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Green Propolis Science

Selective Inhibition of Human Type-5 17β-Hydroxysteroid Dehydrogenase (AKR1C3) by Baccharin, a Component of Brazilian Propolis

Satoshi Endo,*,† Toshiyuki Matsunaga,† Ayano Kanamori,† Yoko Otsuji,† Hiroko Nagai,† Krithika Sundaram,‡ Ossama El-Kabbani,‡ Naoki Toyooka,§,⊥ Shozo Ohta,∥ and Akira Hara†

 

Source
†Laboratory of Biochemistry, Gifu Pharmaceutical University, Gifu 501-1196, Japan
‡Medicinal Chemistry and Drug Action, Monash Institute of Pharmaceutical Sciences, Parkville, Victoria 3052, Australia
§Graduate School of Science and Technology for Research and ⊥Graduate School of Innovative Life Science, University of Toyama, Toyama 930-8555, Japan
∥Nagaragawa Research Center, API Co., Ltd., Gifu 502-0071, Japan

 

Abstract

 

The human aldo-keto reductase (AKR) 1C3, also known as type-5 17β-hydroxysteroid dehydrogenase and prostaglandin F synthase, has been suggested as a therapeutic target in the treatment of prostate and breast cancers. In this study, AKR1C3 inhibition was examined by Brazilian propolis- derived cinnamic acid derivatives that show potential antitumor activity, and it was found that baccharin (1) is a potent competitive inhibitor (Ki 56 nM) with high selectivity, showing no significant inhibition toward other AKR1C isoforms (AKR1C1, AKR1C2, and AKR1C4). Molecular docking and site-directed mutagenesis studies suggested that the non- conserved residues Ser118, Met120, and Phe311 in AKR1C3 are important for determining the inhibitory potency and selectivity of 1. The AKR1C3-mediated metabolism of 17-ketosteroid and farnesal in cancer cells was inhibited by 1, which was effective from 0.2 μM with an IC50 value of about 30 μM. Additionally, 1 suppressed the proliferation of PC3 prostatic cancer cells stimulated by AKR1C3 overexpression. This study is the first demonstration that 1 is a highly selective inhibitor of AKR1C3.

 

 

The effect of propolis on CCL5 and IFN-g expression by peripheral blood mononuclear cells from leishmaniasis patientsjphp_138

Amarante MK, Watanabe MA, Conchon-Costa I, Fiori LL, Oda JM, Búfalo MC, Sforcin JM.

 

Department of Pathological Sciences, UEL, Londrina, PR, Brazil.

 

Abstract

 

Objectives Mucocutaneous leishmaniasis is associated with a strong Th1 immune response to Leishmania, which modulates chemokines and their receptors expres- sion, affecting their migratory capacity. There are no antileishmanial vaccines avail- able and chemotherapy still relies on the potentially toxic pentavalent antimonials. Propolis is a bee product with immunomodulatory and antiparasite activities, and researchers have been attracted to its potential for the development of new drugs. This work investigated the effects of propolis on CCL5 and IFN-g expression by peripheral blood mononuclear cells (PBMC) in order to evaluate a possible immu- nomodulatory action of propolis in patients with leishmaniasis compared to healthy control subjects.

Methods PBMC were incubated in the absence or presence of propolis and the evaluation of a possible cytotoxicity of propolis was carried out using MTT assay. The expression level of CCL5 and IFN-g was determined by real-time PCR.

Key findings Our data indicated that propolis modulates the immune response of leishmaniasis patients in vitro, affecting CCL5 and IFN-g expression by PBMC.

Conclusions Data suggested that propolis drives an anti-inflammatory response depending on concentration. Although propolis is a potential source of new and selective drugs for the treatment of leishmaniasis, its usefulness in the therapeutics
should be further
investigated.

 

Propolis and its direct and indirect hypoglycemic effect.

Al-Hariri MT

 

Department of Physiology, College of Medicine, University of Dammam, Dammam, Saudi Arabia.

 

Abstract

 

Propolis means a gum that is gathered by bees from various plants. It is strongly adhesive resinous substance, collected, transformed, and used by bees to seal holes in their honeycombs. Bees use it to seal holes in their honeycombs, smooth out internal walls, as well as to cover carcasses of intruders who died inside the hive in order to avoid their decomposition. Propolis also protects the colony from diseases because of its antiseptic efficacy and antimicrobial properties. It also has been reported to possess various biological activities, namely anticancer, antioxidant, anti-inflammatory, antibacterial, antifungal, and hypolipidemic. The aim of this review is to evaluate the hypoglycemic effect of propolis since a little number of researches studied this effect when we compare with the huge number of papers that reported many other biological activities.

 

Neuroprotection by Brazilian Green Propolis against In vitro and In vivo Ischemic Neuronal Damage

Masamitsu Shimazawa,1 Satomi Chikamatsu,1 Nobutaka Morimoto,1,2 Satoshi Mishima,3 Hiroichi Nagai,2 and Hideaki Hara1*
1Department of Biofunctional Molecules, Gifu Pharmaceutical University, Gifu, Japan
2Department of Pharmacology, Gifu Pharmaceutical University, Gifu, Japan
3Research Center, API Co. Ltd, Gifu, Japan
*For reprints and all correspondence: Professor H. Hara, PhD, Department of Biofunctional Molecules, Gifu Pharmaceutical University, 5-6-1 Mitahora-higashi, Gifu, 502-8585 Japan. Tel: +81-58-237-3931; Fax: +81-58-237-5979; E-mail: hidehara@gifu-pu.ac.jp
Received January 4, 2005; Accepted March 6, 2005.

Abstract
We examined whether Brazilian green propolis, a widely used folk medicine, has a neuroprotective function in vitro and/or in 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 mice in 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 against in vitro cell death and in vivo focal cerebral ischemia.
Keywords: focal cerebral ischemia, free radical, lipid peroxidation, middle cerebral artery occlusion, PC12 cell culture

Chemical constituents in Baccharis dracunculifolia as the main botanical origin of southeastern Brazilian propolis.

Park YK, Paredes-Guzman JF, Aguiar CL, Alencar SM, Fujiwara FY.
Source
Department of Food Science, College of Food Engineering, State University of Campinas, P.O. Box 6177, 13083-970, Campinas, São Paulo, Brazil. ykpark@fea.unicamp.br
Abstract

Previously, it was reported that one group of propolis (Group 12) was identified in southeastern Brazil, and the botanical origin of the propolis was Baccharis dracunculifolia resinous exudates. It was also observed that honeybee (Africanized Apis mellifera) mainly visited the leaf buds or unexpanded leaves of B. dracunculifolia but rarely expanded leaves. B. dracunculifolia is dioecious with male and female inflorescences, and RPHPLC of the ethanolic extracts of the respective male and female bud resinous exudates showed the same profiles. RPHPLC profiles of propolis G12 leaf buds and unexpanded and expanded leaves of B. dracunculifolia showed similarity, but unexpanded leaves quantitatively decreased in chemical constituents as compared with leaf buds. In the case of expanded leaves, all chemical constituents were severely decreased or disappeared. Artepillin C (3,5-diprenyl-4-hydroxycinnamic acid) was also identified in both propolis and resinous exudates, and both ethanolic extracts contained the highest concentrations of this compound as compared with the rest of the chemical constituents.

Antihypertensive effects of flavonoids isolated from brazilian green propolis in spontaneously hypertensive rats.

Maruyama H, Sumitou Y, Sakamoto T, Araki Y, Hara H.
Source

Nagaragawa Research Center, API Co., Ltd.

Abstract

Propolis, a honeybee product, has become popular as a food and alternative medicine. Its constituents have been shown to exert pharmacological effects, such as anticancer, antimicrobial, and anti-inflammatory effects. The present study was performed to investigate whether Brazilian green propolis exerts antihypertensive effects in spontaneously hypertensive rats (SHR) and which constituents are involved in its effects. Brazilian green propolis was extracted with ethanol and subjected to LH-20 column chromatography eluted with ethanol. The ethanol-eluted fractions at 10 mg/kg were administered orally to SHR for 14 d. Significant decreases in blood pressure were observed in fractions 6 and 7. The active constituents were purified and identified to be four flavonoids: dihydrokaempferide and isosakuranetin in fraction 6 and betuletol and kaempferide in fraction 7. These flavonoids at 10 mg/kg were administered orally to SHR for 28 d, and as a result, isosakuranetin, dihydrokaempferide and betuletol produced significant decrease in blood pressure, especially marked were the effects observed in the group that received isosakuranetin. Brazilian green propolis, fractions 6 and 7, and the 4 active constituents relaxed isolated SHR aorta in a concentration-dependent manner. Therefore, these finding suggest that the vasodilating action may be partly involved in the mechanism of antihypertensive effect. Hence, the ethanol extract of Brazilian green propolis and its main constituents may be useful for prevention of hypertension.

Brazilian propolis-derived components inhibit TNF-α-mediated downregulation of adiponectin expression via different mechanisms in 3T3-L1 adipocytes.

Ikeda R, Yanagisawa M, Takahashi N, Kawada T, Kumazawa S, Yamaotsu N, Nakagome I, Hirono S, Tsuda T.
Source

College of Bioscience and Biotechnology, Chubu University, Kasugai, Aichi 487-8501, Japan.
Abstract
BACKGROUND:

Previous reports suggest that Brazilian propolis has multiple biological functions and may help to restore adiponectin expression and insulin sensitivity. However, little is known about the molecular mechanisms by which these compounds inhibit the downregulation of adiponectin.
METHODS:

The effect of various Brazilian propolis-derived components on inhibition of tumor necrosis factor-α (TNF-α)-mediated downregulation of adiponectin expression in 3T3-L1 adipocytes and molecular mechanism was investigated.
RESULTS AND CONCLUSIONS:

Pretreatment with either artepillin C (C3) or its derivative (C4) significantly inhibited TNF-α-mediated downregulation of adiponectin expression in 3T3-L1 adipocytes. Interestingly, C3 strongly activated peroxisome proliferator-activated receptor γ (PPARγ) transcriptional activity. Treatment of adipocytes with C3 resulted in the upregulation of adiponectin and fatty acid-binding protein 4 expression, but C4 did not significantly induce PPARγ transactivation. C4 did, however, inhibit the TNF-α-induced c-Jun-NH(2)-terminal kinase (JNK) signaling that is involved in adiponectin expression. Molecular docking studies based on hPPARγ with C3 and JNK1 with C4 clearly supported our experimental results. These data demonstrate that 1) both C3 and C4 significantly inhibit the TNF-α-mediated downregulation of adiponectin in adipocytes, 2) C3 functions as a PPARγ agonist, and its inhibition of the effect of TNF-α is due to this PPARγ transactivation, and 3) C4 is an effective inhibitor of JNK activation, thus inhibiting the TNF-α-mediated downregulation of adiponectin.
GENERAL SIGNIFICANCE:

Brazilian propolis-derived components (C3 and C4) can significantly inhibit TNF-α-mediated downregulation of adiponectin in adipocytes, although they do so via different mechanisms.

2011 Elsevier B.V. All rights reserved.

Cell growth inhibitory effect of cinnamic acid derivatives from propolis on human tumor cell lines.

Akao Y, Maruyama H, Matsumoto K, Ohguchi K, Nishizawa K, Sakamoto T, Araki Y, Mishima S, Nozawa Y.
Source

Gifu International Institute of Biotechnology, Kakamigahara, Japan. yakao@giib.or.jp
Abstract

A cell growth inhibitory effect of drupanin and baccharin, ingredients of propolis, was found in human cancer cell lines. These compounds induced apoptosis in the cells characterized by morphological and nucleosomal DNA fragmentation analysis. Their effects were less potent compared with that of artepillin C, which is a known anticancer compound from propolis. Importantly, HL60 cells were more sensitive to drupanin than were Con A-stimulated peripheral blood lymphocytes, whereas the potency of artepillin C was the opposite of that of drupanin.

Antiproliferation of human prostate cancer cells by ethanolic extracts of Brazilian propolis and its botanical origin.

Li H, Kapur A, Yang JX, Srivastava S, McLeod DG, Paredes-Guzman JF, Daugsch A, Park YK, Rhim JS.
Source

Center for Prostate Disease Research, Uniformed Services University of the Health Sciences, Bethesda, MD, USA.
Abstract

Propolis is a resinous substance collected by bees (Apis mellifera) from various tree buds which they then use to coat hive parts and to seal cracks and crevices in the hive. Propolis, a known ancient folk medicine, has been extensively used in diet to improve health and to prevent disease. In the present study, we have evaluated the effects of ethanolic extracts of Brazilian propolis group l2 and bud resins of botanical origin (B. dracunculifolia), and propolis group 3 on proliferation of metastasis (DU145 and PC-3) and primary malignant tumor (RC58T/h/SA#4)-derived human prostate cancer cells. The strongest inhibition was observed in propolis group 3 (sample #3) extracts whereas moderate growth inhibition was observed in human prostate epithelial cells. In the RC58T/h/SA#4 cells, resins of botanical origin of propolis group 12 (sample #1) and propolis group 12 (sample #2) induced growth inhibition that was associated with S phase arrest whereas propolis group 3 (sample #3) induced growth inhibition that was associated with G2 arrest. The mechanisms of cell cycle effects of propolis were investigated. The resins of botanical origin of propolis group 12 and propolis group 12 showed similar inhibition of cyclin D1, CDK4 and cyclin B1 expression. Propolis group 3 showed higher induction of p21 expression but no inhibition of cyclin D1, CDK4 and cyclin B1 expression. The results obtained here demonstrate that the Brazilian propolis extracts have significant inhibitory effect on proliferation of human prostate cancer cells. Inhibition was achieved through regulation of protein expression of cyclin D1, B1 and cyclin dependent kinase (CDK) as well as p21. Our results indicate that the Brazilian propolis extracts show promise as chemotherapeutic agents as well as preventive agents against prostate cancer.

3,4-Dicaffeoylquinic Acid, a Major Constituent of Brazilian Propolis, Increases TRAIL Expression and Extends the Lifetimes of Mice Infected with the Influenza A Virus.

Takemura T, Urushisaki T, Fukuoka M, Hosokawa-Muto J, Hata T, Okuda Y, Hori S, Tazawa S, Araki Y, Kuwata K.
Source

Nagaragawa Research Center, API Co., Ltd., 692-3 Nagara, Gifu 502-0071, Japan.
Abstract

Brazilian green propolis water extract (PWE) and its chemical components, caffeoylquinic acids, such as 3,4-dicaffeoylquinic acid (3,4-diCQA), act against the influenza A virus (IAV) without influencing the viral components. Here, we evaluated the anti-IAV activities of these compounds in vivo. PWE or PEE (Brazilian green propolis ethanol extract) at a dose of 200 mg/kg was orally administered to Balb/c mice that had been inoculated with IAV strain A/WSN/33. The lifetimes of the PWE-treated mice were significantly extended compared to the untreated mice. Moreover, oral administration of 3,4-diCQA, a constituent of PWE, at a dose of 50 mg/kg had a stronger effect than PWE itself. We found that the amount of tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) mRNA in the mice that were administered 3,4-diCQA was significantly increased compared to the control group, while H1N1 hemagglutinin (HA) mRNA was slightly decreased. These data indicate that PWE, PEE or 3,4-diCQA possesses a novel and unique mechanism of anti-influenza viral activity, that is, enhancing viral clearance by increasing TRAIL.

Caffeoylquinic acids are major constituents with potent anti-influenza effects in brazilian green propolis water extract.

Urushisaki T, Takemura T, Tazawa S, Fukuoka M, Hosokawa-Muto J, Araki Y, Kuwata K.
Source

Nagaragawa Research Center, API Co., Ltd., 692-3 Nagara, Yamasaki, Gifu 502-0071, Japan.
Abstract

Influenza A viral infections reached pandemic levels in 1918, 1957, 1968, and, most recently, in 2009 with the emergence of the swine-origin H1N1 influenza virus. The development of novel therapeutics or prophylactics for influenza virus infection is urgently needed. We examined the evaluation of the anti-influenza virus (A/WSN/33 (H1N1)) activity of Brazilian green propolis water extract (PWE) and its constituents by cell viability and real-time PCR assays. Our findings showed strong evidence that PWE has an anti-influenza effect and demonstrate that caffeoylquinic acids are the active anti-influenza components of PWE. Furthermore, we have found that the amount of viral RNA per cell remained unchanged even in the presence of PWE, suggesting that PWE has no direct impact on the influenza virus but may have a cytoprotective activity by affecting internal cellular process. These findings indicate that caffeoylquinic acids are the active anti-influenza components of PWE. Above findings might facilitate the prophylactic application of natural products and the realization of novel anti-influenza drugs based on caffeoylquinic acids, as well as further the understanding of cytoprotective intracellular mechanisms in influenza virus-infected cells.

Green propolis phenolic compounds act as vaccine adjuvants, improving humoral and cellular responses in mice inoculated with inactivated vaccines.

Fischer G, Paulino N, Marcucci MC, Siedler BS, Munhoz LS, Finger PF, Vargas GD, Hübner SO, Vidor T, Roehe PM.
Source
Centro de Ciências Básicas da Saúde, Universidade Federal do Rio Grande do Sul, Porto Alegre, RS, Brasil. geferson.fischer@gmail.com
Abstract
Adjuvants play an important role in vaccine formulations by increasing their immunogenicity. In this study, the phenolic compound-rich J fraction (JFR) of a Brazilian green propolis methanolic extract stimulated cellular and humoral immune responses when co-administered with an inactivated vaccine against swine herpesvirus type 1 (SuHV-1). When compared to control vaccines that used aluminium hydroxide as an adjuvant, the use of 10 mg/dose of JFR significantly increased (p < 0.05) neutralizing antibody titres against SuHV-1, as well as the percentage of protected animals following SuHV-1 challenge (p < 0.01). Furthermore, addition of phenolic compounds potentiated the performance of the control vaccine, leading to increased cellular and humoral immune responses and enhanced protection of animals after SuHV-1 challenge (p < 0.05). Prenylated compounds such as Artepillin C that are found in large quantities in JFR are likely to be the substances that are responsible for the adjuvant activity.

Quercetin and Cancer Chemoprevention

Lara Gibellini, 1 Marcello Pinti, 1 Milena Nasi, 1 Jonas P. Montagna, 1 Sara De Biasi, 1 Erika Roat, 1 Linda Bertoncelli, 1 Edwin L. Cooper, 2 and Andrea Cossarizza 1 *
1Department of Biomedical Sciences, University of Modena and Reggio Emilia School of Medicine, 41125 Modena, Italy
2David Geffen School of Medicine, UCLA Medical Center (CHS), Los Angeles, CA, USA
*Andrea Cossarizza: Email: andrea.cossarizza@unimore.it
Received November 24, 2009; Accepted April 9, 2010.

Abstract
Several molecules present in the diet, including flavonoids, can inhibit the growth of cancer cells with an ability to act as “chemopreventers”. Their cancer-preventive effects have been attributed to various mechanisms, including the induction of cell-cycle arrest and/or apoptosis as well as the antioxidant functions. The antioxidant activity of chemopreventers has recently received a great interest, essentially because oxidative stress participates in the initiation and progression of different pathological conditions, including cancer. Since antioxidants are capable of preventing oxidative damage, the wide use of natural food-derived antioxidants is receiving greater attention as potential anti-carcinogens. Among flavonoids, quercetin (Qu) is considered an excellent free-radical scavenging antioxidant, even if such an activity strongly depends on the intracellular availability of reduced glutathione. Apart from antioxidant activity, Qu also exerts a direct, pro-apoptotic effect in tumor cells, and can indeed block the growth of several human cancer cell lines at different phases of the cell cycle. Both these effects have been documented in a wide variety of cellular models as well as in animal models. The high toxicity exerted by Qu on cancer cells perfectly matches with the almost total absence of any damages for normal, non-transformed cells. In this review we discuss the molecular mechanisms that are based on the biological effects of Qu, and their relevance for human health.

Green Brazilian Propolis Action on Macrophages and Lymphoid Organs of Chronically Stressed Mice

Fabiane Missima and José Maurício Sforcin
Department of Microbiology and Immunology, Biosciences Institute, UNESP, 18618-000 Botucatu, S.P., Brazil
For reprints and all correspondence: José Maurício Sforcin, Biosciences Institute, UNESP, 18618-000 Botucatu, S.P., Brazil. Tel: +551438116058; Fax: +551438153744; E-mail: sforcin@ibb.unesp.br
Received September 6, 2006; Accepted December 4, 2006.

Abstract

Stress is a generic term that summarizes how psychosocial and environmental factors influence physical and mental well-being. The interaction between stress and immunity has been widely investigated, involving the neuroendocrine system and several organs. Assays using natural products in stress models deserve further investigation. Propolis immunomodulatory action has been mentioned and it has been the subject of scientific investigation in our laboratory. The aim of this study was to evaluate if and how propolis activated macrophages in BALB/c mice submitted to immobilization stress, as well as the histopathological analysis of the thymus, bone marrow, spleen and adrenal glands. Stressed mice showed a higher hydrogen peroxide (H2O2) generation by peritoneal macrophages, and propolis treatment potentiated H2O2 generation and inhibited nitric oxide (NO) production by these cells. Histopathological analysis showed no alterations in the thymus, bone marrow and adrenal glands, but increased germinal centers in the spleen. Propolis treatment counteracted the alterations found in the spleen of stressed mice. New research is being carried out in order to elucidate propolis immunomodulatory action during stress.
Keywords: lymphoid organs, macrophages, propolis, stress

Anti-inflammatory effects of a bioavailable compound, Artepillin C, in Brazilian propolis.

Paulino N, Abreu SR, Uto Y, Koyama D, Nagasawa H, Hori H, Dirsch VM, Vollmar AM, Scremin A, Bretz WA.
Source
Programa de Pós-graduação em Farmácia, Universidade Bandeirante de São Paulo, São Paulo, Brazil. niraldop@yahoo.com.br
Abstract
Artepillin C is the major compound in the Brazilian green propolis from Baccharis dracunculifolia. Our aim in this study was to investigate the anti-inflammatory effects, absorption, and bioavailability of Artepillin C in mice. The animals used were male Swiss mice subjected to: paw oedema by carrageenan (300 microg/paw), carrageenan-induced peritonitis, and prostaglandin E(2) determination. We also measured in vitro nitric oxide production by RAW 264.7 cells and NF-kappaB activity in HEK 293 cells. Finally, we measured the absorption and bioavailability of Artepillin C in plasma from mice by means of GC-MS after a single oral dose (10 mg/kg). In vivo, Artepillin C produced a maximal inhibition of 38% after 360 min on paw oedema. Artepillin C also decreased the number of neutrophils during peritonitis (IC(50): 0.9 (0.5-1.4) mg/kg). Treatment with Artepillin C decreased prostaglandin E(2) by 29+/-3% and 58+/-5% at 1 and 10 mg/kg, respectively, with a mean ID(50) of 8.5 (8.0-8.7) mg/kg). Similarly, in in vitro models, Artepillin C (3, 10, or 100 microM) decreased nitric oxide production by RAW 264.7 cells with a mean IC(50) of 8.5 (7.8-9.2) microM. In HEK 293 cells, Artepillin C reduced NF-kappaB activity with a mean IC(50) of 26 (22-30) mug/ml), suggesting anti-inflammatory activity, particularly during acute inflammation. Lastly, Artepillin C was absorbed after an oral dose (10 mg/kg) with maximal peaks found at 1 h (22 microg/ml). Collectively, Artepillin C showed anti-inflammatory effects mediated, at least in part, by prostaglandin E(2) and nitric oxide inhibition through NF-kappaB modulation, and exhibited bioavailability by oral administration.

In vitro Cytotoxic Effect of Brazilian Green Propolis on Human Laryngeal Epidermoid Carcinoma (HEp-2) Cells

Michelle C. Búfalo, João M. G. Candeias, and José Maurício Sforcin
Department of Microbiology and Immunology, Biosciences Institute, UNESP, 18618-000 Botucatu, S.P., Brazil
For reprints and all correspondence: José Maurício Sforcin, Biosciences Institute, UNESP, 18618-000 Botucatu, S.P., Brazil. Tel: +55 14 38116058; Fax: +55 14 38153744; E-mail: sforcin@ibb.unesp.br
Received May 25, 2007; Accepted August 20, 2007.

Abstract
Propolis is a sticky dark-colored material showing a very complex chemical composition that honeybees collect from plants. It has been used in folk medicine since ancient times, due to several biological properties, such as antimicrobial, anti-inflammatory, antioxidant and immunomodulatory activities, among others. Its antitumor action in vivo and in vitro has also been reported, using propolis extracts or its isolated compounds. The goal of this work was to evaluate propolis’s cytotoxic action in vitro on human laryngeal epidermoid carcinoma (Hep-2) cells. These cells were incubated with different concentrations of this bee product for different time periods, and morphology and the number of viable HEp-2 cells analyzed. Data showed that propolis exhibited a cytotoxic effect in vitro against HEp-2 cells, in a dose- and time-dependent way. Propolis solvent had no effects on morphology and number of viable cells, proving that the cytotoxic effects were exclusively due to propolis components. Since humans have been using propolis for a long time, further assays will provide a better comprehension of propolis’s antitumor action.
Keywords: antitumor action, HEp-2 cells, propolis

Intestinal Anti-Inflammatory Activity of Baccharis dracunculifolia in the Trinitrobenzenesulphonic Acid Model of Rat Colitis

Sílvia Helena Cestari, 1 Jairo Kennup Bastos, 2 and Luiz Claudio Di Stasi 1 *
1Laboratory of Phytomedicines, Department of Pharmacology, Instituto de Biociências, São Paulo State University–UNESP, Botucatu 18.618-000, São Paulo, Brazil
2Faculty of Pharmaceutical Sciences, University of São Paulo, Ribeirão Preto 14040-903, São Paulo, Brazil
*Luiz Claudio Di Stasi: Email: ldistasi@ibb.unesp.br
Received January 13, 2009; Accepted May 28, 2009.

Abstract

Baccharis dracunculifolia DC (Asteraceae) is a Brazilian medicinal plant popularly used for its antiulcer and anti-inflammatory properties. This plant is the main botanical source of Brazilian green propolis, a natural product incorporated into food and beverages to improve health. The present study aimed to investigate the chemical profile and intestinal anti-inflammatory activity of B. dracunculifolia extract on experimental ulcerative colitis induced by trinitrobenzenosulfonic acid (TNBS). Colonic damage was evaluated macroscopically and biochemically through its evaluation of glutathione content and its myeloperoxidase (MPO) and alkaline phosphatase activities. Additional in vitro experiments were performed in order to test the antioxidant activity by inhibition of induced lipid peroxidation in the rat brain membrane. Phytochemical analysis was performed by HPLC using authentic standards. The administration of plant extract (5 and 50mgkg−1) significantly attenuated the colonic damage induced by TNBS as evidenced both macroscopically and biochemically. This beneficial effect can be associated with an improvement in the colonic oxidative status, since plant extract prevented glutathione depletion, inhibited lipid peroxidation and reduced MPO activity. Caffeic acid, p-coumaric acid, aromadendrin-4-O-methyl ether, 3-prenyl-p-coumaric acid, 3,5-diprenyl-p-coumaric acid and baccharin were detected in the plant extract.

3,4-Dicaffeoylquinic Acid, a Major Constituent of Brazilian Propolis, Increases TRAIL Expression and Extends the Lifetimes of Mice Infected with the Influenza A Virus

Tomoaki Takemura, 1 Tomohiko Urushisaki, 1 Mayuko Fukuoka, 2, 3 Junji Hosokawa-Muto, 4, 5 Taketoshi Hata, 1 Yumiko Okuda, 4 Sachie Hori, 4 Shigemi Tazawa, 1 Yoko Araki, 1 and Kazuo Kuwata 2, 3, 4 *
1Nagaragawa Research Center, API Co., Ltd., 692-3 Nagara, Gifu 502-0071, Japan
2United Graduate School of Drug Discovery and Medical Information Sciences, Gifu University, 1-1 Yanagido, Gifu 501-1193, Japan
3CREST, Japan Science and Technology Agency, 4-1-8 Honcho, Kawaguchi, Saitama 332-0012, Japan
4Center for Emerging Infectious Diseases, Gifu University, 1-1 Yanagido, Gifu 501-1194, Japan
5First Department of Forensic Science, National Research Institute of Police Science, 6-3-1 Kashiwanoha, Kashiwa, Chiba 277-0882, Japan
*Kazuo Kuwata: Email: kuwata@gifu-u.ac.jp
Academic Editor: Vincenzo De Feo
Received May 12, 2011; Revised July 4, 2011; Accepted July 4, 2011.
This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

Abstract

Brazilian green propolis water extract (PWE) and its chemical components, caffeoylquinic acids, such as 3,4-dicaffeoylquinic acid (3,4-diCQA), act against the influenza A virus (IAV) without influencing the viral components. Here, we evaluated the anti-IAV activities of these compounds in vivo. PWE or PEE (Brazilian green propolis ethanol extract) at a dose of 200mg/kg was orally administered to Balb/c mice that had been inoculated with IAV strain A/WSN/33. The lifetimes of the PWE-treated mice were significantly extended compared to the untreated mice. Moreover, oral administration of 3,4-diCQA, a constituent of PWE, at a dose of 50mg/kg had a stronger effect than PWE itself. We found that the amount of tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) mRNA in the mice that were administered 3,4-diCQA was significantly increased compared to the control group, while H1N1 hemagglutinin (HA) mRNA was slightly decreased. These data indicate that PWE, PEE or 3,4-diCQA possesses a novel and unique mechanism of anti-influenza viral activity, that is, enhancing viral clearance by increasing TRAIL.

Botanical origin and chemical composition of Brazilian propolis.

Park YK, Alencar SM, Aguiar CL.
Source
Department of Food Science, College of Food Engineering, State University of Campinas, 13081-970 Campinas, Sao Paulo, Brazil. ykpark@fea.unicamp.br
Abstract
Brazilian propolis has been classified into 12 groups based on physicochemical characteristics: five in the southern Brazil group (group 3), one in the southeastern Brazil group (group 12), and six in the northeastern Brazil group (group 6). The plant origins of these groups were investigated using reversed-phase high-performance thin-layer chromatography (RPHPTLC), reversed-phase high-performance liquid chromatography (RPHPLC), and gas chromatography-mass spectrometry (GC-MS). It was concluded that the origins of propolis group 3, group 6, and group 12 are resins of the poplar tree, Hyptis divaricata, and Baccharis dracunculifolia, respectively.

Plant Origin of Green Propolis: Bee Behavior, Plant Anatomy and Chemistry

Érica Weinstein Teixeira,1 Giuseppina Negri,2 Renata M.S.A. Meira,3 Dejair Message,4 and Antonio Salatino2*
1Agência Paulista de Tecnologia dos Agronegócios/SAA-SP, Pindamonhangaba, SP, Brazil
2University of São Paulo, Institute of Biosciences, Department of Botany, São Paulo, SP, Brazil
3Viçosa Federal University, Department of Plant Biology, Viçosa, MG, Brazil
4Viçosa Federal University, Department of Animal Biology, Viçosa, MG, Brazil
*For reprints and all correspondence: A. Salatino, University of São Paulo, Institute of Biosciences, Department of Botany, C. Postal. 11461, 05422-970, São Paulo, SP, Brazil. Tel.: +55 11 3091 7532; Fax: +55 11 3091 7416; E-mail: asalatin@ib.usp.br
Received June 4, 2004; Accepted November 15, 2004.
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Abstract
Propolis, a honeybee product, has gained popularity as a food and alternative medicine. Its constituents have been shown to exert pharmacological effects, such as anti-microbial, anti-inflammatory and anticancer. Shoot apices of Baccharis dracunculifolia (alecrim plant, Asteraceae) have been pointed out as sources of resin for green propolis. The present work aimed (i) to observe the collecting behavior of bees, (ii) to test the efficacy of histological analysis in studies of propolis botanical origin and (iii) to compare the chemistries of alecrim apices, resin masses and green propolis. Bee behavior was observed, and resin and propolis were microscopically analyzed by inclusion in methacrylate. Ethanol extracts of shoot apices, resin and propolis were analyzed by gas chromatography/mass spectroscopy. Bees cut small fragments from alecrim apices, manipulate and place the resulting mass in the corbiculae. Fragments were detected in propolis and identified as alecrim vestiges by detection of alecrim structures. Prenylated and non-prenylated phenylpropanoids, terpenoids and compounds from other classes were identified. Compounds so far unreported for propolis were identified, including anthracene derivatives. Some compounds were found in propolis and resin mass, but not in shoot apices. Differences were detected between male and female apices and, among apices, resin and propolis. Alecrim apices are resin sources for green propolis. Chemical composition of alecrim apices seems to vary independently of season and phenology. Probably, green propolis composition is more complex and unpredictable than previously assumed.
Keywords: africanized Apis mellifera, anthracene derivatives, Baccharis dracunculifolia, dehydrocostus lactone, prenylated phenylpropanoids

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