Papers by P. Piyachaturawat
European Journal of Pharmacology, 2016
Styryl lactones are plant-derived compounds from genus Goniothalamus with promising anti-prolifer... more Styryl lactones are plant-derived compounds from genus Goniothalamus with promising anti-proliferation and anticancer properties. However, the exact mechanism and the target for their activities remained unclear. In the present study, we investigated the effect of 5-acetyl goniothalamin (5GTN) from Goniothalamus marcanii on Wnt/β-catenin signaling pathway which is a key regulator in controlling cell proliferation in breast cancer cells (MCF-7 and MDA-MB-231). 5GTN, a naturally occurring derivative of goniothalamin (GTN) mediated the toxicity to MCF-7 and MDA-MB-231 cells in a dose-and time related manner, and was more potent than that of GTN. 5GTN strongly inhibited cell proliferation and markedly suppressed transcriptional activity induced by β-catenin in luciferase reporter gene assay. In consistent with this view, the expression of Wnt/β-catenin signaling target genes including c-Myc, cyclin D1 and Axin2 in MCF-7 and MDA-MB-231 cells were suppressed 2 after treatment with 5GTN. It was concomitant with cell cycle arrest at G 1 phase and cell apoptosis in MCF-7 cells. In addition, 5GTN enhanced glycogen synthase kinase (GSK-3β) activity and therefore reduced the expression of active form of β-catenin protein in MCF-7 and MDA-MB-231 cells. Taken together, 5GTN exhibited a promising anticancer effect against breast cancer cells through an inhibition of Wnt/β-catenin signaling. This pathway may be served as a potential chemotherapeutic target for breast cancer by 5GTN.
BMC Veterinary Research, 2016
Background: The match play patterns in equestrian polo are unique and require specific training p... more Background: The match play patterns in equestrian polo are unique and require specific training programs to ensure sport performance. The effect of commonly used exercise training regimens on the adaptation of skeletal muscle is unclear. The present study investigated the modulating effects of the classic training regimen, comprised of aerobic exercise training with increasing exercise intensities and varying duration combined with match play, on the properties of muscle in polo ponies. Nine healthy adult female polo ponies were subjected to four consecutive subsets of 1 year classic training regimen including basal activity (B), low intensity (L), low to moderate intensity (LM), and low to moderate intensity training plus match play during polo tournament (LMP), respectively. At the end of each training period, gluteus medius muscle samples were taken for determination of muscle fiber type distribution, muscle metabolic capacity, capillary density, and lipid and glycogen content. The expression profile of metabolic genes including succinate dehydrogenase (SDH), phosphofructokinase (PFK), glycogen phosphorylase (PYG), and glycogen synthase (GYS) were also measured. Results: Among all exercise training subsets, only LMP exercise period caused an increase in the number of oxidative fibers (type IIa), along with increases in properties related to oxidative metabolism including high capillary density, intramuscular lipid content, and expression of SDH and PYG genes, with a corresponding decrease in the number of type IIx muscle fibers. Conclusion: The combination of low to moderate and high intensity training in LMP are only sufficient to induce changes in oxidative characteristics. As the first scientific evidence providing such insight about the classic polo training regimen, the data forms a basis for further consideration in training program design.
Asian Pacific Journal of Cancer Prevention : APJCP, 2017
Gastric cancer is the most common cancer in Eastern Asia. Increasing chemoresistance and general ... more Gastric cancer is the most common cancer in Eastern Asia. Increasing chemoresistance and general systemic toxicities have complicated the current chemotherapy leading to an urgent need of more effective agents. The present study reported a potent DNA topoisomerase IIα inhibitory activity of an andrographolide analogue (19-triisopropyl andrographolide, analogue-6) in gastric cancer cells; MKN-45, and AGS cells. The analogue was potently cytotoxic to both gastric cancer cell lines with the half maximal inhibitory concentration (IC50 values) of 6.3±0.7 μM, and 1.7±0.05 μM at 48 h for MKN-45, and AGS cells, respectively. It was more potent than the parent andrographolide and the clinically used, etoposide with the IC50 values of >50 μM in MKN-45 and 11.3±2.9 μM in AGS cells for andrographolide and 28.5±4.4 μM in MKN-45 and 4.08±0.5 μM in AGS cells for etoposide. Analogue-6 at 2 μM significantly inhibited DNA topoisomerase IIα enzyme in AGS cells, induced DNA damage, activated cleaved...
Cosmetics, 2022
Ultraviolet-B (UVB) exposure is one of the primary extrinsic factors causing skin photoaging. It ... more Ultraviolet-B (UVB) exposure is one of the primary extrinsic factors causing skin photoaging. It stimulates inflammatory responses and arrests the cell cycle. Matrix metalloproteinase-1 (MMP-1) secreted by keratinocytes is one of the important extracellular matrixes to attenuate UVB-induced skin aging via collagen degradation. Curcuma aromatica (CA) and Curcuma comosa (CC), the herbaceous plants in the Zingiberaceae family, are commonly used in Thai traditional women’s medicines. The present work was aimed to investigate the potential of the CA and CC extracts and their isolated compounds to attenuate UVB-induced MMP-1 and cell cycle arrest in HaCaT keratinocytes. Total phenolic contents and antioxidant capacities of the extracts were determined. CC extract contains more phenolic components and provides more potent antioxidant activities than CA extract. HaCaTs were pretreated with the extracts or their isolated constituents 1–4 for 24 h and then repeatedly exposed to UVB at 100 mJ/...
Asia Pacific Journal of Pharmacology, 1994
Scientific Reports, 2018
The Wnt/β-catenin signaling pathway plays a key role in the progression of human colorectal cance... more The Wnt/β-catenin signaling pathway plays a key role in the progression of human colorectal cancers (CRCs) and is one of the leading targets of chemotherapy agents developed for CRC. The present study aimed to investigate the anti-cancer effects and molecular mechanisms of 19-O-triphenylmethyl andrographolide (RS-PP-050), an andrographolide analogue and determine its activity in the Wnt/βcatenin pathway. RS-PP-050 was found to potently inhibit the proliferation and survival of HT-29 CRC cells. It induces cell cycle arrest and promotes apoptotic cell death which was associated with the activation of PARP-1 and p53. Furthermore, RS-PP-050 exerts inhibitory effects on β-catenin transcription by suppressing T-cell factor/lymphocyte enhancer factor (TCF/LEF) activity in cells overexpressing β-catenin and by down-regulating the endogenous expression of Wnt target genes. RS-PP-050 also decreased the protein expression of the active form of β-catenin but functions independently of GSK-3β, a negative regulator of Wnt. Interestingly, RS-PP-050 extensively blocks phosphorylation at Ser675 of β-catenin which links to interference of the nuclear translocation of β-catenin and might contribute to Wnt inactivation. Collectively, our findings reveal the underlying anti-cancer mechanism of an andrographolide analogue and provide useful insight for exploiting a newly chemotherapeutic agent in Wnt/β-catenin-overexpressing CRC cells. Colorectal cancer (CRC), is a malignancy that has one of the highest incidence rates in both males and females in the United States 1. Although the early response success rate of CRC to current chemotherapeutic drugs is high, the invariable development of drug resistance as well as patient intolerance of adverse drug side effects limits their usage 2. Thus, searching for new effective chemical entities with greater specificity is urgently needed. Advancement in cancer treatment strategies depend upon gaining a better understanding of the intracellular signaling cascades and molecular pathways involved in tumor survival and progression. The deregulation of Wnt/β-catenin signaling is considered to be a major oncogenic event in the initiation and progression of most colon cancers 3. In the absence of Wnt ligands, the key effector of this signaling, β-catenin, is sequestered in a destruction complex composed of adenomatous polyposis coli (APC), casein kinase 1α (CK1α), Axin, and glycogen synthase kinase-3β (GSK-3β) which maintains the activity of cytosolic β-catenin at a low
American Journal of Physiology-Renal Physiology, 2005
Nephrotoxicity is one of the main side effects caused by cisplatin (CP), a widely used antineopla... more Nephrotoxicity is one of the main side effects caused by cisplatin (CP), a widely used antineoplastic agent. Here, we examined the effect of a novel water-soluble carbon monoxide-releasing molecule (CORM-3) on CP-mediated cytotoxicity in renal epithelial cells and explored the potential therapeutic benefits of carbon monoxide in CP-induced nephrotoxicity in vivo. Exposure of LLC-PK1 cells to CP (50 μM) caused significant apoptosis as evidenced by caspase-3 activation and an increased number of floating cells. Treatment with CORM-3 (1–50 μM) resulted in a remarkable and concentration-dependent decrease in CP-induced caspase-3 activity and cell detachment. This effect involved activation of the cGMP pathway as 1H-oxadiazole [4, 3-a] quinoxaline-1-ore (ODQ), a guanylate cyclase inhibitor, completely abolished the protection elicited by CORM-3. Using a rat model of CP-induced renal failure, we found that treatment with CP (7.5 mg/kg) caused a significant elevation in plasma urea (6.6-fo...
Journal of Ethnopharmacology, 2016
Ethnopharmacological relevance Curcuma comosa Roxb. (C. comosa) or Wan Chak Motluk, Zingiberaceae... more Ethnopharmacological relevance Curcuma comosa Roxb. (C. comosa) or Wan Chak Motluk, Zingiberaceae family, has been used in Thai traditional medicine for the treatment of gynecological problems and inflammation.
Journal of Steroid Biochemistry, 1984
The influence of alloxan diabetes on reproductive function and the estradiol-stimulated increase ... more The influence of alloxan diabetes on reproductive function and the estradiol-stimulated increase in uterine peroxidase was investigated. Alloxan monohydrate in a dose of 75 mg/kg body weight effectively produced permanent diabetes. In adult rats, 20 days of diabetes resulted in cessation of the estrous cycle and a significant reduction in the gain of body weight, the weights of anterior pituitary gland, ovary, uterus, the level of serum progesterone and the activity of the estradiol-stimulated uterine peroxidase (P less than 0.05). After 10 days of insulin treatment, the ovarian weight, the estrous cycle and the level of ovarian hormones were restored to normal whereas the uterine weight and the estradiol-stimulated uterine peroxidase activity were only partially recovered. Persistent depression of the uterine response in the insulin-treated diabetic rats to both endogenous and exogenous ovarian hormone stimulation suggests that the uterus was directly affected by diabetes. The direct effect of diabetes upon the uterus was further demonstrated in the ovariectomized immature rat in which diabetes depressed the stimulatory action of estradiol on both uterine weight and uterine peroxidase activity.
Artery, 1997
The hypolipidemic effect of an ethyl acetate extract of the rhizome of Curcuma comosa Roxb was in... more The hypolipidemic effect of an ethyl acetate extract of the rhizome of Curcuma comosa Roxb was investigated in mice. Intragastric administration of the extract significantly decreased plasma lipid levels of both triglyceride and cholesterol but increased liver triglyceride content. Liver weight and plasma activities of glutamic oxaloacetic transaminase and glutamic pyruvic transaminase were not affected by a single administration. Prolonged treatment did not further decrease plasma lipid level but caused further increases in liver triglyceride content and weight. The lower plasma cholesterol activity of C. comose extract was found to be essentially associated with elevation of plasma HDL cholesterol level, increased excretion of fecal cholesterol and bile salt. The increase persisted throughout the period of treatment. These results suggest that C. comosa has hypolipidemic action. It exerts hypocholesterolemic activity by accelerating mobilization of cholesterol from peripheral tiss...
Research communications in chemical pathology and pharmacology, 1982
The inhibitory effect of cytochalasin E on galactose absorption in everted sacs of mouse jejunum ... more The inhibitory effect of cytochalasin E on galactose absorption in everted sacs of mouse jejunum was studied. Cytochalasin B had highest potency on the inhibition of galactose absorption when it was added in the mucosal solution followed by cytochalasins E, A, C and D respectively. Cytochalasin E at a concentration as low as 2.5 micrograms/ml could inhibit galactose absorption by 17.1% within 60 min incubation and its maximum inhibition was obtained at a concentration of 10.0 micrograms/ml. At this concentration, it inhibited both Na+-dependent and independent galactose absorption. Our results in the present study and previously reported indicate that cytochalasin E inhibits the active intestinal absorption of galactose as well as glucose in the mouse.
Research communications in chemical pathology and pharmacology, 1983
Gastrin-stimulated secretory rate of gastric H+ and pepsin were markedly inhibited (P less than 0... more Gastrin-stimulated secretory rate of gastric H+ and pepsin were markedly inhibited (P less than 0.001) in ovariectomized rat after 7 days of estradiol treatment (80 micrograms/kg/day) in comparison to ovariectomized untreated rat and sham control. In correlation to the secretions, the majority of parietal cells failed to show the typical ultrastructural transformation associated with active secretion. Pyknotic nuclei with dilatation of nuclear envelope and degenerative changes were observed in the parietal cells. Meanwhile, the chief cell showed inactive characteristics in that a large number of pepsinogen granules were retained in the cells. In contrast, in ovariectomized untreated rat, the rate of gastrin-stimulated H+ and pepsin secretion were not significantly different from the sham (P greater than 0.05). Consistent with secretion, after gastrin stimulation, the morphology and ultrastructure of the parietal cell and chief cell showed active secretory features in a pattern simil...
Cell biology international reports, 1986
Effects of cytochalasin E on the secretion of mucus and protein were investigated in gastric fist... more Effects of cytochalasin E on the secretion of mucus and protein were investigated in gastric fistula rats. Direct exposure of the gastric mucosa to cytochalasin E (5-20 micrograms/ml) significantly stimulated the secretory rate of soluble mucus and protein in pentagastrin-stimulated rats. The amount of surface mucus gel was also increased. The stimulatory effect was increased with increased concentrations of cytochalasin. Histological study suggests that the cytochalasin stimulated the release of mucus from the cell. The increase in secretory rate of protein was not due to an increase of pepsin secretion but rather was the consequence of the increase in mucus secretion.
Cell biology international reports, 1988
Formation of gastric mucosal lesions by streptozotocin-induced diabetes was investigated in rats.... more Formation of gastric mucosal lesions by streptozotocin-induced diabetes was investigated in rats. A single intravenous administration of streptozotocin in a dose of 65 mg/kg effectively produced hyperglycemia and damaged the gastric mucosa. Incidence and severity of mucosal lesions were progressively increased with time, from one to six weeks posttreatment. Microscopic lesions of the mucosa included hyperemia, desquamation of the surface epithelium with diffuse hemorrhage, and severe hemorrhage with localized erosion. Concurrent to the hyperglycemia, the histamine stimulated gastric H+-secretion was significantly decreased whereas pepsin secretion was not affected. Both soluble mucus and surface mucus gel were increased. The result suggests that the early lesion of gastric mucosa may be associated with the direct action of streptozotocin, the severity of which may be further aggravated by diabetic state.
Piperine is acutely toxic to mice, rats and hamsters. The LDsc values for a single i.v., i.p., s.... more Piperine is acutely toxic to mice, rats and hamsters. The LDsc values for a single i.v., i.p., s.c., i.g. and i.m. administration of piperine to adult male mice were 15.1, 43, 200, 330 and 400 mg/kg body wt, respectively. The i.p. LD50 value was increased to 60 mg/kg body wt in adult female and 132 mg/kg body wt in weanling male mice. In adult female rats, the i.p. LDso value was 33.5 mg/kg body wt whereas the i.g. LD~o value was increased to 514 mg/kg body wt. Most animals given a lethal dose died of respiratory paralysis within 3-17 min. In subacute toxicity studies, the rats died within l-3 days after treatment. Histopathologic changes included severe hemorrhagic necrosis and edema in gastrointestinal tract, urinary bladder and adrenal glands. Death of these animals may be attributable to multiple dysfunctions in their organs.
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Papers by P. Piyachaturawat