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Lipid nanoemulsions are promising nanodrug delivery carriers that can improve the efficacy and safety of paclitaxel(PTX).However,no intravenous lipid emulsion of PTX has been approved for clinical treatment,and systemic safety profiles have not yet been reported.Here we outline the development of a PTX-loaded tumor-targeting intravenous lipid emulsion(PTX Emul)and describe its characteristics,colloidal stability,and systemic safety profiles in terms of acute toxicity,long-term toxicity,and tox-icokinetics.We also compare PTX Emul with conventional PTX injection.Results showed that PTX Emul exhibited an ideal average particle size(approximately 160 nm)with narrow size distribution and robust colloidal stability under different conditions.Hypersensitivity reaction and hemolysis tests revealed that PTX Emul did not induce hypersensitivity reactions and had no hemolytic potential.In addition,where the alleviated systemic toxicity of PTX Emul may be attributed to the altered toxicokinetic characteristics in beagle dogs,including the decreased AUC and increased plasma clearance and volume of distribution,PTX Emul alleviated acute and long-term toxicity as evidenced by the enhanced the median lethal dose and approximate lethal dose,moderate body weight change,decreased bone marrow suppression and organ toxicity compared with those under PTX injection at the same dose.A fundamental understanding of the systemic safety profiles,high tumor-targeting efficiency,and superior antitumor activity in vivo of PTX Emul can provide powerful evidence of its therapeutic potential as a future treatment for breast cancer.
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@#Due to their good safety, wide application scope and quick onset time, lipid emulsions are full of promise to reverse drug poisoning. In this review, a number of clinical case reports were summarized to analyze the detoxification effect of lipid emulsions on local anesthetic, antiarrhythmic, psychotropic and organophosphate poisoning, as well as the possible adverse reactions of lipid emulsions therapy.Meanwhile, the mechanisms underlying lipid emulsions therapy, such as lipid sink theory, enhanced body basal metabolism and positively affected cardiovascular function, were fully interpreted.Besides, a few potential solutions to the problems still existing in lipid emulsions therapy were proposed, in order to consolidate the understanding of lipid emulsions therapy and promote its rational application in reversing drug poisoning.
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Objective: To evaluate the anti-obesity activity of ethanolic extract of cashew apple using various in vitro and in vivo models. Methods: Phytochemical screening was carried out in ethanolic extract of cashew apple, followed by quantification of phenol and flavonoid. Antioxidant potential was evaluated using 2,2-diphenyl-1-picrylhydrazyl and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) scavenging assays. The inhibitory effect of ethanolic extract of cashew apple on α-amylase and pancreatic lipase was also studied. In addition, anti-obesity activity was determined in two in vivo models, lipid emulsion model and atherogenic diet-induced obese rat model. Levels of postprandial plasma triglycerides were assessed in lipid emulsion model, whereas serum lipid profile, in vivo antioxidants and histopathological studies of the carotid artery and liver were performed in an atherogenic diet-induced obese model. Results: Phytochemical screening revealed the presence of carbohydrates, alkaloids, polyphenols, terpenoids, and steroids. The in vitro assays showed inhibition of α-amylase and pancreatic lipase and strong antioxidant potential. Ethanolic extract of cashew apple showed significant and time-dependent inhibitory activity on postprandial triglycerides after administration of lipid emulsion for 5 h. Ethanolic extract of cashew apple at 200 and 400 mg/kg on day 60 showed a significant reduction in body weight, body mass index and atherogenic index, whereas lipid profile and liver function marker levels in the serum were decreased in a dose-dependent manner at time intervals (day 0, 20, 40, and 60) compared to the atherogenic diet-induced obese rats. Histological observations showed reduced non-alcoholic fatty liver deposits and decreased atherosclerotic fatty streak plaques (carotid artery) after treatment with ethanolic extract of cashew apple. Conclusions: Ethanolic extract of cashew apple ameliorates obesity, which may be partly mediated by its delayed absorption of cholesterol and carbohydrates.
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Objective: To evaluate the anti-obesity activity of ethanolic extract of cashew apple using various in vitro and in vivo models. Methods: Phytochemical screening was carried out in ethanolic extract of cashew apple, followed by quantification of phenol and flavonoid. Antioxidant potential was evaluated using 2,2-diphenyl-1-picrylhydrazyl and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) scavenging assays. The inhibitory effect of ethanolic extract of cashew apple on α-amylase and pancreatic lipase was also studied. In addition, anti-obesity activity was determined in two in vivo models, lipid emulsion model and atherogenic diet-induced obese rat model. Levels of postprandial plasma triglycerides were assessed in lipid emulsion model, whereas serum lipid profile, in vivo antioxidants and histopathological studies of the carotid artery and liver were performed in an atherogenic diet-induced obese model. Results: Phytochemical screening revealed the presence of carbohydrates, alkaloids, polyphenols, terpenoids, and steroids. The in vitro assays showed inhibition of α-amylase and pancreatic lipase and strong antioxidant potential. Ethanolic extract of cashew apple showed significant and time-dependent inhibitory activity on postprandial triglycerides after administration of lipid emulsion for 5 h. Ethanolic extract of cashew apple at 200 and 400 mg/kg on day 60 showed a significant reduction in body weight, body mass index and atherogenic index, whereas lipid profile and liver function marker levels in the serum were decreased in a dose-dependent manner at time intervals (day 0, 20, 40, and 60) compared to the atherogenic diet-induced obese rats. Histological observations showed reduced non-alcoholic fatty liver deposits and decreased atherosclerotic fatty streak plaques (carotid artery) after treatment with ethanolic extract of cashew apple. Conclusions: Ethanolic extract of cashew apple ameliorates obesity, which may be partly mediated by its delayed absorption of cholesterol and carbohydrates.
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Parenteral nutrition - associated liver disease (PNALD)or cholestasis (PNAC)is the main compli-cation of prolonged parenteral nutrition in premature infants. It is characterized by cholestatic jaundice,which is defined as direct serum bilirubin of ≥34. 2 μmol/ L with or without liver enzymes abnormalities,rule out other causes. The risk factors contributing to the incidence of PNALD are premature,low birth weight,the duration of parenteral nutrition (PN),components of PN,sepsis,intestinal disease,genetic susceptibility. Although the damage is frequently mild,and resolves after discontinuation of parenteral nutrition,in some cases it progresses into cirrhotic changes. Ursodeoxycholic acid and lipid emulsions based on fish oil with a high content of long - chain polyunsaturated fatty acids ω - 3 has been proposed to be efficacy. But effective preventive and therapeutic strategies for PNALD have not been established yet. In-novative therapeutic strategies needs to be investigated.
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Objective To investigate the effect of structured lipid emulsion on cellular immune function in patients with gastrointestinal cancer after operation. Methods 76 cases of gastrointestinal cancer patients were chosen as the research object.The patients were divided into the control group and the experimental group according to the nutrition support after the operation,38 cases in each group.The experimental group used 20% structural lipid emulsion injection(medium chain fat milk accounted for 36%,long chain fat milk accounted for 64%,250 ml/ bottles),the control group used 20% physically mixed medium / long chain fat milk(medium chain fat milk and long chain fat milk accounted for 50%, respectively,250 ml/ bottles),and then compared the immune function index of the two groups.Results Immune function index of CD3 +at preoperative,third days and sixth days after the operation in the experi-mental group were 65.92 ± 4.71,60.62 ± 6.33 and 66.51 ± 3.58,respetively.While in the control group were 65.77 ± 4.63,57.86 ± 6.11 and 60.04 ± 3.21.Immune function index of CD4 +at preoperative, third days and sixth days after the operation in the experimental group were 43.75 ± 6.37,38.44 ± 5.68 and 47.98 ± 3.22,respectively.While in the control group were 43.26 ± 6.18,35.32 ± 6.78 and 37.93 ± 7.15,respectively.Immune function index of CD8 +at preoperative,third days and sixth days after the operation in the experimental group were 23.85 ± 7.16,21.96 ± 7.45 and 23.67 ± 5.47,respectively. While in the control group were 23.36 ± 6.69,21.43 ± 7.02 and 22.54 ± 6.12,respectively.Immune function index of CD4 +/CD8 +at preoperative,third days and sixth days after the operation in the experi-mental group were 1.86 ± 0.35,1.72 ± 0.39 and 1.99 ± 0.56,respectively.While in the control group were 1.83 ± 0.31,1.66 ± 0.32 and 1.68 ± 0.41,respectively.Immune function index(CD3 +,CD4 +and CD4 +/CD8 +)in the experimental group were significantly higher than those in the control group after sixth days(P< 0.05).Conclusion Postoperative early structured lipid emulsion nutrition support can correct the immune suppression in patients with gastric intestinal cancer,and improve cellular immune function.
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PURPOSE: Intravenous lipid emulsion (ILE) has been shown to have significant therapeutic effects on calcium channel blocker overdose in animal studies and clinical cases. In this preliminary experiment, we investigated the hemodynamic changes and survival in a rat model of verapamil intoxication. METHODS: Fourteen male Sprague-Dawley rats were sedated and treated with ILE or normal saline (control), followed by continuous intravenous infusion of verapamil (20 mg/kg/h). Mean arterial pressure and heart rate of rats were monitored during the infusion. In addition, the total dose of infused verapamil and the duration of survival were measured. RESULTS: Survival was prolonged in the ILE group (32.43±5.8 min) relative to the control group (24.14±4.3 min) (p=0.01). The cumulative mean lethal dose of verapamil was higher in the ILE group (4.3±0.7 mg/kg) than in the control group (3.2±0.5 mg/kg; p=0.017). CONCLUSION: ILE pretreatment prolonged survival and increased the lethal dose in a rat model of verapamil poisoning.
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Animals , Humans , Male , Rats , Arterial Pressure , Calcium Channels , Heart Rate , Hemodynamics , Infusions, Intravenous , Models, Animal , Poisoning , Rats, Sprague-Dawley , Therapeutic Uses , VerapamilABSTRACT
Objective To detect the protein expression changes of mitochondrial apoptotic pathway during the reverse effects of lipid emulsion on bupivacaine cardiotoxicity, so as to investigate the probable mechanism concerning the reverse effect of lipid emulsion on bupivacaine cardiotoxicity.Methods The ventricular muscles of 15 healthy SD neonatal mice (1-3 d) were chosen to conduct primary culture in vitro.And the cardiomyocytes were cultivated in a medium containing bupivacaine for 24 hours to establish its bupivacaine poisoning model.The cultured cardiomyocytes were divided into three groups: control group (group C);bupivacaine group (group B);and bupivacaine+lipid emulsion group (group BL).Flow cytometry was applied to examine the apoptosis of cardiomyocytes, and the Western blot was employed to detect the protein expression variation of cytochrome C (Cyto-C) and cleaved casepase-3.Results Compared with group C, the apoptosis rate was remarkably increased in both group B and group BL and that of the group B was dramatically higher than that of the group BL, with a statistical significance (P<0.05).Compared with group C, the protein expression levels of both Cyto-C and cleaved casepase-3 were significantly increased in groups B and BL (P<0.05), and the protein expression levels of both Cyto-C and cleaved casepase-3 in group B were significantly higher than those in group BL (P<0.05).Conclusion Lipid emulsion can regulate apoptosis through inhibiting the release of mitochondrial Cyto-C and reducing casepase-3 activation, thus it protects cardiomyocytes.
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OBJECTIVE: To investigate the effects of lipid emulsion on acute liver injury induced by trichloroethylene( TCE)in male rats. METHODS: By random number table method,18 specific pathogen free male rats were randomly divided into control group,TCE exposure group and lipid emulsion intervention group,6 rats in each group. The rats of TCE exposure group and lipid emulsion intervention group were given TCE 3 g / kg body weight by intragastric administration,and rats in control group were given the same amount of peanut oil. Rats in lipid emulsion intervention group were given 20% lipid emulsion( 2 mL / kg body weight) by intravenous injection,and the same amount of 0. 9% sodium chloride solution was given by intravenous injection in control group and TCE exposure group. After 24 hours,the activities of alanine aminotransferase( ALT) and aspartate aminotransferase( AST) in serum. Some liver tissues were used for pathological analysis; some for 10% liver homogenate and the levels of malondialdehyde system( MDA),superoxide dismutase( SOD)and glutathione peroxidase( GSH-Px) were detected. RESULTS: Compared with TCE exposure group,edema of liver cell in lipid emulsion intervention group was significantly reduced. Compared with the control group and the lipid emulsion intervention group,the activities of ALT and AST in serum,and the levels of MOD and SOD in liver homogenate were increased( P < 0. 05). The above 4 indexes in the lipid emulsion intervention group were increased compared with the control group( P < 0. 05). There is no significant difference in GSH-Px level in all three groups( P > 0. 05). CONCLUSION: Administration of lipid emulsion can alleviate TCE-induced acute liver damage in rats through improving the lipid peroxidation mechanism.
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@#The aim of this study was to prepare and characterise docetaxel lipid emulsion injection and to conduct the characterization of its pharmacokinetics in rats after tail-vein injection. High pressure homogenization method was used to prepare docetaxel lipid emulsion. 12 Wistar rats were randomly divided into docetaxel lipid emulsion injection group and docetaxel injection group, and dosed at 6 mg/kg through tail-vein injection. Docetaxel concentration in plasma was determined by HPLC. The pharmacokinetic parameters of docetaxel in rats were obtained using the 3P97 program. Particle size, polydispersion index, Zeta potential of docetaxel lipid emulsion were found to be(221. 6±13. 4)nm, (0. 092±0. 003)and -30. 3 mV, respectively. t1/2(α) of docetaxel lipid emulsion injection and docetaxel injection were(0. 072±0. 014)and(0. 066±0. 015)h; t1/2(β) were(0. 573±0. 253)and(0. 432±0. 184)h; AUC0-12 h were(7. 98±1. 25)and(6. 26±1. 83)μg ·h/mL, respectively. Docetaxel lipid emulsion injection had similar pharmacokinetic characteristics to docetaxel injection. The pharmacokinetic data obtained for both preparations fitted a two-compartment model.
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BACKGROUND: The goal of this in vitro study was to investigate the effect of lipid emulsion on vasodilation caused by toxic doses of bupivacaine and mepivacaine during contraction induced by a protein kinase C (PKC) activator, phorbol 12,13-dibutyrate (PDBu), in an isolated endothelium-denuded rat aorta. METHODS: The effects of lipid emulsion on the dose-response curves induced by bupivacaine or mepivacaine in an isolated aorta precontracted with PDBu were assessed. In addition, the effects of bupivacaine on the increased intracellular calcium concentration ([Ca²⁺]ᵢ) and contraction induced by PDBu were investigated using fura-2 loaded aortic strips. Further, the effects of bupivacaine, the PKC inhibitor GF109203X and lipid emulsion, alone or in combination, on PDBu-induced PKC and phosphorylation-dependent inhibitory protein of myosin phosphatase (CPI-17) phosphorylation in rat aortic vascular smooth muscle cells (VSMCs) was examined by western blotting. RESULTS: Lipid emulsion attenuated the vasodilation induced by bupivacaine, whereas it had no effect on that induced by mepivacaine. Lipid emulsion had no effect on PDBu-induced contraction. The magnitude of bupivacaine-induced vasodilation was higher than that of the bupivacaine-induced decrease in [Ca²⁺]ᵢ. PDBu promoted PKC and CPI-17 phosphorylation in aortic VSMCs. Bupivacaine and GF109203X attenuated PDBu-induced PKC and CPI-17 phosphorylation, whereas lipid emulsion attenuated bupivacaine-mediated inhibition of PDBu-induced PKC and CPI-17 phosphorylation. CONCLUSIONS: These results suggest that lipid emulsion attenuates the vasodilation induced by a toxic dose of bupivacaine via inhibition of bupivacaine-induced PKC and CPI-17 dephosphorylation. This lipid emulsion-mediated inhibition of vasodilation may be partly associated with the lipid solubility of local anesthetics.
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Animals , Rats , Anesthetics, Local , Aorta , Blotting, Western , Bupivacaine , Calcium , Fura-2 , In Vitro Techniques , Mepivacaine , Muscle, Smooth, Vascular , Myosin-Light-Chain Phosphatase , Phorbol 12,13-Dibutyrate , Phosphorylation , Protein Kinase C , Solubility , VasodilationABSTRACT
BACKGROUND: The goal of this in vitro study was to investigate the effect of lipid emulsion on vasodilation caused by toxic doses of bupivacaine and mepivacaine during contraction induced by a protein kinase C (PKC) activator, phorbol 12,13-dibutyrate (PDBu), in an isolated endothelium-denuded rat aorta. METHODS: The effects of lipid emulsion on the dose-response curves induced by bupivacaine or mepivacaine in an isolated aorta precontracted with PDBu were assessed. In addition, the effects of bupivacaine on the increased intracellular calcium concentration ([Ca²⁺]ᵢ) and contraction induced by PDBu were investigated using fura-2 loaded aortic strips. Further, the effects of bupivacaine, the PKC inhibitor GF109203X and lipid emulsion, alone or in combination, on PDBu-induced PKC and phosphorylation-dependent inhibitory protein of myosin phosphatase (CPI-17) phosphorylation in rat aortic vascular smooth muscle cells (VSMCs) was examined by western blotting. RESULTS: Lipid emulsion attenuated the vasodilation induced by bupivacaine, whereas it had no effect on that induced by mepivacaine. Lipid emulsion had no effect on PDBu-induced contraction. The magnitude of bupivacaine-induced vasodilation was higher than that of the bupivacaine-induced decrease in [Ca²⁺]ᵢ. PDBu promoted PKC and CPI-17 phosphorylation in aortic VSMCs. Bupivacaine and GF109203X attenuated PDBu-induced PKC and CPI-17 phosphorylation, whereas lipid emulsion attenuated bupivacaine-mediated inhibition of PDBu-induced PKC and CPI-17 phosphorylation. CONCLUSIONS: These results suggest that lipid emulsion attenuates the vasodilation induced by a toxic dose of bupivacaine via inhibition of bupivacaine-induced PKC and CPI-17 dephosphorylation. This lipid emulsion-mediated inhibition of vasodilation may be partly associated with the lipid solubility of local anesthetics.
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Animals , Rats , Anesthetics, Local , Aorta , Blotting, Western , Bupivacaine , Calcium , Fura-2 , In Vitro Techniques , Mepivacaine , Muscle, Smooth, Vascular , Myosin-Light-Chain Phosphatase , Phorbol 12,13-Dibutyrate , Phosphorylation , Protein Kinase C , Solubility , VasodilationABSTRACT
Cardiovascular drugs are commonly used in clinical medicine,which can cause refractory shock and cardiac arrest when poisoning.Lipid emulsion was mainly used for detoxification of lipophilic anesthetics poisoning in the past.Recently more and more studies and clinical cases suggest that lipid emulsion can be adopted as one of therapies for cardiovascular drugs poisoning.Now we review and focus on the research status of the lipid emulsion in the treatment of cardiovascular drugs poisoning,the related mechanisms of detoxification,therapeutic regimen and adverse effect.
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Objective To investigate the effect of intravenous injection of 20% lipid emulsion on neurotransmitters imbalance in central nerve system induced by local anesthetics.Methods Thirty adult Sprague-Dawley rats were randomly divided into two groups:normal group (group C,n =10) and local anesthetics group (group L,n =20).Based on different treatment,the rats in group L were assigned into two subgroup:control group (group S,n =10)and 20% long-chain lipid emulsion in-jection group (group I,n =10).The rats of group L were injected with 0.75% levobupivacaine at 50μl/min from the right ventricle of brain.When convulsions wave of electroencephalogram EEG ap-peared,20% long-chain lipid emulsion was administrated continuously 0.25 ml·kg-1 ·min-1 (group I)or normal saline (group S).The rats in group C were without any treatment.All the rats were con-tinously monitored by EEG,ECG and SpO 2 .The primary outcome included seizure duration and threshold and rats’mortality of postoperative 24 h.Secondary outcome included the concentrations of neurotransmitters GABA and Glu in cerebrospinal fluid,expression of NMDAR1 in cortex,Glu/GA-BA concentration ratio (Glu/GABA),and analysis the correlation between expression of Glu and NMDAR1.Results The convulsion time and mortality of rats in group S were significantly increased compared with those in group I (P <0.05).The seizure threshold of levobupivacaine was much lower in group S than group I (P <0.05).Compared with group C,the concentrations of Glu and GABA in cerebrospinal fluid,expression of NMDAR1 in hippocampus and Glu/GABA significantly increased in groups S and I(P < 0.05 ),and at same time these data in group S were significantly higher than group I (P < 0.05 ).There is a positive correlation between concentration of Glu in CSF and expression of NMDAR1 in hippocampus (r =0.884,P <0.01 ).Conclusion Intravenous infusion of 20% long-chain lipid emulsion can effectively improve neurotransmitters imbalance in central nerve system induced by intraventricular injection of local anesthetics.
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Lipid emulsion,as an important part of parenteral nutrition support,provides energy and fatty acids.The pro-inflammatory effect of ω-6 polyunsaturated fatty acids has triggered concerns of the possible influence of lipid emulsion on immune function,but few studies prove such adverse immune characteristics.At present new types of lipid emulsion are available by changing the concentration and sources of polyunsaturated acids,mono-unsaturated acid,and saturated fatty acids,attempting to reduce the amount of ω-6 polyunsaturated fatty acids.This paper reviewed the commonly used lipid emulsions at present and related immunoregulation.
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Lipid emulsion has been used not only as nutrition in clinic practice,but also recently as an adjuvant therapy of lipophilic drugs poisioning,which is most likely to cause cardiopulmonary arrest and brings difficulty to conventional treatments.More and more reports of whether studies in labs or clinic cases suggest that lipid emulsion can be adopted as one of therapies for lipophilic drugs poisioning.The article mainly sums up the development of lipid emulsion remedy against lipophilic drugs poisioning in the hope of providing reference for clinical application of lipid emulsion to detoxification.
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Acute organophosphorus pesticides poisoning(AOPP)is one of the common critical emergency problems and the fatality is extremely high. Organophosphorus pesticides(OPS)are highly effective acetylcholinesterase(AChE)inhibitors. The AChE inhibition results in accumulation of acetyl?choline and overestimation of acetylcholine receptors in synapses of the autonomic nervous system, central nervous system,and neuromuscular junctions,causing a series of symptoms including musca?rinic,nicotinic,and central nervous system dysfunctions. In the early stage of AOPP,the core treat?ment is the use of anticholinergic drugs coupled with cholinesterase reactivator. Atropine and penehycli?dine hydrochloride(Tuoning)are the most commonly used anticholinergic drugs,which can effectively compete with acetylcholine receptors,block the effect of acetylcholine,and relieve the symptoms of re?spiratory failure,bronchospasm,pulmonary edema caused by AOPP. Oximes are believed to function as AChE reactivators,that can promote enzymatic reactivation and restore the activity of hydrolysis of ace? tylcholine. Recently,new avproaches,such as intravenous lipid emulsion,new detoxification drugs, blood purification,and traditional Chinese medicine,have attracted more attention. Overall,great prog?ress has been made in AOPP treatments. A better understanding of AOPP mechanism,and the support from pharmacology,toxicology,and related fields can contribute to the treatment of AOPP. Improved medical management of AOPP can also result in fewer deaths from poisoning worldwide.
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Objective To study the influence on common logarithm of partition-coefficient (log P) value of insoluble drugs on nano-lipid emulsion properties ,including drug-loading amount ,in vitro release ,and phase distribution etc .Methods 6 insoluble drugs ,nimodipine (NIM) ,docetaxel (DTX) ,curcumin (CUR) ,paclitaxel (PTX) ,teniposide (TEN) ,silybin (SLB) ,were selected as the model drugs ,to investigate the relationship between log P value and nano-lipid emulsion of the dissolubility in PEG400 ,the amount of drug-loading ,particle diameter ,Zeta potential ,in vitro release ,and phase distribution respectively .Results With the increase of log P value ,drug solubility in PEG400 first increased and then decreased ,drug-loading in nano-lipid emulsion increased ,release rate in vitro of drug slowed down ,drug distribution in oil phase increased while in emulsion layer decreased .Log P value has no correlation with particle diameter and Zeta potential .Conclusion The properties of drug-loading nano-lipid emulsion can be preliminarily judged by log P values and the solubility in PEG400 of drugs .
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Intravenous lipid emulsions( LEs) are relevant for patients receiving parenteral nutrition because they prevent the depletion of essential fatty acids(FAs) and as a highly dense energy source. The prescription of LEs is complex,due mainly to their distinct FAs components,which may alter the immune re-sponse in different ways and distinctly influence inflammation according to their biochemical properties. The patient′s metabolic profile should guide the type of FAs and amount of lipids that are provided. For critically ill hypermetabolic patients,growing evidence indicates that standard LEs based solely on soybean oil should be avoided in favor of new LEs containing medium-chain triglycerides,olive oil,or fish oil to decrease the provision of potentially inflammatory/immunosuppressiveω-6 polyunsaturated fatty acids. As sources of eico-sapentaenoic and docosahexaenoic acids,LEs containing fish oil may be important for critically ill patients be-cause they allow better modulation of the immune response and likely reduce the length of intensive care unit stay. However,current evidence precludes the recommendation of a specific LE for clinical use in this patient population.
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In vitro study revealed that pancreatic lipase inhibitory activity of C. asiatica extract was significantly higher than rutin but lower than orlistat, an anti-obesity drug. α-Amylase inhibitory activities of C. asiatica extract and rutin were significantly lower than acarbose, an anti-diabetic drug. Inhibition of α-glucosidase activity by C. asiatica extract, rutin, and acarbose was not different. The in vivo study substantiated the in vitro results. C. asiatica extract (1000 and 2000 mg/4 mL/kg), rutin (1000 mg/4 mL/kg), and orlistat (45 mg/4 mL/kg) significantly decreased plasma glucose, triglyceride and total cholesterol levels in lipid emulsion-induced hyperlipidemic rats at 3 h. However, plasma aspartate aminotransferase and alanine aminotransferase levels did not show significant change. The present work further supports that the C. asiatica extract and its bioactive rutin may help managing hypolipidemic and hypoglycemic effects.