프로폴리스는 강력한 항산화 활성특성을 갖는 물질이다.이 연구에서는 이 활성특성을 신체의 장내에서 효과를 볼 수 있는지 를 실험하였다. 에틸아세테이트로 추출한 브라질 프로폴리스의 페놀은 Artepillin C 을 포함한 여러가지 성분들을 함유한다. 이 Artepillin C를 첨가한 세포를 산소에 노출시키었을 때 산화에 의한 손상이 억제된다. Artepillin C는 생물학적으로 이용 가능한 항산화 방지제이다.

Kazuo Shimizua Shimizu , Hitoshi Ashidaa, Yukinaga Matsuura b, Kazuki Kanazawaa, Abstract Propolis has strong antioxidative activity. We investigated here whether this activity was available in intestinal Caco-2 and hepatic HepG2 cells. Phenolics in Brazilian propolis, extracted with ethyl acetate after the removal of resin and wax with 90% methanol, included artepillin C at 21 mmol/100 g, p-coumaric acid and cinnamic acid relatives 24 mmol, kaempferol and its derivatives 9.4 mmol, naringenin 2.8 mmol, isosakuranetin 0.9 mmol, chrysin at 0.8 mmol/100 g, and several minor components. When the extract was added to the apical side of Caco-2 monolayers, artepillin C was specifically incorporated into the cells and released to the basolateral side mostly without conjugation. Then, artepillin C was added to HepG2 cells and exposed to reactive oxygens. Artepillin C prevented oxidative damage dose-dependently, and suppressed lipid peroxidation evaluated with thiobarbituric acid reactive substances by 16% and the formation of 8-hydroxy-2′- deoxyguanosine in DNA by 36% at a concentration of 20 μM. Artepillin C is a bioavailable antioxidant.

Artepillin C는 항 종양 활성을 가지는 브라질 프로폴리스의 활성성분이다. 이 연구의 결과는 브라질 프로폴리스의 유효 성분인 Artepillin C가 정상 림프구에의 제한 억제 효과와 항백혈병 효과가 있음을 보여준다.

Kimoto T1, Aga M, Hino K, Koya-Miyata S, Yamamoto Y, Micallef MJ, Hanaya T, Arai S, Ikeda M, Kurimoto M. Abstract Artepillin C (3,5-diprenyl-4-hydroxycinnamic acid) is an active ingredient of Brazilian propolis that possesses anti-tumor activity. When Artepillin C was applied to human leukemia cell lines of different phenotypes, namely, lymphocytic leukemia (7 cell lines of T-cell, 5 cell lines of B-cell), myeloid and monocytic leukemia and non-lymphoid non-myeloid leukemia cell lines in vitro, Artepillin C exhibited potent cytocidal effects and induced marked levels of apoptosis in all the cell lines. The most potent effects were observed in the T-cell lines. Apoptotic bodies and DNA fragmentation were induced in the cell lines after exposure to Artepillin C. DNA synthesis in the leukemia cells was clearly inhibited and disintegration of the cells was confirmed microscopically. Apoptosis of the leukemia cells may be partially associated with enhanced y y y Fas antigen expression and loss of mitochondrial membrane potential. In contrast, although Artepillin C inhibited the growth of pokeweed mitogen (PWM)-stimulated normal blood lymphocytes, it was not cytocidal to normal unstimulated lymphocytes. These results suggested that Artepillin C, an active ingredient of Brazilian propolis, has anti-leukemic effects with limited inhibitory effects on normal lymphocytes.

Artepillin C를 브라질 프로폴리스로부터 추출하였다. Artepillin C는 300.4의 분자량을 가지며, 항균 활성특성을 갖고 있다. Artepillin C는 시험관내 및 생체내에서 인간과 쥐의 악성종양 세포에 적용했을 때, 종양세포에 대한 독성효과와 종양세포의 증식을 명확하게 억제하는 것으로 나타냈다. Artepillin C가 MTT분석법에 의해서 고형종양 및 백혈병 세포에 손상을 일으키 는 것이 관찰을 통하여 밝혀졌다. 인간의 종양세포가 실험용 쥐에 이식되었을 때, Artepillin C의 종양세포에 대한 독성효과 는 암종 및 악성 흑색종에서 가장 현저하게 나타났다. Artepillin C의 주사량을 500㎍ 정도로 종양내 3회 주사한 후 일주일 동안의 관찰을 통하여 세포자멸 및 종양세포의 다량의 괴사를 확인하였다. 이러한 결과는 Artepillin C가 면역체계를 활성화 하고 직접적인 항종양 활성특성을 가지고 있음을 나타낸다.

Kimoto T1, Arai S, Kohguchi M, Aga M, Nomura Y, Micallef MJ, Kurimoto M, Mito K. Abstract Artepillin C was extracted from Brazilian propolis. Artepillin C (3,5-diprenyl-4-hydroxycinnamic acid) has a molecular weight of 300.40 and possesses antibacterial activity. When artepillin C was applied to human and murine malignant tumor cells in vitro and in vivo, artepillin C exhibited a cytotoxic effect and the growth of tumor cells was clearly inhibited. The artepillin C was found to cause significant damage to solid tumor and leukemic cells by the MTT assay, DNA synthesis assay, and morphological observation in vitro. When xenografts of human tumor cells were transplanted into nude mice, the cytotoxic effects of artepillin C were most noticeable in carcinoma and malignant melanoma. Apoptosis, abortive mitosis mitosis, and massive necrosis combined were identified by histological observation after intratumor injection of 500 microg of artepillin C three times a week. In addition to suppression of tumor growth, there was an increase in the ratio of CD4/CD8 T cells, and in the total number of helper T cells. These findings indicate that artepillin C activates the immune system, and possesses direct antitumor activity.

*프로폴리스에서 추출한 phenolic 화합물은 헬리코박터균의 필수효소 “HpPDF”의 생성을 억제한다. *다른 시험관 시험에 의하면 프로폴리스 안에 포함되있는 25개의 혼합물중에 절반에 헬로코박터균에게 효과가 있는것으로 밝혀졌다.

Journal title: Exploring alternative treatments for Helicobacter pylori infection Journal Publication: World Journal of Gastroenterology Journal text: *“A collection of phenolic compounds derived from propolis were evaluated for enzyme inhibition against H. pylori peptide deformylase (HpPDF)” “which is essential for H. pylori survival,” * “In another in vitro study, 25 identified constituents of Brazilian propolis were tested for anti-H. pylori activity; 50% of them were active.”

*프로폴리스에서 추출한 phenolic 화합물은 헬리코박터균의 필수효소 “HpPDF”의 생성을 억제한다. *다른 시험관 시험에 의하면 프로폴리스 안에 포함되있는 25개의 혼합물중에 절반에 헬로코박터균에게 효과가 있는것으로 밝혀졌다.

*“A collection of phenolic compounds derived from propolis were evaluated for enzyme inhibition against H. pylori peptide deformylase (HpPDF)” “which is essential for H. pylori survival,” * “In another in vitro study, 25 identified constituents of Brazilian propolis were tested for anti-H. pylori activity; 50% of them were active.”

플로폴리스에는 약 29개의phenolic 화합물이 있는데 이들은 항산화 효과를 가지고 있다.

Journal title: Effect of Ethanol/Water Solvents on Phenolic Profiles and Antioxidant Properties of Beijing Propolis Extracts. Journal Publication: Evid Based Complement Alternat Med Journal text: 길어서 생략 Journal online: http://www.ncbi.nlm.nih.gov/pubmed/26351514

프로폴리스에 포함되 있는 많은 성분들은 (예를들어chrysin and CAPE (caffeic acid phenethyl ester)는 대장암세포에 대한 항암효과가 있었다. 또한 항염효과도 관찰이 되었다.

“New Zealand propolis is a "European" type propolis obtained by honey bees mainly from exudates of poplar. European type propolis is known to have anti-inflammatory and anti-cancer properties and this activity has been attributed to some of the main constituents such as chrysin and CAPE (caffeic acid phenethyl ester). As part of our studies on how New Zealand propolis might benefit gastro-intestinal health, we carried out in vitro bioactivity-guided fractionation of "Bio30™" propolis using both anti-inflammatory (TNF-α, COX-1, COX-2) and anti-colon cancer (DLD-1 colon cancer cell viability) assays; and determined the phenolic compounds responsible for the activity. The New Zealand wax-free Bio30™ propolis tincture solids had very high levels of the dihydroflavonoids pinocembrin and pinobanksin-3-O-acetate, and high levels of the dimethylallyl, benzyl and 3-methyl-3-butenyl caffeates relative to CAPE. The DLD-1 assays identified strong anti-proliferative activity associated with these components as well chrysin, galangin and CAPE and a number of lesser known or lower concentration compounds including benzyl ferulate, benzyl isoferulate, pinostrobin, 5-phenylpenta-2,4-dienoic acid and tectochrysin. The phenolic compounds pinocembrin, pinobanksin-3-O-acetate, tectochrysin, dimethylallyl caffeate, 3-methyl-3-butenyl caffeate, benzyl ferulate and benzyl isoferulate also showed good broad spectrum activity in anti-proliferative assays against three other gastro-intestinal cancer cell lines; HCT-116 colon carcinoma, KYSE-30 oesophageal squamous cancer, and NCI-N87 gastric carcinoma. Activity is also observed in anti-inflammatory assays although it appears to be limited to one of the first cytokines in the inflammatory cascade, TNF-α.”

말레이시아산과 브라질산 프로폴리스안에서 추출된 ethanolic화합물은 농도에 따라 피부결합조직에 대한 궁극적 상처치료효과를 도와준다.

Journal title: The effects of Malaysian propolis and Brazilian red propolis on connective tissue fibroblasts in the wound healing process. Journal Publication: BMC Complement Altern Med Journal text: Abstract BACKGROUND: To evaluate and compare the effects of ethanolic extracts of Malaysian propolis and Brazilian red propolis at different concentrations on the migration and proliferation of fibroblast cells. CONCLUSION: Malaysian and Brazilian red propolis show potential to assist in wound healing, depending on their concentration. Journal online: http://www.ncbi.nlm.nih.gov/pubmed/26303848