Abstract:Abstract. malignant melanoma (mm) is an aggressive chemoresistant skin cancer characterized by rapid metastasis and a poor prognosis. therefore, the development of innovative effective therapies is critical. mK615 is an extract from the Japanese apricot Prunus mume Sieb. Et Zucc (ume). at a neutral ph, it contains natural chemical substances such as triterpenoids that exert anti-neoplastic effects in several types of cancers. We found that in patients with advanced mm, mK615 dramatically suppressed the cutaneo… Show more
“…In addition, it is worthy of note that a range of concentrations (≤10 μg/ml) of Maesil extract employed in this study are likely to be physiologically and clinically rele- an extract of the Prunus mume, is able to relieve severe symptoms of patients with cancer when 6.5 g of MK615 was administered twice per day [12]. Based on this and other data, the effective concentrations (≤10 μg/ml) of Maesil extract used in this study are comparable to doses administrated in clinical and in vivo studies [12,23]. It is also noteworthy that an advantage of using whole extracts seems likely to appear unexpected efficacy caused by unknown compounds in the whole extracts.…”
Homotypic cell adhesion (homotypic aggregation) in activated monocytes plays a central role in physiological and pathological processes including inflammatory responses, differentiation and migration. The extract of the Prunus mume Sieb. et Zucc. fruit (Maesil) has potential benefits to human health; such as anti-viral, anti-microbial, and anti-cancer activities. Indeed, Maesil extract may modulate inflammatory responses via interference with homotypic aggregation in monocytes. In the present study, the molecular mechanisms underpinning the therapeutic efficacy of Maesil extract in inflammatory diseases were investigated. It was found that Maesil extract inhibited homotypic aggregation in lipopolysaccharide (LPS)-activated monocytes. This was mediated by reduction of nitric oxide (NO) production, partly via inhibition of inducible nitric oxide synthase (iNOS) expression in LPS-activated THP-1 cells. It was confirmed that NO inhibition is a key mechanism in Maesil induced blockade of monocyte aggregation through identification of reversal of this inhibitory effect by the NO-producing agent S-nitroso-N-acetyl penicillamine (SNAP). In addition, Maesil extract significantly attenuated LPS-induced IκB-α phosphorylation and NF-κB translocation into the nucleus. In conclusion, Maesil extract exerts anti-inflammatory effects via inhibition of homotypic aggregation of LPS-activated monocytes through mechanisms involving the suppression of NO production and NF-κB activity, suggesting Maesil extract as a potential therapeutic candidate for the prevention and treatment of chronic inflammatory diseases.
“…In addition, it is worthy of note that a range of concentrations (≤10 μg/ml) of Maesil extract employed in this study are likely to be physiologically and clinically rele- an extract of the Prunus mume, is able to relieve severe symptoms of patients with cancer when 6.5 g of MK615 was administered twice per day [12]. Based on this and other data, the effective concentrations (≤10 μg/ml) of Maesil extract used in this study are comparable to doses administrated in clinical and in vivo studies [12,23]. It is also noteworthy that an advantage of using whole extracts seems likely to appear unexpected efficacy caused by unknown compounds in the whole extracts.…”
Homotypic cell adhesion (homotypic aggregation) in activated monocytes plays a central role in physiological and pathological processes including inflammatory responses, differentiation and migration. The extract of the Prunus mume Sieb. et Zucc. fruit (Maesil) has potential benefits to human health; such as anti-viral, anti-microbial, and anti-cancer activities. Indeed, Maesil extract may modulate inflammatory responses via interference with homotypic aggregation in monocytes. In the present study, the molecular mechanisms underpinning the therapeutic efficacy of Maesil extract in inflammatory diseases were investigated. It was found that Maesil extract inhibited homotypic aggregation in lipopolysaccharide (LPS)-activated monocytes. This was mediated by reduction of nitric oxide (NO) production, partly via inhibition of inducible nitric oxide synthase (iNOS) expression in LPS-activated THP-1 cells. It was confirmed that NO inhibition is a key mechanism in Maesil induced blockade of monocyte aggregation through identification of reversal of this inhibitory effect by the NO-producing agent S-nitroso-N-acetyl penicillamine (SNAP). In addition, Maesil extract significantly attenuated LPS-induced IκB-α phosphorylation and NF-κB translocation into the nucleus. In conclusion, Maesil extract exerts anti-inflammatory effects via inhibition of homotypic aggregation of LPS-activated monocytes through mechanisms involving the suppression of NO production and NF-κB activity, suggesting Maesil extract as a potential therapeutic candidate for the prevention and treatment of chronic inflammatory diseases.
“…However, there has been little clinical data with regard to the effects of MK615 against cancer. One study with a small number of clinical cases showed that MK615 was useful for malignant melanoma [15] , and the clinical efficacy and safety of MK615 has been reported for patients with chronic liver disease [17] . However, the clinical benefit of MK615 for HCC patients has not been evaluated.…”
Section: Discussionmentioning
confidence: 99%
“…Although the activities underlying the antitumor effects have been reported to include the induction of apoptosis [5,8] , autophagy [12,16] and the suppression of aurora A kinase [9,11] , the exact mechanism(s) of action of MK615 are still being elucidated. A large amount of basic data regarding the effects of MK615 against cancer cells in vitro have been published [5][6][7][8][9][10][11][12][13][14][15][16] . However, there has been little clinical data with regard to the effects of MK615 against cancer.…”
Section: Discussionmentioning
confidence: 99%
“…It has been reported that MK615 inhibits cell growth and induces the death of several tumor cell lines [5][6][7] , including gastric cancer [5] , promyelocytic leukemia [5] , breast cancer [8] , pancreatic cancer [9] , HCC [10,11] , colon cancer [12] , esophageal cancer [13] , malignant melanoma [14,15] and lung cancer cells [16] . The activities underlying the anti-tumor effects of MK615 have been reported to include the induction of apoptosis [5,8] , autophagy [12,16] and the suppression of aurora A kinase [9,11] .…”
MK615, a compound extracted from the Japanese apricot "Prunus mume " has been reported to have in vitro anti-tumor activities against several cancer cell lines, including hepatocellular carcinoma (HCC). However, the clinical effects and feasibility of administering MK615 for patients with HCC were unknown. We experienced a case with advanced HCC for which MK615 was effective against both lymph node and pulmonary metastases. A 60-year-old female underwent surgical resection of a 9 cm HCC in the right lobe. The pathological diagnosis was moderately differentiated HCC with vascular invasion. The HCC recurred in the liver 8 mo after the surgery. Radiofrequency ablation and transarterial infusion chemotherapy were performed, but the recurrence was not controlled. One year after the intrahepatic recurrence, pulmonary and lymph metastasis appeared.Sorafenib was administered, but was not effective. Then, MK615 was administered as a final alternative therapy after informed consent was obtained from the patient. Three months later, her alpha-fetoprotein level decrease and both the lymph node and pulmonary metastases decreased in size. The patient has survived for more than 17 mo after the MK615 administration, and was in good condition. Although further investigations are necessary to clarify its safety and efficacy in humans, MK615 may be useful for the treatment of HCC, without serious adverse effects. Key words: MK615; Hepatocellular carcinoma; Japanese apricot; Prunus mume Core tip: We experienced a case with advanced hepatocellular carcinoma (HCC) for which MK615, a compound extracted from the Japanese apricot "Prunus mume " was effective against both lymph node and pulmonary metastases. MK615 was administered as a final alternative therapy. Three months later, her alpha-fetoprotein level decrease and both the lymph node and pulmonary metastases decreased in size. MK615 has been reported to have in vitro anti-tumor activities against several cancer cell lines, including HCC. Although further investigations are necessary to clarify its safety and efficacy in humans, MK615 may be useful for the treatment of HCC, without serious adverse effects.
“…It contains several triterpenoids and has been shown to exert an anti-neoplastic effect against human cancers, such as breast cancer, stomach cancer, hepatocellular carcinoma, colon cancer and malignant melanoma. The mechanisms responsible for the anti-neoplastic effects of MK615 include induction of apoptosis and autophagy, and suppression of Aurora A kinase in cancer cells (Nakagawa et al, 2007;Adachi et al, 2007;Okada et al, 2007;Mori et al, 2007;Matsushita et al, 2010).…”
Section: Anti-cancer Effects Of An Extract From Umementioning
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