Interventional treatments for prolapsing haemorrhoids: network meta-analysis.

BACKGROUND: Multiple treatments for early-moderate grade symptomatic haemorrhoids currently exist, each associated with their respective efficacy, complications, and risks. The aim of this study was to compare the relative clinical outcomes and effectiveness of interventional treatments for grade II-III haemorrhoids. METHODS: A systematic review was conducted according to PRISMA criteria for all the RCTs published between 1980 and 2020; manuscripts were identified using the MEDLINE, Embase, and CENTRAL databases. Inclusion criteria were RCTs comparing procedural interventions for grade II-III haemorrhoids. Primary outcomes of interest were: symptom recurrence at a minimum follow-up of 6 weeks, postprocedural pain measured on a visual analogue scale (VAS) on day 1, and postprocedural complications (bleeding, urinary retention, and bowel incontinence). After bias assessment and heterogeneity analysis, a Bayesian network meta-analysis was performed. RESULTS: Seventy-nine RCTs were identified, including 9232 patients. Fourteen different treatments were analysed in the network meta-analysis. Overall, there were 59 RCTs (73 per cent) judged as being at high risk of bias, and the greatest risk was in the domain measurement of outcome. Variable amounts of heterogeneity were detected in direct treatment comparisons, in particular for symptom recurrence and postprocedural pain. Recurrence of haemorrhoidal symptoms was reported by 54 studies, involving 7026 patients and 14 treatments. Closed haemorrhoidectomy had the lowest recurrence risk, followed by open haemorrhoidectomy, suture ligation with mucopexy, stapled haemorrhoidopexy, and Doppler-guided haemorrhoid artery ligation (DG-HAL) with mucopexy. Pain was reported in 34 studies involving 3812 patients and 11 treatments. Direct current electrotherapy, DG-HAL with mucopexy, and infrared coagulation yielded the lowest pain scores. Postprocedural bleeding was recorded in 46 studies involving 5696 patients and 14 treatments. Open haemorrhoidectomy had the greatest risk of postprocedural bleeding, followed by stapled haemorrhoidopexy and closed haemorrhoidectomy. Urinary retention was reported in 30 studies comparing 10 treatments involving 3116 participants. Open haemorrhoidectomy and stapled haemorrhoidopexy had significantly higher odds of urinary retention than rubber band ligation and DG-HAL with mucopexy. Nine studies reported bowel incontinence comparing five treatments involving 1269 participants. Open haemorrhoidectomy and stapled haemorrhoidopexy had the highest probability of bowel incontinence. CONCLUSION: Open and closed haemorrhoidectomy, and stapled haemorrhoidopexy were associated with worse pain, and more postprocedural bleeding, urinary retention, and bowel incontinence, but had the lowest rates of symptom recurrence. The risks and benefits of each treatment should be discussed with patients before a decision is made.

Prevalence of endocrine complications in transfusion dependent thalassemia in Hospital Pulau Pinang: A pilot study.

INTRODUCTION: Frequent blood transfusions results in iron overload and lead to multiple endocrine complications. In spite of improvements in iron chelation therapy, a significant number of transfusion dependent thalassaemia (TDT) patients still develop endocrine complications. The aim of this study is to evaluate the prevalence of various endocrine complications in our adult TDT patients and to study the correlation with serum ferritin and liver iron concentration (LIC). METHODS: A retrospective review of all TDT patients treated in Haematology Unit, Hospital Pulau Pinang (HPP) was conducted. RESULTS: Of the 45 adult TDT patients, 22 were males and 23 were females with mean age of 28.8±6.9 years old. Majority of TDT in HPP were beta thalassemia major (71.1%), followed by E-Beta thalassemia (24.4%) and HbH-Constant Spring (4.4%). Frequency of transfusion was 3-4 weekly. 40.0% of adult TDT suffered from at least one endocrine complication. Among the adult TDT patients with endocrine complication, 50% have one endocrinopathy, 38.9% with two types of endocrinopathies and 11.1% of them have three or more types of endocrinopathies. Hypogonadism (22.2%) was the commonest endocrine complication, followed by osteoporosis (20%), hypothyroidism (13.3%), diabetes mellitus (6.7%) and hypocortisolism (4.4%). Patients with endocrine complications were significantly older. Mean serum ferritin level and LIC was higher among patients with endocrine complications but both were not statistically significant. CONCLUSION: Endocrinopathy is still prevalent in 40% of adult TDT patients. This leads to higher health-care resource utilization, cost and significant morbidities among patients with TDT. Therefore, regular monitoring and early detection with intensification of chelation therapy is essential.

Effect of Acylglycerol Composition and Fatty Acyl Chain Length on Lipid Digestion in pH-Stat Digestion Model and Simulated In Vitro Digestion Model.

In this study, a pH-stat digestion model and a simulated in vitro digestion model were employed to evaluate the digestion degree of lipids depending on different acylglycerols and acyl chain length (that is, diacylglycerol [DAG] compared with soybean oil representing long-chain triacylglycerol compared with medium-chain triacylglycerol [MCT]). In the pH-stat digestion model, differences were observed among the digestion degrees of 3 oils using digestion rate (k), digestion half-time (t1/2 ), and digestion extent (Φmax). The results showed the digestion rate order was MCT > soybean oil > DAG. Accordingly, the order of digestion half-times was MCT < soybean oil < DAG. In simulated in vitro digestion model, digestion rates (k') and digestion half-times (t'1/2 ) were also obtained and the results showed a digestion rate order of MCT (k' = 0.068 min(-1) ) > soybean oil (k' = 0.037 min(-1) ) > DAG (k' = 0.024 min(-1) ). Consequently, the order of digestion half-times was MCT (t'1/2 = 10.20 min) < soybean oil (t'1/2 = 18.74 min) < DAG (t'1/2 = 29.08 min). The parameters obtained using the 2 models showed MCT was digested faster than soybean oil, and that soybean oil was digested faster than DAG.

Genetic variation of FASN is associated with fatty acid composition of Hanwoo.

The objective of this study was to identify genetic variants in the bovine fatty acid synthase (FASN) gene and to evaluate associations with fatty acid composition from longissimus lumborum muscle using 90 purebred Hanwoo steers. Sequence alignments observed 6 genetic variants located in exons 20, 24, 32, 34, and 39, and PCR-RFLP analysis confirmed these variations. Genotypes of the g.15532A>C locus were significantly associated with Linolenic acid (C18:3), and genotypes of the g.17924G>A locus were significantly associated with Palmitic (C16:0), Palmitoleic (C16:1), Oleic (C18:1), saturated fatty acids, and unsaturated fatty acids. The analysis revealed that SFA and UFA showed significant correlations with fatty acid composition (Myristic (C14:0), Palmitic (C16:0), Stearic (C18:0), Oleic (C18:1), and Eicosenoic (C20:1) acids). Oleic acid (C18:1) was negatively correlated with Myristic (C14:0), Palmitic (C16:0), and Palmitoleic (C16:1) acids (P<0.001).

Farnesoid X receptor, overexpressed in pancreatic cancer with lymph node metastasis promotes cell migration and invasion.

BACKGROUND: Lymph node metastasis is one of the most important adverse prognostic factors for pancreatic cancer. The aim of this study was to identify novel lymphatic metastasis-associated markers and therapeutic targets for pancreatic cancer. METHODS: DNA microarray study was carried out to identify genes differentially expressed between 17 pancreatic cancer tissues with lymph node metastasis and 17 pancreatic cancer tissues without lymph node metastasis. The microarray results were validated by real-time PCR. Immunohistochemistry and western blotting were used to examine the expression of farnesoid X receptor (FXR). The function of FXR was studied by small interfering RNA and treatment with FXR antagonist guggulsterone and FXR agonist GW4064. RESULTS: Farnesoid X receptor overexpression in pancreatic cancer tissues with lymph node metastasis is associated with poor patient survival. Small interfering RNA-mediated downregulation of FXR and guggulsterone-mediated FXR inhibition resulted in a marked reduction in cell migration and invasion. In addition, downregulation of FXR reduced NF-κB activation and conditioned medium from FXR siRNA-transfected cells showed reduced VEGF levels. Moreover, GW4064-mediated FXR activation increased cell migration and invasion. CONCLUSIONS: These findings indicated that FXR overexpression plays an important role in lymphatic metastasis of pancreatic cancer and that downregulation of FXR is an effective approach for inhibition of pancreatic tumour progression.

Enzymatic production of trans-free hard fat stock from fractionated rice bran oil, fully hydrogenated soybean oil, and conjugated linoleic Acid.

Rice bran oil (RBO) was fractionated into 2 phases, solid (S-RBO) and liquid (L-RBO), using acetone at -18 degrees C and the weight yield of each S-RBO and L-RBO was 45.5% and 54.5%, respectively. Then, trans-free hard fat was synthesized from trans-free substrate of S-RBO and fully hydrogenated soybean oil (FHSBO) at different molar ratios (S-RBO : FHSBO; 1 : 1, 1 : 1.5, 1 : 2, and 1 : 3) with Lipozyme TL IM lipase (10% of total substrate). Conjugated linoleic acid (CLA, 20% of total substrate) was used as functional fatty acids for the production of trans-free hard fat. After fatty acid analysis, CLA (12.2% to 14.2%) was found on the triacylglycerol (TAG) backbone of the interesterified products along with stearic (37.6% to 49%), palmitic (15% to 17.9%), and oleic acids (13.3% to 19.2%). The interesterified product contained higher level of saturated fatty acid (62.6% to 70.1%) at sn-2 position. Total tocopherols (alpha-, gamma-, and delta-; 1.4 to 2.6 mg/100 g) and phytosterols (campesterol, stigmasterol, and beta-sitosterol; 220.5 to 362.7 mg/100 g) were found in the interesterified products. From DSC results, solid fat contents of the interesterified products (S-RBO : FHSBO 1 : 1, 1 : 1.5, 1 : 2, and 1 : 3) at 25 degrees C were 23.1%, 27%, 30.1%, and 44.9%. The interesterified products consisted mostly of beta' form crystal with a small portion of beta form. The interesterified product (S-RBO : FHSBO 1 : 1.5) was softer than the physical blend but slightly harder than commercial shortenings as measured by texture analyzer. Thus, trans-free hard fat stock, which may have a potential functionality could be produced with various physical properties.

Physicochemical and volatiles characterization of trans-free solid fats produced by lipase-catalyzed interesterification.

Trans-free solid fats were synthesized from fully hydrogenated soybean oil (FHSBO), olive oil (OO), and palm stearin (PS) at different substrate weight ratios (10:20:70, 10:40:50 and 10:50:40) via lipase-catalyzed interesterification. The interesterified products contained mostly TAG (98.8% to 99.0%), and small amounts of MAG and DAG as by-products. The major fatty acids were oleic acid, palmitic acid, and stearic acid in the interesterified products, and the melting points ranged from 39 to 45 degrees C. The amount of alpha-tocopherol was reduced by 75% to 92%. Volatile analysis by solid-phase microextraction indicated that OO and PS had distinct volatile profiles, in which 18 volatiles were retained in interesterified products. Furthermore, some volatiles disappeared or formed during processing. Electronic nose showed that the odors of substrates (OO and PS) were different from each other, and the odors of interesterified products were distinguishable from that of OO or PS. Among the interesterified products, the odor of blend FHSBO:OO:PS of 10:40:50 or 10:50:40 was different from that of blend FHSBO:OO:PS (10:20:70). However, no odor difference was observed between products blend FHSBO:OO:PS 10:40:50 and 10:50:40.

Compositional study on rice bran oil after lipase-catalyzed glycerolysis and solvent fractionations.

Rice bran oil (RBO) was modified through lipase-catalyzed glycerolysis. After 48 h reaction, the reactant (RBO-G, solved in hexane) containing 0.14 mg/mL of MAG, 0.19 mg/mL of DAG, and 0.93 mg/mL of TAG was obtained. Extending the reaction to 72 h resulted in 0.37 mg/mL of DAG with concomitant reduction in TAG (0.68 mg/mL). Two solvent fractionation methods, independent and sequential fractionation, were performed with acetone and hexane at 0, -8, -14, or -35 degrees C. The fraction with most unsaturated fatty acids (Sigma UFA) was liquid fraction from independent fractionation at -35 degrees C (-35 In) from hexane, showing 88.3%Sigma UFA content. Nevertheless, when yield (wt%) was considered, the highest amount of UFA was obtained from 0 In (liquid fraction from independent fractionation at 0 degrees C) with hexane, resulting in 82.3%Sigma UFA with 97.9 wt% recovery. Normal-phase HPLC was conducted for the compositional study of RBO-G. Overall, solid fractions from sequential fractionation at 0 degrees C (0 SeSo) and independent fractionation at -35 degrees C (-35 InSo) with hexane contained the high concentration of total MAG and DAG, ranging from 0.94 to 1.35 (mg/mL).

The anti-diabetic effects of ethanol extract from two variants of Artemisia princeps Pampanini in C57BL/KsJ-db/db mice.

The anti-diabetic effects of two variants of Artemisia princeps Pampanini, sajabalssuk (SB) and sajuarissuk (SS), were investigated in type 2 diabetic animal using their ethanol extracts. Male C57BL/KsJ-db/db (db/db) mice were divided into control, SB ethanol extract (SBE), SS ethanol extract (SSE), or rosiglitazone (RG) groups and their age-matched littermates (db/+) were used. Supplementation of the SBE (0.171 g/100g diet), SSE (0.154 g/100g diet), and RG (0.005 g/100g diet) improved glucose and insulin tolerance and significantly lowered blood glycosylated hemoglobin levels, as compared to the control group. Plasma insulin, C-peptide and glucagon levels in db/db mice were higher in the db/+ mice, however these values were significantly lowered by SBE, SSE or RG-supplement. Hepatic GK activity was significantly lower in the db/db mice than in the db/+ mice, while hepatic G6Pase activity was vice versa. Supplementation of SBE, SSE and RG reversed these hepatic glucose-regulating enzyme activities. In addition, SBE and SSE markedly increased the hepatic glycogen content and muscle ratio as compared to the control group, but they did not alter the food intake, body weight and plasma leptin level. The RG group, however, showed a significant increase in the food intake, body weight and plasma leptin. These results suggest that SBE and SSE exert an anti-diabetic effect in type 2 diabetic mice.

Ex vivo purging of leukemia cells using tumor-necrosis-factor-related apoptosis-inducing ligand in hematopoietic stem cell transplantation.

The aim of this study was to evaluate the potential of tumor-necrosis-factor-related apoptosis-inducing ligand TRAIL to eradicate leukemia cell lines, while sparing normal hematopoietic stem cells. Human Jurkat and Molt-4 cell lines were used to optimize the purging process in umbilical cord blood (UCB) mononuclear cells. The Jurkat cell line was TRAIL sensitive and TRAIL-resistant Molt-4 cell line became sensitive after being treated with TRAIL and a low dose of doxorubicin (0.1 micro M), but UCB mononuclear cells remained resistant. DR4 expression was increased when Jurkat cells were treated with TRAIL, and DR5 expression increased after exposing Molt-4 cells to TRAIL plus a low dose of doxorubicin for 24 h. The expression of DR4 and DR5 in UCB mononuclear cells was unchanged after treatment with TRAIL, a low-dose doxorubicin, or TRAIL plus a low dose of doxorubicin. In TRAIL-sensitive Jurkat cells, caspases 8, 9, 3, and 7 were activated by TRAIL treatment and activation of caspases was augmented by TRAIL plus a low dose of doxorubicin than TRAIL or a low dose of doxorubicin alone in Molt-4 cells. Experiments involving mixture of UCB mononuclear cells and Jurkat or Molt-4 cells showed a marked eradication of leukemia cells and the limiting dilution assay demonstrated an eradication rate of more than 4 logs after 24 h incubation with 100 ng/ml of TRAIL in Jurkat cells. In the case of Molt-4 cells, the eradication rate was about 3 logs when TRAIL was used in combination with a low dose of doxorubicin. No significant decrease in the number of granulocyte-macrophage colony-forming unit) (CFU-GM) colonies was detected when UCB mononuclear cells were treated with TRAIL in combination with a low dose of doxorubicin. These results suggest that TRAIL offers the possibility of being used as an ex vivo purging agent for autologous transplantation in hematologic malignancies.

Constituents of the essential oil of the Cinnamomum cassia stem bark and the biological properties.

GC-MS analysis on the essential oil (CC-oil) of Cinnamomum cassia stem bark led to the identification of cinnamaldehyde (CNA, 1), 2-hydroxycinnamaldehyde (2-CNA), coumarin (2), and cinnamyl acetate. The major volatile flavor in CC-oil was found to be 2-CNA. Coumarin was first isolated from this plant by phytochemical isolation and spectroscopic analysis. CNA and CC-oil showed potent cytotoxicity, which was effectively prevented by N-acetyl-L-cysteine (NAC) treatment. Intraperitoneal administration with CNA considerably decreased malondialdehyde (MDA) formation and glutathione S-transferase activity in rats. These results suggest that CC-oil and CNA can regulate the triggering of hepatic drug-metabolizing enzymes by the formation of a glutathione-conjugate.

Tectorigenin, an isoflavone of Pueraria thunbergiana Benth., induces differentiation and apoptosis in human promyelocytic leukemia HL-60 cells.

Cytotoxic effects of six isoflavonoids, tectorigenin, glycitein, tectoridin, glycitin, 6''-O-xylosyltectoridin, and 6''-O-xylosylglycitin isolated from the flower of Pueraria thunbergiana Benth. together with genistein, a known differentiation and apoptosis inducer, were examined. Among these isoflavonoids, tectorigenin and genistein exhibited cytotoxicity against various human cancer cells; glycitein showed only mild cytotoxicity. These results suggest that the isoflavone structure and 5-hydroxyl group are crucial for the cytotoxic properties and that glycosides are inactive. Moreover, tectorigenin induced differentiation of human promyelocytic leukemia HL-60 cells to granulocytes and monocytes/macrophages, and caused apoptotic changes of DNA in the cells, as did genistein. Tectorigenin also inhibited autophosphorylation of epidermal growth factor (EGF) receptor by EGF and decreased the expression of Bcl-2 protein, with less activity than genistein. From these results, tectorigenin may be a possible therapeutic agent for leukemia.

Toxicology of Kalopanax pictus extract and hematological effect of the isolated anti-rheumatoidal kalopanaxsaponin A on the Freunds complete adjuvant reagent-treated rat.

We have reported that kalopanaxsaponin A (KPS-A) isolated from Kalopanax pictus have anti-rheumatoidal activity in the rat treated with Freunds complete adjuvant (FCA) reagent. In addition, it has been also reported that KPS-A is a potent antioxidant in the rheumatoidal rat. This research was undertaken to examine whether the saponins of KPS-A and -I could adjust the abnormal lipid metabolisms and hematological changes in immunological diseases. KPS-A significantly inhibited the increases in both triglycerides and total proteins in addition to the decrease in total cholesterol induced by FCA reagent treatment. KPS-A treatment decreased the number of leucocytes elevated by FCA reagent treatment. Excess dose of the methanol extract produced no severe toxicity on the body weight, wet organ weights and hepatic functions. Since LD50 value of K. pictus methanol extract was shown to be 4,033 mg/kg, it could be estimated to be a safe agent for anti-rheumatoidal herbal medicines.

Kalopanaxsaponin A is a basic saponin structure for the anti-tumor activity of hederagenin monodesmosides.

Hederagenin, delta-hederin [hederagenin alpha-L-arabinoside], kalopanax-saponin A [hederagenin 3-O-alpha-L-rhamnosyl(1-->2)-alpha-L- arabinoside], kalopanaxsaponin I [hederagenin 3-O-beta-D-xylosyl(1-->3)-alpha-L- rhamnosyl(1-->2)-alpha-L-arabinoside], and sapindoside C [hederagenin 3-O-beta-D-glucosyl(1-->4)-beta-D-xylsyl (1-->3)-alpha-L-rhamnosyl(1-->2)-alpha-L-arabinoside] were isolated from stem bark of Kalopanax pictus Nakai (Araliaceae). Among glycosides of hederagenin, disaccharide (kalopanaxsaponin A, commonly also called alpha-hederin), trisaccharide (kalopanaxsaponin I), and tetrasaccharide (sapindoside C) showed significant cytotoxicity on several types of tumor cells, while hederagenin itself exhibited only weak cytotoxicity and its monosaccharide (delta-hederin) was non-cytotoxic. From these results, it suggests that the arabinosyl moiety at C-3 blocks the activity of hederagenin and the position of the second sugar for glycoside linkage is also important for cytotoxicity. In the in vivo experiments, kalopanaxsaponin A (15 mg/kg, i.p.) apparently increased the life span of mice bearing Colon 26 and 3LL Lewis lung carcinoma, as well as cisplatin (3 mg/kg, i.p.). These results indicated that kalopanaxsaponin A has potential anti-tumor applications.

Costunolide induces apoptosis by ROS-mediated mitochondrial permeability transition and cytochrome C release.

Costunolide is an active compound isolated from the root of Saussurea lappa Clarks, a Chinese medicinal herb, and is considered a therapeutic candidate for various types of cancers. Nevertheless, the pharmacological pathways of costunolide are still unknown. In this study, we investigate the effects of costunolide on the induction of apoptosis in HL-60 human leukemia cells and its putative pathways of action. Using apoptosis analysis, measurement of reactive oxygen species (ROS), and assessment of mitochondrial membrane potentials, we show that costunolide is a potent inducer of apoptosis, and facilitates its activity via ROS generation, thereby inducing mitochondrial permeability transition (MPT) and cytochrome c release to the cytosol. ROS production, mitochondrial alteration, and subsequent apoptotic cell death in costunolide-treated cells were blocked by the antioxidant N-acetylcystein (NAC). Cyclosporin A, a permeability transition inhibitor, also inhibited mitochondrial permeability transition and apoptosis. Our data indicate that costunolide induces the ROS-mediated mitochondrial permeability transition and resultant cytochrome c release. This is the first report on the mechanism of the anticancer effect of costunolide.

Constituents and the antitumor principle of Allium victorialis var. platyphyllum.

To search for cytotoxic components from Allium victorialis, MTT assays on each extract and an isolated component, gitogenin 3-O-lycotetroside, were performed against cancer cell lines. Cytotoxicities of most extract were shown to be comparatively weak, though IC50 values of CHCl3 fraction was found to be <31.3-368.4 microg/ml. From the incubated methanol extract at 36 degrees C, eleven kinds of organosulfuric flavours were predictable by GC-MS performance. The most abundant peak was revealed to be 2-vinyl-4H-1,3-dithiin (1) by its mass spectrum. Further, this extract showed significant cytotoxicities toward cancer cell lies. Silica gel column chromatography of the n-butanol fraction led to the isolation of gitogenin 3-O-lycotetroside (3) along with astragalin (4) and kaempferol 3, 4'-di-O-beta-D-glucoside (5). This steroidal saponin exhibited significant cytotoxic activities (IC50, 6.51-36.5 microg/ml) over several cancer cell lines. When compound 3 was incubated for 24 h with human intestinal bacteria, a major metabolite was produced and then isolated by silica gel column chromatography. By examining parent- and prominent ion peak in FAB-MS spectrum of the metabolite, the structure was speculated not to be any of prosapogenins of 3, suggesting that spiroketal ring were labile to the bacterial reaction. These suggest that disulfides produced secondarily are the antitumor principles.

Anti-lipid peroxidative principles from the stem bark of Kalopanax pictus Nakai.

Hepatic lipid peroxide contents were examined in bromobenzene-treated rats firstly after the oral administration of MeOH extract of Kalopanax pictus stem barks, its n-BuOH fraction, EtOAc fraction and an alkaline hydrolysate of the n-BuOH fraction, and secondly after the intraperitoneal administration of hederagenin monodesmosides and bisdesmosides. Two hederagenin monodesmosides, kalopanaxsaponin A (KPS-A) and sapindoside C, exhibited significant anti-lipid peroxidation effects after intraperitoneal administration at doses of 10-30 micromole/kg, whereas their bisdesmosides did not exhibit any significant activity. These results suggest that it is the hederagenin monodesmosides that are responsible for anti-lipid peroxidation in vivo. The activity of KPS-A was established by the observation of decreased aminopyrine N-demethylase activity and increased epoxide hydrolase activity.

Nutritional effects of enzymatically modified soybean oil with caprylic acid versus physical mixture analogue in obese Zucker rats.

Enzymatically modified soybean oil with caprylic acid (SL), a physical mixture of tricaprylin and soybean oil (PHY), and soybean oil as control were fed (20% of diet weight) to female obese Zucker rats. Both lipids (SL and PHY) have similar total fatty acid composition containing 23.4 mol % caprylic acid (C8:0) but have different lipid structures. After 21 days of feeding, the body weight gain was 36.4% in the SL-fed group and 35.2% in the PHY-fed group, respectively; whereas the body weight of the control group increased 41.6%. Significant differences in the respiratory exchange ratio were observed between the SL and PHY groups. However, the contents of glucose, total and high density lipoprotein (HDL) cholesterol, and very low density and low density lipoprotein (VLDL + LDL) cholesterol in serum were not significantly different between the SL- and PHY-fed groups or among the three dietary groups (control, SL, and PHY) (p < 0.05). On the other hand, plasma total cholesterol and plasma triacylglycerol (TAG) were significantly higher in SL- and PHY-fed groups than in the control group. In the liver and inguinal adipocyte TAG, C8:0 was found in the SL-fed group, whereas it was not observed in the liver and inguinal adipocyte TAG of the PHY-fed group, which suggests that positional distribution of C8:0 of the TAG molecule is an important consideration in the metabolism of lipids. This study showed that different positional distribution in TAG molecules lead to different metabolic fates, resulting in the change of fatty acid composition in liver and inguinal adipose TAG in female Zucker rats.

Hypoglycemic and hypolipidemic effects of tectorigenin and kaikasaponin III in the streptozotocin-lnduced diabetic rat and their antioxidant activity in vitro.

Tectorigenin and kaikasaponin III from the flowers of Pueraria thunbergiana showed potent hypoglycemic and hypolipidemic effects in the streptozotocin-induced diabetic rats. Intraperitoneal administration of these two compounds with 5 and 10 mg/kg, respectively, for seven days to streptozotocin-induced rats significantly reduced the blood glucose, total cholesterol, LDL- and VLDL-cholesterol and triglyceride levels when compared with those of control group. Glycitein in which 5-OH is unlinked and tectoridin (7-O-glycoside of tectorigenin) isolated from the flowers of P. thunbergiana did not improve hyperglycemia and hyperlipidemia. In addition, tectorigenin showed in vitro antioxidant effects on 1,1diphenyl-2-pirylhydrazyl (DPPH) radical, xanthine-xanthine oxidase superoxide anion radical, and lipid peroxidation in rat microsomes induced by enzymatic and non-enzymatic methods. We further found that tectorigenin and kaikasaponin III protected the Vero cell line (normal monkey kidney) from injury by hydrogen peroxide. From these findings, it seems likely that the antioxidant action of tectorigenin and kaikasaponin III may alleviate the streptozotocin-induced toxicity and contribute to hypoglycemic and hypolipidemic effects.

Essential moiety for antimutagenic and cytotoxic activity of hederagenin monodesmosides and bisdesmosides isolated from the stem bark of Kalopanax pictus.

For the elucidation of the antimutagenic and cytotoxic principles from the stem bark of Kalopanax pictus, seven isolated components of this crude drug were tested in the Ames test and the MTT test. Hederagenin and its monodesmosides, kalopanaxsaponin A and I in addition to its bisdesmosides, kalopanaxsaponin B and H, showed potent antimutagenic activities against aflatoxin B1 (AFB1). However, they had no inhibitory effects on mutagenicity induced by the direct mutagen, N-methyl-N'-nitro-N-nitrosoguanidine (MNNG). This suggested that hederagenin glycosides might effectively prevent the metabolic activation of AFB1 or scavenge the electrophilic intermediate capable of inducing mutation. Hederagenin was found to be an essential moiety for the exhibition of antimutagenicity. Moreover, hederagenin and its 3-O-glycosides were found to be cytotoxic on various tumor cell lines, P-388, L-1210, U-937, HL-60, SNU-5 and HepG2, while 3,28-di-O-glycosides of hederagenin were not cytotoxic. Hence, hederagenin and its 3-O-glycosides could be suitable for cancer treatment chemopreventive drugs.