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Bio-derived and biocompatible nanogels based on poly(lactic acid) (PLA) and silk sericin (SS) have been synthesized for the first time.

Background and aim Metabolic disease encompasses most contemporary non-communicable diseases, especially cardiovascular and fatty liver disease. Mulberry fruits of Morus alba L. are a favoured food and a traditional medicine. While they are anti-atherosclerotic and reduce hyperlipidemic risk factors, studies need wider scope that include ameliorating cardiovascular and liver pathologies if they are to become clinically effective treatments. Therefore, the present study sought to show that freshly dried mulberry fruits (dMF) might counteract the metabolic/cardiovascular pathologies in mice made hyperlipidemic by high-fat diet (HF). Experimental procedure C57BL/6J mice were fed for 3 months with either: i) control diet, ii) HF, iii) HF+100 mg/kg dMF, or iv) HF+300 mg/kg dMF. Body weight gain, food intake, visceral fat accumulation, fasting blood glucose, plasma lipids, and aortic, heart, and liver histopathologies were evaluated. Adipocyte lipid accumulation, autophagy, and bile acid binding were also investigated. Results and conclusion HF increased food intake, body weight, visceral fat, plasma total cholesterol (TC) and low-density lipoprotein (LDL), TC/HDL ratio, blood glucose, aortic collagen, arterial and cardiac wall thickness, and liver lipid. Both dMF doses prevented hyperphagia, body weight gain, and visceral fat accumulation, lowered blood glucose, plasma TG and unfavourable TC/HDL and elevated plasma HDL beyond baseline. Arterial and cardiac wall hypertrophy, aortic collagen fibre accumulation and liver lipid deposition ameliorated in dMF-fed mice. Clinical trials on dMF are worthwhile but outcomes should be holistic commensurate with the constellation of disease risks. Here, dMF should supplement the switch to nutrient-rich from current energy-dense diets that are progressively crippling national health systems., Graphical abstract Image 1, Highlights • Uses modest amounts of whole unextracted mulberries as in traditional medicine. • Studies important pathologies found in metabolic syndrome, the number one challenge to modern medicine. • dMF reduces risk factors associated with dyslipidemia. • dMF prevents weight gain, visceral fat and hepatic fat accumulation with fatty diets. • dMF ameliorates vascular fibrosis and cardiac hypertrophy, thereby preventing myocardial infarction risk.

Reduction of intestinal glucose absorption might result from either delayed carbohydrate digestion or blockage of glucose transporters. Previously, oxyresveratrol was shown to inhibit α-glucosidase, but its effect on glucose transporters has not been explored. The present study aimed to assess oxyresveratrol-induced inhibition of the facilitative glucose transporter 2 and the active sodium-dependent glucose transporter 1. An aqueous extract of Artocarpus lacucha, Puag Haad, which is oxyresveratrol-enriched, was also investigated. Glucose transport was measured by uptake into Caco-2 cells through either glucose transporter 2 or sodium-dependent glucose transporter 1 according to the culture conditions. Oxyresveratrol (40 to 800 µM) dose-dependently reduced glucose transport, which appeared to inhibit both glucose transporter 2 and sodium-dependent glucose transporter 1. Puag Haad at similar concentrations also inhibited these transporters but with greater efficacy. Oxyresveratrol and Puag Haad could help reduce postprandial hyperglycemic peaks, which are considered to be most damaging in diabetics.

Non-alcoholic fatty liver disease (NAFLD) has become a major world-wide health problem and is characterized by lipid accumulation in the liver induced by high fat diet (HFD) consumption. It is usually associated with inflammation, oxidative stress, and insulin resistance. Roselle extract (Hibiscus sabdariffa) is an herb which is used in traditional medicine. However, further study is necessary to represent the mechanism of NAFLD and find new preventive strategies. This study aims to investigate the protective effects of roselle extract on NAFLD rat models. Male Sprague–Dawley rats (n = 35) were divided into 5 groups, control, HFD, HFD + Simvastatin (HFD + SIM), HFD + 250 mg/kg BW, and HFD + 500 mg/kg BW of roselle extract (HFD + R250 and HFD + R500, respectively). The results showed that roselle extract reduced hepatic lipid contents, de novo lipogenesis enzymes, microsomal triglyceride transfer protein, inflammatory cytokines, malondialdehyde, and increased antioxidant properties, transporter related with lipoprotein uptake, and insulin signal proteins. Comparing to SIM, the HFD + R500 group exhibited the greater benefit in terms of anti-hepatic steatosis, antioxidant properties, and an ability to improve insulin resistance. This study demonstrates that roselle extract improved antioxidant properties and attenuated hepatic steatosis, liver inflammation, oxidative stress, and insulin resistance in HFD-induced NAFLD in rats, which could be used for NAFLD prevention.

In this work, a novel semi-interpenetrating polymer network (semi-IPN) hydrogel scaffold based on silk sericin (SS) and poly(N-hydroxyethyl acrylamide) (PHEA) was successfully fabricated via conventional free-radical polymerization. The porous structure of the scaffolds was introduced using a lyophilization technique and the effect of cross-linker (XL) on morphology, gelation time and physical properties of hydrogel scaffold was first studied. The results show that using low cross-linker content (0.125, 0.25 and 0.5 wt% XL) produced flexible scaffolds and appropriate gelation times for fabricating the scaffold. Therefore, the polymerization system with a constant percentage of XL at 0.5 wt% was chosen to study further the effect of SS on the physical properties and cell culture of the scaffolds. It was observed that the hydrogel scaffold of PHEA without SS (PHEA/SS-0) had no cell proliferation, whereas hydrogel scaffolds with SS enhanced cell viability when compared to the positive control. The sample of PHEA/SS at 1.25 wt% of SS and 0.5 wt% of cross-linker was the most suitable for HFF-1 cells to migrate and cell proliferation due to possessing a connective porous structure, along with silk sericin. The results proved that this novel porous semi-IPN hydrogel has the potential to be used as dermal reconstruction scaffold.

Hypercholesterolemia has been considered as a risk factor for Alzheimer’s disease (AD). In addition to low density lipoprotein (LDL), oxidized LDL plays some roles in AD pathology. Neurodegenerative effect of oxidized LDL was supported by the increased oxidative stress in neurons. To further investigate the role of oxidized LDL, the present study aimed to test its effect on amyloid precursor protein (APP) processing. The release of soluble APP (sAPP) was evaluated in differentiated SH-SY5Y neuroblastoma cells exposed to native (non-oxidized) or oxidized human LDL including mildly and fully oxidized LDL (mox- and fox-LDL). Non-amyloidogenic and amyloidogenic pathways were investigated using specific antibody against sAPPα and sAPPβ. The results demonstrate that oxidized LDL induced neuronal death in dose-dependent patterns. Mox-LDL mediated caspase-3 dependent apoptosis, whereas fox-LDL notably damaged cell membrane. At subtoxic concentration, only native but not oxidized LDL induced the release of sAPP dominantly in amyloidogenic pathway with no change in β-secretase activity. These results suggest that LDL and oxidized LDL play critical roles in AD pathogenesis via different pathways. Elevated serum LDL level together with high oxidative stress may aggravate the progression of AD.

The main risk of cardiovascular diseases comes from incorrect eating habits. Restricting unhealthy diets is hard for most people; an alternative dietary intervention is necessary. Dietary products ...

The beneficial effect of cholesterol-lowering proteins and/or peptides derived from various dietary sources is continuously reported. A non-dietary protein from silk cocoon, sericin, has also demonstrated cholesterol-lowering activity. A sericin hydrolysate prepared by enzymatic hydrolysis was also expected to posses this effect. The present study was aimed at investigating the cholesterol-lowering effect of sericin peptides, so called “sericin-derived oligopeptides” (SDO) both in vivo and in vitro. The results showed that SDO at all three doses tested (10 mg kg−1 day−1, 50 mg kg−1 day−1, and 200 mg kg−1 day−1) suppressed serum total and non-HDL cholesterol levels in rats fed a high-cholesterol diet. Triglyceride and HDL-cholesterol levels were not significantly changed among all groups. The fecal contents of bile acids and cholesterol did not differ among high-cholesterol fed rats. SDO dose-dependently reduced cholesterol solubility in lipid micelles, and inhibited cholesterol uptake in monolayer Caco-2 cells. SDO also effectively bound to all three types of bile salts including taurocholate, deoxytaurocholate, and glycodeoxycholate. Direct interaction with bile acids of SDO may disrupt micellar cholesterol solubility, and subsequently reduce the absorption of dietary cholesterol in intestines. Taking all data together, SDO or sericin peptides exhibit a beneficial effect on blood cholesterol levels and could be potentially used as a health-promoting dietary supplement or nutraceutical product.

The present study aims to investigate the effects of five dietary plants including Azadirachta indica A. Juss. var. siamensis Valeton (flowers), Bombax ceiba Linn (pollen), Citrus hystrix DC (leaves), Polygonum odoratum Lour (leaves), and Solanum torvum Sw (fruits) on activity of pancreatic lipase, micellar cholesterol solubilization and bile acids binding. Two different organic solvents (methanol and ethanol) and distilled water (H2O) were used for plants extraction. Crude extracts in different solvents can inhibit pancreatic lipase activity especially, the ethanolic extracts of P. odoratum which exhibited the strongest activity with IC50 value of 6.04 mg/mL. Aqueous extract of P. odoratum reduced cholesterol solubility by approximately 86%. Ethanolic extract of S. torvum had the highest ability to bind to taurodeoxycholic acid upto 97%. Ethanolic and methanolic extracts of P. odoratum bound to taurocholic acid 75% and glycodeoxycholic acid 40%, respectively. These findings suggest that lipid lowering activity of these plants were distinguished by organic solvents and water extraction. Key words: Dietary plant, cholesterol, pancreatic lipase, micelles solubility, bile acid binding

Background Spirogyra neglecta (SN) has many nutritional benefits and it is commonly used to ameliorate different human conditions including inflammation, gastric ulcer, hyperglycemia, and hyperlipidemia. However, the mechanism of the hypocholesterolemic effect of SN still remains unclear. Therefore, the present study was aimed to evaluate the effect of SN extract particularly on cholesterol absorption and synthesis mechanisms. Methods For cholesterol absorption, the uptake of cholesterol was measured by using tritium radiolabeling of cholesterol in Caco-2 cells. Bile acid binding, micelles size, and cholesterol solubility were analyzed in in vitro assays, while cholesterol synthesis was evaluated by using a 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase assay kit. Results SN extract was found to decrease cholesterol uptake in Caco-2 cells and decreased the solubility of cholesterol in micelles. The SN extract bound to taurocholate, taurodeoxycholate, and glycodeoxycholate bile acids, and increased micelles size. SN has also demonstrated an inhibitory effect on HMG-CoA reductase (HMGR) enzymatic activity. For further experimentation, the treatment combination of SN and ezetimibe (0.04mg/mL) showed a greater significant reduction in cholesterol uptake than the extract alone. Conclusion These observations suggested that inhibitory cholesterol absorption effects of SN could be mediated through the modulation of size and solubility of cholesterol micelles, resulting in interference of cholesterol uptake. In addition, SN inhibited the rate limiting step of cholesterol synthesis. This study provides supporting evidence for the potential usage of SN as a cholesterol lowering agent.

This work is concerned with the study of the conformational structure and crystallinity of sericin from silk cocoon ( Bombyx mori ) and the role these play in the physical and chemical properties of the final materials. Silk sericin (SS) powders were prepared by degumming processes with different storage temperatures before drying into the final powders; defined as RT-SS (room, 25 °C), C-SS (10 °C) and F-SS (freezing, 0 °C), and then fabricated into films and scaffolds by reacting with poly(vinyl alcohol) (PVA) in the presence of a new cross-linker (dimethylolurea; DMU). RT-SS and C-SS structures favour random coil structuring as witnessed by Amide I (C O stretching), II (N H bending) and III (in phase combination of N H in plane-bending and C N stretching vibrations) being observed at 1661, 1538, and 1232 cm −1 , respectively. Whereas, F-SS favours β-sheets structure proved by the amide bands shifting to a lower frequency. The N H stretching (3200–2400 cm −1 ) of F-SS is also observed at a lower frequency with a broader band than RT-SS and C-SS due to the hydrogen bonding in the β-sheets. The differences in the X-ray peaks between RT- and C-SS ( d spacing = 1.9–5.2 A) and F-SS ( d spacing = 3.0 A and 5.2–8.2 A) were also measured. Films of PVA/RT-SS/DMU showed better properties than that of PVA/F-SS/DMU films in terms of the interactions (hydrogen bonding) between the components that formed the network. Therefore, RT-SS was chosen for the preparation of 3D porous scaffolds with different concentrations of DMU. All scaffolds showed good support for skin fibroblast cells, as well as promoted cell proliferation. However, a minimal amount of cross-linker, 10% DMU PVA/RT-SS scaffold with average pore diameter between 20 and 30 μm, was the best composition for cell viability and cell adhesion. In this work, therefore, a novel scaffold based on biomaterials was explored for tissue engineering scaffolds with the potential to be a new technology platform for skin tissue regeneration.

This study was to assess the impact of different colors of coffee fruit (green, yellow and red) on adipogenesis and/or lipolysis using 3T3-L1 adipocytes. Characterization of chemical constituents in different colors of coffee fruit extracts was determined by ESI-Q-TOF-MS. The cytotoxicity of the extracts in 3T3-L1 preadipocytes were evaluated by MTT assay. Oil-red O staining and amount of glycerol released in 3T3-L1 adipocytes were measured for lipid accumulation and lipolysis activity. All coffee fruit extracts displayed similar chromatographic profiles by chlorogenic acid > caffeoylquinic acid > caffeic acid. Different colors of raw coffee fruit possessed inhibitory adipogenesis activity in 3T3-L1 adipocytes, especially CRD decreased lipid accumulation approximately 47%. Furthermore, all extracts except CYF and their major compounds (malic, quinic, and chlorogenic acid) increased glycerol release. Our data suggest that different colors of coffee fruit extract have possessed anti-adipogenic and lipolytic properties and may contribute to the anti-obesity effects.

Enhancing of radioresponsiveness of tumors by using radiosensitizers is a promising approach to increase the efficacy of radiation therapy. Recently, the ethanolic extract of the medicinal plant, Derris scandens Benth has been identified as a potent radiosensitizer of human colon cancer HT29 cells. However, cell death mechanisms underlying radiosensitization activity of D scandens extract have not been identified. Here, we show that treatment of HT-29 cells with D scandens extract in combination with gamma irradiation synergistically sensitizes HT-29 cells to cell lethality by apoptosis and mitotic catastrophe. Furthermore, the extract was found to decrease Erk1/2 activation. These findings suggest that D scandens extract mediates radiosensitization via at least two distinct modes of cell death and silences pro-survival signaling in HT-29 cells.

In this study, Pasteurella multocida-loaded alginate microparticles (MPs) for subcutaneous vaccination was developed by emulsification-cross-linking technique. Formulation parameter was varied as a ratio of polymer and bacterin. Optical microscopy revealed spherical particles with uniformly distribution. A mean particle size of approximately 6 µm has been successfully constructed using simple mixer and ultrasonic probe. The zeta potential of the MPs showed negatively charge of approximately -23 mV determined by Zeta Pals® analyzer. The entrapment efficiency and the in vitro bacterin released profile could be controlled by varying the amount of alginate. The high entrapment efficiency up to 69% was achieved with low concentration of alginate. The MPs possessed a slow bacterin release profile, up to 30 days. In vivo safety and potency tests were proved that the alginate MPs were safe and induced protective immunity in mice. In addition, after storage for 6 months at either 4 °C or room temperature, the protective immunity in mice was maintained.

Carotenoids are efficient antioxidants that are of great importance for human health. Lutein and zeaxanthin are carotinoids present in high concentrations in the human retina which are involved in the photoprotection of the human eye. Lutein may also protect the skin from ultraviolet (UV)-induced damage. The present study investigated the protective effect of lutein extracted from yellow silk cocoons of Bombyx mori on human keratinocytes against UVB irradiation. A human keratinocyte cell line and primary human keratinocytes were used to investigate the UVB protection effects of silk lutein and plant lutein. Silk lutein showed no cytotoxicity to keratinocytes. Treatment with silk lutein prior to UVB irradiation enhanced cell viability and cell proliferation, and reduced cell apoptosis. The protective effects of silk lutein may be superior to those of plant lutein. Silk lutein may have a benefit for protection of keratinocytes against UVB-irradiation.

Colon cancer is one of the most common cancers in many regions of the world and is prevented by dietary interventions. This study aimed to examine the chemopreventive effect of silk protein, sericin, against 1,2-dimethylhydrazineinduced colon tumorigenesis in rats in comparison with control casein diet. The result showed that 5 out of 14 of casein fed rats developed colon tumors, whereas only 1 from 14 sericin fed rats exhibited tumors. Consumption of sericin prior to or during carcinogen exposure reduced the number of aberrant crypt foci. In addition to crypt number, crypt multiplicity was less progressive in sericin fed group. The sericin diet also exhibited anti-oxidant activity as evidenced by reduced lipid peroxidation in the colons. This finding suggests that consumption of sericin may reduce the progression of colon tumor development possibly by suppressing the initiation and promotion stages of colon tumorigenesis.

Six sesquiterpenes: germacrone (1), zederone (2), dehydrocurdione (3), curcumenol (4), zedoarondiol (5) and isocurcumenol (6) were isolated from rhizomes of Curcuma aeruginosa Roxb. (Zingiberaceae). They inhibited 5α-reductase which converts testosterone to dihydrotestosterone (DHT). Germacrone (1) was the most potent (IC(50)=0.42±0.05 mg/mL). Compound 1 was anti-androgenic in LNCaP cells when proliferation was testosterone-induced. The growth of flank gland of male Syrian hamsters is dependent on circulating androgen and when maintained with testosterone, 1 (3, 30, 100μg) inhibited growth but was ineffective against DHT. The similar activity profile was observed on the 5α-reductase inhibitor, finasteride (100 μg) treatment group. The androgen receptor binding assay showed that 1 did not bind to the androgen receptor. In conclusion, 1 showed anti-androgenic effect on in vitro and in vivo assays. One of the possible mechanisms was inhibition 5α-reductase activity. Thus, 1 is a potential lead compound for treatment of androgen-dependent disorders.

The ethanolic extract from stems of a Thai medicinal plant, Alstonia macrophylla Wall. ex G. Don (Apocynaceae) showed a significant inhibitory effect on acetylcholinesterase (AChE) determined by using Ellman assay. Four compounds i.e., a bisindole alkaloid, macralstonine (1), a new bisindole alkaloid, thungfaine (2), a secoiridoid glycoside, sweroside (3) and a new secoiridoid glycoside, naresuanoside (4) were isolated. Compound 4 showed moderate AChE and butyrylcholinesterase (BChE) inhibitory effects. Interestingly, compound 4 inhibited cell growth on human androgen-sensitive prostate cancer cell line (LNCaP) but no effect on viability of human foreskin fibroblast cells (HF).

A cholesterol lowering effect of sericin was investigated both in vivo and in vitro. Rats were dosed with cholesterol with and without sericin for 14 days. Non-high-density lipoprotein (HDL) and total serum cholesterols were reduced in rats fed high-cholesterol diet with all three tested doses of sericin (10, 100, and 1000 mg kg(-1) day(-1)). The potential mechanism of actions was determined by measuring the uptake of radiolabeled cholesterol into differentiated Caco-2 cells and cholesterol solubility in mixed lipid micelles. Concentration of sericin as low as 25 and 50 μg/mL inhibited 30% of cholesterol uptake into Caco-2 cells whereas no effect was found at higher concentration. Cholesterol micellar solubility was reduced in the presence of sericin. This study suggests the cholesterol lowering effect of sericin results from its inhibition of cholesterol absorption in intestinal cells and its reduction of cholesterol solubility in lipid micelles.

Artocarpus lakoocha is a traditional plant found in South/Southeast Asia, which has been used for centuries as antelmenthic in form of an aqueous extract. This extract, also called puag haad in Thailand, contains oxyresveratrol, a stilbene, as a major active compound of puag haad. To evaluate biological activity of these tested compounds, cytotoxicity study was conducted to determine proper doses of the tested compounds in SH-SY5Y neuroblastoma cells. SH-SY5Y cells are a neuroblastoma cell line which can be used to study several neurodegenerative diseases in cell cultural models. This study aimed to examine cytotoxicity of A. lakoocha aqueous extract and oxyresveratrol in SH-SY5Y neuroblastoma cells by XTT and LDH assays. The result of this study demonstrated that ≤25µg/ml of puag haad and ≤200 µM of oxyresveratrol did not show toxicity to SH-SY5Y neuroblastoma cells. The concentrations at ≤25µg/ml of puag haad and ≤200 µM of oxyresveratrol could be used to investigate neuroprotective effect using SH-SY5Y neuroblastoma cells. Further studies are required to investigate the effect of A. lakoocha aqueous extract and oxyresveratrol related to neurodegenerative disease in cell culture system

Aim of the study Bacopa monnieri (Brahmi) is extensively used in traditional Indian medicine as a nerve tonic and thought to improve memory. To examine the neuroprotective effects of Brahmi extract, we tested its protection against the beta-amyloid protein (25–35) and glutamate-induced neurotoxicity in primary cortical cultured neurons. Materials and Methods Neuroprotective effects were determined by measuring neuronal cell viability following beta-amyloid and glutamate treatment with and without Brahmi extract. Mechanisms of neuroprotection were evaluated by monitoring cellular oxidative stress and acetylcholinesterase activity. Results Our result demonstrated that Brahmi extract protected neurons from beta-amyloid-induced cell death, but not glutamate-induced excitotoxicity. This neuroprotection was possibly due to its ability to suppress cellular acetylcholinesterase activity but not the inhibition of glutamate-mediated toxicity. In addition, culture medium containing Brahmi extract appeared to promote cell survival compared to neuronal cells growing in regular culture medium. Further study showed that Brahmi-treated neurons expressed lower level of reactive oxygen species suggesting that Brahmi restrained intracellular oxidative stress which in turn prolonged the lifespan of the culture neurons. Brahmi extract also exhibited both reducing and lipid peroxidation inhibitory activities. Conclusions From this study, the mode of action of neuroprotective effects of Brahmi appeared to be the results of its antioxidant to suppress neuronal oxidative stress and the acetylcholinesterase inhibitory activities. Therefore, treating patients with Brahmi extract may be an alternative direction for ameliorating neurodegenerative disorders associated with the overwhelming oxidative stress as well as Alzheimer's disease.

A new nanoparticulate delivery system for amphotericin B (AmB) has been developed by means of the polyelectrolyte complexation technique. Two opposite charged polymers were used to form nanoparticles through electrostatic interaction, chitosan (CH) as a positively charged polymer and dextran sulfate (DS) as a polymer with a negative charge, together with zinc sulfate as a crosslinking and hardening agent. The AmB nanoparticles obtained possessed a mean particle size of 600-800 nm with a polydispersity index of 0.2, indicating a narrow size distribution. The measured zeta potential of the nanoparticle surface was approximately -32 mV indicating a strong negative charge at the particle's surface. Scanning electron microscopy revealed spherical particles with a smooth surface. Drug association efficacy of up to 65% was achieved. Dissolution studies demonstrated a fast release behavior suggesting that AmB exhibits only moderate interaction with the weakly crosslinked polymers of the nanoparticles. Although, electronic absorbance spectra showed that the aggregation state of AmB was modified within the nanoparticles, a reduction of nephrotoxicity was observed in an in vivo renal toxicity study.

Oxidative stress (OS) causes extensive cell death in the CA1 but not the CA3 region of the hippocampus. We found that the CA1 region of hippocampus explants, cultured under normal conditions, had significantly higher superoxide levels and expressed both anti-oxidant genes and genes related to the generation of reactive oxygen species at significantly higher levels than the CA3. These observations were indicative of high intrinsic OS in CA1.

Objective: Artocarpus lakoocha Roxb. is a traditional medical plant native to Southeast Asia and used as a dried aqueous extract so-called puag haad. Its role (and its major ingredient, oxyresveratrol) as an antioxidant neuroprotectant were explored. Methods: Differentiated SH-SY5Y neuroblastoma cells in 96-well plates were challenged with 200 µM H 2 O 2 for 4 h and either Trolox (100 µM), oxyresveratrol (5-100 µM), or puag haad (1.2-25 µg/ml) applied 2 h before H 2 O 2 or for 20 h after H 2 O 2 washout. Cell viability, mitochondrial function, intracellular ROS, and lipid peroxidation were assessed. Results: Continuous presence of both H 2 O 2 and antioxidant reduced mitochondrial function by ~50% but only by 30% with antioxidant. Sustained 24 h H 2 O 2 showed no recoveries with antioxidants. Cell viability was modestly restored when antioxidants accompanied H 2 O 2 for 4 h and both washed for another 20 h, but little recovery of mitochondrial function even though antioxidants removed ROS and prevent lipid peroxidation. Antioxidants added for 20 h after H 2 O 2 marginally improve mitochondria and modestly restore cell viability, but lipid peroxidation was completely reversed. Conclusion: These results show that mitochondrial protection was illusive, yet both tested compounds, puag haad and oxyresveratrol, improved cell viability and especially ROS levels and lipid peroxidation. The potency oxyresveratrol on the redox-sensitive expression of antioxidant enzymes and its pharmacokinetics suggests that oral puag haad could provide effective protection in transient neurodegenerative disease.

Hyperlipidemia, low density lipoproteins (LDL) and their oxidized forms, and oxidative stress are suspected to be a key combination in the onset of AD and acetylcholinesterase (AChE) plays a part in this pathology. The present study aimed to link these parameters using differentiated SH-SY5Y human neuroblastoma cells in culture. Both mildly and fully oxidized human LDL (mox- and fox-LDL), but not native (non-oxidized) LDL were cytotoxic in dose- and time-dependent patterns and this was accompanied by an increased production of intracellular reactive oxygen species (ROS). Oxidized LDL (10-200 μg/mL) augmented AChE activity after 4 and 24h treatments, respectively while the native LDL was without effect. The increased AChE with oxidized LDLs was accompanied by a proportionate increase in intracellular ROS formation (R=0.904). These findings support the notion that oxidized LDLs are cytotoxic and that their action on AChE may reduce central cholinergic transmission in AD and affirm AChE as a continued rational for anticholinesterase therapy but in conjunction with antioxidant/antihyperlipidemic cotreatments.

Ethnopharmacological relevance Bacopa monnieri has a long history in Ayurvedic medicine for neurological and behavioral defects. To assess its efficacy in improving cognitive function. Materials and methods MEDLINE, EMBASE, CINAHL, AMED, Cochrane Central of clinical trial, WHO registry, Thai Medical Index, Index Medicus Siriraj library and www.clinicaltrial.gov were searched from the inception date of each database to June 2013 using scientific and common synonyms of Bacopa monnieri , cognitive performance or memory. The reference lists of retrieved articles were also reviewed. Randomized, placebo controlled human intervention trials on chronic ≥12 weeks dosing of standardized extracts of Bacopa monnieri without any co-medication were included in this study. The methodological quality of studies was assessed using Cochrane's risk of bias assessment and Jadad's quality scales. The weighted mean difference and 95% confidence interval (95% CI) were performed using the random-effects model of the Dersimonian–Laird method. Results Nine studies met the inclusion criteria using 518 subjects. Overall quality of all included trials was low risk of bias and quality of reported information was high. Meta-analysis of 437 eligible subjects showed improved cognition by shortened Trail B test (−17.9 ms; 95% CI −24.6 to −11.2; p p Conclusion This meta-analysis suggests that Bacopa monnieri has the potential to improve cognition, particularly speed of attention but only a large well designed ‘head-to-head’ trial against an existing medication will provide definitive data on its efficacy on healthy or dementia patients using a standardized preparation.

Objectives Curcuma aeruginosa Roxb. extract is a 5α-reductase antagonist that can be used to treat hair loss. We aimed to study the stability of antiandrogenic constituents, germacrone and other sesquiterpene components in the extract. Methods Germacrone and the extract were analyzed as solid forms or solublized with polyethylene glycol-40 (PEG-40) or methanol using high-performance liquid chromatography and gas chromatography with flame ionization detector. The effects of pH, temperature and light on their stability were studied. Key findings Degradation of antiandrogenic compounds in C. aeruginosa was highly sensitive to temperature especially pure anhydrous germacrone, which was completely lost within 3 days at 45°C. Curiously, degradation was slower than as a dried extract. Paradoxically, when solubilized with PEG-40, it was largely intact even after 90 days at 45°C. The MS spectrum of a major degradation product suggested that it was elemenone probably produced by Cope rearrangement. Two other putative degradation products were germacrone-1,10-epoxide and germacrone-4,5-epoxide suggesting that oxidation of double bonds was an important mechanism. Germacrone stability was unaffected by pH (2.0–9.0) but only as dried extract it was slightly degraded by light. Conclusion Antiandrogenic constituents of C. aeruginosa were instable at high temperature and in solid form. Thus, the extract would be optimately stored as a solution or otherwise as solid form at low temperature.

Black pepper (Piper nigrum L.) lowers blood lipids in vivo and inhibits cholesterol uptake in vitro, and piperine may mediate these effects. To test this, the present study aimed to compare actions of black pepper extract and piperine on (1) cholesterol uptake and efflux in Caco-2 cells, (2) the membrane/cytosol distribution of cholesterol transport proteins in these cells, and (3) the physicochemical properties of cholesterol micelles. Piperine or black pepper extract (containing the same amount of piperine) dose-dependently reduced cholesterol uptake into Caco-2 cells in a similar manner. Both preparations reduced the membrane levels of NPC1L1 and SR-BI proteins but not their overall cellular expression. Micellar cholesterol solubility of lipid micelles was unaffected except by 1 mg/mL concentration of black pepper extract. These data suggest that piperine is the active compound in black pepper and reduces cholesterol uptake by internalizing the cholesterol transporter proteins.

Sericin is a silk protein woven from silkworm cocoons (Bombyx mori). In animal model, sericin has been reported to have anti-tumoral action against colon cancer. The mechanisms underlying the activity of sericin against cancer cells are not fully understood. The present study investigated the effects of sericin on human colorectal cancer SW480 cells compared to normal colonic mucosal FHC cells. Since the size of the sericin protein may be important for its activity, two ranges of molecular weight were tested. Sericin was found to decrease SW480 and FHC cell viability. The small sericin had higher anti-proliferative effects than that of the large sericin in both cell types. Increased apoptosis of SW480 cells is associated with increased caspase-3 activity and decreased Bcl-2 expression. The anti-proliferative effect of sericin was accompanied by cell cycle arrest at the S phase. Thus, sericin reduced SW480 cell viability by inducing cell apoptosis via caspase-3 activation and down-regulation of Bcl-2 expression. The present study provides scientific data that support the protective effect of silk sericin against cancer cells of the colon and suggests that this protein may have significant health benefits and could potentially be developed as a dietary supplement for colon cancer prevention.

Several Thai spices/dietary ingredients were previously shown to have hypocholesterolaemic effects. These studies were mostly conducted in animal models in which the mechanisms of action were not yet well-established. Therefore, this study aimed to investigate the potential mechanism of hypocholesterolaemic action of 12 selected plants, namely Hibiscus sabdariffa L., Moringa oleifera Lam., Cucurbita moschata Duchesne, Ananas comosus (L.) Merr., Zingiber officinale, Morus alba L., Camellia sinensis (L.) Kuntze, Piper nigrum L., Alpinia galanga (L.) Willd., Curcuma zedoaria Rose, Bacopa monnieri (L.) Wettst. and Piper retrofractum Vahl., widely used as spices and ingredients in various types of Thai food. The extract of P. nigrum at 100 µg mL(-1) was found to be the most effective cholesterol uptake inhibitor whereas those of A. galanga and C. sinensis effectively inhibited pancreatic lipase activity with IC50 values of 8.99±3.41 and 12.36±1.23 µg mL(-1), respectively. The potency of extracts from H. sabdariffa, M. oleifera and C. moschata at 100 µg mL(-1) were found to be similar to 0.4 µg mL(-1) pravastatin in inhibiting HMG-CoA reductase and possibly reduced cholesterol biosynthesis. This study also demonstrated that several of the tested plants possessed multiple sites of action that were possibly responsible for their cholesterol-lowering effect in the in vivo model.

Introduction Phosphodiesterases (PDEs) are a group of enzymes that have powerful effects on cellular signaling because they regulate the second messenger, cAMP or cGMP. PDE inhibitors have been used for treatment of many indications such as cardiovascular diseases, chronic obstructive pulmonary diseases, erectile dysfunction and pulmonary hypertension. The aim of the study The aim of the study was to search for sources of PDE inhibitors from Thai biodiversity. Materials and methods Some Thai medicinal plants used as aphrodisiac and neurotonic agents together with plants from Leguminosae collected from the North of Thailand were screened for PDE inhibitory activity using a radioassay. Results Seven from nineteen aphrodisiac and neurotonic plants as well as three from twelve Leguminosae plants showed potent PDEs inhibitory activity. The concentrations that could inhibit 50% PDE activity (IC50) of the active extracts were determined in comparison to the standard inhibitor, 3-isobutyl-1-methylxanthine (IBMX). Betula alnoides, Hiptage benghalensis, Leea indica and Senna surrattensis showed IC50 values in the range of microgram per milliliter while IBMX standard showed an IC50 value of 0.68 ± 0.13 μg/ml. Conclusion Thai biodiversity was the great sources of PDE inhibitors.

The aim of this study was to clarify the melanogenesis-inhibitory and antioxidant activity of Thai breadfruit's heartwood extract for application as a skin-lightening agent. The heartwood of breadfruit (Artocarpus incisus ) grown in Phitsanulok Province, Thailand, was extracted by using diethyl ether or methanol. The amount of artocarpin, a major component of A. incisus extract, was determined by using the HPLC method. The artocarpin content found in ether extract was 45.19 +/- 0.45% w/w, whereas that in methanol extract was 19.61 +/- 0.05% w/w. The ether extract was then evaluated for tyrosinase-inhibitory, melanogenesis-inhibitory, and antioxidant activities. The tyrosinase-inhibitory activity was tested in vitro by monitoring the inhibition of the extract against the formation of DOPAchrome by tyrosinase enzyme. The results showed that the tyrosinase-inhibitory activity of the extract was in a dose-dependent manner. The obtained IC50 value was 10.26 +/- 3.04 microg/ml, while kojic acid, a well-known tyrosinase inhibitor, provided an IC50 of 7.89 +/- 0.18 microg/ml. Melanocyte B16F1 melanoma cells (ATCC No. CRL-6323) were then used for determination of the melanogenesis-inhibitory activity of the extract, comparing it to hydroquinone, kojic acid, and purified artocarpin. The amount of melanin produced by the cells was monitored by measuring an absorbence at 490 nm. The obtained results indicated that A. incisus extract at a concentration of 2 to 25 microg/ml was able to decrease the melanin production of the melanocyte B16F1 cells. The obtained micrograph also confirmed that the extract did not change the cell morphology but reduced the melanin content by inhibiting melanin synthesis, whereas the purified artocarpin at a concentration of 4.5 microg/ml caused changes in cell morphology. Additionally, the extract exhibited antioxidant activity in a dose-dependent manner at an EC50 of 169.53 +/- 9.73 microg/ml, according to DPPH assay. The obtained results indicated that the ether extract of A. incisus 's heartwood has the potential of acting as a skin-lightening agent for application in cosmetics.

Dietary proteins have been reported to be beneficial for lipid metabolism, tissue growth, development, and repair, as well as immune response. The interactions of dietary proteins and their digested products may regulate the physiology and metabolism of the gastrointestinal tract. However, proteins are largely digested before reaching the large intestine. The present study investigated the use of the non-dietary protein, silk sericin, in rats. Rats were fed either with casein or sericin proteins. Their body weight, food consumption, and complete blood count were measured. The results showed that during the experimental periods, rats fed with casein and sericin diets had no significant changes on body weight, food consumption, or complete blood count. Sericin-fed rats had a significantly decreased CD8a and CD80 positive cells when compared with standard casein protein. In conclusion, dietary proteins may have a differential impact on the leukocyte profile. The mechanisms underlying these changes are not clear but they might be due to the different amino acid compositions of the proteins studied.