Neuroprotective Effect of Sterculia setigera Leaves Hydroethanolic Extract.

Plants are a valuable source of information for pharmacological research and new drug discovery. The present study aimed to evaluate the neuroprotective potential of the leaves of the medicinal plant Sterculia setigera. In vitro, the effect of Sterculia setigera leaves dry hydroethanolic extract (SSE) was tested on cultured cerebellar granule neurons (CGN) survival when exposed to hydrogen peroxide (H2O2) or 6-hydroxydopamine (6-OHDA), using the viability probe fluorescein diacetate (FDA), a lactate dehydrogenase (LDH) activity assay, an immunocytochemical staining against Gap 43, and the quantification of the expression of genes involved in apoptosis, necrosis, or oxidative stress. In vivo, the effect of intraperitoneal (ip) injection of SSE was assessed on the developing brain of 8-day-old Wistar rats exposed to ethanol neurotoxicity by measuring caspase-3 activity on cerebellum homogenates, the expression of some genes in tissue extracts, the thickness of cerebellar cortical layers and motor coordination. In vitro, SSE protected CGN against H2O2 and 6-OHDA-induced cell death at a dose of 10 µg/mL, inhibited the expression of genes Casp3 and Bad, and upregulated the expression of Cat and Gpx7. In vivo, SSE significantly blocked the deleterious effect of ethanol by reducing the activity of caspase-3, inhibiting the expression of Bax and Tp53, preventing the reduction of the thickness of the internal granule cell layer of the cerebellar cortex, and restoring motor functions. Sterculia setigera exerts neuroactive functions as claimed by traditional medicine and should be a good candidate for the development of a neuroprotective treatment against neurodegenerative diseases.

Functionalization of sterculia gum for making platform hydrogels via network formation for use in drug delivery.

Recently, various advancements have been made in the development of functional polymeric materials for innovative applications. Herein this work, functionalization of sterculia gum (SG) was carried out via grafting of poly(2-(methacryloyloxy) ethyltrimethylammonium chloride) (METAC)-polyvinyl pyrrolidone (PVP) to develop hydrogel dressings as a platform for use in drug delivery (DD). The innovation of the present work is the exploration of inherent antioxidant and antimicrobial properties of the SG along with antimicrobial characteristic of poly(METAC) and PVP, to design the doxycycline encapsulated hydrogel dressings for better wound healing. FESEM, EDS and AFM analyzed the surface morphology of hydrogels. FTIR, 13C NMR and XRD inferred inclusion of poly(METAC)-PVP into polymers. 13C NMR confirmed the incorporation of poly(METAC) and PVP onto gum by the presence of a peak at 54.74 ppm because of methyl carbon attached to quaternary nitrogen of poly(METAC) and at 45.48 ppm due to the ring carbon of PVP along with FTIR peak at 949 cm-1 because of CN bending of quaternary nitrogen of poy (METAC). Thermal characterization of copolymers has been performed using TGA analysis. One gram of copolymeric hydrogel dressing absorbed 6.51 ± 0.03 g simulated salivary fluid (SSF) and 7.65 ± 0.03 g simulated wound fluid (SWF). Release of doxycycline drug occurred in a sustained manner and followed the Non-Fickian diffusion mechanism from hydrogels. The release profile was most effectively described by Hixon-Crowell kinetic model. Hydrogel demonstrated biocompatibility and expressed thrombogenicity 79.7 ± 4.9 % during its polymer-blood interactions. Copolymer revealed mucoadhesive property, requiring a force of 77.00 ± 0.01 mN to detach from bio-membrane. Additionally, it exhibited antioxidant features, showing 43.81 ± 0.286 % free radical scavenging. Hydrogel dressings were mechanically stable and revealed 0.76 ± 0.09 N mm-2 tensile strength and 9.18 ± 0.01 N burst strength. Polymer films were permeable to oxygen and water vapor and were impermeable to microorganisms. Hydrogel dressings exhibited antimicrobial properties against Pseudomonas aeruginosa and Staphylococcus aureus bacteria. Overall, these properties displayed the suitability of hydrogels for wound dressing (WD) applications which may actively enhance wound healing.

In vitro-in silico pharmacology and chemistry of Stercularin, isolated from Sterculia diversifolia.

Stercularin is a coumarin, isolated from the ethyl acetate fraction of stem bark and leaves of S. diversifolia. Pharmacologically it is active against cancer, diabetes, and inflammation etc. The molecule is further screened for in vitro pharmacological activities. In addition, a detailed description on its drug likeness and pharmacokinetic profile has been established to further explore its fate as a drug candidate. Stercularin exhibited antiglycation, immunomodulatory, and leishmanicidal activity in three different in vitro models. The IC50 values obtained in these three assays were 80.22 ± 0.46 mg/ml, 12.8 ± 1.6 µg/ml, and 8.32 ± 0.42 µg/ml, respectively. In case of drug likeness evaluation, Stercularin has acceptable physicochemical properties and compliant with major drug likeness descriptors i.e., Lipinski rule, Pfizer rule, GSK rule, and "golden triangle". Accepting Lipinski rule implies the oral drug development of Stercularin. Pharmacokinetically, Stercularin is permeable to Caco-2 and MDCK cell lines. 'Boiled-egg' plot suggest intestinal route of absorption, blood brain barrier nonpermeating, and not affected by p-glycoprotein. Stercularin has high plasma protein binding with low free fraction circulating in the plasma. Stercularin proved to be the substrate and/or inhibitor of CYP 450 system with a moderate half-life and clearance rate to allow flexible dosing regimen. Finally, slight risk of toxicity exists for Stercularin, but not being limiting factors of drug knock out. A nature isolated Stercularin possess pharmacological activities and is predicted to have acceptable pharmacokinetic profile. Further drug development and in vivo studies are desirable for optimization.

Removal of cationic and anionic toxic pollutants from simulated solutions using Sterculia foetida pod (SFP): equilibrium isotherm, kinetics, and characterization.

The present work explores the sorption performance of Sterculia foetida pod (SFP) for the removal of methylene blue (MB) and chromium (Cr6+) from simulated solutions separately. The material characteristics namely textural analysis (specific surface area: 2.45 m2/g), morphological behavior (heterogeneous morphology containing pores and cavities), functional analysis (COO- stretching, C-O-C stretching vibrations, and -OH stretching) and thermal behavior (279.4 °C) were examined by various analytical techniques namely BET, SEM, FTIR, and TGA. Using non-linear Langmuir isotherm analysis, the maximal sorption capacity of SFP for the removal of MB and Cr6+ was predicted to be 74.1 mg/g and 27.3 mg/g, respectively. The optimized condition for sorption of MB and Cr6+ onto SFP was: dosage: 0.07 mg/L, initial pH: 7 (MB), and 2 (Cr6+). Thermodynamic data analysis confirmed the endothermic, favorable, spontaneous, and physisorption nature of sorption. The SFP has shown significant regeneration capacity in the consecutive runs (MB: 92.5% removal till 5th trial; Cr6+: 97.6% removal till 3rd trial). Based on these findings, SFP is a promising low-cost and eco-friendly candidate for the removal of anionic and cationic toxic pollutants in the absence of energy and chemical expenditure.NOVELTY STATEMENTSterculia foetida pod (SFP) explored for the removal of anionic and cationic toxic pollutants in the absence of energy and chemical expenditure.Mechanism for the interaction between toxic pollutants and SFP was predicted.Better sorption capacity (MB: 74.1 mg/g; Cr6+: 27.8 mg/g) and better regeneration capacity (MB: 92.5% for 5th trial; Cr6+: 97.6% for 3rd trial) was achieved.A feasible and spontaneous nature of sorption process toward the removal of MB and Cr6+ was demonstrated using thermodynamic relations.

Antibacterial and Healing Effect of Chicha Gum Hydrogel (Sterculia striata) with Nerolidol.

Chicha gum is a natural polymer obtained from the Sterculia striata plant. The hydroxyl groups of its structure have a chemical affinity to form hydrogels, which favors the association with biologically active molecules, such as nerolidol. This association improves the biological properties and allows the material to be used in drug delivery systems. Chicha gum hydrogels associated with nerolidol were produced at two concentrations: 0.01 and 0.02 g mL-1. Then, the hydrogels were characterized by thermogravimetry (TG), Fourier Transform Infrared spectroscopy (FTIR), and rheological analysis. The antibacterial activity was tested against Staphylococcus aureus and Escherichia coli. The cytotoxicity was evaluated against Artemia salina. Finally, an in vivo healing assay was carried out. The infrared characterization indicated that interactions were formed during the gel reticulation. This implies the presence of nerolidol in the regions at 3100-3550 cm-1. The rheological properties changed with an increasing concentration of nerolidol, which resulted in less viscous materials. An antibacterial 83.6% growth inhibition effect was observed using the hydrogel with 0.02 g mL-1 nerolidol. The in vivo healing assay showed the practical activity of the hydrogels in the wound treatment, as the materials promoted efficient re-epithelialization. Therefore, it was concluded that the chicha hydrogels have the potential to be used as wound-healing products.

Adsorption profile of anionic and cationic dyes through Fe3O4 embedded oxidized Sterculia gum/Gelatin hybrid gel matrix.

Hazardous effluents from textile industries being major contributors of water pollution and impose potential adverse effects on environment. In present study, Fe3O4 embedded oxidized Sterculia gum/Gelatin hybrid matrix have been fabricated and evaluated for enrichment of methyl orange (MO) and methylene blue (MB). Newly synthesized matrix was characterized through powdered XRD, FTIR, FESEM, TEM and TGA. Integrated nanoparticles improved dye enrichment and facilitated removal of matrix from the aqueous solution under the influence of magnetic field. Influence of various reaction parameters viz.: contact time, adsorbent dose, initial dye concentration, temperature & pH of the adsorption medium on dye enrichment have been evaluated. Maximum adsorption (90 % and 88 % for MO and MB respectively) has been achieved. Langmuir, Freundlich and Tempkin adsorption isotherms have been evaluated. Experimental results validate well fitted Freundlich isotherm for MO and Temkin isotherm for MB. Adsorption kinetics has been analyzed through Pseudo first order, second order kinetic and intra particle diffusion models. Adsorption of both dyes was best explained via pseudo second order kinetic model. Negative value of Gibb's free energy change (-26.487 KJ mol -1 and - 24.262 KJ mol -1) for MB and MO at 303 K was an indication of spontaneity of the reaction.

X-ray-based machine vision technique for detection of internal defects of sterculia seeds.

An online machine learning system based on X-ray nondestructive quality evaluation technique was developed to detect internal defects of boat-fruited sterculia seed. The X-ray images of boat-fruited sterculia seed were first acquired by the detection system. Then, a boat-fruited sterculia seed net (BSSNet) was trained to identify the defective boat-fruited sterculia seeds based on the X-ray images. The BSSNet was evaluated with the accuracy, precision, specificity, and sensitivity as 94.64%, 93.51%, 92.37%, and 96.64%, respectively. Further, three classical CNN models including VGG16, Resnet, and Inception were trained on the same dataset with accuracy of 95.71%, 94.29%, and 94.64%, respectively. Compared with the classical CNN models, the BSSNet achieved similar or higher accuracy in X-ray images classification. Finally, an independent dataset containing 200 X-ray images was used to validate the performance of the BSSNet and obtained an accuracy of 96.5%. The results presented above demonstrated that this classification method has a great potential for industrial applications. PRACTICAL APPLICATION: An X-ray online detection system integrated with a machine vision model was used to evaluate the quality of boat-fruited sterculia seed. A low-power x-ray detection system can detect internal defects of the object and ensure safety in the production process. The developed machine vision can sort the boat-fruited sterculia seed with an accuracy of 96.5%. The proposed nondestructive detection system showed a good potential to be used in industrial applications.

Detailed approach toward the anti-hyperglycemic potential of Sterculia diversifolia G. Don against alloxan-induced in vivo hyperglycemia model.

OBJECTIVE: To investigate Sterculia diversifolia G. Don for potential anti-diabetic activity in the in vivo mouse model of alloxan-induced hyperglycemia. METHODS: Sterculia diversifolia (S. diversifolia) was subjected to extraction and isolation techniques and structural characterization of the isolated compounds were performed using spectroscopic methods. The acute toxicity test was performed by orally administering S. diversifolia in doses of 500-2000 mg/kg. For the assessment of anti-hyperglycemic activity, S. diversifolia bark and leaves extracts were administered orally in doses of 50, 100, and 200 mg/kg, along with metformin (150 mg/kg, i.p) as positive control, after confirmation of alloxan (150 mg/kg, i.p.) induced hyperglycemia in BALB/c mice. Serum biochemical parameters were monitored for the period of study. RESULTS: The phytochemical studies showed the presence of quercetin and kaempferol in S. diversifolia. The IC50 values in the in vivo acute toxicity study revealed the safety margin of S. diversifolia bark (1166.66 mg/kg) and leaves (683.34 mg/kg) extracts. A significant attenuation of alloxan induced hyperglycemia was produced by S. diversifolia extracts at 50 mg/kg (P < 0.05), 100 mg/kg (P < 0.05, < 0.01), and 150 mg/kg (P < 0.05, < 0.01, < 0.001) during 1-4 h, which was comparable to metformin (P < 0.001). Significant (P < 0.001) improvement appeared in blood hemoglobin, protein, cholesterol, triglycerides, urea, creatinine, HDL, and LDL of the stem bark and leaves extracts treated diabetic mice. CONCLUSION: These findings connote the usefulness of S. diversifolia as an anti-diabetic in traditional medicine and this might be attributed to the presence of quercetin and kaempferol, among other phytochemicals.

Protective role of Sterculia tragacantha aqueous extract on pancreatic gene expression and oxidative stress parameters in streptozotocin-induced diabetic rats.

OBJECTIVES: The current study evaluates the protective role of aqueous extract of Sterculia tragacantha leaf (AESTL) on pancreatic gene expressions (insulin, PCNA, PDX-1, KI-67 and GLP-1R) and oxidative stress parameters in streptozotocin-induced diabetic rats. METHODS: Diabetes mellitus was induced into the experimental Wistar animals via intraperitoneal (IP) injection of streptozotocin (35 mg/kg body weight) and 5% glucose water was given to the rats for 24 h after induction. The animals were categorized into five groups of 10 rats each as follows normal control, diabetic control, diabetic rats administered AESTL (150 and 300 mg/kg body weight) and diabetic rats administered metformin (200 mg/kg) orally for two weeks. Thereafter, the animals were euthanized, blood sample collected, pancreas harvested and some pancreatic gene expressions (such as insulin, PCNA, PDX-1, KI-67, and GLP-1R)s as well as oxidative stress parameters were analyzed. RESULTS: The results revealed that AESTL significantly (p<0.05) reduced fasting blood glucose level, food and water intake, and lipid peroxidation in diabetic rats. Diabetic rats administered different doses of AESTL showed a substantial upsurge in body weight, antioxidant enzyme activities, and pancreatic gene expressions (insulin, PCNA, PDX-1, KI-67, and GLP-1R). CONCLUSIONS: It can therefore be concluded that AESTL has the ability to protect the pancreas during diabetes mellitus conditions.

Sterculia tragacantha Lindl Aqueous Leaf Extract Ameliorate Cardiomyopathy in Streptozotocin-induced Diabetic Rats via Urotensin II and FABP3 Expressions.

Sterculia tragacantha (ST) Lindl leaf is commonly used locally in the management of diabetes mellitus (DM) and its complications. This study was aimed at assessing the valuable effects of ST leaf on streptozotocin-diabetic cardiomyopathy (DCM). Streptozotocin was administered intraperitoneally to the experimental animals to induce DM, and hence, placed on different doses of ST for 14 days. Thereafter, on the 15th day of the experiment, the animals were euthanized, and a number of cardiomyopathy indices were investigated. The diabetic rats exhibited a momentous increase in hyperlipidemia, lipid peroxidation as well as a significant (p < 0.05) decline in antioxidant enzyme activities. The serum creatine kinase MB (CK-MB), C-reactive protein (CRP), cardiac troponin I, tumour necrosis factor-alpha (TNF-α) and urotensin II expression revealed a significant (p < 0.05) upsurge in diabetic rats. Also, the expression of GLUT4 and fatty acid-binding protein 3 (FABP3) were significantly (p < 0.05) reduced in diabetic rats. However, at the conclusion of the experimental trial ST significantly (p < 0.05) attenuated hyperlipidemia, oxidative stress biomarkers by augmenting the antioxidant enzyme activities and decrease in lipid peroxidation, ameliorated CK-MB, CRP, cardiac troponin I, TNF-α, and urotensin-II levels, and improved GLUT4 and FABP3 expressions. Similarly, the administration of ST prevented histological alterations in the heart of diabetic animals. Therefore, the obtained results suggest that ST could mitigate DCM in streptozotocin-induced diabetic rats.

In vivo laxative, anti-diarrheal, hepatoprotective and diuretic investigations of Sterculia diversifolia and its isolated compound.

OBJECTIVE: To investigated the laxative, anti-diarrheal, hepatoprotective and diuretic activity of Sterculia diversifolia and its isolated compounds. METHODS: The laxative activity was studied by counting wet stools while anti-diarrheal activity was performed by measuring gastrointestinal tract motility. Hepatoprotective activity was studied by biochemical and histo-pathological analysis while diuretic activity was performed by urine collection protocol. RESULTS: Doses of 30 and 100 mg/kg of crude methanolic extract of Sterculia diversifolia (MESD) stem bark and leaves, significantly (P < 0.05, P < 0.01) produced wet feces in subjects pretreated with atropine while 8-hydroxyquercetin and dihydroquercetin showed highly significant (P < 0.001) results by increasing fecal weight and water contents without producing diarrhea. MESD stem bark and leaves also dose-dependently lowered diarrhea while 8-hydroxyquercetin and dihydroquercetin showed highly significant (P < 0.001) results by producing shaped stools in mice. MESD, 8-hydroxyquercetin and dihydroquercetin offered significant protection against histopathological changes in the liver. Diuretic activity of Crude MESD stem bark and leaves extracts shows highly significant diuretic effect while dihydroquercetin showed better results than 8-hydroxyquercetin. CONCLUSION: It is concluded that Sterculia diversifolia and its isolated compounds bears laxative, anti-diarrheal, hepatoprotective and diuretic effects.

Recent advances of Sterculia gums uses in drug delivery systems.

Trees of the genus Sterculia produce polysaccharide-rich exudates, such as karaya gum (Sterculia urens), chicha gum (Sterculia striata), and Sterculia foetida gum. These anionic biomaterials are biodegradable, with high viscosity, low toxicity, and gelling properties in aqueous media. According to these properties, they show promising applications as a polymer matrix for use in drug delivery systems. For this application, both the chemically modified and the unmodified polysaccharide are used. This review focuses on analyzing the state of the art of recent studies on the use of Sterculia gums in a variety of pharmaceutical forms, such as tablets, hydrogels, micro/nanoparticles, and mucoadhesive films. Sterculia gums-based delivery systems have potential to be explored for new drug delivery systems.

Effect of Cryostructuring Treatment on Some Properties of Xanthan and Karaya Cryogels for Food Applications.

Cryogels are novel materials because the manufacturing process known as cryostructuring allows biopolymers to change their properties as a result of repeated controlled freeze-thaw cycles. Hydrogels of xanthan and karaya gums were evaluated after undergoing up to four controlled freeze-thaw cycles in indirect contact with liquid nitrogen (up to -150 °C) to form cryogels. Changes in structural, molecular, rheological, and thermal properties were evaluated and compared to those of their respective hydrogels. Samples were also analyzed by Scanning Electron Microscopy (SEM), Fourier Transform Infrared Spectroscopy with Attenuated Total Reflection (FTIR-ATR), Rotational Rheology (RR), Modulated Differential Scanning Calorimetry (MDSC) and zeta potential (ζ). In general, significant differences (p < 0.05) between the numbers of freeze-thaw cycles were found. Karaya cryogels were not stable to repeated cycles of cryostructuring such as the three-cycle xanthan cryogel, which has the best structural order (95.55%), molecular interactions, and thermal stability, which allows the generation of a novel material with improved thermal and structural properties that can be used as an alternative in food preservation.

Optimization, in vitro release and toxicity evaluation of novel pH sensitive itaconic acid-g-poly(acrylamide)/sterculia gum semi-interpenetrating networks.

BACKGROUND: In recent era, pH sensitive polymeric carriers that combines the materials engineering and medicine is gaining researcher's attention as they maximizes drug concentration at site of absorption and reduces side effects for e.g. orally administered cetirizine HCl (CTZ HCl) upsets the stomach and furthermore shows high intestinal absorption. Thus, development of pH sensitive hydrogels with sufficient mechanical strength will be good candidate to address this issue. METHODS: Here, we developed pH sensitive itaconic acid-g-poly(acrylamide)/sterculia gum (IA-g-poly(AM)/sterculia gum) semi-interpenetrating network (semi-IPN) by free radical polymerization technique for intestinal delivery of CTZ HCL. RESULTS: Optimized formulation (I5) with 6% w/w IA showed negligible swelling at pH 1.2, and maximum swelling at pH 7.4. Solid state characterization of optimized formulation showed successful development of semi-IPN structure and incorporation of drug without any noticeable drug-carrier interaction. In vitro release study showed biphasic pH dependent release of CTZ HCl, where initial burst release was observed at acidic pH followed by sustained release at basic pH. Acute oral toxicity and histopathological studies confirmed the non-toxic nature of IA-g-poly(AM)/sterculia gum. CONCLUSION: Conclusively, developed biocompatible semi-IPN hydrogels with sufficient pH sensitivity and mechanical strength could serve as a potential carrier for intestinal delivery of CTZ HCL to maximize its absorption and reduce side effects.

Chemical constituent with cytotoxicity from Sterculia diversifolia.

One new coumarin (stercularin), along with eleven known compounds, was isolated for the first time from ethyl acetate fraction of Sterculia diversifolia. The structures of isolated compounds were characterized by spectroscopic techniques such as EIMS, 1H-NMR and 13C-NMR. Compound 1 showed significant cytotoxicity by brine shrimp lethality assay (LD50: 8.00 µg/ml) and PC-3 cell lines protocol (IC50: 3.92 ± 0.20 µg/ml), respectively.

Stercufoetin A, new oleanane-type triterpenoid from the leaves of Sterculia foetida L.

From the leaves of Sterculia foetida L., one new oleanane-type triterpenoid, named stercufoetin A (1) together with four known ones, vergatic acid (2), ß-amyrin (3), oleanolic acid (4) and maslinic acid (5) were purified by diversely chromatographic methods. Their structures were proposed by HR-APCI-MS and NMR experiments. Compounds (2-5) were notified for the first time from this species. Compound 1 showed weak cytotoxic effect against three human cancer cell lines (MCF-7, HepG2 and HeLa) using SRB assay.

Characterization of raft microdomains in bovine mammary tissue during lactation: How they are modulated by fatty acid treatments.

The objective of the current study was first to characterize lipid raft microdomains isolated as detergent-resistant membranes (DRM) from mammary gland tissue, and second to determine how dietary fatty acids (FA) such as conjugated linoleic acid (CLA), 19:1 cyclo, and long-chain n-3 polyunsaturated FA affect lipid raft markers of mammary cells, and to finally establish relationships between these markers and lactation performance in dairy cows. Eight Holstein cows were used in a replicated 4 × 4 Latin square design with periods of 28 d. For the first 14 d, cows received daily an abomasal infusion of (1) 406 g of a saturated FA supplement (112 g of 16:0 + 230 g of 18:0) used as a control; (2) 36 g of a CLA supplement (13.9 g of trans-10,cis-12 18:2) + 370 g of saturated FA; (3) 7 g of Sterculia fetida oil (3.1 g of 19:1 cyclo, STO) + 399 g of saturated FA; or (4) 406 g of fish oil (55.2 g of cis-5,cis-8,cis-11,cis-14,cis-17 20:5 + 59.3 g of cis-4,cis-7,cis-10,cis-13,cis-16,cis-19 22:6, FO). Mammary biopsies were harvested on d 14 of each infusion period and were followed by a 14-d washout interval. Cholera toxin subunit B, which specifically binds to ganglioside M-1 (GM-1), a lipid raft marker, was used to assess its distribution in DRM. Infusions of CLA, STO, and FO were individually compared with the control, and significance was declared at P ≤ 0.05. Milk fat yield was decreased with CLA and FO, but was not affected by STO. Milk lactose yield was decreased with CLA and STO, but was not affected by FO. Mammary tissue shows a strong GM-1-signal enrichment in isolated DRM from mammary gland tissue. Caveolin (CAV) and flotillin (FLOT) are 2 proteins considered as lipid raft markers and they are present in DRM from mammary gland tissue. Distributions of GM-1, CAV-1, and FLOT-1 showed an effect of treatments determined by their subcellular distributions in sucrose gradient fractions. Regardless of treatments, data showed positive relationships between the yield of milk fat, protein, and lactose, and the abundance GM-1 in DRM fraction. Milk protein yield was positively correlated with relative proportion of FLOT-1 in the soluble fraction, whereas lactose yield was positively correlated with relative proportion of CAV-1 in the DRM fractions. Infusion of CLA decreased mRNA abundance of CAV-1, FLOT-1, and FLOT-2. Regardless of treatments, a positive relationship was observed between fat yield and mRNA abundance of FLOT-2. In conclusion, although limited to a few markers, results of the current experiment raised potential links between variation in specific biologically active component of raft microdomains in bovine mammary gland and lactation performances in dairy cows.

Phthalic anhydride esterified chicha gum: characterization and antibacterial activity.

The objective of this research was to modify chicha gum with phthalic anhydride to obtain a new biologically active material. The chemical modification of the gum structure was proven through FTIR, elemental analysis, XRD, TG, and DSC. The derived materials demonstrated excellent inhibitory effect against P. aeruginosa and K. pneumoniae species (rating 100% inhibition) and could also inhibit Escherichia coli growth. The best antimicrobial activity observed for the derivatives suggests that chicha gum hydrophobization due to the addition of phthalic groups improved the interaction of these derivatives with bacterial cell wall components. On the other hand, the derivatives increased CC50 in macrophages but did not present acute toxicity or hemolytic activity, indicating that they are promising for use in prophylaxis or treatment of infections caused by Gram-negative bacteria.

Modulation of Drug Release from Natural Polymer Matrices by Response Surface Methodology: in vitro and in vivo Evaluation.

PURPOSE: The present work aimed at challenging the efficacy of natural gums, karaya and locust bean gum, as matrix-forming polymers for the formulation of sustained-release tablets of diltiazem, a model drug. METHODS: Central design composite was adopted for the formulation and optimization of tablet formulations. The two gums have been selected as independent variables. The dependent factors chosen were the amount of drug released in 1st hour (Y1), amount of drug released after 12 h (Y2), diffusion exponent (Y3), and time for half of the total drug released (T50%) (Y4). Wet granulation approach was used for the formulation of tablets. FT-IR, DSC, in vitro dissolution, swelling-erosion investigations, SEM, and stability studies were carried out. RESULTS AND DISCUSSION: It was evident that the release pattern from the prepared formulations was significantly influenced by the quantity of gum(s) in the tablet. FT-IR and DSC results confirm drug-polymer compatibility. Polynomial equations were used for the prediction of quantitative impact of independent factors at different levels on response variables. After ANOVA analysis, the significant factors were considered for constrained optimization to get the optimized formula. The optimized formula generated by the response surface methodology was evaluated both for in vitro and in vivo properties. The optimized formula and a sustained-release marketed product were subjected to in vivo studies in rabbits and the results of the t-test demonstrated insignificant variation in pharmacokinetic parameters among the two formulations, confirming that the prepared tablet showed sustained-release profile. CONCLUSION: The results indicated that karaya and locust bean gum can be effectively used to formulate sustained-release tablets.

Sterculia striata gum as a potential oral delivery system for protein drugs.

Natural polysaccharides have been investigated as vehicles for oral insulin administration. Because of their non-toxic, renewable, low cost and readily available properties, gums find multiple applications in the pharmaceutical industry. This work aimed to develop a Sterculia striata gum-based formulation associated with additional biopolymers (dextran sulfate, chitosan, and albumin), a crosslinking agent (calcium chloride) and stabilizing agents (polyethylene glycol and poloxamer 188), to increase the oral bioavailability of proteins. Insulin was used as a model drug and the methods used to prepare the formulation were based on ionotropic pregelation followed by electrolytic complexation of oppositely charged biopolymers under controlled pH conditions. The developed formulation was characterized to validate its efficacy, by the determination of its average particle size (622 nm), the insulin encapsulation efficiency (70%), stability in storage for 30 days, and the in vitro mucoadhesion strength (92.46 mN). Additionally, the developed formulation preserved about 64% of initial insulin dose in a simulated gastric medium. This study proposed, for the first time, a Sterculia striata gum-based insulin delivery system with potential for the oral administration of protein drugs, being considered a valid alternative for efficient delivery of those drugs.