1.Quercetin Relaxed the Smooth Muscle of Rabbit Penile Corpus Cavernosum by Activating the NO-cGMP Signaling Pathway.
Bo Ram CHOI ; Hye Kyung KIM ; Jong Kwan PARK
Natural Product Sciences 2017;23(3):169-174
The aim of this study was to investigate the effect and action mechanism of quercetin on penile corpus cavernosum smooth muscle (PCCSM). PCCSM precontracted with phenylephrine (Phe) was treated with four different concentrations of quercetin (10−7, 10−6, 10−5 and 10−4 M). PCCSM were preincubated with N-Nitro-L-arginine methyl ester hydrochloride (L-NAME) and 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one (ODQ) to block nitric oxide synthase and guanylate cyclase, respectively. The changes in PCCSM tension were recorded, and cyclic nucleotides in the perfusate were measured by radioimmunoassay. The interactions of quercetin with phosphodiesterase type 5 inhibitors (PDE5-Is) such as sildenafil, udenafil and mirodenafil, were also evaluated. PCCSM relaxation induced by quercetin occurred in a concentrationdependent manner. The application of quercetin to PCCSM pre-treated with L-NAME and ODQ significantly inhibited the relaxation. Quercetin significantly increased cGMP in the perfusate. Furthermore, quercetin enhanced PDE5-Is-induced relaxation of PCCSM. Quercetin relaxed the PCCSM by activating the NO-cGMP signaling pathway, and it may be a therapeutic candidate or an alternative treatment for patients with erectile dysfunction who do not completely respond to PDE5-Is.
Erectile Dysfunction
;
Guanylate Cyclase
;
Humans
;
Male
;
Muscle, Smooth*
;
NG-Nitroarginine Methyl Ester
;
Nitric Oxide Synthase
;
Nucleotides, Cyclic
;
Phenylephrine
;
Phosphodiesterase 5 Inhibitors
;
Quercetin*
;
Radioimmunoassay
;
Relaxation
;
Sildenafil Citrate
2.Inhibitory Activity of Cordyceps bassiana Extract on LPS-induced Inflammation in RAW 264.7 Cells by Suppressing NF-κB Activation.
Deok Hyo YOON ; Changwoo HAN ; Yuanying FANG ; Shankariah GUNDETI ; In Sook HAN LEE ; Won O SONG ; Ki Chul HWANG ; Tae Woong KIM ; Gi Ho SUNG ; Haeil PARK
Natural Product Sciences 2017;23(3):162-168
Cordyceps bassiana has long been used as an oriental medicine and reported to possess diverse biological activities. The fruiting bodies of Cordyceps bassiana was extracted with ethanol and then further fractionated with n-hexane, ethyl acetate, n-butanol and water. The butanol fraction from Cordyceps bassiana (CBBF) exhibited the most effective in anti-inflammatory activity in RAW 264.7 macrophages and the roles of CBBF on the anti-inflammation cascade in LPS-stimulated RAW 264.7 cells were studied. To investigate the mechanism by which CBBF inhibits NO, iNOS and COX-2, the activation of IκB and MAPKs in LPS-activated macrophage were examined. Our present results demonstrated that CBBF inhibits NO production and iNOS expression in LPS-stimulated RAW 264.7 macrophage cells, and these effects were mediated through the inhibition of IκB-α, JNK and p38 phosphorylation. Also, CBBF suppressed activation of MAPKs including p38 and SAPK/JNK. Furthermore, CBBF significantly suppressed LPS-induced intracellular ROS generation. Its inhibition on iNOS expression, together with its antioxidant activity, may support its anti-inflammatory activity. Thus Cordyceps bassiana can be used as a useful medicinal food or drug for further studies.
1-Butanol
;
Cordyceps*
;
Ethanol
;
Fruit
;
Inflammation*
;
Macrophages
;
Medicine, East Asian Traditional
;
Phosphorylation
;
RAW 264.7 Cells*
;
Water
3.Reserpine treatment activates AMP activated protein kinase (AMPK).
Rackhyun PARK ; Kang Il LEE ; Hyunju KIM ; Minsu JANG ; Thi Kim Quy HA ; Won Keun OH ; Junsoo PARK
Natural Product Sciences 2017;23(3):157-161
Reserpine is a well-known medicine for the treatment of hypertension, however the role of reserpine in cell signaling is not fully understood. Here, we report that reserpine treatment induces the phosphorylation of AMP activated protein kinase (AMPK) at threonine 172 (T172) in PC12 cells. Phosphorylation of AMPK T172 is regulated by upstream signaling molecules, and the increase of phospho-T172 indicates that AMPK is activated. When we examined the FOXO3a dependent transcription by using the FHRE-Luc reporter assay, reserpine treatment repressed the FHRE-Luc reporter activity in a dose dependent manner. Finally, we showed that reserpine treatment induced the phosphorylation of AMPK as well as cell death in MCF-7 cells. These results suggest that AMPK is a potential cellular target of reserpine.
AMP-Activated Protein Kinases*
;
Animals
;
Cell Death
;
Hypertension
;
MCF-7 Cells
;
PC12 Cells
;
Phosphorylation
;
Reserpine*
;
Threonine
4.New Azafluorenone Derivative and Antibacterial Activities of Alphonsea cylindrica Barks.
Munirah Abdul TALIP ; Saripah Salbiah Syed Abdul AZZIZ ; Chee Fah WONG ; Khalijah AWANG ; Humera NAZ ; Yuhanis Mhd BAKRI ; Mohamad Syahrizal AHMAD ; Marc LITAUDON
Natural Product Sciences 2017;23(3):151-156
A phytochemical study of Alphonsea cylindrica King (unreported) has led to the isolation of six alkaloids. The compounds were identified as kinabaline (1; azafluorenone alkaloid), muniranine (2), O-methylmoschatoline (3; oxoaporphine alkaloid), lysicamine (4), atherospermidine (5) and N-methylouregidione (6; 4, 5-dioxoaporphine alkaloid). The structures of the isolated compounds were determined based on the spectroscopic techniques and by comparison with data reported in the literature. Alkaloid 2 was isolated as a new derivative of azafluorenone while alkaloids 1, 3 - 6 were isolated for the first time from Alphonsea species. In addition, alkaloid 3 and 4 showed inhibition zone against Staphylococcus aureus, Pseudomonas aeruginosa and Bacillus cereus in disc diffusion test. The minimum inhibition concentration (MIC) values of lysicamine (4) against S. aureus, B. cereus and P. aeruginosa were found to be smaller than O-methylmoschatoline (3). Therefore, the reported antibacterial activity showed the potential of this plant as natural antibacterial agent and supported the documented traditional use of Alphonsea sp. in the treatment of diarrhea and fever.
Alkaloids
;
Bacillus cereus
;
Diarrhea
;
Diffusion
;
Fever
;
Plants
;
Pseudomonas aeruginosa
;
Staphylococcus aureus
5.Microbial Transformation of Two Prenylated Naringenins.
Natural Product Sciences 2017;23(4):306-309
Microbial transformation of (±)-6-(1,1-dimethylallyl)naringenin (6-DMAN, 1) and (±)-5-(O-prenyl) naringenin-4′,7-diacetate (5-O-PN, 2) was performed by using fungi. Scale-up fermentation studies with Mucor hiemalis, Cunninghamella elegans var. elegans, and Penicillium chrysogenum led to the isolation of five microbial metabolites. Chemical structures of the metabolites were determined by spectral analyses as (±)-8-prenylnaringenin (3), (2S)-5,4′-dihydroxy-7,8-[(R)-2-(1-hydroxy-1-methylethyl)-2,3-dihydrofurano]flavanone (4), (±)-5-(O-prenyl)naringenin-4′-acetate (5), (±)-naringenin-4′-acetate (6), and (±)-naringenin (7), of which 5 was identified as a new compound.
Cunninghamella
;
Fermentation
;
Fungi
;
Mucor
;
Penicillium chrysogenum
6.Protective Effects of Cinnamic Acid Derivatives on Gastric Lesion.
Sun Yi LEE ; In Young HWANG ; Choon Sik JEONG
Natural Product Sciences 2017;23(4):299-305
P-methoxycinnamic acid and 3,4,5-trimethoxycinnamic acid are the compounds found in Polygalae Radix, the root of Polygala tenuifolia Willdenow, and have been reported to have hepatoprotective and anti-neurodegenerative effects. On the other hand, there are no reports of their effects on gastric lesions. This study examined the inhibitory effects of cinnamic acids, including p-methoxycinnamic acid, 3,4,5-trimethoxycinnamic acid, and 8 compounds (cinnamic acid, 2-(trifluoromethyl) cinnamic acid, 3-(trifluoromethyl) cinnamic acid, trans-4-(trifluoromethyl) cinnamic acid, 4-(dimethylamino) cinnamic acid, 3,4-(methylenedioxy) cinnamic acid and 3,4-dihydroxycinnamic acid), which were selected based on their presence in medicinal herbs and molecular weight, against gastric lesions. Animal models were used to confirm the protective effects on acute gastritis caused by the administration of HCl/EtOH. Gastric acid inhibition was examined by an acid-neutralizing test and the proton pump (H⁺/K⁺-ATPase) inhibiting activity. In addition, antioxidant tests were performed and the gastric emptying rate was determined. The results showed that cinnamic acid, p-methoxycinnamic acid, and 3,4,5-trimethoxycinnamic acid had an inhibitory effect on gastric lesions.
Gastric Acid
;
Gastric Emptying
;
Gastritis
;
Hand
;
Models, Animal
;
Molecular Weight
;
Plants, Medicinal
;
Polygala
;
Proton Pumps
7.Cytotoxicity and Structure Activity Relationship of Dammarane-Type Triterpenoids from the Bark of Aglaia elliptica against P-388 Murine Leukemia Cells.
Ace Tatang HIDAYAT ; Kindi FARABI ; Desi HARNETI ; Rani MAHARANI ; DARWATI ; NURLELASARI ; Tri MAYANTI ; Arlette Suzy SETIAWAN ; Unang SUPRATMAN ; Yoshihito SHIONO
Natural Product Sciences 2017;23(4):291-298
Six dammarane-type triterpenoids, dammar-24-en-3β-ol (1), 3β-epicabraleahydroxy lactone (2), (E)-25-hydroperoxydammar-23-en-3β,20-diol (3), dammar-24-en-3β,20-diol (4), 3β-acetyl-20S,24S-epoxy-25-hydroxydammarane (5), and 3β-epiocotillol (6) were isolated from the methanolic extract of the bark of Aglaia elliptica. The chemical structure were identified on the basis of spectroscopic evidence and by comparison with those spectra previously reported. Compounds 1 – 6 were isolated first time from this plant. Compounds 1 – 6, along with a known synthetic analog, cabraleone (7) were evaluated their cytotoxic activity against P-388 murine leukimia cells in vitro. Among those compounds 3β-acetyl-20S,24S-epoxy-25-hydroxydammarane (5) showed strongest cytotoxic activity with IC₅₀ value of 8.02 ± 0.06 µM.
Aglaia*
;
In Vitro Techniques
;
Leukemia*
;
Meliaceae
;
Methanol
;
Plants
;
Structure-Activity Relationship*
8.Anti-inflammatory and Anti-bacterial Effects of Aloe vera MAP against Multidrug-resistant Bacteria.
Natural Product Sciences 2017;23(4):286-290
Multidrug-resistant Acinetobacter baumannii and Pseudomonas aeruginosa are highly dangerous nosocomial pathogens, cause the symptoms of skin infections, pressure sores, sepsis, blood stream and wound infections. Unfortunately, these pathogens are immune to the most common antibiotics, such as, carbapenem, aminoglycoside and fluoroquinolone. Therefore, it is imperative that new and effective antibiotics be developed. In the present study, the antimicrobial effects of Aloe vera MAP (modified Aloe polysaccharide) on Staphylococcus aureus and Bacillus subtilis, Escherichia coli and Enterobacter aerogenes, and clinical Pseudomonas aeruginosa and clinical Acinetobacter baumannii were comprehensibly investigated. Prior to the growth inhibition effect measurement and antibiotic disc diffusion assay on gram-positive and gram-negative bacteria and selected multidrug-resistant Pseudomonas aeruginosa and Acinetobacter baumannii, antimicrobial resistance screening was performed for the multidrug-resistant bacteria obtained from clinical isolates. The results for showed the Aloe vera MAP had a concentration-dependent effect on all of examined bacteria, particularly on Pseudomonas aeruginosa. Anti-inflammatory and anti-oxidant experiments were also performed dose dependently effects to confirm the beneficial physiological effects of Aloe vera MAP.
Acinetobacter baumannii
;
Aloe*
;
Anti-Bacterial Agents
;
Bacillus subtilis
;
Bacteria*
;
Diffusion
;
Enterobacter aerogenes
;
Escherichia coli
;
Gram-Negative Bacteria
;
Mass Screening
;
Pressure Ulcer
;
Pseudomonas aeruginosa
;
Rivers
;
Sepsis
;
Skin
;
Staphylococcus aureus
;
Wound Infection
9.Anti-tumor Activity of Saussurea laniceps against Pancreas Adenocarcinoma.
Keyong Ho LEE ; Byeong Soo KIM ; Ki Hyeong RHEE
Natural Product Sciences 2017;23(4):281-285
The purpose of this study was to confirm the anti-tumor activity of an ethanol extract of Saussurea laniceps against pancreatic tumor and to isolate the active compound from S.laniceps extract. Treatment with S.laniceps extract and hispidulin inhibited proliferation of pancreatic cell lines, such as Capan-1, Capan-2, Panc-1 and S2-013 in a dose-dependent manner using the hollow fiber assay. Hispidulin showed typical hallmarks of apoptotic cell death a significant anti-tumor activity on Capan-2 cells at a dose of 100 mg/kg and 200 mg/kg. S.laniceps has potential cytotoxic and apoptotic effects on human pancreatic carcinoma cells. Its mechanism of action might be associated with the apoptotic cell death through DNA fragmentation.
Adenocarcinoma*
;
Cell Death
;
Cell Line
;
DNA Fragmentation
;
Ethanol
;
Humans
;
Pancreas*
;
Saussurea*
10.Phenolic Compounds from the Leaves of Homonoia riparia and their Inhibitory Effects on Advanced Glycation End Product Formation.
Ik Soo LEE ; Seung Hyun JUNG ; Chan Sik KIM ; Jin Sook KIM
Natural Product Sciences 2017;23(4):274-280
In a search for novel treatments for diabetic complications from natural resources, we found that the ethyl acetate-soluble fraction from the 80% ethanol extract of the leaves of Homonoia riparia has a considerable inhibitory effect on advanced glycation end product (AGE) formation. Bioassay-guided isolation of this fraction resulted in identification of 15 phenolic compounds (1 – 15). These compounds were evaluated in vitro for inhibitory activity against the formation of AGE. The majority of tested compounds, excluding ethyl gallate (15), markedly inhibited AGE formation, with IC₅₀ values of 2.2 – 89.9 µM, compared with that of the positive control, aminoguanidine (IC₅₀ = 962.3 µM). In addition, the effects of active isolates on the dilation of hyaloid-retinal vessels induced by high glucose (HG) in larval zebrafish was investigated; (–)-epigallocatechin-3-O-gallate (6), corilagin (7), and desmanthine-2 (11) significantly decreased HG-induced dilation of hyaloid–retinal vessels compared with the HG-treated control group.
Diabetes Complications
;
Ethanol
;
Euphorbiaceae
;
Glucose
;
In Vitro Techniques
;
Natural Resources
;
Phenol*
;
Zebrafish