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On the local anaesthetic action of propolis and some of its constituents.

An ethanolic propolis extract and some constituents isolated from propolis were tested on the cornea of the rabbit and of the mouse for local anaesthetic activity. Total anaesthesia was obtained with the total extract as well as with the compounds 5,7-dihydroxyflavanone (pinocembrin), 5-hydroxy-7-methoxyflavanone (pinostrobin) and with a mixture of caffeic acid esters. Each of these compounds was nearly thrice as potent as the total extract. Propoxypiperocaine which was tested for the purpose of comparison was still efficient in an almost 10-fold lower concentration. When applied subcutaneously, pinocembrin and the mixture of caffeic acid esters produced nearly the same anaesthesia as lidocaine.

Anesthesia, Intravenous↗

The effect of an aqueous propolis extract, of rutin and of a rutin-quercetin mixture on experimental influenza virus infection in mice.

Investigations were performed on the effect of an aqueous propolis extract, of rutin and of a rutin-quercetin mixture on experimental infection with influenza virus A/PR8/34 (H0N1) in mice. Propolis extract administered intranasally 3 hours before virus inoculation led to a reduction of the HA titers recorded in the lung suspensions from infected mice, but to no reduction in mortality or increase in mean survival length. When the extract was administered 3 hours after virus inoculation, the reduction in HA titer was accompanied by a slight decrease in mortality and increase in mean survival length, Rutin and the rutin-quercetin mixture caused an increase in both HA titer and mortality.

Animals↗

Bactericidal effect of propolis in vitro against agents causing upper respiratory tract infections.

Propolis is a natural product of bees which exhibits an antimicrobial effect. In the study the existence of a bactericidal effect against several strains isolated from patients with infections in their upper respiratory tracts is demonstrated. In light of the use of propolis as a therapeutic agent in natural medicine for common colds and inflammatory processes this effect is discussed.

Anti-Bacterial Agents↗

[Propolis extract. II. Wound healing the the rat and rabbit].

This work is related to wounds healing properties of a propolis extract. In first study on the Albinos Rabbit, the activity of a propolis extract is compared with these of a Peru balsam. Optimal concentrations of them in ointments are evaluated by applications on deep cutaneous scarifications. In order to go further into details, we have chosen in second part, another assay on the Rat, allowing the obtention of deeper wounds; By this way, more complete quantification of retained parameters and a better appraising of the wounds healing process evolution are possible.

Animals↗

[Propolis: its use in technology and research].

Analytical procedure more advanced allowed to identify, to isolate, and assay the compounds present in propoli which is is developed to be a valuable biological product as food resource as medical resource. Analytical procedure more and more sophisticated allowed (us) to assay the propoli composition without operate the derivatization of phenolic constituents making use the capacity of different detector used. These phenolic contents were analysed by capillary gas chromatography using an electron-capture detector. This detector shown a good electron capture response of these compounds, which belong to the so-called "conjugated electrophores".

Anti-Infective Agents↗

[The use of ocular drug films of propolis in the sequelae of ophthalmic herpes].

There was studied the therapeutic efficiency of ocular medical propolis films (OMF) in 35 patients with postherpetic trophic keratitis and in 20 with postherpetic nebula. OMF were applied behind the lower eyelid at bedtime during 10-15 days. All the patients endured the propolis films well. OMF accelerated the cornea epithelization. Epitheliopathy and micropoint edema of cornea epithelium rapidly disappeared. Time of patients recovery reduced nearly twice (P,001) in comparison with the control group--from 14.1 to 7.6 days. On the average their visual acuity increased in two times--from 0.12 to 0.27 (P > 0.001).

Administration, Topical↗

[Isolation and identification of a new cinnamate ester from liaoxi propolis].

A new cinnamate ester drivitive (II) and three flavonoids (I, III, IV) were isolated from Liaoxi propolis. Their chemical structures were established as benzyl caffeate (II), 7-O-methylchrysin (I), genkwanin (III) and rhamnazin (IV) by spectral analysis. II is a new natural compound; I, III and IV were found from the propolis for the first time.

Animals↗

Comparison of Radical Scavenging Activity, Cytotoxic Effects and Apoptosis Induction in Human Melanoma Cells by Taiwanese Propolis from Different Sources.

Propolis is a sticky substance that is collected from plants by honeybees. We previously demonstrated that propolins A, B, C, D, E and F, isolated from Taiwanese propolis (TP), could effectively induce human melanoma cell apoptosis and were strong antioxidant agents. In this study, we evaluated TP for free radical scavenging activity by DPPH (1,2-diphenyl-2-picrylhydrazyl). The phenolic concentrations were quantified by the Folin-Ciocalteu method. The apoptosis trigger activity in human melanoma cells was evaluated. TP contained a higher level of phenolic compounds and showed strong capability to scavenge free radicals. Additionally, TP1g, TP3, TP4 and TP7 exhibited a cytotoxic effect on human melanoma cells, with an IC(50) of approximately 2.3, 2.0, 3.3 and 3.3 μg/ml, respectively. Flow cytometric analysis for DNA fragmentation indicated that TP1g, TP2, TP3 and TP7 could induce apoptosis in human melanoma cells and there is a marked loss of cells from the G2/M phase of the cell cycle. To address the mechanism of the apoptosis effect of TP, we evaluated its effects on induction of apoptosis-related proteins in human melanoma cells. The levels of procaspase-3 and PARP [poly(ADP-ribose) polymerase] were markedly decreased. Furthermore, propolins A, B, C, D, E and F in TP were determined using HPLC. The results indicate that TP is a rich source of these compounds. The findings suggest that TP induces apoptosis in human melanoma cells due to its high level of propolins.

Journal Article↗

Artepillin C in Brazilian propolis induces G(0)/G(1) arrest via stimulation of Cip1/p21 expression in human colon cancer cells.

Potential chemopreventive agents exist in foods. Artepillin C in Brazilian propolis was investigated for its effects on colon carcinogenesis. We had found that artepillin C was a bioavailable antioxidant, which could be incorporated into intestinal Caco-2 and hepatic HepG2 cells without any conjugation and inhibited the oxidation of intracellular DNA. Artepillin C was then added to human colon cancer WiDr cells. It dose-dependently inhibited cell growth, inducing G(0)/G(1) arrest. The events involved a decrease in the kinase activity of a complex of cyclin D/cyclin-dependent kinase 4 and in the levels of retinoblastoma protein phosphorylated at Ser 780 and 807/811. The inhibitors of the complex, Cip1/p21 and Kip1/p27, increased at the protein level. On the other hand, Northern blotting showed that artepillin C did not affect the expression of Kip1/p27 mRNA. According to the experiments using isogenic human colorectal carcinoma cell lines, artepillin C failed to induce G(0)/G(1) arrest in the Cip1/p21-deleted HCT116 cells, but not in the wild-type HCT116 cells. Artepillin C appears to prevent colon cancer through the induction of cell-cycle arrest by stimulating the expression of Cip1/p21 and to be a useful chemopreventing factor in colon carcinogenesis.

Blotting, Northern↗

Use of propolis and ultragriseofulvin to inhibit aflatoxigenic fungi.

Propolis ethanolic extract (PEE) at 3 and 4 g/L and ultragriseofulvin (UG) at 0.75 and 1 g/L reduced the percentage of conidia germination in two Aspergillus flavus isolates. PEE at 1-4 g/L decreased the mycelial dry mass of A. flavus isolates by 11-80%, and aflatoxin B1 production by 34-100%. UG concentrations of 0.25-1 g/L reduced the growth and aflatoxin B1 production of the isolates by 16-88 and 48-98%, respectively. Any increase in PEE and UG concentration was accompanied by a clear decrease in the per cent conidia germination, growth and aflatoxin B1 production. At equal concentration, UG was about 4-times more effective than PEE.

Aflatoxin B1↗

Immunomodulatory action of propolis: IV. Prophylactic activity against gram-negative infections and adjuvant effect of the water-soluble derivative.

The efficacy of the water-soluble derivative (WSD) of natural propolis (bee glue) was examined for augmentation of host resistance against experimental infections caused by Gram-negative pathogens (Klebsiella pneumoniae, Proteus vulgaris, Escherichia coli, Pseudomonas aeruginosa). The substance was found to induce significant non-specific protection, but did not inhibit the in vitro growth of the same strains. Pretreatment with WSD prior to the standard scheme for tumour necrosis factor (TNF) induction (BCG and two weeks later lipopolysaccharide (LPS)) provoked an interval-dependent reduction in the lytic capacity of serum against L 929 target cells. The replacement of the triggering or priming signal with WSD markedly increased TNF production. In vivo administration of WSD led to a rapid and route-dependent change in the alternative complement pathway haemolysis. The alteration in C1q complement component and total protein synthesis, and also in nitroblue tetrazolium reduction, suggests that macrophage activation makes a major contribution to the capacity of WSD to prevent infections.

Adjuvants, Immunologic↗

Immunomodulatory action of propolis. VI. Influence of a water soluble derivative on complement activity in vivo.

The water soluble derivative (WSD) of propolis in a dose of 150 mg/kg was administered intravenously (i.v.), intraperitoneally (i.p.) and orally (p.o.) to mice. The alteration of serum alternative pathway (AP) complement level was observed. The WSD also influenced the process of acute inflammation provoked by zymosan in mice. The effect was strongly dependent on the route of WSD administration.

Adjuvants, Immunologic↗

Immunomodulatory action of propolis. V. Anticomplementary activity of a water-soluble derivative.

The effect of a water-soluble derivative (WSD) of propolis on the classical pathway (CP) and the alternative (AP) complement activity has been investigated. The in vitro experiments show that WSD inhibits both pathways and the effect depends on the source of complement. The suppression of complement-mediated haemolysis proves to be time- and temperature-related. High WSD concentrations cause direct damage of the target erythrocytes. The estimation of C3-residual activity indicates that the preparation diminishes C3 functional activity.

Animals↗

Redox intermediates of flavonoids and caffeic acid esters from propolis: an EPR spectroscopy and cyclic voltammetry study.

The redox properties of flavonoids: chrysin (1), tectochrysin (2), galangin (3), isalpinin (4), pinostrobin (5), pinobanksin (6), pinobanksin-3-acetate (7), and of caffeic acid ester (8) and diacetylcaffeic acid ester (9), all isolated from propolis, were investigated by cyclic voltammetry in acetonitrile. The choice of aprotic solvent lowered the reactivity of the radical intermediates and made possible to identify redox steps and intermediates not detected so far. The oxidation potentials (vs. saturated calomel electrode) of the investigated compounds were in the region of 1.5 V for 3 and 4; 1.9 V for 1, 2, and 5; 2.0 V for 6 and 7; 1.29 V for 8; and 2.3 V for 9. These oxidation potentials were mainly influenced by the presence of a double bond in 2,3-position and substituent R1 in position 3. Comparison with our earlier data revealed that flavonoids, 1-4, and caffeic acid ester 8 with lower oxidation potentials showed the maximal lipid antioxidant activity, whereas those with higher potentials (5, 6, 7, and 9) are less active. On reduction of 1-9 several one-electron-steps were typically observed in the potential regions: -1.5 V, -1.8 V, and -2 V. where in simultaneous EPR experiments anion radicals of 1 and 3 were observed with the center of unpaired spin density on ring A. Upon oxidation of flavonoids 1-4 carbonyl carbon-centered radicals, .C(O)R, were identified as consecutive products using the EPR spin trapping technique.

Antioxidants↗

Antitumor, hematostimulative and radioprotective action of water-soluble derivative of propolis (WSDP).

Several studies suggest that dietary supplementation with antioxidant can influence the response to chemotherapy as well as the development of adverse side effects caused by treatment with chemotherapeutic agents. Using CBA mouse model, we investigated a clinically potential use of a water-soluble derivative of propolis (WSDP) in the treatment of various cytopenias induced by radiation and/or chemotherapy. Also, the antimetastatic efficiency of WSDP given intraperitoneally alone or in combination with chemotherapeutic agents and their effects on the blood leukocytes count as well as on hematopoiesis were studied. Tumor was a transplantable mammary carcinoma (MCa) of CBA mouse. Metastases in the lung were generated by injecting viable tumor cells intravenously (iv). WSDP (50 or 150 mg/kg) exerted a significant antimetastatic effect (P < 0.001) when given either before or after tumor cell inoculation. In combined treatment WSDP and Epirubicin profoundly inhibited metastasis formation; this synergistic effect is maximal when Epirubicin and WSDP were administrated after tumor cell inoculation. Positive outcome of combined treatment with WSDP and Epirubicin was also found regarding the number of red and white blood cells in peripheral blood while in mice treated with Epirubicin alone the significant drop in all hematological parameters was noticed on day 13 after tumor cell inoculation. Furthermore, when WSDP (50 mg/kg) was given perorally (po) for 20 consecutive days an increased number of exogenous CFUs was found in treated mice. WSDP given either for 20 or 40 days increased cellularity of hematopoietic tissue and the number of leucocytes in peripheral blood; prolonged treatment with WSDP also elevated myeloid and megakaryocytic types of CFUs. To conclude, these findings indicate that the combination of WSDP with chemotherapeutics could increase the antimetastatic potential of chemotherapeutic agents; these findings suggest the benefits of potential clinical trials using WSDP combined with chemotherapeutic agents in order to maximize their antitumor activity and minimize postchemotherapeutic or radiotherapeutic deteriorated reactions.

Administration, Oral↗

Apoptosis of human melanoma cells induced by the novel compounds propolin A and propolin B from Taiwenese propolis.

We recently demonstrated that two new prenylflavanones, propolin A and propolin B, isolated and characterized from Taiwanese propolis, induced cytotoxicity effect in human melanoma A2058 cells and shows a strong capability to scavenge free radicals. In this study, propolin A effectively induced a cytotoxic effect on five different cancer cell lines. Similar results were obtained for propolin B. DNA flow cytometric analysis and DNA fragmentation ladder indicated that propolin A and propolin B actively induced apoptosis in A2058 cells. To address the mechanism of the apoptosis effect of propolin A and propolin B, we evaluated the apoptosis-related proteins in A2058 cells. The levels of procaspase-8, Bid, procaspase-3, DFF45, and PARP were decreased in dose- and time course-dependent manners. Furthermore, also found propolin A and propolin B was capable of releasing cytochrome c from mitochondria to cytosol. The findings suggest that propolin A and propolin B may activate a mitochondria-mediated apoptosis pathway. On the other hand, our data show that propolin B inhibitied xanthine oxidase activity more efficiently than propolin A or CAPE. However, CAPE suppressed ROS-induced DNA strand breakage more efficiently than propolin A or propolin B. All these results indicated that propolin A and propolin B may trigger apoptosis of A2058 cells through mitochondria-dependent pathways and also shown that propolin A and propolin B were strong antioxidants.

Apoptosis↗

New polyisoprenylated benzophenones from Venezuelan propolis.

Two new polyisoprenylated benzophenones, 18-ethyloxy-17-hydroxy-17,18-dihydroscrobiculatone A and 18-ethyloxy-17-hydroxy-17,18-dihydroscrobiculatone B, together with the known scrobiculatones A and B, were isolated from Venezuelan propolis. The scrobiculatones A and B showed significant antibacterial activity and moderate toxicity to Artemia salina nauplii.

Animals↗