The Alleviating Effect of Lagerstroemia indica Flower Extract on Stretch Marks through Regulation of Mast Cells.

Striae distensae (SD) or stretch marks are common linear scars of atrophic skin with disintegrating extracellular matrix (ECM) structures. Although fibroblasts contribute to the construction of ECM structure in SD, some studies have reported that mast cell degranulation causes the disruption of ECM in early SD lesions. Lagerstroemia indica flower (LIF) has traditionally been used in India as a diuretic. However, little is known about the effect and molecular action of Lagerstroemia indica flower extract (LIFE) on alleviating SD. This study evaluated the effects of LIFE on mast cell degranulation and the synthesis of ECM components in fibroblasts. LIFE inhibits the adhesion of rat basophilic leukemia (RBL) cells, RBL-2H3 on fibronectin (FN) and the expression of integrin, a receptor for FN, thereby reducing focal adhesion kinase (FAK) phosphorylation. In addition, LIFE attenuated the allergen-induced granules and cytokine interleukin 3 (IL-3) through the adhesion with FN. Moreover, the conditioned medium (CM) of activated mast cells decreases the synthesis of ECM components, and LIFE restores the abnormal expressions induced by activated mast cells. These results demonstrate that LIFE suppresses FN-induced mast cell activation and promotes the synthesis of ECM components in fibroblast, which indicates that LIFE may be a useful cosmetic agent for SD treatment.

Lagerstroemia ovalifolia Exerts Anti- Inflammatory Effects in Mice of LPSInduced ALI via Downregulating of MAPK and NF-κB Activation.

Lagerstroemia ovalifolia Teijsm. & Binn. (LO) (crape myrtle) has reportedly been used as traditional herbal medicine (THM) in Java, Indonesia. Our previous study revealed that the LO leaf extract (LOLE) exerted anti-inflammatory effects on lipopolysaccharide (LPS)-stimulated RAW264.7 macrophages. Based on this finding, the current study aimed to evaluate the protective effects of LOLE in a mouse model of LPS-induced acute lung injury (ALI). The results showed that treatment with LPS enhanced the inflammatory cell influx into the lungs and increased the number of macrophages and the secretion of the inflammatory cytokines in the bronchoalveolar lavage fluid (BALF) of mice. However, these effects were notably abrogated with LOLE pretreatment. Furthermore, the increase of inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2) and monocyte chemoattractant protein-1 (MCP-1) expression in the lung tissues of mice with ALI was also reversed by LOLE. In addition, LOLE significantly suppressed the LPS-induced activation of the MAPK/NF-κB signaling pathway and led to heme oxygenase-1 (HO-1) induction in the lungs. Additionally, in vitro experiments showed that LOLE enhanced the expression of HO-1 in RAW264.7 macrophages. The aforementioned findings collectively indicate that LOLE exerts an ameliorative effect on inflammatory response in the airway of ALI mice.

Evaluation of a Nutraceutical Product with Probiotics, Vitamin D, Plus Banaba Leaf Extracts (Lagerstroemia speciosa) in Glycemic Control.

BACKGROUND: Dysbiosis is related to changes in the composition and behaviour of intestinal microbiota, which may contribute to an age-related decline in metabolic and immune system functioning (immune-senescence). OBJECTIVE: The microbiota-targeted dietary and probiotic interventions have been shown to favorably affect the host health by an enhancement of antioxidant activity, improving immune homeostasis, suppression of chronic inflammation, regulation of metabolism and prevention of insulin resistance. RESULTS: In our study, the use of specific probiotics strains improved the serum concentration of glycemic markers, thereby promoting better overall health. CONCLUSION: Probiotics may help correct defects in the gut microbial environment improving metabolic parameters, such as blood sugar levels, glycosylated hemoglobin and a decrease in body weight.

Corosolic Acid Attenuates Hepatic Lipid Accumulation and Inflammatory Response via AMPK/SREBPs and NF-κB/MAPK Signaling Pathways.

Corosolic acid (CA) is the main active component of Lagetstroemia speciosa and has been known to serve as several different pharmacological effects, such as antidiabetic, anti-oxidant, and anticancer effects. In this study, effects of CA on the hepatic lipid accumulation were examined using HepG2 cells and tyloxapol (TY)-induced hyperlipidemia ICR mice. CA significantly inhibited hepatic lipid accumulation via inhibition of SREBPs, and its target genes FAS, SCD1, and HMGCR transcription in HepG2 cells. These effects were mediated through activation of AMPK, and these effects were all abolished in the presence of compound C (CC, an AMPK inhibitor). In addition, CA clearly alleviated serum ALT, AST, TG, TC, low-density lipoprotein cholesterol (LDL-C), and increased high-density lipoprotein cholesterol (HDL-C) levels, and obviously attenuated TY-induced liver steatosis and inflammation. Moreover, CA significantly upregulated AMPK, ACC, LKB1 phosphorylation, and significantly inhibited lipin1, SREBPs, TNF-α, F4/80, caspase-1 expression, NF-κB translocation, and MAPK activation in TY-induced hyperlipidemia mice. Our results suggest that CA is a potent antihyperlipidemia and antihepatic steatosis agent and the mechanism involved both lipogenesis and cholesterol synthesis and inflammation response inhibition via AMPK/SREBPs and NF-κB/MAPK signaling pathways.

The anti-diabetic effect of eight Lagerstroemia speciosa leaf extracts based on the contents of ellagitannins and ellagic acid derivatives.

Previously, we have reported the opposite effects of compounds isolated from Lagerstroemia speciosa leaves on a glucose transport (GLUT4) assay. Ellagitannins from L. speciosa activated GLUT4, while ellagic acid derivatives showed an inhibitory effect. As part of our continuing research on anti-diabetic nutritional supplements, we herein compared the anti-diabetic effects of several extracts (LE1-8) from leaves of L. speciosa using different manufacturing processes based on the contents of ellagitannins and ellagic acid derivatives. Their anti-diabetic effects were evaluated through glucose uptake and adipocyte differentiation in 3T3-L1 cells in vitro as well as alloxan induced diabetic mice in vivo. These extracts were given to mice by gavage at doses of 0.25, 1.0, and 4.0 g per kg body weight once a day for 21 consecutive days. Results showed that LE1 (1.0 g kg-1), LE3 (1.0 or 4.0 g kg-1), LE4 (1.0 or 4.0 g kg-1), LE5 (0.25 or 1.0 or 4.0 g kg-1) and LE7 (1.0 or 4.0 g kg-1) showed significant anti-diabetic effects in alloxan-induced diabetic mice as indicated by the decreased levels of fasting blood glucose, body weight, serum biomarkers, tissue weight and body fat, and increased final insulin levels. LE8 (1.0 g kg-1) showed a moderate anti-diabetic effect as illustrated by the reduced fasting blood glucose level while LE2 and LE6 showed slight effects in alloxan-induced diabetic mice. The potential correlation of the content of ellagitannins, ellagic acid derivatives, and corosolic acid with the anti-diabetic activity was discussed.

Ethanolic Extract of Lagerstroemia Speciosa (L.) Pers., Induces Apoptosis and Cell Cycle Arrest in HepG2 Cells.

Lagerstroemia speciosa (L.) Pers., (Lythraceae) also called Banaba is a native plant of southeast Asia and is widely used in traditional medicinal system. Herbal tea from banaba leaves are used to reduce weight and diabetes. We investigated the cytotoxic potentials of ethanolic banaba leaves extract (EBLE) against human hepatocellular carcinoma (HepG2) cell line. Lagerstroemia speciosa leaves were extracted and obtained from M/s. Quimico Herbal Extract Manufacturer, Bengaluru, India, and it contains 20% corosolic acid. Cells were treated with 50, 100, and 150 µg/ml of EBLE for 24 h, and cytotoxicity was evaluated by MTT assay. Apoptosis-related morphology was investigated by DAPI nuclear staining. Protein and gene expressions of p-Akt, FOXO1, p53, MDM2, p21, p27, CDK4, cyclin D1, and E1 were evaluated through Western blotting and qPCR. EBLE treatments caused significant, concentration-dependent cytotoxicity. DAPI staining and flow cytometry studies showed chromatin condensation, increased apoptotic cell population and cell cycle arrest at subG0/G1 phase upon EBLE treatments respectively. Furthermore, EBLE treatments significantly increased the expressions of p53, p21, p27, FOXO1, while p-Akt, MDM2, CDK4, cyclin D1, and E1 expressions were downregulated. These findings suggested that EBLE induces G1-phase of cell cycle arrest and apoptosis in HepG2 cells. EBLE may serve as a therapeutic agent against hepatocellular carcinoma.

Lagerstroemia speciosa (L.) Pers Leaf Extract Attenuates Lung Tumorigenesis via Alleviating Oxidative Stress, Inflammation and Apoptosis.

One of the major etiological factors that account for lung cancer is tobacco use. Benzo(a)pyrene [B(a)P], one of the main constituents of tobacco smoke, has a key role in lung carcinogenesis. The present study was conducted to investigate the cytotoxicity of an aqueous ethanolic extract of Lagerstroemia speciosa (L.) Pers leaves (LLE) on human lung adenocarcinoma cells (A549), as well as its in vivo antitumor effect on a lung tumorigenesis mice model. Our results revealed that LLE possesses cytotoxic activity against the A549 cell line. Mice orally administered B(a)P (50 mg/kg body weight) showed an increase in relative lung weight with subsequent decrease in final body weight. Serum levels of tumor marker enzymes AHH, ADA and LDH and the inflammatory mediator NF-κB increased, while total antioxidant capacity (TAC) decreased. In addition, we observed the increased activity of metalloproteinases (MMP-2 and MMP-12) and levels of the tumor angiogenesis marker VEFG and the lipid peroxidation marker MDA, as well as decreased levels of the non-enzymatic antioxidant GSH and enzymatic antioxidants CAT and GSH-Px in lung tissues. Moreover, B(a)P administration up-regulated the expression of the COX-2 gene, pro-inflammatory cytokines TNF-α and IL-6, and an anti-apoptotic gene Bcl-2, and at the same time down-regulated expression of pro-apoptotic genes BAX and caspase-3 and the p53 gene. Pre- and post-treatment with LLE (250 mg/kg body weight) attenuated all these abnormalities. Histopathological observations verified the protective effect of LLE. Overall, the present data positively confirm the potent antitumor effect of L. speciosa leaves against lung tumorigenesis.

Investigation of biological activities of the flowers of Lagerstroemia speciosa, the Jarul flower of Bangladesh.

BACKGROUND: Lagerstroemia speciosa (L.) Pers. (Family: Lythraceae) is used in traditional medicine in the treatment of diarrhea, diabetes and other diseases. The study was performed to conduct antioxidant, cytotoxic, thrombolytic, membrane stabilizing, antimicrobial, peripheral and central analgesic and hypoglycemic activity assays and phenobarbitone sodium-induced sleeping time test using crude methanol extract of flowers of L. speciosa and its different partitionates. METHOD: The antioxidant potential was evaluated by determining the ability of the samples to scavenge 1, 1-diphenyl-2-picrylhydrazyl (DPPH) free radical. The cytotoxic potential was examined following the procedures of brine shrimp lethality bioassay. Thrombolytic potential was assayed using streptokinase as standard. The samples were subjected to membrane stabilizing activity assay under heat induced condition. Antimicrobial potential was observed by disc diffusion method. The ability of the extract to inhibit writhing induced by acetic acid was determined in peripheral analgesic activity assay. The extract was also tested for central analgesic and hypoglycemic activities by tail flicking and tail tipping methods in Swiss albino mice model, respectively. CNS depressant activity was evaluated by an assay in which sleep was induced in mice using phenobarbitone sodium. RESULTS: The chloroform soluble fraction of L. speciosa extract demonstrated the highest antioxidant activity (IC50 = 4.20 ± 0.41 µg/ml) while the most prominent cytotoxic potency was showed by hexane soluble fraction (LC50 = 2.00 ± 0.31 µg/ml). Among the test samples, the carbon tetrachloride soluble fraction induced clot lysis (64.80 ± 0.27%) and prevented heat induced haemolysis (41.90 ± 0.10%) to the maximum extent. The largest zone of inhibition (19.0 mm) against Staphylococcus aureus, was also observed for the same fraction. In peripheral analgesic activity assay, 16.68% inhibition of writhing was documented for the L. speciosa extract (400 mg/kg body weight dose). The extract (400 mg/kg dose) also reduced blood sugar level by 56.12% after three hours of administration of glucose solution. In CNS depressant activity assay, mice of the sample group slept for shorter period of time compared to control group. CONCLUSIONS: From our investigation, it can be suggested that, the extract should be further studied for possible phytochemicals responsible for the observed biological activities.

Isolation of quercetin from the methanolic extract of Lagerstroemia speciosa by HPLC technique, its cytotoxicity against MCF-7 cells and photocatalytic activity.

The flavonoids present in the leaves of Lagerstroemia speciosa were extracted, characterized by spectral methods and studied for its cytotoxicity activity against MCF-cell lines and photocatalytic activity against azo dye. Direct and sequential soxhlet extraction was performed and its concentrated crude extract was subjected to high performance liquid chromatography. The yield obtained by the isolated compound (MEI-quercetin) from leaves of L. speciosa was found to be 1.8g from the methanolic extract. The phytochemical analysis and the Rf value of the isolated flavonoid was found to be 3.59. The isolated compound was characterized by Infrared Spectroscopy, NMR and Mass. Based on the characterization, the structure was elucidated as quercetin - a flavonoid. The isolated compound showed the significant in vitro cytotoxicity activity against MCF-7 cell lines at 500µg/ml when compared to the crude extract. Among the various concentrations (25, 50, 100, 250, and 500µg/ml), at higher concentration the cell viability was pronounced and also compared with that of the control. It was first time to report that the isolated flavonoid showed photocatalytic against azo dye-methyl orange. The dye degradation was monitored by UV-Vis spectrophotometry. The isolated compound showed dye degradation of 91.66% with the crude extract 82.47% at 160min. Hence in the present findings, the photocatalytic degradation of MO dye under UV irradiation was investigated over isolated compound of L. speciosa. Hence we expect that this can be used to treat the waste water in near future based on the photocatalytic technique.

Solar catalysed activity against methyl orange dye, cytotoxicity activity of MCF-7 cell lines and identification of marker compound by HPTLC of Lagerstroemia speciosa.

The investigation was aimed to quantify the Gallic acid present in Lagerstroemia speciosa leaves (Lythraceae). The High-Performance Thin Layer Chromatography (HPTLC) quantification was performed for acetone (AE), methanolic (ME) and chloroform (CE) extract of leaves of L. speciosa. The pre-coated silica gel 60 F254 was used for complete separation of compounds using the mobile phase pet. Ether: ethyl acetate: formic acid (5:5:1v/v).The validation of the extracts was carried out using ICH guidelines for precision, repeatability and accuracy showing the Rf 0.49 against standard Gallic acid. Linearity range for Gallic acid was done from 200 to 1000ng/spot (AE) and200 ng to 600ng/spot (ME), with Correlation, coefficient r=0.99 (AE) and 0.54 (ME) in the said concentrations. The composition in crude leaf extract was determined to be of 49.712mg (AE) and 20.125mg (ME), while it was not found in chloroform extract against standard Gallic acid. Hence the proposed method was very simple, precise, accurate and easy for the screening of the bioactive compounds present in the acetone and methanolic extracts of the leaves of L. speciosa. It was observed that the acetone extract subjected to cytotoxicity showed promising activity at higher concentrations (100 and 200µg/ml) showed 92.9% and 87.13% inhibition against MCF-7 cell lines respectively. The photocatalytic activity of the acetone and methanolic extracts of methyl orange was found to be 90.25% (190min) and 89.03% (180min) respectively. Therefore this can be used as an indicator of purity of herbal drugs and formulation containing L. speciosa.

Biofilm inhibition formation of clinical strains of Pseudomonas aeruginosa mutans, photocatalytic activity of azo dye and GC-MS analysis of leaves of Lagerstroemia speciosa.

The investigation was conducted to analyse the bioactive compounds from the leaf extracts of L. speciosa by GC-MS. The extracts were screened for antibacterial and antibiofilm activities against potential clinical strains. The bioactive compounds from the leaves of L. speciosa were extracted by soxhlet continuous extraction method and their chemical composition was analysed by Gas Chromatography-Mass Spectroscopy (GC-MS). The antibacterial activity was evaluated against clinical strain like Staphylococcus aureus, Escherichia coli, P. aeruginosa and Salmonella typhi by well diffusion technique. We also screened for antibacterial property against common food borne pathogens namely Listeria monocytogenes and Bacillus cereus at varied concentration 250µml-1 to 1000µml-1. Thereafter antibiofilm assay was carried out at from 250 to 1000µg/ml against P. aeruginosa (high biofilm forming pathogen) clinical strain by cover slip technique and the morphology of the pathogen was observed using Scanning Electron Microscopy-(SEM). It was observed that diverse class of secondary metabolites were found by GC-MS analysis for all the extracts upon the continuous extraction. It was found that only minimum inhibition was seen in alcoholic extract for antibacterial activity, whereas all other extracts showed negligible activity. P. aeruginosa biofilm inhibited to 93.0±2% and 91±2% at higher concentration (1000µg/ml) for methanolic and ethanolic extract respectively. Absence of extracellular matrix structure and the surface cracking of biofilm were viewed by SEM, which confirmed the antibiofilm activity. Hence this study reveals that L. speciosa showed significant antibiofilm activity against P. aeruginosa due to the phytoconstituents present in the leaf extracts which was well documented in the alcoholic extracts by GC-MS analysis. The methanolic and ethanolic extract showed good photocatalytic activity of 77.44% and 96.66% against azo dye degradation respectively. Further, isolating the novel phyto-compounds would yield better promising biological activities.

Radical Scavenging Activities of Lagerstroemia speciosa (L.) Pers. Petal Extracts and its hepato-protection in CCl4-intoxicated mice.

BACKGROUND: Lagerstroemia speciosa (L.) Pers. has medicinal importance. Bioactive phytochemicals isolated from different parts of L. speciosa, have revealed hypoglycemic, antibacterial, anti-inflammatory, antioxidant and hepato protective properties. Despite one report from Philippines detailing the use of L. speciosa as curative for fever and as well as diuretic, there is no experimental evidence about the hepatoprotective activity of the flower extracts. METHODS: Several spectroscopic methods, including GC-MS, were used to characterize phytochemicals present in the petal extract of L. speciosa. Ethanol extract of petals was evaluated for anti-oxidant and free radical scavenging properties by using methods related to hydrogen atom transfer, single electron transfer, reducing power, and metal chelation. This study has also revealed the in vitro antioxidant and in vivo hepatoprotective properties of petal extract against carbon tetra chloride (CCl4)-induced liver toxicity in Swiss albino mice. Hepatoprotection in CCl4 -intoxicated mice was studied with the aid of histology and different enzymatic and non-enzymatic markers of liver damage. Cytotoxicity tests were done using murein spleenocytes and cancareous cell lines, MCF7 and HepG2. RESULT: GCMS of the extract has revealed the presence of several potential antioxidant compounds, of them γ-Sitosterol and 1,2,3-Benzenetriol (Pyrogallol) were the predominant ones. The antioxidants activities of the flower-extract were significantly higher than curcumin (in terms of Nitric oxide scavenging activity; p = 0.0028) or ascorbic acid (in terms of 2,2-Diphenyl-1-Picrylhydrazyl (DPPH) assay; p = 0.0022). The damage control by the flower extract can be attributed to the reduction in lipid peroxidation and restoration of catalase activity. In vitro cytotoxicity tests have shown that the flower extract did not affect growth and survivability of the cell lines. It left beyond doubt that a flower of L. speciosa is a reservoir of antioxidant and hepatoprotective agents capable of reversing the damage inflicted by CCl4-intoxication. CONCLUSION: Results from the present study may be used in developing a potential hepato-protective health drink enriched with antioxidants from Lagerstroemia speciosa (L.) Pers.

Fluoride Exposure Aggravates the Testicular Damage and Sperm Quality in Diabetic Mice: Protective Role of Ginseng and Banaba.

Fluoride toxicity is known to pose infertility in fluoride-intoxicated animals as well as in people residing in fluoride endemic zones. The present study addresses the degree of impairments caused due to co-exposure of high fluoride toxicity in diabetic mice. Swiss mice, Mus musculus, were subjected to fluoride toxicity by providing fluoride-supplemented drinking water (600 ppm NaF) for a period of 30 days after the confirmation of streptozotocin-induced diabetes(STZ, 50 mg/kgbw). Consequently, aggravated hyperglycemia and tissue fluoride accumulation were witnessed in fluoride-intoxicated diabetic mice; later, these toxicated mice were treated with ginseng extract (GE) and banaba leaf extract, (BLE) at dose of 150 mg/kgbw/day alone and in combination for 15 and 30-day duration to check the efficacy of phytoextracts in reversing the toxicity. The spermatological indices studied, such as sperm density, motility, viability and morphology as well as the testicular biochemical parameters showed enhanced impairment in reproductive status of fluoride-intoxicated diabetic mice. Further, 15-days administration of GE and BLE in combination at a dose of 150 mg/kgbw/day was found to be beneficial in normalizing the alterations observed upon fluoride intoxication to diabetic mice. However, the correlates showed moderate association between blood glucose levels and the spermatological as well as biochemical indices wherein the tissue fluoride levels correlate least.

Antibiofilm efficacy of green synthesized graphene oxide-silver nanocomposite using Lagerstroemia speciosa floral extract: A comparative study on inhibition of gram-positive and gram-negative biofilms.

Biofilm architecture provides bacteria with enhanced antibiotic resistance, thus raising the need to search for alternative therapies that can inhibit the bacterial colonization. In the present study, we synthesized graphene oxide-silver nanocomposite (GO-Ag) by non-toxic and eco-friendly route using a floral extract of Legistromia speciosa (L.) Pers. The gas chromatography-mass spectrometry (GC-MS) analysis of plant extract revealed the presence of compounds which can simultaneously act as reducing and capping agents. The sub-inhibitory concentrations of synthesized GO-Ag reduced the biofilm formation in both gram-negative (E. cloacae) and gram-positive (S. mutans) bacterial models. Growth curve assay, membrane integrity assay, scanning electron microscopy (SEM) and confocal scanning laser microscopy (CSLM) revealed different mechanisms of biofilm inhibition in E. cloacae and S. mutans. Moreover, quantitative RT-PCR (qRT-PCR) results suggested GO-Ag is acting on S. mutans biofilm formation cascade. Biofilm inhibitory concentrations GO-Ag were also found to be non-toxic against HEK-293 (human embryonic kidney cell line). The whole study highlights the therapeutic potential of GO-Ag to restrain the onset of biofilm formation in bacteria.

Amelioration of an LPS-induced inflammatory response using a methanolic extract of Lagerstroemia ovalifolia to suppress the activation of NF-κB in RAW264.7 macrophages.

Lagerstroemia ovalifolia Teijsm. & Binn. has traditionally been used as an herbal medicine and possesses anti-inflammatory properties. However, the mechanisms underlying its anti-inflammatory effects remain poorly understood. For this purpose, we aimed to investigate the effects of methanolic extract of L. ovalifolia (LOME) on nitric oxide (NO) and prostaglandin E2 (PGE2) production, as well as the underlying molecular mechanisms responsible for these effects, in lipopolysaccharide (LPS)­stimulated RAW264.7 macrophages. We examined the effects of LOME on the production of NO and PGE2 in LPS-stimulated RAW264.7 cells. To explore the anti-inflammatory mechanisms of LOME, we measured the mRNA or protein expression of the pro­inflammatory mediators induced by LOME in the LPS-stimulated RAW264.7 cells. LOME significantly inhibited the production of NO, PGE2, interleukin (IL)-6, IL-1ß, and tumor necrosis factor-α (TNF-α) in LPS-stimulated RAW264.7 cells. Moreover, LOME suppressed the mRNA and protein expression of inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2) and inhibited the phosphorylation of the mitogen-activated protein kinases (MAPKs), with a reduction in the nuclear translocation of nuclear factor (NF)-κB in LPS-stimulated RAW264.7 cells. Taken together, these findings suggest that LOME may exert anti-inflammatory effects in vitro in LPS-stimulated RAW264.7 macrophages and thus, may have potential for use as an adjuvant treatment of inflammatory diseases.

A new triterpene glycoside from the stems of Lagerstroemia indica.

A bioassay-guided fractionation and chemical investigation of the stems of Lagerstroemia indica resulted in the isolation and identification of a new triterpene glycoside, lagerindiside (1), along with nine known triterpenes (2-10). The structure of this new compound was elucidated on the basis of 1D and 2D nuclear magnetic resonance spectroscopic data analysis as well as chemical method. The cytotoxic activities of the isolates (1-10) were evaluated by determining their inhibitory effects on four human tumor cell lines (A549, SK-OV-3, SK-MEL-2, and HCT15) using a sulforhodamine B bioassay. Compounds 3 and 4 showed potent cytotoxicity on the tumor cell lines with IC50 values ranging from 3.38 to 6.29 µM.

Insulin sensitizer in prediabetes: a clinical study with DLBS3233, a combined bioactive fraction of Cinnamomum burmanii and Lagerstroemia speciosa.

BACKGROUND: The aim of this paper is to evaluate the efficacy and safety of DLBS3233, a novel bioactive fraction derived from Cinnamomum burmanii and Lagerstroemia speciosa, in improving insulin resistance and preserving ß-cell performance in patients with impaired glucose tolerance (IGT). PATIENTS AND METHODS: Eighty adult subjects with IGT, defined as 2-hour postprandial glucose level of 140-199 mg/dL, were enrolled in this two-arm, 12-week, double-blind, randomized, placebo-controlled preliminary study. Eligible subjects were randomly allocated to receive either DLBS3233 at a dose of 50-100 mg daily or placebo for 12 weeks. The study mainly assessed the improvement of homeostatic model-assessed insulin resistance (HOMA-IR), the 15-minute and 2-hour plasma insulin levels, and the oral disposition index. RESULTS: After 12 weeks, DLBS3233 improved insulin resistance better than placebo as reflected by a reduced HOMA-IR (-27.04%±29.41% vs -4.90%±41.27%, P=0.013). The improvement of the first- and second-phase insulin secretion was consistently greater in DLBS3233 group than placebo group (-144.78±194.06 vs -71.21±157.19, P=0.022, and -455.03±487.56 vs -269.49±467.77, P=0.033, respectively). Further, DLBS3233 also significantly better improved oral disposition index than placebo. No serious hypoglycemia, edema, or cardiovascular-related adverse events were found in either groups. CONCLUSION: This study has shown that DLBS3233 at the dose of 50-100 mg once daily was well tolerated, and promisingly efficacious in improving insulin sensitivity as well as preserving ß-cell performance in subjects with IGT.

Antidiabetic and antihyperlipidemic activities of a novel polyherbal formulation in high fat diet/streptozotocin induced diabetic rat model.

OBJECTIVE: To investigate the antidiabetic and antihyperlipidemic activities of polyherbal formulation (PHF) containing hydroalcoholic extracts of four plants namely Salacia oblonga, Salacia roxbhurgii, Garcinia indica and Lagerstroemia parviflora in streptozotocin (STZ)-induced diabetic rats by administering oral doses (200 and 400 mg/kg body weight). MATERIALS AND METHODS: Animals were divided into diabetic and nondiabetic groups. Rats were fed with a high-fat diet (HFD) and induced with a single low dose of STZ (35 mg/kg) i.p. Diabetic rats were treated with formulation (200 and 400 mg/kg) and metformin 250 mg/kg. Blood glucose levels were measured using blood glucose test strips with ACCU CHEK glucometer. Lipid profile and gluconeogenic enzymes were determined in normal and STZ-induced diabetic rats after oral administration of the PHF for 28 days. Histopathological changes in diabetic rat organs (pancreas, liver, and kidney) were also observed after PHF treatment. RESULTS: Treatment of diabetic rats with PHF and metformin decreased plasma glucose and lipid profile levels. Blood glucose level showed significant reduction after 28 days of treatment with formulation at 200 and 400 mg/kg and in metformin. Formulation treated rats showed significant (P < 0.001) decrease in the activities of gluconeogenic enzymes. Histological examination of various organ tissues of normal control, diabetic control, and drug-treated rats revealed significant results. Treatment with PHF reverses the most blood and tissue changes toward the normal level. CONCLUSION: These findings suggested the antihyperglycemic and antihyperlipidemic properties of the PHF and thus help in preventing future complications of diabetes.

Inhibitory effects of eucalyptus and banaba leaf extracts on nonalcoholic steatohepatitis induced by a high-fructose/high-glucose diet in rats.

Nonalcoholic steatohepatitis (NASH) is a liver disease associated with metabolic syndrome. The aim of this work was to examine whether eucalyptus (Eucalyptus globulus) leaf extract (ELE) and banaba (Lagerstroemia speciosa L.) leaf extract (BLE) inhibited NASH induced by excessive ingestion of fructose in rats. Wistar rats were divided into four groups according to four distinct diets: starch diet (ST), high-fructose/high-glucose diet (FG), FG diet supplemented with ELE, or FG diet supplemented with BLE. All rats were killed after 5 weeks of treatment. Serum alanine aminotransferase and total cholesterol levels were significantly lower in the BLE group than in the FG group. Liver histopathology, including steatosis, lipogranulomas, and perisinusoidal fibrosis, was significantly attenuated in the ELE and BLE groups compared with the FG group. Levels of 2-thiobarbituric acid reactive substances (TBARS), which reflect oxidative injury to the liver, were significantly suppressed by ELE and BLE. Western blotting analysis indicated that interleukin-6 expression levels were significantly lower in the ELE and BLE groups than in the FG group. These results suggest that ELE and BLE reduced lipogenesis, oxidative stress, and inflammatory cytokine expression and thus inhibited NASH induced by excessive ingestion of fructose in rats.

Two new phenolic glucosides from Lagerstroemia speciosa.

Two new phenolic glucosides, 1-O-benzyl-6-O-E-caffeoyl-ß-d-glucopyranoside and 1-O-(7S,8R)-guaiacylglycerol-(6-O-E-caffeoyl)-ß-d-glucopyranoside, were isolated from the aerial parts of Lagerstroemia speciosa, along with ten known compounds. The structures of the isolated compounds were determined based on 1D- and 2D-NMR, Q-TOF MS and optical rotation spectroscopic data. All of the compounds showed moderate inhibitory activities against nitric oxide production in lipopolysaccharide-treated RAW264.7 cells, with IC50 values of 69.5-83.3 µM.