ◽

Vol 56 (2) ◽

pp. 658-665 ◽

Cited By ~ 14

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.

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Hepatoprotective and antineoplastic potencial of red propolis produced by the bees Apis mellifera in the semiarid of Rio Grande do Norte, Brazil

Pesquisa Veterinária Brasileira ◽

10.1590/1678-5150-pvb-6214 ◽

2019 ◽

Vol 39 (9) ◽

pp. 744-756

Author(s):

Jardel B. Silva ◽

Kaliane A.R. Paiva ◽

Kizzy M.F.M. Costa ◽

Geysa A. Viana ◽

Hélio N. Araújo Júnior ◽

...

Keyword(s):

Ethanolic Extract ◽

The Other ◽

Hepatoprotective Effect ◽

Normal Cells ◽

Propolis Extract ◽

Regenerative Nodules ◽

Serum Biochemical ◽

The Mean

ABSTRACT: The objective of this study was to evaluate the hepatoprotective effect of the honey bee Apis mellifera ethanolic extract of the red propolis, obtained in four municipalities of the Rio Grande do Norte semi-arid region, through an in vitro evaluation of the antineoplastic potential in human hepatic carcinoma (HepG2) and normal cell lines (L929), and from the comet assay in hepatic cell lines (ZF-L hepatocytes) to evaluate the genoprotective potential of the extract. The hepatoprotective effect was also evaluated in vivo by the induction of chronic experimental hepatic lesions in rodents (Rattus norvegicus Berkenhout, 1769), Wistar line, by intraperitoneal administration of thioacetamide (TAA) at the dose of 0.2g/kg. The animals were distributed in the following experimental groups: G1 (control), G2 (treated with 500mg/kg ethanolic extract of propolis), G3 (treated with 500mg/kg of ethanolic extract and TAA) and G4 (treated with TAA). All rats were submitted to serum biochemical, macroscopic, histological and stereological biochemical exams of the liver. It was verified the genoprotective effect of red propolis since the mean damages promoted to DNA in cells tested with the extract were significantly lower than the mean of the positive control damage (hydrogen peroxide). The red propolis extract did not present cytotoxic activity to the tumor cells of human liver cancer, as well as to normal ones. The absence of cytotoxicity in normal cells may indicate safety in the use of the propolis extract. The results of the serum biochemical evaluation showed that the serum levels of the aminotransferase enzymes (AST) did not differ significantly between G1, G2 and G3 when compared to each other. G4 showed significant increase in levels compared to the other groups, indicating that the administration of the extract did not cause liver toxicity, as well as exerted hepatoprotective effect against the hepatic damage induced by TAA. The G3 and G4 animals developed cirrhosis, but in G3 the livers were characterized by the presence of small regenerative nodules and level with the surface of the organ, whereas in G4 the livers showed large regenerative nodules. The livers of the G1 and G2 animals presented normal histological appearance, whereas the livers of the G3 animals showed regenerative nodules surrounded by thin septa of connective tissue, and in G4 the regenerative nodules were surrounded by thick septa fibrous connective tissue. The analysis of the hepatic tissues by means of stereology showed that there was no statistical difference between the percentage of hepatocytes, sinusoids, and collagens in G1 and G2. In G3 the percentage of hepatocytes, sinusoids, and collagen did not differ significantly from the other groups. It was concluded that the ethanolic extract of the red propolis exerted a hepatoprotective effect, because it promoted in vitro reduction of the damage to the DNA of liver cells, antineoplastic activity in human hepatocellular carcinoma cell line (HepG2) and did not exert cytotoxic effect in normal cells or was able to reduce liver enzyme activity and the severity of cirrhosis induced by TAA in vivo.

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Preclinical approaches in vulvovaginal candidiasis treatment with mucoadhesive thermoresponsive systems containing propolis

PLoS ONE ◽

10.1371/journal.pone.0243197 ◽

2020 ◽

Vol 15 (12) ◽

pp. e0243197

Author(s):

Amanda Pohlmann Bonfim ◽

Karina Mayumi Sakita ◽

Daniella Renata Faria ◽

Glaucia Sayuri Arita ◽

Franciele Abigail Vilugron Rodrigues Vendramini ◽

...

Keyword(s):

Vulvovaginal Candidiasis ◽

Fungal Resistance ◽

Vaginal Mucosa ◽

Childbearing Age ◽

Propolis Extract ◽

Low Toxicity ◽

Fluconazole Resistant ◽

Pharmaceutical Properties

Vulvovaginal candidiasis (VVC) is a common vaginitis that affects women, especially in childbearing age, caused by Candida albicans in almost 80% of cases. Considering the limited drug arsenal available and the increasing fungal resistance profile, the search for new therapeutic sources with low toxicity and easy administration should be supported. Propolis has been used as a traditional medicine for multiple diseases, considering its particular composition and pharmaceutical properties that permits its wide applicability; it has also emerged as a potential antifungal agent. Thus, this study performed an in vitro and in vivo investigation into the efficacy of a new mucoadhesive thermoresponsive platform for propolis delivery (MTS-PRPe) in a preclinical murine model of VVC treatment caused by C. albicans. The methodologies involved chemical analysis, an assessment of the rheological and mucoadhesive properties of propolis formulations, in vitro and in vivo antifungal evaluations, histological evaluations and electron microscopy of the vaginal mucosa. The results demonstrated the antifungal activity of propolis extract and MTS-PRP against the standard strain and a fluconazole-resistant clinical isolate of C. albicans, in both in vitro and in vivo assays. These results were similar and even better, depending on the propolis concentration, when compared to nystatin. Thus, the formulation containing propolis exhibited good performance against C. albicans in a vulvovaginal candidiasis experimental model, representing a promising opportunity for the treatment of this infection.

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In vitro and in vivo investigation of polypharmacology of propolis extract as anticancer, antibacterial, anti-inflammatory, and chemical properties

Open Chemistry ◽

10.1515/chem-2021-0076 ◽

2021 ◽

Vol 19 (1) ◽

pp. 864-874

Author(s):

Nael Abutaha ◽

Mohammed AL-Zharani ◽

Amal Alotaibi ◽

Mary Anne W. Cordero ◽

Asmatanzeem Bepari ◽

...

Keyword(s):

Chemical Properties ◽

Acid Methyl Ester ◽

Cost Effective ◽

Skin Inflammation ◽

Hexane Extract ◽

Major Constituent ◽

Propolis Extract ◽

Anti Inflammatory

Abstract Numerous compounds derived from natural sources such as microbes, plants, and insects have proven to be safe, efficacious, and cost-effective therapeutics for human diseases. This study examined the bioactivities of propolis, a structural sealant and antibacterial/antifungal agent produced by honey bees. Chinese propolis was extracted in methanol or hexane. Propolis significantly reduced the numbers of viable cancer cells when applied as a methanol extract (IC50 values in μg/mL for the indicated cell line: MDA-MB-231, 74.12; LoVo, 74.12; HepG2, 77.74; MCF7, 95.10; A549, 114.84) or a hexane extract (MDA-MB-231, 52.11; LoVo, 45.9; HepG2, 52.11; MCF7, 78.01; A549, 67.90). Hexane extract also induced apoptosis of HepG2 cells according to activated caspase-3/7 expression assays (17.6 ± 2.9% at 150 μg/mL and 89.2 ± 1.9% at 300 μg/mL vs 3.4 ± 0.4% in vehicle control), suppressed the growth of Candida albicans and multiple multidrug-resistant and nonresistant Gram-positive bacteria, and inhibited croton oil-induced skin inflammation when applied as topical treatment. GC-MS identified hexadecanoic acid methyl ester as a major constituent (33.6%). Propolis hexane extract has potential anticancer, antimicrobial, and anti-inflammatory activities.

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Prophylactic Effect Of Aqueous Propolis Extract Against Acute Experimental Hepatotoxicity In Vivo

Zeitschrift für Naturforschung C ◽

10.1515/znc-2002-3-430 ◽

2002 ◽

Vol 57 (3-4) ◽

pp. 379-385 ◽

Cited By ~ 10

Author(s):

Aiman S. El-Khatib ◽

Azza M. Agha ◽

Laila G. Mahran ◽

Mohamed T. Khayyal

Keyword(s):

Reduced Glutathione ◽

Wide Spectrum ◽

Folk Medicine ◽

Lipid Peroxide ◽

Isolated Hepatocytes ◽

Propolis Extract ◽

Single Intraperitoneal Injection ◽

Liver Homogenates

Propolis has been extensively used in folk medicine for the management of a wide spectrum of disorders. In a previous study, we demonstrated the protective effect of the aqueous propolis extract (APE) against the injurious effects of carbon tetrachloride (CCl4) on hepatocytes in vitro. The present investigation was carried out to show whether the hepatoprotective effect of the extract could also be manifested in vivo. Rats were given APE orally for 14 consecutive days, before being subjected to a single intraperitoneal injection of CCl4. One day after the CCl4 injection, the animals were sacrificed, hepatocytes were isolated and liver homogenates were prepared for the assessment of liver injury. In isolated hepatocytes, APE afforded protection against CCl4-induced injury as manifested by a decrease in the leakage of the cytosolic enzyme lactate dehydrogenase (LDH), decreased generation of lipid peroxide and maintenance of cellular reduced glutathione (GSH) content. In principle, similar findings were observed in liver homogenates. The present findings show that APE has in vivo hepatoprotective potential which could be attributed at least in part to the maintenance of cellular GSH content. The latter effect seems to play an important role in conserving the integrity of biomembranes as it was associated with a decrease in lipid peroxidation and reduced leakage of cytosolic LDH

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

Antimicrobial Agents and Chemotherapy ◽

10.1128/aac.43.7.1776 ◽

1999 ◽

Vol 43 (7) ◽

pp. 1776-1778 ◽

Cited By ~ 41

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.

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