Synthesis, antimicrobial evaluation, and structure-activity relationship of α-pinene derivatives.

Several (+)- and (-)-α-pinene derivatives were synthesized and evaluated for their antimicrobial activity toward Gram-positive bacteria Micrococcus luteus and Staphylococcus aureus, Gram-negative bacterium Escherichia coli, and the unicellular fungus Candida albicans using bioautographic assays. (+)-α-Pinene 1a showed modest activity against the test organisms, whereas (-)-α-pinene 1b showed no activity at the tested concentration. Of all the α-pinene derivatives evaluated, the ß-lactam derivatives (10a and 10b) were the most antimicrobial. The increase in the antimicrobial activity of 10a compared to 1a ranged from nearly 3.5-fold (C. albicans) to 43-fold (S. aureus). The mean ± standard deviation for the zone of inhibition (mm) for 10a (C. albicans) was 31.9 ± 4.3 and that for S. aureus was 51.1 ± 2.9. Although (-)-α-pinene 1b was not active toward the test microorganisms, the corresponding ß-lactam 10b, amino ester 13b, and amino alcohol 14b showed antimicrobial activity toward the test microorganisms. The increase in the antimicrobial activity of 10b compared to 1b ranged from 32-fold (S. aureus) to 73-fold (M. luteus). The mean ± standard deviation for the zone of inhibition (mm) for 10b (S. aureus) was 32.0 ± 0.60 and that for M. luteus was 73.2 ± 0.30.

Use of laser-induced breakdown spectroscopy for the detection of glycemic elements in Indian medicinal plants.

The demand for interdisciplinary research is increasing in the new millennium to help us understand complex problems and find solutions by integrating the knowledge from different disciplines. The present review is an excellent example of this and shows how unique combination of physics, chemistry, and biological techniques can be used for the evaluation of Indian medicinal herbs used for treating diabetes mellitus. Laser-induced breakdown spectroscopy (LIBS) is a sensitive optical technique that is widely used for its simplicity and versatility. This review presents the most recent application of LIBS for detection of glycemic elements in medicinal plants. The characteristics of matrices, object analysis, use of laser system, and analytical performances with respect to Indian herbs are discussed.

A Scientific Validation of Antihyperglycemic and Antihyperlipidemic Attributes of Trichosanthes dioica.

The present study was undertaken to scientifically validate the antidiabetic activity of aqueous fruit extract of Trichosanthes dioica Roxb. (Family: Cucurbitaceae) which has been traditionally used for managing diabetes mellitus. This plant commonly known as "Sespadula" in English has not been explored scientifically so far for its glycemic potential except by our research group. The study was conducted with variable doses on normal, mild, and severe diabetics models, and several biochemical parameters including blood glucose level (BGL) were assessed. Maximum fall in BGL of 23.8% in normal rats and of 31.3% in mild diabetic rats was observed during their fasting blood glucose (FBG) and glucose tolerance test (GTT) with the dose of 1000 mg kg(-1). In severely diabetic animals after 4 weeks treatment with FBG, postprandial glucose, total cholesterol, and triglyceride levels were reduced by 28.7, 30.7, 57.2, and 18.5%, whereas high density lipoprotein, total protein, hemoglobin, and body weight were increased by 33.0, 36.7, 15.7 and 16.7%, respectively. Moreover, urine sugar was reduced from +4 to +1. Thus, the study scientifically validates the traditional use of T. diocia in diabetes management and could be developed as an effective oral agent for treating diabetes mellitus and complications associated with it.

Biomedical applications of nano-antioxidant.

For centuries now, antioxidants have been known to provide better health by neutralizing the free radicals which are continuously produced in the human body. In normal circumstances, self-antioxidant defense system of the human body is capable of quantitatively managing the free radicals. However, in certain cases, which are at the threshold of developing diseases like diabetes and Alzheimer's, the human body calls for an external source of antioxidants. Since orally delivered antioxidants are easily destroyed by acids and enzymes present in the human system, only a small portion of what is consumed actually gets absorbed. Hence, there is a recognized and urgent need to develop effective methods for efficiently delivering antioxidants to the required sites. This chapter provides an in-depth overview and analysis of two such methods and processes-nano-encapsulation and nano-dendrimers. Among the various nanoscale delivery mechanisms, nano-encapsulation has emerged as a key and efficient delivery process. Designed as a spongelike polymer, nano-encapsulated antioxidants provide a protective vehicle which keeps antioxidants from being destroyed in the human gut and ensures their better absorption in the digestive tract. In fact, the nano-capsules bind themselves to the intestinal walls and pour antioxidants directly into the intestinal cells, which allow them to be absorbed directly into the blood stream. Another distinguished and popular mode for delivering antioxidants is that of nano-polymers known as dendrimers. Dendrimers involve multiple branches and sub-branches of atoms radiating out from a central core. Dendrimers afford a high level of control over their architectural design, including their size, shape, branching length or density, and surface functionality. Such flexibility makes these nanostructures ideal carriers in biomedical applications such as drug delivery, gene transfection, and imaging. Antioxidant dendrimers, made out of numerous units of antioxidants connected with each other in a branched fashion, provide numerous possible sites to couple with an active species and have enhanced free radicals scavenging potency. These dendrimer chains are biocompatible, biodegradable with nontoxic degradation products, and well suited for targeted drug delivery and other biomedical applications. Recent successes in simplifying and optimizing the synthesis of dendrimers, such as the "lego" and "click" approaches, provide a large variety of structures while at the same time reducing the cost of their production. The use of these highly branched, nanometer-sized, polymeric materials as nano-antioxidants for prevention and treatment of human diseases, associated with oxidative stress, is of immense public health relevance globally.

Role of Moringa oleifera in regulation of diabetes-induced oxidative stress.

OBJECTIVE: To evaluate the antioxidant activity of aqueous extract of Moringa oleifera (M. oleifera) young leaves by in vivo as well as in vitro assays. METHODS: In vitro study included estimation of total phenolic, total flavonol, total flavonoid and total antioxidant power (FRAP assay). In addition, in vivo study was done with the identified most effective dose of 200 mg/kg of its lyophilized powder on normal and diabetic rats. Its effect on different oxidative free radical scavenging enzymes,viz, superoxide dismutase (SOD), catalase (CAT), glutathione-S-transferase (GST), lipid peroxide (LPO) contents were measured. RESULTS: Significant increase in activities of SOD, CAT, GST while, a decrease in LPO content was observed. Whereas, total phenolic, flavonoid and flavonol contents in the extract were found to be 120 mg/g of GAE, 40.5 mg/g of QE and 12.12 mg/g of QE, respectively. On the other hand, FRAP assay results of M. oleifera leaves was (85.00 ± 5.00) µM/g of extract powder. CONCLUSIONS: The significant antioxidant activities of M. oleifera leaves from both in vivo as well as in vitro studies suggests that the regular intake of its leaves through diet can protect normal as well as diabetic patients against oxidative damage.

Controlled synthesis, characterization, and application of iron oxide nanoparticles for oral delivery of insulin.

Impurity-free, controlled synthesis of iron oxide nanoparticle, in ultrapure water and chitosan, using laser ablation technique and its application for type II diabetes management through oral delivery of insulin-loaded iron oxide-chitosan nanocomposite is presented. The purity of the nanoparticle is monitored by laser-induced breakdown spectroscopy technique. The synthesized iron oxide nanoparticle was characterized by UV/Vis absorption spectroscopy, and morphological study was performed by scanning electron microscope. The intensity of absorption peak and wavelength corresponding to peak of the nanoparticle prepared in water and chitosan is dependent on the laser energy used for ablation purpose. Red shift in the absorption peak wavelength was observed by increasing laser energy. In addition to red shift, an increase in intensity of absorption peak was also seen when ablating laser energy was increased. The appearance of a weak peak around 295 nm was observed in iron oxide-chitosan nanocomposite. The spherical shape of the nanoparticle synthesized at the lower laser energy has gradually changed to triangular and irregular shaped structures as ablating laser energy was increased. The spherical nanoparticles loaded with insulin were used for oral delivery for diabetic management. The iron oxide-chitosan nanocomposite loaded with insulin has resulted in reduction in blood glucose level in mild diabetic, subdiabetic, and severely diabetic rats; more than 51 % reduction in blood glucose level, compared to the control group, has been achieved in the present work.

Antidiabetic effect of Raphanus sativus root juice.

CONTEXT: Many plants have been explored scientifically and systematically and claimed to be useful for the treatment of diabetes mellitus by various research groups worldwide. The present study is a further effort in the direction of developing a novel oral antidiabetic agent of high potential with minimal or no side effects. OBJECTIVE: This study screened the glycemic attributes of Raphanus sativus L. (Brassicaceae) root juice in normal as well as sub- and mild-diabetic models. MATERIALS AND METHODS: The variable doses of 100, 200, 300, and 400 mg kg(-1) body weight (bw) of the extract were administered orally to normal and streptozotocin (STZ)-induced sub- and mild-diabetic rats in order to define its glycemic potential. Glibenclamide was used as a reference drug. RESULTS: The dose of 300 mg kg(-1)bw was identified as the most effective dose which lowers the blood glucose level (BGL) by 33.4% (p < 0.001) at 6 h during fasting blood glucose (FBG) studies in normal rats. However, the glucose tolerance test (GTT) revealed the maximum reduction of 15.9% (p < 0.001) in BGL at 3 h in normal rats with the same dose, whereas the reduction observed was by 23.8 and 28.3% (p < 0.001) in sub- and mild-diabetic rats, respectively, at the same interval of time. DISCUSSION AND CONCLUSION: This evidence clearly indicates that Raphanus sativus root juice possesses good hypoglycemic potential coupled with antidiabetic efficacy.

Hypolipidaemic & hepatoprotective effects of Psidium guajava raw fruit peel in experimental diabetes.

BACKGROUND & OBJECTIVES: The study evaluated the hypolipidaemic and hepatoprotective effects of unripe Psidium guajava fruit peel aqueous extract in streptozotocin (STZ) induced severely diabetic rats by assaying their triglyceride (TG), total cholesterol (TC), high density lipoprotein (HDL) cholesterol, alkaline phosphatase (ALKP), asperate amino transeferase (AST), alanine amino transferase (ALT) and creatanine (CRTN) levels. METHOD: Severely diabetic albino Wister rats of same age group were treated orally once a day upto 3wk with a dose of 400 mg/kg bw of lyophilized extract. TG, TC, HDL, ALKP, AST, ALT and CRTN were estimated. LDL and VLDL cholesterol levels were calculated from the above measurements by using Friedwald formula. RESULTS: A significant decrease in TG (P<0.01), TC (P<0.01), HDL (P<0.001) VLDL (P<0.001) and LDL (P<0.01), ALKP (P<0.01), AST (P<0.05), ALT (P<0.05) and CRTN (P<0.001) levels were observed after 21 days treatment of aquous extract of raw fruit peel compared to pre treatment levels. INTERPRETATION & CONCLUSION: The extract showed significant hypolipidaemic activity in addition to its hypoglycaemic and antidiabetic activity. In view of its relative non-toxic nature P. guajava raw fruit peel may be a potential antidiabetic agent.

Determination of erythrocyte fragility as a marker of pesticide-induced membrane oxidative damage.

Erythrocytes are readily available cells and a good model system to study the health status of individuals with pathologic complications. It can also serve as a meaningful target to study toxicant/xenobiotic-induced damages. We have prepared different concentrations of a carbamate pesticide (carbofuran) and carried out experiments to determine its toxicity on erythrocytes in terms of mean erythrocyte fragility (MEF). We observed a significant alteration in the osmotic fragility upon treatment with carbofuran. In our earlier studies we have observed a good correlation between OF and OS in diabetic subjects. Study reveals OF as a potential biomarker of oxidative membrane damage in pathologic conditions as well as toxicant/xenobiotic/pesticide-induced oxidative membrane damage to erythrocytes.

LIBS-based detection of antioxidant elements: a new strategy.

The present study deals with the scientific evaluation of antioxidant potential of aqueous extract of Trichosanthes dioica fruits on diabetes-induced oxidative stress of diabetic rats. The most effective dose of mg/kg bw of fruit aqueous extract was given orally to diabetic rats for 30 days. Different oxidative stress parameters were analyzed in various tissues of control and treated diabetic rats. The observed elevated level of lipid peroxidation (LPO) comes down significantly (p < 0.05) and decreased activities of antioxidant enzymes such as catalase (CAT), superoxide dismutase (SOD), glutathione peroxidase (GPx), and glutathione-S-transferase (GST) got increased (p < 0.05) significantly of diabetic rats on extract treatment. Laser-Induced Breakdown Spectroscopy (LIBS) has been used as an analytical tool to detect major and minor elements like Mg, Fe, Na, K, Zn, Ca, H, O, C, and N present in the extract. The higher concentration of Ca(2+), Mg(2+), and Fe(2+), as reflected by their intensities are responsible for antioxidant potential of T. dioica.

Induced cytomictic diversity in maize (Zea mays L.) inbred.

Mutation breeding has been used for improving oligogenic and polygenic characters, disease resistance and quantitative characters including yielding ability. The cytological stability of maize inbred lines is an important consideration in view of their extensive use in genetics and plant breeding research. Investigation in Zea mays L. confirms that the migration of chromosomes is a real event that cannot be misunderstood as an artifact produced by fixation or mechanical injuries. During present investigation, we found that out of six inbred lines of Zea mays L. viz. CM-135, CM-136, CM-137, CM-138, CM-142 and CM-213 at various treatment doses of gamma irradiations viz. 200, 400 and 600 Gy, some of the plants of inbred line CM- 138 at 200 Gy dose displayed characteristic cytoplasmic connections during all the stages of meiosis. Four plants from this treatment set were found to be engaged in a rare phenomenon reported as "Cytomixis". It elucidates that in inbred of Zea mays L., induced cytomixis through gamma rays treatment may be considered to be a possible source of production of aneuploid and polyploid gametes. This phenomenon may have several applications in Zea mays L. improvement in the sense of diversity and ever yield potential.

Antidiabetic effect of Ficus bengalensis aerial roots in experimental animals.

ETHNOPHARMACOLOGICAL RELEVANCE: Herbal preparations of Ficus bengalensis had been considered as effective, economical and safe ethnomedicines for various ailments in Indian traditional system of medicine. AIM OF STUDY: The present study was aimed to explore scientifically the antidiabetic potential of Ficus bengalensis aerial roots as its bark had already been reported to possess antidiabetic efficacy. MATERIALS AND METHODS: Effect of variable doses of aqueous extract of Ficus bengalensis aerial roots on blood glucose level (BGL) of normal-, sub- and mild-diabetic models have been studied and the results were compared with the reference drug Glipizide and elemental Mg and Ca intake as glycemic elements. RESULTS: The dose of 300 mg kg(-1) showed the maximum fall of 43.8 and 40.7% in BGL during FBG and glucose tolerance test (GTT) studies of normal rats, respectively. The same dose showed a marked reduction in BGL of 54.3% in sub- and 51.7% in mild-diabetic rats during GTT. The concentration of Mg (1.02%) and Ca (0.85%) identified through laser induced breakdown spectroscopy (LIBS) in the most effective dose could be responsible for this high percentage fall in BGL as they take part in glucose metabolism. CONCLUSION: The hypoglycemic effect in normoglycemic and antidiabetic effect in sub- and mild-diabetic models of aqueous extract of aerial roots of Ficus bengalensis are due to the presence of these glycemic elements in high concentration with respect to other elements.

Role of glycemic elements of Cynodon dactylon and Musa paradisiaca in diabetes management.

The study defined the scientific evaluation of glycemic elements of extracts of Cynodon dactylon and Musa paradisiaca. A dose of 500 mg/kg body weight (bw) of C. dactylon produced maximum falls of 23.2% and 22.8% in blood glucose levels of normoglycemic rats during studies of fasting blood glucose and glucose tolerance, respectively, whereas the same dose of M. paradisiaca produced a rise of 34.9% and 18.4%. In diabetic rats during glucose tolerance tests, a fall of 27.8% and a rise of 17.5% were observed with the same dose of C. dactylon and M. paradisiaca, respectively. Laser-induced breakdown spectroscopy used for detection of glycemic elements present in both the extracts indicated that C. dactylon was rich in magnesium (Mg), whereas M. paradisiaca was rich in potassium (K) and sodium (Na), comparatively, suggesting thereby the defined roles of these elements in diabetes management.

Antidiabetic effect of Withania coagulans in experimental rats.

The present study defines the systematic evaluation and the role of minerals in glycemic potential of aqueous extract of Withania coagulans fruits in order to develop an effective and safe alternative treatment for diabetes mellitus. Laser Induced Breakdown Spectroscopy was used for glycemic element detection. The study is based on the results of lowering in blood glucose levels of normal, sub, mild and severely diabetic rats assessed during fasting blood glucose, glucose tolerance test and post prandial glucose studies. The dose of 1000mg/ kg was identified as the most effective dose, which reduces the Fasting Blood Glucose level maximum by 33.2% at 4h in normal rats during fasting blood glucose studies. Glucose tolerance test studies of normal, sub and mild diabetic rats showed the maximum reduction of 15.7, 28.9 and 37.8% at 3h respectively. Long-term study in case of severely diabetic rats showed reduction of 52.9 and 54.1% in Fasting Blood Glucose and Post Prandial Glucose levels respectively after 30 days of treatment. The present study, besides confirming hypoglycemic and antidiabetic activities of aqueous extract of W. coagulans, helps in identifying the role of trace minerals like Mg & Ca responsible for antidiabetic potential of this potent indigenous shrub.

Cartap and carbofuran induced alterations in serum lipid profile of Wistar rats.

Wistar rats of 6-8 weeks in age weighing between 120-150 g were exposed to the fixed doses of each of the carbamate pesticides such as cartap (50% LD(50)) and carbofuran (50% LD(50)) as well as a combination of these two with 25% LD(50) of each for one week. The effect of treatments was studied in terms of serum lipid parameters such as high-density lipoprotein, total cholesterol, triglyceride, low-density lipoprotein and very low-density lipoprotein. Treatment with individual doses of carbofuran (50% LD(50)) and cartap (50 % LD(50)) caused significant alterations in the levels of serum lipid parameters. The pesticides treatment resulted in marked decrease in the level of serum high-density lipoprotein where as that of other lipids got significantly elevated. Further, the rats exhibited relatively higher impact of pesticides when treated with the compounds in combination (25 % LD(50) of each). The results indicated that these compounds when used together may exert enhanced effect on the levels of serum lipids in rat.

Curative effect of Cynodon dactylon against STZ induced hepatic injury in diabetic rats.

The aim of the study was to ascertain the role of ethanolic extract of Cynodon dactylon against hepatic complications in streptozotocin (STZ) induced type 2 diabetic models. Effect of the pre identified most effective dose of 500 mg/kg body weight was studied on hepatic injury caused by chemically induced diabetes by 55 mg/kg body weight i.p. injection of STZ in male Wistar rats. The dose of 500mg/kg body weight given once daily for 14 days reduced the levels of serum glutamate oxaloacetate transaminase, serum glutamate pyruvate transaminase, alkaline phosphatase, creatinine and urine sugar significantly (P<0.05) with increase in total protein, haemoglobin and body weight was increased. High LD(50) validates its high margin of safety.

Evidence-based Critical Evaluation of Glycemic Potential of Cynodon dactylon.

The present study is an extension of our previous work carried out on Cynodon dactylon. This study deals with the critical evaluation of glycemic potential of ethanolic extract of defatted C. dactylon. The doses of 250, 500 and 750 mg kg(-1) bw of the extract were administered orally to normal as well as Streptozotocin-induced diabetic rats to study its glycemic potential. The effect of repeated oral administration of the same doses of ethanolic extract was also studied on serum lipid profile of severely diabetic (SD) rats. The dose of 500 mg kg(-1) bw was identified as the most effective dose as it lowered the blood glucose levels of normal by 42.12% and of diabetic by 43.42% during fasting blood glucose (FBG) and glucose tolerance test respectively. The SD rats were also treated daily with this identified dose of 500 mg kg(-1) bw for 2 weeks and a significant reduction of 56.34% was observed in FBG level. Total cholesterol, low density lipoprotein and triglyceride levels were also decreased by 32.94, 64.06 and 48.46% respectively in SD rats whereas, cardioprotective high density lipoprotein increased by 16.45%. The reduced urine sugar level and increased body weight are additional advantages. These evidences clearly indicate that the ethanolic extract of defatted C. dactylon has high antidiabetic potential along with good hypolipidemic profile.

Study of glycemic profile of Cajanus cajan leaves in experimental rats.

The present study deals with the evaluation of glycemic profile of aqueous extract of Cajanus cajan leaves in streptozotocin induced type 2 diabetic rats. Single oral administration of graded doses of aqueous extract of Cajanus cajan leaves showed significant increment of 14.3 % in fasting blood glucose levels of normal rats. The sub diabetic and mild diabetic models have also shown hyperglycemic effect from the same variable doses of the extract. The dose of 1000 mg/kg showed the maximum rise of 17.1, 71.2 and 50.7 % in Blood glucose levels of normal, sub and mild diabetic rats respectively during glucose tolerance test. The study of leaves was taken into consideration on the basis of earlier reported hypoglycemic activity of Cajanus cajan seeds. However the results observed were found just opposite and therefore it may be useful in controlling hypoglycemia, occasionally caused due to excess of insulin and other hypoglycemic drugs.

Effect of water extract of Trichosanthes dioica fruits in streptozotocin induced diabetic rats.

In rats with streptozotocin induced severe diabetes mellitus, aqueous extract of Trichosanthes dioica fruits at a dose of 1000mg/kg body weight daily once for 28 days reduced the levels of fasting blood glucose, postprandial glucose, asparate amino transferase, alanine amino transferase, alkaline phosphatase, creatinine, urine sugar and urine protein where as total protein and body weight was increased. No toxic effect was observed during LD50. Our study suggests that further detailed toxicity studies and mechanism of action of T. dioica would be useful for undertaking human trials.

Assessment of glycemic potential ofMusa paradisiaca stem juice.

The present study reveals the effect of Musa paradisiaca stem juice on blood glucose level (BGL) of normal & diabetic rats. The dose of 500 mg/kg bodyweight produces a significant rise of 28.3% in blood glucose level after 6h of oral administration in normal rats. Whereas, in sub diabetic rats the same dose produces a rise of 16.4% in blood glucose levels within 1h during glucose tolerance test (GTT) and a rise of 16% after 4 h in fasting blood glucose levels of severe diabetic cases. These results were unexpected and important to report as other species of Musa like Musa sapientum has been reported for its hypoglycemic effect.