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[Identification of an antimicrobially active constituent isolated from propolis (author's transl)].

On isolating and identifying antimicrobially active propolis constituents, the authors detected a substance that must be regarded as a mixture of caffeic acid esters. The caffeic acid moiety was unequivocally identified by various chemical and spectroscopic methods. The results obtained from the gas chromatographic study of the alcohol fraction after hydrolysis of the isolated compound identify benzyl alcohol, phenyl ethyl alcohol and cinnamic alcohol as ester components. Furthermore, the mass spectroscopic findings are indicative of the presence of a caffeic acid pentenyl ester in the mixture. Attempts to separate this ester mixture by recrystallization and thin-layer chromatography failed.

Anti-Bacterial Agents↗

[Pharmacokinetic studies of the propolis constituent pinocembrin in the rat (author's transl)].

The present investigation into the pharmacokinetic behaviour of the propolis constituent pinocembrin which produces a relatively good antimicrobial effect in vitro, points to possible causes of its therapeutical failure when mice infected with Candida albicans were used as a model. The biological half-life periods for the phases of invasion and elimination were 26 and 268 min, respectively. The biological availability was 25%. Almost 15% of pinocembrin are excreted unchanged in faeces and urine. Even in case of oral application of doses of up to 500 mg/kg, the serum pinocembrin concentrations did not equal the MIC (minimal inhibitor concentration) values required in vitro. A considerable first-pass effect and accelerated processes of elimination are discussed as possible causes. It appears from the present findings that pinocembrin may be utilizable only for the external treatment of stomatomycoses.

Animals↗

Biological properties and clinical application of propolis. XI. Histophathological analysis after intravenous application of ethanol extract of poprolis (EEP).

Mice were given i.v. injections of water solutions of ethanol extract of propolis (EEP) over a varying period of time. Some of the animals were sacrificed immediately following the last injection and some within 2--4 weeks after the last injections. Internal organ samples were taken and underwent a microscopic examination. Insignificant pathological changes in the liver were observed. These changes were transient and regressed within 2--4 weeks after the application of EEP.

Animals↗

In vitro studies on the cytostatic activity of propolis extracts.

Extracts from propolis have been investigated for cytostatic activity in vitro, by method of tissue culture on human KB and HeLa cell lines. Diethyl ether extract (DEEP) sowed the greatest activity and therefore it was further fractionated. Secondary DEEP fractions obtained by extraction with BuOH (ED50 = 2.6 micrograms/ml) and AcOEt (ED50 = 3.3 micrograms/ml) have been qualified to further in vivo studies.

Cell Division↗

[The liver-protective properties of the pediatric drug form of propolis in animals of different age groups].

The pharmacological activity of a pediatric formulation of the phenolic hydrophobic drug propolis was studied in the experiments on albino rats of various age with toxic liver damages of various duration and in acute hepatic ischemia. In all models of hepatic abnormalities, the drug was found to show antioxidative properties which were moderate (30-60%). In addition, there were improvements in hepatic secretion of bile, cholic acids, and cholesterol. On the other hand, the membrane-stabilizing effect of the drug was exerted in not all the tested models of hepatic damage.

Acute Disease↗

Synergistic effect of ethanolic extract of propolis and antibiotics on the growth of staphylococcus aureus.

Ethanolic extract of propolis (EEP), known to possess marked antibacterial activity, was incubated with 8 different common antibiotics in culture medium containing a fixed amount of a standard strain of Staphylococcus aureus. The antibiotic compounds used were: penicillin G, doxycycline, streptomycin, cloxacillin, chloramphenicol, cefradine, ampicillin and polymyxin B. They were used in varying levels, ranging between 0.000005-125.0 micrograms/ml or units, resp. Firstly, their minimal inhibitory concentrations were established in the absence of EEP, than EEP was added in concentrations up to 600 micrograms/ml. EEP had a marked synergistic effect on the antibacterial activity of streptomycin and cloxacillin, and a moderate synergistic effect on the others, except ampicillin.

Anti-Bacterial Agents↗

[Vaginal parasites and acute cervicitis: local treatment with propolis. Preliminary report].

A prospective study is performed in patients who sought for medical care at 2 selected medical offices from "26 de Julio" Teaching Polyclinics, Playa municipality, during July 1st, 1991 and July 31, 1992. These patients presented with acute cervicitis and had vaginal smears with positive cultures of some kind of infection. A study group and a control group were formed and the study was double-blind according to a random sample created for that purpose. Vaginal dressings using 5% propolis were applied to the study group, while daily dressings with Lugol were applied to the control group for 10 consecutive days. A survey was designed and results collected. It is concluded that all patients from the study group did not present with any other symptoms after treatment was completed since negative results were attained in 100% of the smears and 90% achieved a total epithelization of the cervix within 10 days of treatment. The importance of nursing care for the success of treatment is highlighted.

Acute Disease↗

Histopathological evaluation on the effect of red propolis on liver damage induced by CCl4 in rats.

A histopathological evaluation was performed on liver of rats treated with carbon tetrachloride (CCl4) and 25,50 and 100 mg/kg of Cuban red propolis (RP) extract. Additionally, alanine aminotransferase (ALT) in serum and liver triglycerides were determined in all animals. The morphometric study included the count of ballooned cells at the zone III of the Rappaport acini and the assessment of a software program to estimate the extension of steatosis area. A significant reduction of ballooned cells count in liver was observed at three dose levels of RP extract with respect to rats treated only with CCl4. Also, a certain reduction of steatosis degree as well as decreased concentration of liver triglycerides and ALT activity were found in three groups of rats treated with RP extract and CCl4 in relation to those treated with the hepatotoxin. Taken together, the histopathological and biochemical findings show hepatoprotective effects of RP extract in CCl4-induced liver damage in rats, probably due to the antioxidant effect of RP.

Alanine Transaminase↗

The protective effect of aqueous propolis extract on isolated rat hepatocytes against carbon tetrachloride toxicity.

The protective effect of honeybee aqueous propolis extract (APE) against the hepatotoxicity of carbon tetrachloride was investigated using isolated liver-cell suspensions as the experimental model. Various concentrations of the extract were preincubated with the hepatocyte suspensions for 30 min before being subjected to the hepatotoxin for a further 30 min. The hepatocyte toxicity was assessed using three parameters, namely, the release of lactate dehydrogenase, the formation of lipid peroxides and the depletion of intracellular reduced glutathione. It was found that a dose-related protection against the induced cell injury was conferred by APE as evidenced by its inhibitory influence on the changes induced by CCl4 on the measured parameters. The hepatocyte protective effect of APE is probably a result of its antioxidant and free-radical-scavenging properties which in turn help to maintain the intracellular level of reduced glutathione.

Animals↗

Anticomplement activity of lysine complexes of propolis phenolic constituents and their synthetic analogs.

Several phenolic constituents of propolis and their synthetic analogs were derivatized with L-lysine. The ability of these complexes to alter complement activity was estimated in vitro in human serum. The influence of selected complexes on C3 hemolytic activity via classical pathway (CP) and alternative pathway (AP) and on zymosan-induced AP activation was determined. The results suppose that the anticomplement effect of the complexes might be related to the interaction with C3 complement component.

Complement Inactivator Proteins↗

Natural propolis extract NIVCRISOL in the treatment of acute and chronic rhinopharyngitis in children.

In the work there are shown the results of a "case control" study carried out in a children collectivity (preschool children and school-children), regarding the action of an aqueous propolis extract, NIVCRISOL, in acute and chronic inflammatory diseases of the upper airways. The preparation, which had a rich content of flavonoids, was administered to a group of preschool children and school-children treated during the whole cold season 1994-1995. The monitoring of the subgroups investigated was performed by clinical observation of the health state and recording of the incidence of symptoms characteristic to acute or chronic rhinopharyngeal diseases, as well as by a periodical laboratory examination for the detection and characterization of viral, microbial and fungal germs carriage. The analysis of the data obtained pointed out the favourable effects of this local treatment, expressed by lowering of the number of cases with acute or chronic symptoms, and decrease and sometimes suppression of the viral-microbial flora carriage of the upper airways. These positive results, the good tolerance of the preparation, the advantages of the therapy with natural products and more economic criteria entitle us to propose the administration of this preparation as an adjuvant medication in the local treatment of some clinical forms of acute or chronic rhinopharyngeal diseases.

Acute Disease↗

Preferential cytotoxicity to tumor cells of 3,5-diprenyl-4-hydroxycinnamic acid (artepillin C) isolated from propolis.

A tumoricidal substance was isolated from Brazilian propolis as guided by cytotoxicity assay on HuH 13 (human hepatocellular carcinoma) cell and was characterized to be 3-[4-hydroxy-3,5-bis (3-methyl-2-butenyl) phenyl]-2-propenoic acid (3,5-diprenyl-4-hydroxycinnamic acid (artepillin C)). It exhibited preferential cytotoxicity to tumor cells cultured in vitro. The cytotoxicity observed seemed to be partly attributable to apoptosis-like DNA fragmentation. The compound showed anti-tumor activity more effective than that of 5-fluorouracil to transplantable human tumor cell lines when tested on histoculture drug response assay system.

Antineoplastic Agents↗

Effects of propolis flavonoids on virus infectivity and replication.

The effect of five propolis flavonoids on the infectivity and replication of some herpesvirus, adenovirus, coronavirus and rotavirus strains has been studied. Experiments were performed in vitro in cell cultures using the viral plaque reduction technique. The cytotoxicity of flavonoids, including chrysine, kaempferol, acacetin, galangin and quercetin, was evaluated on uninfected monolayers to determine their effect on cell growth and viability. Chrysine and kaempferol caused a concentration-dependent reduction of intracellular replication of herpes-virus strains when monolayers were infected and subsequently cultured in a drug-containing medium. However, virus infectivity was not significantly affected. Acacetin and galangin had no effect on either the infectivity or replication of any of the viruses studied. Quercetin reduced infectivity and intracellular replication, but only at the highest concentrations tested.

Animals↗

Role of caffeic acid phenethyl ester, an active component of propolis, against cisplatin-induced nephrotoxicity in rats.

We have investigated the effect of caffeic acid phenethyl ester (CAPE) on cisplatin-induced nephrotoxicity in rats. Administration of a single dose of cisplatin resulted in the elevation of blood urea nitrogen and creatinine in serum, as well as nitric oxide in kidney tissue of rats. Cisplatin also caused reduction of catalase (P < 0.0001), superoxide dismutase (P = 0.149) and glutathrone peroxidase (P < 0.0001) activities in kidney tissue. Although cisplatin caused elevation in malondialdehyde levels and myeloperoxidase activities in kidney tissue, they were not statistically significant. Caffeic acid phenethyl ester was found to be protective against cisplatin-induced antioxidant enzyme reductions. Treatment with free-radical scavenger CAPE attenuated the increase in plasma blood urea nitrogen and kidney nitric oxide levels, and showed histopathological protection against cisplatin-induced acute renal failure. Extensive epithelial cell vacuolization, swelling, desquamation and necrosis were observed in the kidney of the cisplatin-treated rat. There were also larger tubular lumens in cisplatin-treated rats than those of the control and the CAPE groups. Caffeic acid phenethyl ester caused a marked reduction in the extent of tubular damage. It is concluded that administration of cisplatin imposes an oxidative stress to renal tissue and CAPE confers protection against the oxidative damage associated with cisplatin. This mechanism may be attributed to its free-oxygen-radical scavenging activity.

Acute Kidney Injury↗

The protective effects of Propolis on hepatic injury and its mechanism.

AbstractPropolis (PP) is a sticky substance that is collected from plants by honeybees. The purpose of this study was to investigate the protective effects of PP on hepatotoxicity induced by acetaminophen (AA, paracetamol) and the mechanism of its hepatoprotective effect. In rat hepatocyte culture, pretreatment with PP (1, 10, 100, 200 and 400 microg/mL, 24 h) significantly decreased the cytotoxicity of AA (0.5 mm) in a dose-dependent manner. In mice, pretreatment with PP (10 and 25 mg/kg, p.o., 7 days) also decreased the mortality and the incidence and severity of hepatic necrosis induced by AA (400 mg/kg, i.p.). After treatment with PP for 7 days, the hepatic enzyme activities of cytochrome P450 monooxygenases (P450s), UDP-glucuronyltransferase, phenolsulphotransferase (PST), glutathione S-transferase (GST) were measured in both rats and mice. In rats, PP (50 and 100 mg/kg, p.o.) decreased the activity of P4502E1, but significantly increased the activities of GST and PST. On the other hand, in mice treated with PP (10 and 25 mg/kg, p.o.), the activities of P4501A2, 2B1, 3A4 and 2E1 were dramatically inhibited, and the activity of PST was significantly enhanced. These results suggest that PP has a protective effect on hepatic injury, and that its effect may be explained by inhibition of phase I enzymes and induction of phase II enzymes.

Acetaminophen↗