著者

Bahar Ahmed Adnan Jathlan Al-Rehaily Tawfeq Abdullah Al-Howiriny Khaled Abdelatee El-Sayed Mohammad Shamim Ahmad

出版者

公益社団法人日本薬学会

雑誌

Biological and Pharmaceutical Bulletin (ISSN:09186158)

巻号頁・発行日

vol.26, no.4, pp.462-467, 2003 (Released:2003-04-01)

参考文献数

17

被引用文献数

21 48

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Five iridoid glycosides, including the two new compounds scropolioside-D2 (1) and harpagoside-B (2), were isolated from the aerial parts of Scrophularia deserti DEL (Scrophulariaceae). Their structures were elucidated on the basis of spectral data to be 6-O-[2″,4″-di-O-acetyl-3″-O-trans-cinnamoyl)-α-L-rhamnopyranosyl]-8α-hydroxymethyl-1α,5β,6α,7α,9β-pentahydro-7(8)-epoxy-2-oxaind-3-ene-1-O-β-D-glucopyranoside-6′-O-acetate (1) and 5-O-β-hydroxy-8-O-β-trans-cinnamoyl-8α-methyl-1,6,7,9-tetrahydro-2-oxaind-3-ene-1-O-β-D-glucopyranoside (2), respectively. In addition, three more iridoid glycosides, scropolioside-D (3), koelzioside (4), and 8-O-acetyl-harpagide (5), were also isolated and characterized from this source. The biological activity and the structure activity relationship of the compounds were also studied, and scropolioside-D (3) and harpagoside-B (2) were found to possess significant antidiabetic and antiinflammatory activity, respectively.

著者

Seong Soo Joo Yeong Min Yoo Byung Woo Ahn Sang Yun Nam Yun-Bae Kim Kwang Woo Hwang Do Ik Lee

出版者

公益社団法人日本薬学会

雑誌

Biological and Pharmaceutical Bulletin (ISSN:09186158)

巻号頁・発行日

vol.31, no.7, pp.1392-1396, 2008-07-01 (Released:2008-07-01)

参考文献数

26

被引用文献数

26 77

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Considering the importance of inflammation and apoptosis in neurodegenerative conditions, the potential suppressive effects of the Rg3, a by-product obtained during the steaming of red ginseng, may indicate that Rg3 could provide a beneficial therapeutic approach to treating or preventing neurodegenerative disease. We investigated the effect of Rg3 on Aβ42-mediated microglial activation and inflammation-mediated neurotoxicity in murine BV-2 microglial and Neuro-2a neuroblastoma cells, respectively. Rg3 effectively reduced inflammatory cytokine expression in Aβ42-treated BV-2, and inhibited the binding of NF-κB p65 to its DNA consensus sequences, and significantly reduced the expression of TNF-α in activated microglia. Pretreatment with Rg3 increased the survival rate of Neuro-2a exposed to TNF-α. These observations suggest that Rg3 reduced neurotoxicity by inhibiting chronic inflammation through the suppression of activated microglia. In addition, the expression of pro-inflammatory cytokines in BV-2 stimulated by Aβ42 was decreased but not eliminated by Rg3 when binding to the macrophage scavenger receptor type A (MSRA) was blocked with fucoidan. This implies that the inflammatory response may not be exclusively triggered via MSRA. More interestingly, iNOS was almost completely inhibited in the presence of Rg3 when MSRA binding was blocked with fucoidan. Moreover, Rg3 increased the expression of MSRA in BV-2 transfected with siRNA targeting MSRA mRNA, and this increased MSRA expression may play a role in the phagocytosis of Aβ42 peptides. Our results indicate that inhibition of the inflammatory repertoire of microglia, neuroprotection, and increased MSRA expression induced by Rg3 may at least partly explain its therapeutic effects in chronic neurodegenerative diseases.

著者

Makoto Kajizono Hikaru Sada Yuhko Sugiura Yoshihiko Soga Yoshihisa Kitamura Junji Matsuoka Toshiaki Sendo

出版者

公益社団法人日本薬学会

雑誌

Biological and Pharmaceutical Bulletin (ISSN:09186158)

巻号頁・発行日

vol.38, no.12, pp.1850-1855, 2015-12-01 (Released:2015-12-01)

参考文献数

46

被引用文献数

3 47

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Zoledronic acid and denosumab are two antiresorptive drugs currently in use for treating osteoporosis. They have different mechanisms of action, but both have been shown to delay the onset of skeletal-related events in patients with advanced cancer. However, medication-related osteonecrosis of the jaw (MRONJ) has been reported in cancer patients treated with zoledronic acid or denosumab. We studied 155 patients with several types of advanced cancer who were treated with zoledronic acid or denosumab in our hospital during the period from April 2010 through March 2013. Thirteen of these 155 patients (8.4%) developed MRONJ. MRONJ development was significantly associated with the number of zoledronic acid or denosumab infusions (p<0.001) and the duration of zoledronic acid or denosumab therapy (p<0.001). Logistic regression analysis showed that diabetes [odds ratio (OR)=6.699, 95% confidence interval (CI), 1.435–31.277, p=0.016], anemia [OR=14.559, 95% CI, 2.161–98.069, p=0.006], and pus discharge [OR=6.491, 95% CI, 1.514–27.835, p=0.012] significantly increased the risk of developing MRONJ. However, the risk of MRONJ was significantly lower [OR=0.137, 95% CI, 0.020–0.944, p=0.043] when patients received periodical dentistry maintenance. Diabetes, anemia, and pus discharge may also play roles in its development. These findings suggest that the active inclusion of dentistry maintenance in bisphosphonate or denosumab treatment of cancer patients can reduce MRONJ development.

著者

Ryogo Umetsu Junko Abe Natsumi Ueda Yamato Kato Toshinobu Matsui Yoko Nakayama Yasutomi Kinosada Mitsuhiro Nakamura

出版者

公益社団法人日本薬学会

雑誌

Biological and Pharmaceutical Bulletin (ISSN:09186158)

巻号頁・発行日

vol.38, no.11, pp.1689-1699, 2015-11-01 (Released:2015-11-01)

参考文献数

38

被引用文献数

1 23

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Selective serotonin reuptake inhibitors (SSRIs) are prescribed for the treatment of depression worldwide. SSRIs are suspected to increase the risk of suicidal ideation and behavior (suicidality) in children, adolescents, and young adults. We examined the association between SSRI therapy and suicidality by applying a logistic regression model to age-stratified data from the Food and Drug Administration (FDA) Adverse Event Reporting System database. We attempted to mitigate the effect of patient-related factors by data subsetting. We selected case reports for SSRIs as referred to in the World Health Organization Anatomical Therapeutic Chemical classification code N06AB. The association between SSRIs and “suicidal events” or “self-harm events” was calculated as a reporting odds ratio (ROR) and adjusted for covariates by logistic regression. For subjects <18 years old (y.o.) the adjusted RORs (95% confidence interval) of SSRI therapy with suicidal events were 9.58 (8.97–10.23) in the whole data analysis and 4.64 (4.15–5.19) in the subset analysis; those with self-harm events were 31.40 (27.71–35.58) and 16.31 (13.12–20.29), respectively. Although the adjusted RORs were lower in the subset analyses than in the whole data analyses, both analyses indicated associations between SSRI treatment and suicidal and self-harm events. In both analyses these associations were stronger in the <18 y.o. group than other age groups. Children and adolescents should be closely monitored for the occurrence of suicidality when they are prescribed SSRIs. In addition, we found that data subsetting might mitigate the effect of an intrinsic risk among patients taking the suspected drug.

著者

Quan Feng Liu Jang Ho Lee Young-Mi Kim Soojin Lee Yoon Ki Hong Soojin Hwang Youngje Oh Kyungho Lee Hye Sup Yun Im-Soon Lee Songhee Jeon Young-Won Chin Byung-Soo Koo Kyoung Sang Cho

出版者

公益社団法人日本薬学会

雑誌

Biological and Pharmaceutical Bulletin (ISSN:09186158)

巻号頁・発行日

pp.b15-00459, (Released:2015-10-10)

参考文献数

58

被引用文献数

3 37

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Alzheimer’s disease (AD) is the most common neurodegenerative disorder, characterized by progressive neuronal loss with amyloid β-peptide (Aβ) plaques. Despite several drugs currently used to treat AD, their beneficial effects on AD progress remains under debate. Here, we established a rapid in vivo screening system using Drosophila AD models to assess the neuroprotective activities of medicinal plants that have been used in traditional Chinese medicine. Among 23 medicinal plants tested, the extracts from five plants, Coriandrum sativum, Nardostachys jatamansi, Polygonum multiflorum (P. multiflorum), Rehmannia glutinosa, and Sorbus commixta (S. commixta), showed protective effects against the Aβ42 neurotoxicity. We further characterized the neuroprotective activity of ethanol extracts from P. multiflorum and S. commixta. Aβ42-expressing flies that we used showed AD neurological phenotypes, such as decreased survival and motility and increased cell death and reactive oxygen species level. However, feeding these flies extracts from P. multiflorum or S. commixta showed strong suppression of such phenotypes. Similar results were observed in human cells, so that the treatment of P. multiflorum and S. commixta extracts increased the viability of Aβ-treated SH-SY5Y cells. Moreover, 2, 3, 5, 4'-tetrahydroxystilbene-2-O-β-D-glucoside, one of the main constituents of P. multiflorum, also showed similar protective activity against Aβ42 cytotoxicity in both Drosophila and human cells. Taken together, our results suggest that both P. multiflorum and S. commixta have therapeutic potential for the treatment of neurodegenerative diseases, such as AD.

著者

Hiroshi Fukasawa Madoka Nakagomi Naoko Yamagata Hiroshi Katsuki Kohichi Kawahara Kazuyoshi Kitaoka Takami Miki Koichi Shudo

出版者

公益社団法人日本薬学会

雑誌

Biological and Pharmaceutical Bulletin (ISSN:09186158)

巻号頁・発行日

vol.35, no.8, pp.1206-1212, 2012-08-01 (Released:2012-08-01)

参考文献数

69

被引用文献数

17 75

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Tamibarotene (Am80), a synthetic retinoid approved in Japan for treatment of acute promyelocytic leukemia (APL), is a retinoic acid receptor (RAR) agonist with high specificity for RARα and RARβ over RARγ. Temporarily and spatially specific expression of RARs suggests their pivotal roles in the adult brain. Am80 is considered to be a promising candidate drug for treatment of Alzheimer’s disease (AD) because of its transcriptional controls of multiple target genes involved in etiology and pathology of AD. In APP23 AD model mice, administration of Am80 decreased the deposition of insoluble amyloid-β(42). In senescence-accelerated mice (SAMP8), Am80 ameliorated the decrease of cortical acetylcholine, as well as reducing anxiety in behavioral tests and improving the sleep deficit. Am80 also effected a significant improvement of memory in the rat scopolamine-induced memory deficit model. Like other retinoids, Am80 also has an immunomodulatory effect and reduces secretion of proinflammatory cytokines and chemokines by astrocytes and microglia surrounding amyloid-β plaques. In a rat experimental autoimmune encephalomyelitis model, Am80 reduced inflammatory cytokines and showed significant efficacy. Retinoids also promote differentiation of neural stem cells, and Am80 improved the recovery of spinal cord-injured rats. Am80 may also improve vascular factors involved in onset and/or progression of AD. Am80 has been in clinical use for treatment of APL in Japan since 2005, and has been reported to have fewer side effects than other retinoids. We have recently started a clinical study to evaluate the efficacy and safety of Am80 for the treatment of Alzheimer’s disease.

著者

Noriaki Nagai Atsushi Takeda Yuri Itanami Yoshimasa Ito

出版者

公益社団法人日本薬学会

雑誌

Biological and Pharmaceutical Bulletin (ISSN:09186158)

巻号頁・発行日

vol.35, no.12, pp.2230-2237, 2012-12-01 (Released:2012-12-01)

参考文献数

42

被引用文献数

3 8

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Non-steroidal anti-inflammatory drugs (NSAIDs) comprise one of the most frequently used classes of medicines in the world; however, NSAIDs have significant side effects, such as gastroenteropathy, and rheumatoid arthritis patients taking NSAIDs are more susceptible to NSAID-induced gastric lesions as compared to patients with other diseases. In Asian countries, loxoprofen has been used clinically for many years as a standard NSAID. We demonstrate the preventive effect of the co-administration of water containing magnesium ion (magnesium water, 1–200 µg/kg) on the ulcerogenic response to loxoprofen in adjuvant-induced arthritis (AA) rats. Oral administration of loxoprofen (100 mg/kg) caused hemorrhagic lesions in the gastric mucosa of AA rats 14 d after adjuvant injection, and, following loxoprofen administration, the lesion score of AA rats was significantly higher than that of normal rats. The expression of inducible nitric oxide synthase (iNOS) mRNA and nitric oxide (NO) production in the gastric mucosa of AA rats were also increased by the administration of loxoprofen, and the increase in lesions and NO were prevented by the administration of aminoguanidine, an iNOS inhibitor. The co-administration of magnesium water decreased the ulcerogenic response to loxoprofen in AA rats. In addition, the co-administration of magnesium water attenuated the increase in iNOS mRNA expression and NO production in AA rats receiving loxoprofen. These results suggest that the oral co-administration of magnesium water to AA rats has a potent preventive effect on the ulcerogenic response to loxoprofen, probably by inhibiting the rise in iNOS and NO levels in the gastric mucosa.

著者

Takayoshi Mamiya Takamasa Asanuma Mitsuo Kise Yukihiko Ito Aya Mizukuchi Hiromichi Aoto Makoto Ukai

出版者

公益社団法人日本薬学会

雑誌

Biological and Pharmaceutical Bulletin (ISSN:09186158)

巻号頁・発行日

vol.27, no.7, pp.1041-1045, 2004 (Released:2004-07-10)

参考文献数

21

被引用文献数

30 44

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We evaluated the effects of pre-germinated brown rice (hatsuga genmai, PGR) on learning and memory and compared them with those of polished rice or cornstarch. In mice that were fed pellets of polished rice or PGR for two weeks, the learning ability in the Morris water maze test was significantly enhanced compared with mice that were fed cornstarch pellets. In the Y-maze test, the intake of food pellets for two weeks failed to affect spontaneous alternation behavior. β-Amyloid25—35 (Aβ25—35: 3 nmol/mouse, i.c.v.) protein impaired spontaneous alternation behavior in mice that were fed pellets of cornstarch or polished rice. In contrast, PGR pellets prevented the Aβ25—35-induced impairment of spontaneous alternation behavior. These results suggest that polished rice and PGR have facilitating effects on spatial learning. In particular, it is surmised that PGR may prevent Alzheimer's disease associated with Aβ.

著者

Shigeyuki Ohta Sayaka Sakaguchi Yuki Kobayashi Norikazu Mizuno Kenji Tago Hiroshi Itoh

出版者

公益社団法人日本薬学会

雑誌

Biological and Pharmaceutical Bulletin (ISSN:09186158)

巻号頁・発行日

vol.38, no.4, pp.594-600, 2015-04-01 (Released:2015-04-01)

参考文献数

26

被引用文献数

1 24

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GPR56 is a member of the adhesion G protein-coupled receptor (GPCR) and is highly expressed in parts of tumor cells. The involvement of GPR56 in tumorigenesis has been reported. We generated agonistic monoclonal antibodies against human GPR56 and analyzed the action and signaling pathway of GPR56. The antibodies inhibited cell migration through the Gq and Rho pathway in human glioma U87-MG cells. Co-immunoprecipitation analysis indicated that the interaction between the GPR56 extracellular domain and transmembrane domain was potentiated by agonistic antibodies. These results demonstrated that functional antibodies are invaluable tools for GPCR research and should open a new avenue for therapeutic treatment of tumors.

著者

Manabu Murakami Hidetoshi Niwa Tetsuya Kushikata Hiroyuki Watanabe Kazuyoshi Hirota Kyoichi Ono Takayoshi Ohba

出版者

公益社団法人日本薬学会

雑誌

Biological and Pharmaceutical Bulletin (ISSN:09186158)

巻号頁・発行日

vol.37, no.5, pp.834-839, 2014-05-01 (Released:2014-05-01)

参考文献数

20

被引用文献数

7 34

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The effects of inhalation anesthesia (2% isoflurane, sevoflurane, or enflurane) and intraperitoneal anesthesia with pentobarbital (65 mg/kg) were compared in rats using an electrocardiogram (ECG) and determination of blood oxygen saturation (SPO2) levels. Following inhalation anesthesia, heart rate (HR) and SPO2 were acceptable while pentobarbital anesthesia decreased HR and SPO2 significantly. This indicates that inhalation anesthesia is more preferable than pentobarbital anesthesia when evaluating cardiovascular factors. Additionally, pentobarbital significantly increased HR variability (HRV), suggesting a regulatory effect of pentobarbital on the autonomic nervous system, and resulted in a decreased response of the baro-reflex system. Propranolol or atropine had limited effects on ECG recording following pentobarbital anesthesia. Taken together, these data suggest that inhalation anesthesia is suitable for conducting hemodynamic analyses in the rat.

著者

Young-Hoon Song Soo-Jin Jeong Hee-Young Kwon Bonglee Kim Sung-Hoon Kim Dong-Youl Yoo

出版者

公益社団法人日本薬学会

雑誌

Biological and Pharmaceutical Bulletin (ISSN:09186158)

巻号頁・発行日

vol.35, no.7, pp.1022-1028, 2012-07-01 (Released:2012-07-01)

参考文献数

33

被引用文献数

13 39

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Although ursolic acid isolated from Oldenlandia diffusa (Rubiaceae) was known to have anticancer activities in prostate, breast and liver cancers, the underlying mechanism of ursolic acid in ovarian cancer cells was not investigated so far. In the present study, the apoptotic mechanism of ursolic acid was elucidated in SK-OV-3 ovarian cancer cells by 2,3-bis(2-methoxy-4-nitro-5-sulphophenyl)-2H-tetrazolium-5-carboxanilide (XTT) assay, cell cycle analysis and Western blotting. Ursolic acid exerted cytotoxicity against SK-OV-3 and A2780 ovarian cancer cells with IC50 of ca. 50 and 65 µM, respectively. Apoptotic bodies were observed in ursolic acid treated SK-OV-3 cells. Also, ursolic acid significantly increased ethidium homodimer stained cells and sub-G1 apoptotic portion in SK-OV-3 cells. Consistently, Western blotting revealed that ursolic acid effectively cleaved poly(ADP-ribose) polymerase (PARP), caspase-9 and -3, suppressed the expression of survival genes such as c-Myc, Bcl-xL and astrocyte elevated gene (AEG)-1, and upregulated phosphorylation of extracellular signal-regulated kinase (ERK) in SK-OV-3 cells. Interestingly, ursolic acid suppressed β-catenin degradation as well as enhanced phosphorylation of glycogen synthase kinase 3 beta (GSK 3β). Furthermore, GSK 3β inhibitor SB216763 blocked the cleavages of caspase-3 and PARP induced by ursolic acid and proteosomal inhibitor MG132 disturbed down-regulation of β-catenin, activation of caspase-3 and decreased mitochondrial membrane potential (MMP) induced by ursolic acid in SK-OV-3 cells. Overall, our findings suggest that ursolic acid induces apoptosis via activation of caspase and phosphorylation of GSK 3β in SK-OV-3 cancer cells as a potent anti-cancer agent for ovarian cancer therapy.

著者

Kensuke Yamamura Junichi Kitagawa Masayuki Kurose Shinichiro Sugino Hanako Takatsuji Rahman Md Mostafeezur Hossain Md Zakir Yoshiaki Yamada

出版者

公益社団法人日本薬学会

雑誌

Biological and Pharmaceutical Bulletin (ISSN:09186158)

巻号頁・発行日

vol.33, no.11, pp.1786-1790, 2010-11-01 (Released:2010-11-01)

参考文献数

47

被引用文献数

14 39

---

Swallowing involves several motor processes such as bolus formation and intraoral transport of a food bolus (oral stage) and a series of visceral events that occur in a relatively fixed timed sequence but are to some degree modifiable (pharyngeal stage or swallow reflex). Reflecting the progressive aging of society, patients with swallowing disorders (i.e., dysphagia) are increasing. Therefore, there is expanding social demand for the development of better rehabilitation treatment of dysphagic patients. To date, many dysphagia diets have been developed and are available commercially to help bring back the pleasure of mealtimes to dysphagia patients. Texture modification of food to make the food bolus easier to swallow with less risk of aspiration is one of the important elements in dysphagia diets from the viewpoint of safety assurance. However, for the further development of dysphagia diets, new attempts based on new concepts are needed. One of the possible approaches is to develop dysphagia diets that facilitate swallow initiation. For this approach, an understanding of the mechanisms of swallow initiation and identification of factors that facilitate or suppress swallow initiation are important. In this review, we first summarize the neural mechanisms of swallowing and effects of taste and other inputs on swallow initiation based on data mainly obtained from experimental animals. Then we introduce a recently established technique for eliciting swallowing using electrical stimulation in humans and our ongoing studies using this technique.

著者

Kyung-Ah Jung Tae-Chul Song Daeseok Han In-Ho Kim Young-Eon Kim Chang-Ho Lee

出版者

公益社団法人日本薬学会

雑誌

Biological and Pharmaceutical Bulletin (ISSN:09186158)

巻号頁・発行日

vol.28, no.9, pp.1782-1785, 2005 (Released:2005-09-01)

参考文献数

27

被引用文献数

43 88

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It is currently accepted that the consumption of fruit-derived antioxidants such as vitamin C, carotenoids, and flavonoids provides a preventive effect against cardiovascular disease. The purpose of the present study was to investigate potential cardiovascular protective properties of aqueous and 70% ethanol extracts from kiwifruit by analyzing the antioxidative, antihypertensive, hypocholesterolemic, and fibrinolytic activities in vitro. Aqueous and 70% ethanol extracts at 50 mg/ml showed DPPH-radical scavenging activities of 72.31% and 70.75%, respectively. Total antioxidant activity in linoleic acid emulsion was 85—88% at 10 mg/ml and 96—98% at 50 mg/ml of kiwifruit extract. Inhibitory activities against angiogensin I-converting enzyme of kiwifruit extracts were 21—26% at 10 mg/ml and 46—49% at 50 mg/ml, and inhibitory activities on HMG-CoA reductase were 13—14% at 10 mg/ml and 19—30% at 50 mg/ml. Fibrinolytic activity of kiwifruit was also observed at a high concentration of 100 mg/ml in both aqueous and 70% EtOH extracts. Based on our results, kiwifruit have potential cardiovascular protective properties in vitro.

著者

Seong-Gyu Ko Seung-Hee Koh Chan-Yong Jun Chang-Gyu Nam Hyun-Su Bae Min-Kyu Shin

出版者

公益社団法人日本薬学会

雑誌

Biological and Pharmaceutical Bulletin (ISSN:09186158)

巻号頁・発行日

vol.27, no.10, pp.1604-1610, 2004 (Released:2004-10-01)

参考文献数

28

被引用文献数

25 56

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We performed this study to understand the molecular basis underlying the antitumor effects of Saussurea lappa, Pharbitis nil, Plantago asiatica and Taraxacum mongolicum, which have been used for herbal medicinal treatments against cancers in East Asia. We analyzed the effects of these medicinal herbs on proliferation and on expression of cell growth/apoptosis related molecules, with using an AGS gastric cancer cell line. The treatments of Saussurea lappa and Pharbitis nil dramatically reduced cell viabilities in a dose and time-dependent manner, but Plantago asiatica and Taraxacum mongolicum didn't. FACS analysis and Annexin V staining assay also showed that both Saussurea lappa and Pharbitis nil induce apoptotic cell death of AGS. Expression analyses via RT-PCR and Western blots revealed that Saussurea lappa, but not Pharbitis nil, increased expression of the p53 and its downstream effector p21Waf1, and that the both increased expression of apoptosis related Bax and cleavage of active caspase-3 protein. We also confirmed the translocation of Bax to mitochondria. Collectively, our data demonstrate that Saussurea lappa and Pharbitis nil induce growth inhibition and apoptosis of human gastric cancer cells, and these effects are correlated with down- and up-regulation of growth-regulating apoptotic and tumor suppressor genes, respectively.

著者

Tetsuo Watanabe Yuki Nakajima Tetsuya Konishi

出版者

公益社団法人日本薬学会

雑誌

Biological and Pharmaceutical Bulletin (ISSN:09186158)

巻号頁・発行日

vol.31, no.1, pp.111-117, 2008-01-01 (Released:2008-01-01)

参考文献数

40

被引用文献数

8 18

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Basidiomycetes-X (BDM-X) is a novel edible mushroom recently identified as a new fungi species and registered to the database of the NPO organization for International Patent Organism Depositing (IPOD) in the Industrial Technology Institute of Japan (PCT/JP2004/006418). In the present study, we examined anti-oxidant activity of hot water extract of this novel fungus both in vitro and in vivo together with Agaricus Blazei Murill (ABM), a commercially available medicinal mushroom, and other reference antioxidants. As results, the hot water extract of BDM-X showed more potent anti-oxidative actions compared with that of ABM, when evaluated by 1,1′-diphenyl-2-picrylhydrazyl (DPPH) scavenging activity, Ferric Reducing Potential (FRP), and also the inhibition of 2,2′-azobis(2-amidino-propane) dihydrochloride (AAPH)-induced lipid peroxidation of rat liver homogenates. Further, the protective activity of BDM-X extract towards lipopolysaccharide (LPS)-induced hepatic oxidative damage was compared with ABM and α-lipoic acid in the mice pre-administered with these antioxidants. It was revealed that all of these antioxidants inhibited the LPS-induced oxidative tissue damage but the hot water extract of BDM-X showed the strongest protection among them. For example, the dose for 50% inhibition of carbonyl formation in liver was 0.53 g dry weight/kg body weight/d for BDM-X and the value corresponded to 16 mmol of α-lipoic acid as an antioxidant reference/kg body weight/d.

著者

Katsuhiro YAMASAKI Masami NAKANO Takuya KAWAHATA Haruyo MORI Toru OTAKE Noboru UEDA Isao OISHI Rie INAMI Megumi YAMANE Miki NAKAMURA Hiroko MURATA Tsutomu NAKANISHI

出版者

公益社団法人日本薬学会

雑誌

Biological and Pharmaceutical Bulletin (ISSN:09186158)

巻号頁・発行日

vol.21, no.8, pp.829-833, 1998-08-15 (Released:2008-04-10)

参考文献数

14

被引用文献数

75 158

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The anti-HIV-1 activity of aromatic herbs in Labiatae was evaluated in vitro. Forty five extract from among 51 samples obtained from 46 herb species showed significant inhibitory effects against HIV-1 induced cytopathogenicity in MT-4 cells. In particular, the aqueous extracts of Melissa officinalis, a family of Mentha×piperita "grapefruit mint", Mentha×piperita var. crispa, Ocimum basilicum cv "cinnamon", Perilla frutescens var. crispa f.viridis, Prunella vulgaris subsp. asiatica and Satureja montana showed potent anti-HIV-1 activity (with an ED of 16μg/ml). The active components in the extract samples were found to be water-solubel polar substances, not nonpolar compounds such as essential oils. In addition, these aqueous extracts inhibited giant cell formation in co-culture of Molt-4 cels with and without HIV-1 infection and showed inhibitory activity against HIV-1 reverse transcriptase.

著者

Shuso Takeda

出版者

公益社団法人日本薬学会

雑誌

Biological and Pharmaceutical Bulletin (ISSN:09186158)

巻号頁・発行日

vol.37, no.9, pp.1435-1438, 2014-09-01 (Released:2014-09-01)

参考文献数

43

被引用文献数

4 19

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Δ9-Tetrahydrocannabinol (Δ9-THC), a biologically active constituent of marijuana, possesses a wide variety of pharmacological and toxicological effects (e.g., analgesia, hypotension, reduction of inflammation, and anti-cancer effects). Among Δ9-THC’s biological activities, its recognized anti-estrogenic activity has been the subject of investigations. Since Δ9-THC is used as both a drug of abuse (marijuana) and as a preventive therapeutic to treat pain and nausea in cancer patients undergoing chemotherapy in the United States and other countries (synthesized Δ9-THC; dronabinol), it is important to investigate the mechanistic basis underlying the anti-estrogenic activity of Δ9-THC. Since Δ9-THC has “no” binding potential for estrogen receptor α (ERα) which can be activated by estrogen (E2), the question of how Δ9-THC exerts its inhibitory effect on ERα is not resolved. We have recently reported that ERβ, a second type of ER, is involved in the Δ9-THC abrogation of E2/ERα-mediated transcriptional activity. Here we discuss the possible mechanism(s) of the Δ9-THC-mediated disruption of E2/ERα signaling by presenting our recent findings as well.

著者

Mamoru Tanaka Akihiro Tanaka Katsuya Suemaru Hiroaki Araki

出版者

公益社団法人日本薬学会

雑誌

Biological and Pharmaceutical Bulletin (ISSN:09186158)

巻号頁・発行日

vol.36, no.2, pp.222-227, 2013-02-01 (Released:2013-02-01)

参考文献数

23

被引用文献数

1 3

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Antithrombotic drugs have been increasingly used for treating ischemic cardiovascular diseases among the elderly in Japan. However, antithrombotic drugs are known to be risk factors for gastrointestinal injury. Therefore, we conducted a pharmacoepidemiologic study on patients receiving antithrombotic drugs to identify the risk factors for gastrointestinal injury. This retrospective case-control study included patients who were prescribed antithrombotic drugs at the Ehime University Hospital between April and September 2010. Of the 3271 patients who received antithrombotic drug therapy, 172 (5.3%) developed gastrointestinal injuries, including gastric ulcers, duodenal ulcers, and hemorrhagic gastrointestinal injuries. Further, the incidence of gastrointestinal injury was higher in patients with hypertension than in those without (p<0.0001). Multivariate adjusted odds ratios and 95% confidence intervals were calculated using stepwise logistic regression. The adjusted odds ratios for gastrointestinal injury were 1.56 (95% confidence interval 1.07–2.36) for hypertension, 1.70 (1.17–2.50) for low-dose aspirin, 2.77 (1.70–4.49) for clopidogrel, 1.95 (1.23–3.08) for warfarin, and 4.13 (2.88–5.95) for nonsteroidal anti-inflammatory drugs. On the other hand, the non-adjusted odds ratio for drug-associated gastrointestinal injury was 0.43 (0.20–0.84) for eicosapentaenoic acid (EPA). In addition, we found that patients aged 70 years or older were at increased risk of drug-associated gastrointestinal injury. These findings suggest that while many antithrombotic drugs are risk factors for gastrointestinal injury, EPA may be a safe option for suppressing or preventing gastrointestinal injury.

著者

Shuso Takeda Kentaro Yaji Kenji Matsumoto Toshiaki Amamoto Mitsuru Shindo Hironori Aramaki

出版者

公益社団法人日本薬学会

雑誌

Biological and Pharmaceutical Bulletin (ISSN:09186158)

巻号頁・発行日

vol.37, no.2, pp.331-334, 2014-02-01 (Released:2014-02-01)

参考文献数

13

被引用文献数

1 4

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Few studies have examined xanthocidin, a biotic isolated from Streptomyces xanthocidicus in 1966, because its supply is limited. Based on its chemical structure, xanthocidin has the potential to become a lead compound in the production of agrochemicals and anti-cancer drugs; however, it is unstable under both basic and acidic conditions. We recently established the total synthesis of xanthocidin using the FeCl3-mediated Nazarov reaction, and obtained two stable derivatives (#1 and #2). The results of the present study demonstrated that these derivatives exhibited the inhibitory activity of topoisomerase IIα, known as a molecular target for cancer chemotherapy, and this was attributed to the respective exo-methylene ketone group without DNA intercalation. The results obtained also suggest that these derivatives may have value as lead compounds in the synthesis of topoisomerase IIα inhibitors.

著者

Ryohei Aoyagi Megumi Funakoshi-Tago Yosuke Fujiwara Hiroomi Tamura

出版者

公益社団法人日本薬学会

雑誌

Biological and Pharmaceutical Bulletin (ISSN:09186158)

巻号頁・発行日

pp.b14-00378, (Released:2014-09-11)

参考文献数

24

被引用文献数

5 35

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Recent epidemiological studies showed that coffee consumption is associated with a lower risk of type 2 diabetes, presumably due to suppression of excess fat accumulation in adipocytes. However, the mechanism underlying the effect of coffee on adipocyte differentiation has not been well documented. To elucidate the mechanism, we investigated the effect of coffee on the differentiation of mouse preadipocyte 3T3-L1 cells. Coffee reduced the accumulation of lipids during adipocytic differentiation of 3T3-L1 cells. At 5% coffee, the accumulation of lipids decreased to half that of the control. Coffee also inhibited the expression of the peroxisome proliferator-activated receptor γ (PPARγ), a transcription factor controlling the differentiation of adipocytes. Furthermore, coffee reduced the expression of other differentiation marker genes, aP2, adiponectin, CCAAT-enhancer-binding protein α (C/EBPα), GLUT4, and lipoprotein lipase (LPL), during adipocyte differentiation. Major bioactive constituents in coffee extracts, such as caffeine, trigonelline, chlorogenic acid, and caffeic acid, showed no effect on PPARγ gene expression. The inhibitory activity was produced by the roasting of the coffee beans.