Papers by Chadarat Ampasavate
Frontiers in Pharmacology, Sep 19, 2023
Objective: Larvae of Hermitia illucens, or black soldier fly larvae (BSFL), have been recognized ... more Objective: Larvae of Hermitia illucens, or black soldier fly larvae (BSFL), have been recognized for their high lipid yield with a remarkable fatty acid profile. BSFL oil (SFO) offers the added value of a low environmental footprint and a sustainable product. In this study, the characteristics and cosmetic-related activities of SFO were investigated and compared with rice bran oil, olive oil and krill oil which are commonly used in cosmetics and supplements. The physicochemical characteristics were determined including acid value, saponification value, unsaponifiable matter and water content of SFO. The fatty acid composition was determined using GC-MS equipped with TR-FAME. The in vitro antioxidant properties were determined using DPPH, FRAP and lipid peroxidation inhibition assays. Antihyaluronidase (anti-HAase) activity was measured by detecting enzyme activity and molecular docking of candidate compounds toward the HAase enzyme. The safety assessment towards normal human cells was determined using the MTT assay and the UVB protection upon UVB-irradiated fibroblasts was determined using the DCF-DA assay. The whitening effect of SFO was determined using melanin content inhibition. Results: SFO contains more than 60% polyunsaturated fatty acids followed by saturated fatty acids (up to 37%). The most abundant component found in SFO was linoleic acid (C18:2 n-6 cis). Multiple anti-oxidant mechanisms of SFO were discovered. In addition, SFO and krill oil prevented hyaluronic acid (HA) degradation via strong HAase inhibition comparable with the positive control, oleanolic acid. The molecular docking confirmed the binding interactions and molecular recognition of major free fatty acids toward HAase. Furthermore, SFO exhibited no cytotoxicity on primary human skin fibroblasts, HaCaT keratinocytes
Pharmaceuticals, Jun 9, 2023
This article is an open access article distributed under the terms and conditions of the Creative... more This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY
Twenty plants in the family Rubiaceae collected from Northern Thailand were extracted and compare... more Twenty plants in the family Rubiaceae collected from Northern Thailand were extracted and compared for their cytotoxic activities against a human cervix carcinoma cell line (KB-3-1). MTT assay was the technique utilized for cell survival determination. These plants were classified into three groups as active, moderately active, and inactive plants, according to their cytotoxic activity. Gardenia obtusifolia and Gardenia sootepensis were the species possessing the highest activity (IC50 ≤ 4 µg/ml) against the KB-3-1 cell line when compared to the other rubiaceous species. Other three plants categorized as the moderately active species (20 µg/ml < IC50 < 100 µg/ml) were Ixora cibdela, Mussaenda pava and Psychotria ophioxyloides. The results from this study revealed 25% success rate in discovering plants with high and moderate cytotoxic activity. The usefulness of taxonomy in plant selection was confirmed in this study.
Phytomedicine, Jun 1, 2007
Multidrug resistance (MDR) is the result of overexpression of membrane bound proteins that efflux... more Multidrug resistance (MDR) is the result of overexpression of membrane bound proteins that efflux chemotherapeutic drugs from the cells. Two proteins, P-glycoprotein (P-gp) and multidrug-resistance associated protein-1 (MRP-1) efflux chemotherapeutic agents out of the cancer cell that decrease intracellular drug accumulation, thereby decreasing the effectiveness of many chemotherapeutic agents. In the present study, the ethanolic extract of the roots of Stemona curtisii Hook. was tested for the potential ability to modulate the MDR phenotype and function of P-gp and MRP-1. The S. curtisii extract reversed the resistance to putative chemotherapeutic agents, including vinblastine, paclitaxel and colchicine of KB-V1 cells (MDR human cervical carcinoma with high P-gp expression) in a dose-dependent manner, but not in KB-3-1 cells (drug sensitive human cervical carcinoma, which lack P-gp expression). The root extract also increased the intracellular uptake and retention of 3 [H]-vinblastine in KB-V1 cells dose dependently. The extract did not influence MDR phenotype-mediated MRP-1 in MRP1-HEK293 (human embryonic kidney cells stably transfected with pcDNA3.1-MRP1-H10 which show high MRP-1 expression) and pcDNA3.1-HEK293 (wild type). In summary, the S. curtisii root extract modulated P-gp activity but not MRP-1 activity. The result obtained from this study strongly indicated that S. curtisii extract may play an important role as a P-gp modulator as used in vitro and may be effective in the treatment of multidrug-resistant cancers. The purified form of the active components of S. curtisii extract should be investigated in more details in order to explain the molecular mechanisms involved in P-gp modulation. This is the first report of new biological activity in this plant, which could be a potential source of a new chemosensitizer.
Bioconjugate Chemistry, Nov 13, 2007
Targeted delivery of therapeutics possesses the potential to localize therapeutic agents to a spe... more Targeted delivery of therapeutics possesses the potential to localize therapeutic agents to a specific tissue as a mechanism to enhance treatment efficacy and abrogate side effects. Antibodies have been used clinically as therapeutic agents and are currently being explored for targeting drug-loaded nanoparticles. Peptides such as RGD peptides are also being developed as an inexpensive and stable alternative to antibodies. In this study, cyclo(1,12)PenITDGEATDSGC (cLABL) peptide was used to target nanoparticles to human umbilical cord vascular endothelial cells (HUVEC) monolayers that have upregulated intercellular cell-adhesion molecule-1 (ICAM-1) expression. The cLABL peptide has been previously demonstrated to possess high avidity for ICAM-1 receptors on the cell surface. Poly(DL-lactic-co-glycolic acid) nanoparticles conjugated with polyethylene glycol and cLABL demonstrated rapid binding to HUVEC with upregulated ICAM-1, which was induced by treating cells with the proinflammatory cytokine, interferon-γ. Binding of the nanoparticles could be efficiently blocked by pre-incubating cells with free peptide suggesting that the binding of the nanoparticles is specifically mediated by surface peptide binding to ICAM-1 on HUVEC. The targeted nanoparticles were rapidly endocytosed and trafficked to lysosomes to a greater extent than the untargeted PLGA-PEG nanoparticles. Verification of peptide-mediated nanoparticle targeting to ICAM-1 may ultimately lead to targeting therapeutic agents to inflammatory sites expressing upregulated ICAM-1.
International Journal of Cosmetic Science, Aug 1, 2008
The aim of this research was to develop and validate a spectrofluorimetric method for determinati... more The aim of this research was to develop and validate a spectrofluorimetric method for determination of tranexamic acid in hydrogel patch formulations. Tranexamic acid (trans-4-aminomethylcyclohexanecarboxylic acid, trans-AMCHA) is an antifibrinolytic drug that recently gained attention as a skin-whitening agent due to its inhibitory effect on ultraviolet (UV)-induced pigmentation in vivo. Derivatization with naphthalene-2,3-dicarboxaldehyde (NDA) in the presence of cyanide ion (CN) to produce a fluorescent 1-cyanobenz[f]isoindole (CBI) product ()•ex = 420 nm,)•e,• = 480 nm) is for the first time reported for the determination of tranexamic acid in hydrogel patch formulations. Other separation techniques were not used in the analysis of the CBI-fluorescent product as required in the previous studies. The developed method was proven to be precise and accurate with percent recoveries ranging between 98.0% and 101.8% at the concentration range of 8.4-84.0 pg/ml (R 2 > 0.999). The intra-and inter-day precisions as expressed by the relative standard deviations (RSD) were below 1.85%. Derivatization of tranexamic acid with NDA/CN was completed within five minutes and was stable for at least 30 minutes. The method has been applied to the analysis of drug content and release profiles in tranexamic hydrogel patch formulations.
薬剤抵抗性癌細胞におけるP糖蛋白抗体によるクルクミン含有PLGA(ナノ粒子)の細胞取込みおよび細胞毒性の増強
Effect of pure curcumin, demethoxycurcumin, and bisdemethoxycurcumin on WT1 gene expression in leukemic cell lines
Cancer Chemotherapy and Pharmacology, Nov 23, 2007
Leukemias are groups of hematological malignancies with high incidence and mortality rates in pat... more Leukemias are groups of hematological malignancies with high incidence and mortality rates in patients worldwide. There have been shown in many studies that Wilms&amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;#39; tumor1 (WT1) gene were highly expressed in leukemic blast cells. Curcuminoids, major active components of the spice turmeric, are well known for its anticancer. Curcuminoids consist of pure curcumin, demethoxycurcumin, and bisdemethoxycurcumin. In this study, the effect of each curcuminoids&amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;#39;components on WT1 gene expression in leukemic cell lines (K562, HL60, U937, and Molt4) was investigated. The levels of WT1 mRNA and WT1 protein in leukemic cell lines were assessed by RT-PCR and Western blot analysis, respectively. It was found that the WT1 mRNAs were detected in all 4 types of leukemic cell lines. However, the WT1 protein levels were found only in the cell lines K562 and Molt4. Pure curcumin exhibited a strong inhibitory effect on WT1 mRNA and WT1 protein expression. The treatment of leukemic cell lines with non-cytotoxic doses (5, 10, and 15 microM) of pure curcumin for 2 days reduced the level of WT1 mRNA expression and WT1 protein in a dose-dependent manner. In addition, pure curcumin at 10 microM significantly decreased the level of WT1 mRNA and protein in a time-dependent manner. Pure curcumin, an excellent curcuminoid derivative, decreased WT1 gene expression in both transcriptional and translational levels. Thus, pure curcumin is one of a potential chemotherapeutic agent used for treatment of human leukemia. However, its chemotherapeutic property will need to be studied more in future.
Effects of FLT3-Specific Peptide-Polymeric Micelle Encapsulated Curcumin on EoL-1 Cell Line
Aaps Pharmscitech, May 29, 2010
The aim of this study was to evaluate the effects of preparation method and the type of surfactan... more The aim of this study was to evaluate the effects of preparation method and the type of surfactant on the properties of cephalexin (CPX) microspheres in order to obtain delivery systems suitable for the treatment of dairy mastitis. Microspheres were obtained using various preparation conditions and their physicochemical characteristics such as size, loading efficiency, morphology, and drug crystallinity were investigated. Antibacterial activity of microspheres from the optimum preparation condition was also studied. CPX microspheres were prepared by two different W/O/W emulsion solvent evaporation methods using PLGA as a matrix forming polymer. Several types of surfactants including nonionic, cationic, and anionic at different concentrations were used for preparation of the particles. The type and concentration of surfactant did neither affect the size nor morphology of the microspheres but showed a pronounced effect on the CPX encapsulation efficiency. It was found that Tween 80 showed the highest drug encapsulation efficiency (66.5%). Results from X-ray diffraction diffractograms and differential scanning calorimetry thermograms indicated that CPX entrapped in these microparticles was amorphous. Assessment of antibacterial activity showed that the obtained CPX microspheres exhibited good inhibition with minimum inhibitory concentration and minimum bactericidal concentration values of 128 µg/mL and 2,048 mg/mL against Staphylococcus aureus ATCC 25923, 512 µg/mL and 4,096 mg/mL against Escherichia coli ATCC 25922, respectively.
Peptide transport and metabolism across the placenta
Advanced Drug Delivery Reviews, Jun 1, 1999
Advances made in the field of DNA and recombinant technology have led to the emergence of peptide... more Advances made in the field of DNA and recombinant technology have led to the emergence of peptides and proteins as an important class of therapeutic compounds. While a significant amount of information exists regarding the transport and metabolism of peptides across different barriers (e.g. gastro-intestinal, nasal, and blood-brain barrier), limited attention has been paid towards their transport and metabolism across the placental barrier. The mechanism of placental transport of peptides is of importance in assessing the exposure of these drugs to the fetus, particularly when the drugs potentially may have adverse effects on the developing fetus.The absence of a well accepted, simple and convenient animal model may be a reason for the limited information available on the placental transport and metabolism of peptides. Although several in vivo models have been utilized to study the transport and metabolism of drugs across the placenta, species differences in the placental physiology and anatomy of the animal models with regard to the human placenta have prevented their widespread use. The in vitro human placental cell culture models are morphologically similar to the trophoblasts and often express the enzymes and carrier systems found in the human placenta. They can provide an easy and rapid method to determine the mechanisms of transport and metabolism of drugs across the placental barrier. These in vitro models have been utilized in the determination of transport mechanisms of drugs of abuse across the placenta.This article overviews the available literature on the placental transport of peptides and describes the application of an in vitro cell culture model (BeWo) to determine the mechanisms of transport of opioid peptides and their analogues across the placenta.
African Journal of Microbiology Research, Sep 16, 2011
During January-February 2010, a black root rot (BRR) disease of carrot (Daucus carota L.) was obs... more During January-February 2010, a black root rot (BRR) disease of carrot (Daucus carota L.) was observed in vegetable markets of Riyadh, Saudi Arabia. The recovery of Thielaviopsis basicola from local carrot fields indicated its appearance in propagules ranged between 8.32-10.15 (total count/g soil). This report describes the first evidence of black root rot disease of carrot caused by T. basicola in vegetable markets of Riyadh (Saudi Arabia).
International Journal of Pharmaceutics, Feb 1, 2002
In keeping with the advance of biotechnology, cell culture becomes an important tool for investig... more In keeping with the advance of biotechnology, cell culture becomes an important tool for investigating the transport and the metabolism phenomena. A cell line of human origin, the BeWo choriocarcinoma cell line, was used for the study of the transport and metabolism of opioid peptides across the in vitro model of the placental barrier. Opioid peptides, both naturally occurring and their synthetic analogs, are of interest to be developed as potent analgesics and were included in this study. The apparent permeability coefficients of the peptides containing 4 to 11 amino acid or analog residues were in the range of 0.23-14.60 x 10-5 cm/sec. The apparent permeability coefficients of these peptides were comparable to those of sucrose or dextrans, hydrophilic markers. Molecular weight and size of the peptides were inversely correlated to the permeability across the BeWo monolayers. Lipophilicity and charges of the peptides were also investigated and found to be the minor factors regulating the extent of peptide permeation. Contrasting to the transport of DPDPE peptide analog across the blood-brain barrier, the transport of DPDPE across the BeWo monolayers were not found to be via carrier-mediated transport. The major transport pathway of the opioid peptides across the BeWo monolayers was found to be via paracellular route. In metabolism studies, aminopeptidase was found to be a major enzyme type responsible for the degradation of naturally occurring peptides but not for the synthetic analogues. The finding obtained from the present study reveal the applicability of the BeWo cell line to be used as the in vitro cell culture model for the transport and metabolism screening of the opioid peptides.
Effective encapsulation of ascorbic acid bioactive in chitosan nanoparticles
Ascorbic acid or vitamin C is a water-soluble and strong antioxidant presented in many vegetables... more Ascorbic acid or vitamin C is a water-soluble and strong antioxidant presented in many vegetables and fruits. Ascorbic acid is essential for collagenesis in living organism, which protect tissue and cells from oxidation reactions by free radicals and other reactive oxygen-derived species. In cosmeceutical field, ascorbic acid has been scientifically proven that it can promote the synthesis of collagen and visibly reduce the effects of skin wrinkles (Zhang 1999). Besides that it can enhance the efficacy of other fat soluble antioxidants such as α-tocopherol (vitamin E) and β-carotene (Basu 1999, Gallarate1999). Ascorbic acid is notoriously unstable when exposed to air, humidity, light, heat, oxygen and base. In addition, with its water-soluble property, the permeability of the unmodified vitamin C (an active form) through skin is obstructed by a major barrier, stratum corneum (Zhang 1999). Therefore, a carefully-designed topical delivery system for ascorbic acid is of importance for ...
The Bulletin of Chiang Mai Associated Medical Sciences, 2006
The cytotoxic effect of curcumin, demethoxycurcumin and bisdemethoxycurcumin purified from Turmer... more The cytotoxic effect of curcumin, demethoxycurcumin and bisdemethoxycurcumin purified from Turmeric powder on leukemic cell lines $ongyot Anuchapreedr', Wlttrwat Srdjapong', Chadarst Duangratb, and pornngarm Limtrakul. Curcuminoids, major active components of the food flavor turmeric (Curcuma /onga Linn.); consist of curcumin, demethoxycurcumin and bisdemethoxycurcumin that exhibit anticarcinogenic properties in vivo. Fhis study was aimed to investigate the effect of curcuminoids on the cytotoxicity of lhe leukemic cells, HL60 (human promyeloid leukemia), U937 (human monocytic leukemia) and K562 (human erythroid leukemia). In this experimenl, three major nalural curcuminoids, pure curcumin, demethorycurcumin and bisdemethoxycurcumtn, isolated from turmeric powder, were compared for cytotoxicity on leukemic cell lines by MTT assay and trypan blue exclusion method. The result showed that all three curcuminoids exhibited an excellent cytotoxic activity on leukemic cell lines with the inhibitory concentration at 507o (lC5o) approximately 7 pg/mL in HL60 and U937 and 20 pg/mL in K562 cell line. Demethorycurcumin seem to be the most effective in all leukemic cell lines. The inhibitory effect of three forms of curcuminoids was not statistically different in each leukemic cell line. These results indicate that three major forms of curcuminoids affect the cell viability in all leukemic cell lines by MTT assay and Trypan blue exclusion method. Thus curcuminoid treatment may provide a guideline for molecular study and clinical treatment in leukemic patients in future. Bu[ chirng Msi Assoc Med sci 2006;39:60-71.
Phytomedicine, 2010
The effects of Curcuma longa (khamin chan) and Curcuma sp. ''khamin-oi'' (khamin-oi), as well as ... more The effects of Curcuma longa (khamin chan) and Curcuma sp. ''khamin-oi'' (khamin-oi), as well as isolated major curcuminoids on intestinal P-gp functions were evaluated in vitro. The accumulation of R123 in Caco-2 cells was increased and the R123 efflux ratios were significantly decreased by both Curcuma longa and Curcuma sp. ''khamin-oi'' extracts, indicating their roles on efflux transporters. The a-b transport of daunorubicin was increased by curcumin, demethoxycurcumin and bisdemethoxycurcumin while the b-a transport was significantly decreased by curcumin and demethoxycurcumin. However, calcein-AM uptake into the human P-gp overexpression cell line, LLC-GA5-COL300, was increased by curcumin and demethoxycurcumin in a concentration-dependent manner but not affected by bisdemethoxycurcumin. These results show that curcumin and demethoxycurcumin could inhibit P-gp but bisdemethoxycurcumin may modulate the function of other efflux transporters such as MRP. Taken together, the information may indicate the impact of Curcuma longa and Curcuma sp. ''khamin-oi'' on pharmacokinetics of orally administered drugs that are P-gp substrates.
Pharmacokinetics and analytical determination of acyclovir in Asian elephant calves (Elephas maximus)
Veterinary and Animal Science, 2021
Highlights • Pharmacokinetic and bioavailability data of acyclovir following intravenous and oral... more Highlights • Pharmacokinetic and bioavailability data of acyclovir following intravenous and oral administration are reported for Asian elephant calves.• Data represent the first comprehensive LC-MS/MS analysis of plasma acyclovir concentrations after i.v. and oral administration in elephants.
Pharmaceuticals
Chronic inflammation and tissue damage can result from uncontrolled inflammation during SARS-CoV-... more Chronic inflammation and tissue damage can result from uncontrolled inflammation during SARS-CoV-2 or COVID-19 infections, leading to post-acute COVID conditions or long COVID. Curcumin, found in turmeric, has potent anti-inflammatory properties but limited effectiveness. This study developed nanocurcumin, a curcumin nanoparticle, to enhance its physical and chemical stability and investigate its in vitro anti-inflammatory properties upon CoV2-SP induction in lung epithelial cells. Nanocurcumin was prepared by encapsulating curcumin extract in phospholipids. The particle size, polydispersity index, and zeta potential of nanocurcumin were measured using dynamic light scattering. The encapsulated curcumin content was determined using HPLC analysis. The encapsulation efficiency of curcumin was 90.74 ± 5.35% as determined by HPLC. Regarding the in vitro release of curcumin, nanocurcumin displayed a higher release content than non-nanoparticle curcumin. Nanocurcumin was further investiga...
Additional file 2: Figure S2. of Down-regulatory mechanism of mammea E/BB from Mammea siamensis seed extract on Wilmsâ Tumor 1 expression in K562 cells
13C NMR spectrum (101Â MHz, CDCl3) of mammea E/BB performed on a Bruker AVANCE 400 NMR spectromet... more 13C NMR spectrum (101Â MHz, CDCl3) of mammea E/BB performed on a Bruker AVANCE 400 NMR spectrometer. (TIF 136Â kb)
Low doses of partially purified fraction of kaffir lime (Citrus hystrix DC.) leaf extract induce cell death in Molt4 cells
Introduction: Kaffir lime ( Citrus hystrix DC.) is a medicinal plant found in Southeast Asia, bot... more Introduction: Kaffir lime ( Citrus hystrix DC.) is a medicinal plant found in Southeast Asia, both fruit and leaf have been used in Thai traditional medicine and food recipes. Objectives: Previous report demonstrated that partially purified fraction F9 of kaffir lime has anti-leukemic activity. This study aimed to investigate the anti-proliferative effects of low doses of F9 in Molt4 (human acute lymphoblastic leukemia) cell line. Effects on cell cycle progression as well as cell cycle regulatory proteins at the related phases after treatment were also studied. Materials and methods: Cytotoxic effect of F9 was studied by MTT assay, and its effect on cell cycle progression in Molt4 cells was further examined by flow cytometry. The effect on regulatory proteins was determined by Western blot analysis. Results: The F9 showed cytotoxic activity with an IC50 value of 24.5 μg/mL and low dose at the concentration of IC20 (2.5 μg/mL) of F9 induced cell death (sub-G1) as analyzed by flow cytometry. The F9 also increased p53 level while decreased cyclin A, cyclin B, and cdc2 (regulatory proteins in S and G2/M phases) protein expressions in a time- and dose-dependent manner. Conclusion: The F9 from kaffir lime leaf at low doses induced cell death. Moreover, it also inhibited cell cycle regulatory proteins. This new knowledge will be further investigated to determine active compounds in the future.
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Papers by Chadarat Ampasavate