DePo Yang

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Name: 杨得坡; DePo Yang
Organization: Sun Yat-sen University
Department: School of Pharmaceutical Sciences
Title: Professor
Co-reporter:Cai Zi-zhe, Yang De-po, Wu Sheng-qing, Wang Yong, Martin J.T. Reaney, Zhao Zhi-min, Zhu Long-ping, Sun Guo, Niu Yi, Zheng Dong, Niu Hui-ran, Yang Wen-zhe
Fuel 2017 Volume 210(Volume 210) pp:
Publication Date(Web):15 December 2017
DOI:10.1016/j.fuel.2017.08.109
•Housefly larvae were used to convert poultry manure to biodiesel feedstock.•Growth parameters of housefly larva were evaluated.•The free fatty acids and acylglycerol were separated by physical refinery.•The distillate and residue were processed separately to avoid energy waste.•Esterification product were neutralized by glycerol phase from transesterification.Fatty acid methyl esters (FAMEs) were produced from housefly (Musca domestica L.) larvae fed by poultry manure. The larval lipid output was 23.6 g from 1 kg poultry (107.3 g fresh larva), under conditions: inoculum density of 8000 larvae/kg, 28 °C, and 4 days. A practical method involving physical refining were developed specifically for housefly larval lipid (acid value = 15.1 mg KOH/g). With evaporator temperature of 155 °C, fatty acids distilled from molecular distillation were esterified with methanol catalyzed by benzenesulfonic acid (BSA) and residue, acylglycerols (fatty acids removal rate: 96.96%wt.), were transesterified with methanol using NaOH catalyst to produce fatty acid methyl ester biodiesel. Residual alkali catalyst in glycerol after transesterification was used to neutralize the acid catalyst and FFA from esterification. Acid value (AV) of esterification product (2.72 mg KOH/g) were lowered to 0.34 mg KOH/g. Biodiesel produced from housefly larval oil (HLO) satisfies the ASTM D6751-10 standard.
Co-reporter:Sheng-qing Wu, Zi-zhe Cai, Yi Niu, Dong Zheng, Guo-rui He, Yong Wang, De-po Yang
Renewable Energy 2017 Volume 113(Volume 113) pp:
Publication Date(Web):1 December 2017
DOI:10.1016/j.renene.2017.05.094
•A lipid source with high acid value (AV) was obtained from housefly larva fed with kitchen waste.•Simple oven drying was performed to hydrolyze larval lipid.•Excess 2-ethyl-1-hexanol was effectively removed by molecular distillation.•Unreacted fatty acids from esterification were processed through alkali refining.•Tribological properties of high-purity 2-ethylhexyl fatty acid esters were examined.Biolubricants are gaining increased attention because of their low toxicity, high biodegradability, and miscibility with additives. These features render them ideal for lubrication, especially in total-loss processes. In this study, housefly (Musca domestica) larvae were used as low-cost, non-food biolubricant feedstock. A larval lipid with high acid value (AV) of 63 mg KOH/g was used as feedstock for esterification to produce 2-ethylhexyl fatty acid esters (2-EH esters). We developed a method of producing high-purity 2-EH esters in which housefly larva free fatty acids (HLFFAs) were derived from larvae fed with kitchen waste. HLFFAs were esterified with 2-ethyl-1-hexanol (2-EHOH) catalysed with benzenesulfonic acid (BSA). The optimum esterification conditions were as follows: catalyst loading, 0.5 wt%; 2-EHOH-to-HLFFAs molar ratio, 3:1; temperature, 130 °C; and reaction time, 2 h. These conditions yielded 98.6% esterification rate. Excess 2-EHOH was removed by molecular distillation at 80 Pa and 110 °C. Residual fatty acids were neutralised by alkali refining. The chemical and physical properties, including the tribological properties, of the produced high-purity 2-EH esters (>99.7%) were also tested.
Co-reporter:Zi-Zhe Cai, Yong Wang, Ying-Lai Teng, Ka-Man Chong, Jia-Wei Wang, Jie-Wen Zhang, De-Po Yang
Fuel Processing Technology 2015 Volume 137() pp:186-193
Publication Date(Web):September 2015
DOI:10.1016/j.fuproc.2015.04.017
•A practical two-step process was developed to convert WCO with a high FFA content into FAME.•Crude glycerol from the second step was recycled as reactant for the first step.•An alkali catalyst was used in the esterification to lower FFA content of WCO.•Excess glycerol separation is not needed in the esterification step.•Significant energy and time saving have been achieved as compared to the traditional methanol esterification with methanol.A novel biodiesel production process using waste cooking oil (WCO) as feedstock was developed in this work. Free fatty acids (FFAs) from WCO were esterified by crude glycerol catalyzed by NaOH, which lowered the content of free fatty acids of WCO. The conversion of FFA in the WCO (acid value: 124.9 mg KOH/g) to acylglycerols is 99.6% under the optimal conditions (1.4:1 molar ratio of glycerol to FFA, 4 h, 210 °C, catalyst loading 0.5 wt.% based on WCO weight). After the transesterification of esterified WCO with methanol catalyzed by NaOH, the yield of the final product is 93.1 wt.% with 98.6 wt.% of fatty acid methyl ester (FAME). The crude glycerol and the catalyst from transesterification were recycled as reactant for esterification during the biodiesel production. Soap formed from the subsequent processes maintained a high catalyzing activity for FFA esterification after being recycled for 13 times. This new glycerol esterification process using alkali (soap) catalyst provides a promising solution to convert feedstock with high FFA levels to biodiesel. This biodiesel production process has distinct advantages compared with traditional two-step methods, including lower cost of catalyst for both esterification and transesterification processes, less energy consumption for methanol recovery, recycling of the glycerol byproduct and catalyst (soap), and no requirement of anti-corrosive equipment.
Co-reporter:Hang Li, Jing-jun Zhao, Jin-long Chen, Long-ping Zhu, Dong-mei Wang, Lin Jiang, De-po Yang, Zhi-min Zhao
Phytochemistry 2015 Volume 117() pp:400-409
Publication Date(Web):September 2015
DOI:10.1016/j.phytochem.2015.07.005
•Sixteen ent-pimarane diterpenoids including eight previously unknown diterpenoids were isolated from Flickingeria fimbriata.•Their structures were elucidated by detailed spectroscopic analysis, including absolute configurations.•Several compounds displayed potential NF-κB inhibitory activities.Chemical investigation of the aerial parts of Flickingeria fimbriata (Bl.) Hawkes resulted in isolation of sixteen ent-pimarane diterpenoids, including five rare 16-nor-ent-pimarane diterpenoids, two 15,16-dinor-ent-pimarane diterpenoids and one ent-pimarane diterpenoid. Structures were mainly elucidated by extensive spectroscopic analysis, and their absolute configurations were unequivocally determined by the exciton chirality method, the modified Mosher’s method, the CD experiments (including Snatzke’s method) and chemical transformations, respectively. All the isolated compounds were screened for inhibitory effects on the nuclear factor-kappaB (NF-κB) in lipopolysaccharide (LPS) induced murine macrophage RAW264.7 cells, using a NF-κB-dependent luciferase reporter gene assay. Several of these compounds displayed comparable or even better activities than the positive control pyrrolidinedithiocarbamate (PDTC) (IC50 = 26.3 μM) with IC50 values in the range of 14.7–29.2 μM and structure–activity relationships are briefly proposed.Rare 16-nor-ent-pimarane type diterpenoids (1–5), two 15,16-dinor-ent-pimarane type (6–7) and one ent-pimarane diterpenoid (11), together with eight known analogs were isolated from Flickingeria fimbriata.
Co-reporter:Tie-xin Tang;Wei-yan Guo;Ye Xu;Si-ming Zhang;Xin-jun Xu;Dong-mei Wang;Zhi-min Zhao;Long-ping Zhu;De-po Yang
Phytochemical Analysis 2014 Volume 25( Issue 3) pp:266-272
Publication Date(Web):
DOI:10.1002/pca.2502

ABSTRACT

Introduction

Poplar tree gum has a similar chemical composition and appearance to Chinese propolis (bee glue) and has been widely used as a counterfeit propolis because Chinese propolis is typically the poplar-type propolis, the chemical composition of which is determined mainly by the resin of poplar trees. The discrimination of Chinese propolis from poplar tree gum is a challenging task.

Objective

To develop a rapid thin-layer chromatographic (TLC) identification method using chemometric fingerprinting to discriminate Chinese propolis from poplar tree gum.

Methods

A new TLC method using a combination of ammonia and hydrogen peroxide vapours as the visualisation reagent was developed to characterise the chemical profile of Chinese propolis. Three separate people performed TLC on eight Chinese propolis samples and three poplar tree gum samples of varying origins. Five chemometric methods, including similarity analysis, hierarchical clustering, k-means clustering, neural network and support vector machine, were compared for use in classifying the samples based on their densitograms obtained from the TLC chromatograms via image analysis.

Results

Hierarchical clustering, neural network and support vector machine analyses achieved a correct classification rate of 100% in classifying the samples. A strategy for TLC identification of Chinese propolis using chemometric fingerprinting was proposed and it provided accurate sample classification.

Conclusion

The study has shown that the TLC identification method using chemometric fingerprinting is a rapid, low-cost method for the discrimination of Chinese propolis from poplar tree gum and may be used for the quality control of Chinese propolis. Copyright © 2014 John Wiley & Sons, Ltd.

Co-reporter:Dong Leung, Depo Yang, Zhuoxue Li, Zhimin Zhao, Jianping Chen, and Longping Zhu
Industrial & Engineering Chemistry Research 2012 Volume 51(Issue 2) pp:1036-1040
Publication Date(Web):December 14, 2011
DOI:10.1021/ie201403r
The advancement of biodiesel production emphasizes the finding of new, low-cost, and plentiful raw materials. Insects, as one of the most plentiful biological resources worldwide, could be potential candidates for biodiesel production. In this study, Zophobas morio (Coleoptera: Tenebrionidae) was evaluated as an insect feedstock, attempting to prove the feasibility of producing qualified biodiesel. The oil content in dried Z. morio larvae was found to be 33.80 wt %. Biodiesel from Z. morio larva oil was prepared by acid esterification followed by alkaline transesterification. The parameters of the reaction were optimized at 1.25 wt % potassium hydroxide catalyst, a 5:1 methanol to oil ratio, a reaction temperature of 50 °C, and a reaction time of 45 min. Under these conditions, the maximum fatty acid methyl ester yield was 92.35 wt %. The biodiesel obtained was verified to be in compliance with the ASTM D6751 standard. This study supports the use of Z. morio larva oil as a viable and valuable raw feedstock for biodiesel production and indicates the potential use of insects as feedstock for applications in energy production.
Co-reporter:Qingqian Zeng;Lin Jiang;Dongmei Wang;Shanshan Huang
Plant Growth Regulation 2012 Volume 68( Issue 3) pp:467-473
Publication Date(Web):2012 December
DOI:10.1007/s10725-012-9736-9
The effect of plant growth regulators (PGRs) on the accumulation of the alkaloid camptothecin (CPT) and its analogue 10-hydroxycamptothecin (HCPT) in tender leaves of Camptotheca acuminata saplings was studied. In screening experiments for PGRs, 40 mg/L dose of thiourea, triacontanol, and ascorbic acid (VC) had no positive effects on the accumulation of the alkaloids. However, treatments with 40 mg/L of chlormequat chloride (CCC), choline chloride, paclobutrazol (PBZ), and daminozide (B9) induced CPT and HCPT accumulation in both pre-harvest and postharvest stages. On that basis, five levels of PGRs at 0, 20, 40, 60, 80 mg/L were sprayed on tender leaves of C. acuminata saplings at pre-harvest and postharvest stages. Treatment by 40 mg/L CCC dramatically enhanced HCPT production by 308 % in pre-harvest, treatment by 60 mg/L CCC enhanced HCPT production by 100 % in postharvest. Spraying the leaves with 60 mg/L choline chloride resulted in 94 % increase of CPT and spraying with 40 mg/L of the PGRs reached 167 % increase of HCPT in the pre-harvest treatment, respectively; treatments with 60 mg/L choline chloride resulted in 64 % increase of CPT and 525 % increase of HCPT in postharvest, respectively. 52 % increase of CPT and 86 % increase of HCPT in pre-harvest, 22 % increase of CPT and 33 % increase of HCPT in postharvest were obtained by spraying leaves with 60 mg/L PBZ. Treatments with 40 mg/L B9 had the highest impact on CPT (12 % increase in pre-harvest, 11 % increase in postharvest) and HCPT (167 % increase in pre-harvest, 173 % increase in postharvest) accumulation. The optimal PGR for obtaining the highest levels of CPT and HCPT was treatment with 60 mg/L choline chloride. In most case, the pre-harvest treatment was better than the postharvest one. These preliminary results suggest that the application of PGRs may be a useful and feasible method to increase CPT and HCPT levels in C. acuminata.
Co-reporter:Dali Kang;Hongli Zhang;Qingqian Zeng;Xiaolu Mo
Acta Physiologiae Plantarum 2011 Volume 33( Issue 3) pp:711-716
Publication Date(Web):2011 May
DOI:10.1007/s11738-010-0595-6
Plants in their natural environment are usually affected by mechanical stress because of their sessile growth habit. This work was aimed at determining the effects of mechanical vibration on the growth rate, physiological indexes, and secondary metabolite biosynthesis of Camptotheca acuminata calli. In this study, mechanical vibrations of 1–4 Hz in frequency were applied to stimulate the C. acuminata calli; we found that a mechanical vibration of moderate frequency (2 Hz) can clearly promote the growth rate and increase the soluble protein content and superoxide dismutase (SOD) activity. Under a mechanical vibration of a 2 Hz frequency, camptothecin (CPT), the main secondary metabolite produced by C. acuminata, was increased by about fourfold compared to the control group, In contrast, the increased accumulation disappears at higher frequencies. The optimal vibration time for obtaining the highest levels of biomass and CPT was 60 min. This study showed that there are neutral frequencies and optimal periods of mechanical vibration on C. acuminata calli.
Co-reporter:Zhen Li, Van H. Tran, Rujee K. Duke, Michelle C.H. Ng, Depo Yang, Colin C. Duke
Chemistry and Physics of Lipids 2009 Volume 158(Issue 1) pp:39-45
Publication Date(Web):March 2009
DOI:10.1016/j.chemphyslip.2008.12.004
Allylic hydroxylated derivatives of the C18 unsaturated fatty acids were prepared from linoleic acid (LA) and conjugated linoleic acids (CLAs). The reaction of LA methyl ester with selenium dioxide (SeO2) gave mono-hydroxylated derivatives, 13-hydroxy-9Z,11E-octadecadienoic acid, 13-hydroxy-9E,11E-octadecadienoic acid, 9-hydroxy-10E,12Z-octadecadienoic acid and 9-hydroxy-10E,12E-octadecadienoic acid methyl esters. In contrast, the reaction of CLA methyl ester with SeO2 gave di-hydroxylated derivatives as novel products including, erythro-12,13-dihydroxy-10E-octadecenoic acid, erythro-11,12-dihydroxy-9E-octadecenoic acid, erythro-10,11-dihydroxy-12E-octadecenoic acid and erythro-9,10-dihydroxy-11E-octadecenoic acid methyl esters. These products were purified by normal-phase short column vacuum chromatography followed by high-performance liquid chromatography (HPLC). Their chemical structures were characterized by liquid chromatography–mass spectrometry (LC–MS) and nuclear magnetic resonance spectroscopy (NMR). The allylic hydroxylated derivatives of LA and CLA exhibited moderate in vitro cytotoxicity against a panel of human cancer cell lines including chronic myelogenous leukemia K562, myeloma RPMI8226, hepatocellular carcinoma HepG2 and breast adenocarcinoma MCF-7 cells (IC50 10–75 μM). The allylic hydroxylated derivatives of LA and CLA also showed toxicity to brine shrimp with LD50 values in the range of 2.30–13.8 μM. However these compounds showed insignificant toxicity to honeybee at doses up to 100 μg/bee.
Co-reporter:Xuanxuan Cheng;Dongmei Wang;Lin Jiang
Chemistry & Biodiversity 2008 Volume 5( Issue 7) pp:1335-1344
Publication Date(Web):
DOI:10.1002/cbdv.200890121

Abstract

Chemical studies of the Chinese herb Corydalis saxicolaBunting led to the isolation and identification of 14 alkaloids, 114. Seven of these compounds, 49 and 11, were obtained from this plant for the first time. Feruloylagmatine (7) is the first guanidine-type alkaloid to be identified in the family Papaveraceae and in dicotyledonous plants. All of the isolated compounds were assayed for inhibitory activity against human DNA topoisomerase I. A DNA cleavage assay demonstrated that these alkaloids specifically inhibit topoisomerase through stabilization of the enzyme–DNA complex. Among the isolated alkaloids, (−)-pallidine (8) and (−)-scoulerine (11) showed strong inhibitory activities toward topoisomerase I that were comparable to camptothecin, a typical topoisomerase I inhibitor. A preliminary structure–activity relationship study suggested that the quaternary ammonium ion might play an important role in topoisomerase I inhibition by the isoquinoline alkaloids. These data indicated that DNA topoisomerase I inhibition represents probably one of the anticarcinogenic mechanisms of C. saxicola.

Co-reporter:Zhen Li;Lin Jiang;Junfeng Ji
Bioprocess and Biosystems Engineering 2007 Volume 30( Issue 5) pp:331-336
Publication Date(Web):2007 September
DOI:10.1007/s00449-007-0129-9
Lipase-catalyzed esterification of conjugated linoleic acid (CLA) with l-carnitine in solvent-free system and acetonitrile was studied. Three lipases (Novzym 435, Amamo AY30 and Amano AYS) have been assayed as suitable biocatalysts in the reaction. It was found that Amano AY30 was the most effective biocatalyst in both solvent-free system and acetonitrile. The conversion rate varied from 8.05 to 60.9% in terms of reaction conditions such as the amount of lipase, the presence of water, the amount of molecular sieves and reaction time. The conversions of substrate in solvent-free system were higher than that in acetonitrile. When the substrates were 1 mmol CLA and 1 mmol l-carnitine, the maximum conversion (60.9%) was obtained in solvent-free system with 150 mg lipase AY30, 50% water content and 150 mg molecular sieves at the reaction time of 24 h. A novel CLA ester product was successfully isolated and characterized by ESI-MS and 1H NMR.
Co-reporter:Z.L. Liu, P. Chen, J.M. Li, S.B. Lin, D.M. Wang, L.P. Zhu, D.P. Yang
Livestock Science (November 2008) Volume 118(Issue 3) pp:255-261
Publication Date(Web):1 November 2008
DOI:10.1016/j.livsci.2008.02.002
The objective of this study is to examine whether CLA would help to improve negative responses in lactating cows during heat stress. During a 2-week adjustment period, all cows were fed a control diet supplemented with 400 g of calcium salts of palm oil fatty acids. After the adjustment period, cows (n = 9 per group) were randomly assigned by block to one of four treatments: control or three diets containing 100, 200, or 400 g of CLA (70% of which were mixed isomers of CLA). Milk fat percentage and yield decreased by supplementation of CLA (P < 0.01), but milk yield and other nutrient components did not vary (P > 0.05). The concentrations of short and medium-chain fatty acids (C4–C14) decreased and long-chain fatty acids (C18) increased in milk fat for cows fed CLA. Moreover, the contents of cis9, trans11 and trans10, cis12-CLA in milk fat increased markedly (P < 0.01). Respiration rate was lower (P < 0.05) for cows fed 200 g of CLA and rectal temperature decreased (P < 0.01) in all CLA groups during day 15 to day 28. Contents of aspartate aminotransferase, creatine kinase, thyroxin, potassium, sodium, calcium and chlorine were altered by CLA supplements, whereas other plasma parameters were not affected (P > 0.05). Lower concentrations of aspartate aminotransferase and creatine kinase in blood for cows fed 200 g or 400 g of CLA suggested that CLA protected cows from muscle damage. In addition, higher concentrations of electrolytes and thyroxin in blood in these groups suggested that CLA could improve heat stress situations in cows. Overall, the results showed that supplementations with 200 or 400 g/day of CLA moderated the negative responses in heat-stressed cows.
Co-reporter:Dongmei Wang, Jie Bai, Feng Sun, Depo Yang
Phytomedicine (May 2010) Volume 17(Issue 6) pp:410-413
Publication Date(Web):1 May 2010
DOI:10.1016/j.phymed.2009.07.015
Hypericum enshiense L. H. Wu et F. S. Wang is a new species of Hypericum occurring in China, which was first identified and denominated by our laboratory. No research has been reported on the antidepressant activity and chemical constituents of this new species. In this study, the qualitative and quantitative analyses of the chemical constituents in the hydroalcoholic extract of this species were performed using HPLC/DAD/ESI-MS online method. Hypericin, pseudohypericin and some flavonoids were identified or tentatively identified. Furthermore, H. enshiense had a high content of hypericins than H. perforatum. In addition, the antidepressant activity of the hydroalcoholic extract of the species was investigated using forced swimming test (FST) and tail suspension test (TST). The extract significantly shortened the immobility time in FST and TST, while did not alter the locomoter activity of mice. These results suggested for the first time that the hydroalcoholic extract of H. enshiense might possess potential antidepressant-like activity in the animal behavioral models, and this species might act as a new potential resource for developing antidepressants to treat depressive disorders.
Co-reporter:Yi Niu, Dong Zheng, Binghua Yao, Zizhe Cai, Zhimin Zhao, Shengqing Wu, Peiqing Cong, Depo Yang
Waste Management (March 2017) Volume 61() pp:455-460
Publication Date(Web):1 March 2017
DOI:10.1016/j.wasman.2016.10.054
•A novel method for treatment of food waste.•The value-added products (maggot protein and oil) were attained from the food waste disposal progression.•A new kind of biodiesel was prepared with the maggot oil.Food waste, as a major part of the municipal solid waste has been generated increasingly worldwide. Efficient and feasible utilization of this waste material for productivity process is significant for both economical and environmental reasons. In the present study, Musca domestica larva was used as the carrier to conduct a bioconversion with food waste to get the value-added maggot protein, oil and organic fertilizers. Methods of adult flies rearing, culture medium adjuvant selection, maggot culture conditions, stocking density and the valorization of the waste have been explored. From the experimental results, every 1000 g culture mediums (700 g food waste and 300 g adjuvant) could be disposed by 1.5 g M. domestica eggs under proper culture conditions after emergence in just 4 days, 42.95 ± 0.25% of which had been consumed and the culture medium residues could be used as good organic fertilizers, accompanying with the food waste consumption, ∼53.08 g dried maggots that contained 57.06 ± 2.19% protein and 15.07 ± 2.03% oil had been produced. The maggot protein for its outstanding pharmacological activities is regarded as a good raw material in the field of medicine and animal feeding. Meanwhile, the maggot oil represents a potential alternative feedstock for biodiesel production. In our study, the maggot biodiesel was obtained after the procedure of transesterification reaction with methanol and the productivity was 87.71%.
Co-reporter:Yang Depo, Ji Junfeng, Huang Yongping, Lu Binshan, Liang Linhua
World Science and Technology (April 2010) Volume 12(Issue 2) pp:155-159
Publication Date(Web):1 April 2010
DOI:10.1016/S1876-3553(11)60013-6
Ecocare methodology is a science of health care, which focuses on human health and the relationship between human body and its external environment using modern ecological balance theory and basic theory of traditional Chinese medicine (TCM). It is the reflection of natural healthy principle of “correspondence between man and universe,” the concept of holism of “body-soul unity,” the idea of “prevention treatment of disease” that prevention is more important than therapy and the methodology of treatment combined with rehabilitation through care, rest, and nourishment and treatment focusing on relieving both the secondary and primary symptoms. In this system, its core values are a healthy attitude (Yang xin). Everyone should first determine his or her own appropriate ecological niche well, which is the best way to promote healthy and harmonious development. The core connotation of Ecocare is the balance of body ecosystem that is to achieve a relative balance between yin and yang of human tissue, organ, physiology, and psychology by removing the disadvantageous factors, replenishing the advantageous ones, and adjusting the body functions. The theory of Ecocare can be widely used in clinical TCM, health care by Chinese medicine, and research and development of TCM health products, as well as in agriculture, gardens, landscape, and leisure vacation designs for the demands of health care by Chinese Materia Medica.
Co-reporter:Jin-Yun Liu, Zhong Liu, Dong-Mei Wang, Man-Mei Li, Shao-Xiang Wang, Rui Wang, Jian-Ping Chen, Yi-Fei Wang, De-Po Yang
Chemico-Biological Interactions (25 April 2011) Volume 190(Issues 2–3) pp:91-101
Publication Date(Web):25 April 2011
DOI:10.1016/j.cbi.2011.02.026
Hyperforin is an abundant phloroglucinol-type constituent isolated from the extract of the flowering upper portion of the plant Hypericum perforatum L. The dicyclohexylammonium salt of hyperforin (DCHA-HF) has exhibited antitumor and antiangiogenic activities in various cancer cells. Here, the antitumor effects of DCHA-HF on the chronic myeloid leukemia K562 cell line were investigated for the first time. DCHA-HF exhibited dose- and time-dependent inhibitory activities against K562 cells, with IC50 values of 8.6 and 3.2 μM for 48 h and 72 h of treatment, respectively, which was more effective than that of the hyperforin. In contrast, little cytotoxic activity was observed with DCHA-HF on HUVECs. DCHA-HF treatment resulted in induction of apoptosis as evidenced from DNA fragmentation, nuclear condensation and increase of early apoptotic cells by DAPI staining analysis, TUNEL assay and Annexin V-FITC/PI double-labeled staining analysis, respectively. Moreover, DCHA-HF elicited dissipation of mitochondrial transmembrane potential that commenced with the release of cytochrome c through down-regulation of expression of anti-apoptotic proteins and up-regulation of expression of pro-apoptotic proteins. DCHA-HF treatment induced activation of the caspase 3, 8, and 9 cascade and subsequent PARP cleavage, and DCHA-HF-induced apoptosis was significantly inhibited by caspase inhibitors. Treated cells were arrested at the G1 phase of the cell cycle and the expression of p53 and p27Kip1, two key regulators related to cell cycle and apoptosis, was up-regulated. These results suggest that DCHA-HF inhibits K562 cell growth by inducing caspase-dependent apoptosis mediated by a mitochondrial pathway and arresting the cell cycle at the G1 phase. Therefore, DCHA-HF is a potential chemotherapeutic antitumor drug for chronic myeloid leukemia therapy.
Cerberic acid B
4-(6,6-dimethyl-4-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-indazol-1-yl)-2-((1r,4r)-4-hydroxycyclohexylamino)benzamide
Caspase-9
Caspase-3
2-ETHOXY-1-METHYLNAPHTHALENE
GENIPOSIDIC ACID
Isobutyryl-L-carnitine