Natural Products Journal, The - Volume 6, Issue 1, 2016

Genistein is a natural compound belonging to the chemical class of isoflavone. This molecule is present in the significant portion of our diet in the form of Soy food products. This is the most extensively studied isoflavone due to its significance affinity towards targets of potential pharmacological and neutraceutical benefits. The potential pharmacological applications of this molecule have been found as anti-cancer, anti-obesity, anti-diabetic, neuroprotective, antiosteoporosis, and cardio protective agent. This review provides comprehensive coverage of the chemistry, pharmacology, toxicity and extraction of genistein.

Black cumin, Nigella sativa (NS), which is also known as black seed (Kalijeera), is an annual flowering plant from the Ranunculaceae family. Its seeds were used in most ancient medical systems. For ages it was considered to be a panacea. It is rooted in our traditions and has flourished into an intensively investigated medicinal plant. There is an abundance of reports on the biological activities of Nigella sativa seeds or extracts. The spectrum of its activity is impressive and includes antimicrobial, antiviral, anticancer, antimalarial as well as an antidiabetic or immunostimulatory potency. In this review both in vitro and in vivo results are gathered and the results of clinical trials are discussed. Patents and the industrial use of NS as both a food supplement and as animal feed are also mentioned. An analysis of the literature data showed that the comprehensive investigations of Nigella sativa are fairly well translated into actual everyday healthcare. The data presented in this review reveals future use of this valuable plant.

To ensure the quality, the processing of artisanal corn meal in a production unit located in the southeastern state of São Paulo was evaluated. It handles an average of 15 tons/months, all under GMP and HACCP regulations. Of the 153 items examined on a checklist, only 42 were in compliance. In addition, the following Control Points (CPs) were identified: humidification of hominy and corn. The Critical Control Points (CCPs) were: the water, the oven, the screen that covered the humidification tank and final product. Some steps were not GMP-compliant, so corrective measures based on the CP and CCPs were suggested. One important factor was the need to comply with the specific legislation about folic acid and iron supplementation in the product. Another was the technique used to add them to the product.

The study was undertaken to obtain the scientific evidence to the efficacious claim of the use of Jambrushila Tablet in the management of type-2 diabetes. The SD rats were divided into 4 groups: normal control, disease control, diseased treated with metformin (10 mg/kg) and diseased treated with Jambrushila Tablet (100 mg/kg). Type 2 diabetes was induced in male Sprague Dawley rats by feeding them a high-fat diet in combination streptozotocin (35 mg/kg). Treatment was given for a period of 4 weeks. Insulin resistant rats developed characteristic features with insulin resistance syndrome such as hyperglycemia, hyperinsulinemia hypertriglyceridemia, hypercholesterolemia, glucose intolerance. Treatment with formulation and metformin exhibited significant decrease in body weight, serum glucose and insulin levels as compared to disease control rats. Following the administration of formulation and metformin, it was observed that there was an increase in HDL levels and decrease in the serum cholesterol, triglyceride, LDL-cholesterol and VLDL-cholesterol levels when compared to disease control group. The treatment also exhibited significant reduction in AUCglucose and AUCinsulin in oral glucose tolerance test. Homeostasis model assessment of insulin resistance (HOMAIR) and quantitative insulin sensitivity check index (QUICKI) were found to be significantly improved without significant modification of fasting glucoses to insulin ratio (FGIR) and HOMA-β index. Our findings indicate that Jambrushila Tablet can be beneficial for treatment of hyperglycemia and hyperlipidemia associated with type-2 diabetes.

Crocin is an apocarotenoid present in Nyctanthes arbortrisits (NAT) flower calyx extract in abundant quantity of about 36.7% w/w. The carotenoid rich extract of NAT exhibited dose dependant anti-angiogenic effect in chick-chorioallantoic membrane (CAM) assay. The anti-angiogenic activity of NAT extract (1 mg/ml) was observed to be equivalent to Heparin (1 mg/ml) with the IC50 value of 0.5 mg/ml. The antiangiogenic activity of NAT was further confirmed by in-vivo Matrigel Matrix model of Balb/c mice with VEGF inhibitor, sunitinib malate (1 μM) as the anti-angiogenic control. The in-vivo study revealed significant (P<0.01) reduction in hemoglobin levels and inhibited angiogenesis as compared to angiogenic control viz. VEGF loaded matrigel matrix. The anti-angiogenic activity of NAT calyx ethanolic extract is likely to be due to the presence of Crocin since carotenoids possess inherent strong anti-oxidant potential. Our result brings out a new naturally occurring anti-angiogenic agent which may find its utility in the treatment of conditions like cancer, diabetic retinopathy and cataract.

Objective: The root and stem barks of Eleutherococcus senticosus have been used to treat emotional and physical fatigue in China, Russia, Korea, and Japan. The effects of E. senticosus on recovery from physical fatigue and the expenditure of energy currently remain unclear. We herein examined the effects of E. senticosus extract on recovery from physical fatigue after the forced swimming test as well as fatty acid β-oxidation in the liver and skeletal muscle of mice. Methods: 1) Physical fatigue; E. senticosus extract (500 and 1000 mg/kg, twice daily) was administered orally to ICR male mice for 7 consecutive days. After swimming had been performed for 15 min, each mouse was placed on the cover of a 100-mm culture plate, and the time for each mouse to move away from the cover was measured. 2) Fatty acid β-oxidation in the liver and skeletal muscle; E. senticosus extract (500 and 1000 mg/kg) was administered orally twice daily to C57BL/6J male mice for 21 consecutive days. The initial and final body and liver weight were measured, and then fatty acid β-oxidation activity in the liver and skeletal muscle was measured by methods using [1-14C] palmitic acid. Key Findings: Recovery times after forced swimming were shorter in E. senticosus extract (500 and 1000 mg/kg)-treated mice than in vehicle-treated mice. The body and liver weight had no effect by the oral administration of E. senticosus extract, vitamin mixture and L-carnitine. Fatty acid β-oxidation activity in skeletal muscle was increased by E. senticosus extract (500 and 1000 mg/kg). Conclusion: E. senticosus may enhance recovery from physical fatigue induced by forced swimming by accelerating energy changes through fatty acid β-oxidation in skeletal muscle.

Myrsine africana L. (Family Myrsinaceae) commonly known as mirting, is an evergreen shrub found wildly in tropical Asia to Africa. The plant has been traditionally used to treat various diseases and extensively used in folk medicine. The reported literature reveals that there is no pharmacological activities carried out on the fruits of M. africana in order to validate its traditional claim. The aim of the present study is to evaluate the anti-inflammatory and analgesic activity of methanolic and hydro-alcoholic extracts of fruits of M. africana at a dose level of 100, 200 and 500 mg/kg. The safety of drug was evaluated by sub-acute toxicity study as per OECD guidelines. The anti-inflammatory activity was carried out by carrageenan induced paw edema model and analgesic activity was done by hot plate, tail flick and acetic acid induced writhing methods. The maximum per cent inhibition of paw edema was found to be 57% in hydro-alcoholic extract at a dose level of 500 mg/kg in carrageenan induced paw edema model as compared to the standard drug ibuprofen (74.6%). The average response time at the dose of 500 mg/kg in tail flick and hot plate models was found to be 6.6 ± 0.79 mins and 6.89 ± 0.17 mins (at 120 mins and 90 mins) respectively which is comparable with the standard drug. In acetic acid writhing test both the extracts showed significant reduction in writhes as compared to standard. The pharmacological activities were found to be dose dependent. The acute toxicity study confirmed the drug to be non-toxic and safe. So it has been observed that the fruit of M. africana has marked beneficial effects against centrally and peripherally inflammation models and can be used to treat various disorders associated with inflammation.

Background: Metformin hydrochloride, an oral hypoglycaemic, shows better absorption from upper part of the gastric region. Natural/herbal substances have been investigated for the development of natural polymer-based drug delivery systems owing to the desirable properties like biodegradability, biocompatibility, aqueous solubility, swelling ability, easy availability and cost effectiveness. Method: Therefore, three natural macromolecules: Glycine max (soya chunks), Metroxylon sagu (sago starch) and Plantago ovata (psyllium husk) were used for developing its gastroretentive floating microparticles for expected improvement in bioavailability. The macromolecules and the prepared microparticles were evaluated for physicochemical properties, FTIR, XRPD, DSC and dug release. Result: The percent drug content was in the range of 60.353 ± 1.25 to 92.682 ± 2.47 % for all the microparticles. All the formulations showed good swelling and floating properties (the formulation prepared with P. ovata showed the best swelling and in vitro floatability). The FTIR studies showed that the herbal carriers were compatible with the drug. XRD and DSC studies showed a transition in the physical state of the drug in the formulations from crystalline state to amorphous state. In vitro drug release studies showed good percent cumulative drug release from all the formulations (72.13 to 87.06 % at the end of 6 hour) with non-fickian diffusion process. Conclusion: Therefore, it was concluded that the herbal macromolecules may be the potential, safe and effective carriers for improving the drug delivery of the metformin like drugs by developing, effective gastroretentive floating drug delivery systems.

Background: Metformin hydrochloride, an oral hypoglycaemic, shows better absorption from upper part of the gastric region. Natural/herbal substances have been investigated for the development of natural polymer-based drug delivery systems owing to the desirable properties like biodegradability, biocompatibility, aqueous solubility, swelling ability, easy availability and costeffectiveness. Method: Therefore, three natural macromolecules: Glycine max (soya chunks), Metroxylon sagu (sago starch) and Plantago ovata (psyllium husk) were used for developing its gastroretentive floating microparticles for expected improvement in bioavailability. The macromolecules and the prepared microparticles were evaluated for physicochemical properties, FTIR, XRPD, DSC and dug release. Result: The percent drug content was in the range of 60.353±1.25 to 92.682±2.47% for all the microparticles. All the formulations showed good swelling and floating properties (the formulation prepared with P. ovata showed the best swelling and in vitro floatability). The FTIR studies showed that the herbal carriers were compatible with the drug. XRD and DSC studies showed a transition in the physical state of the drug in the formulations from crystalline state to amorphous state. In vitro drug release studies showed good percent cumulative drug release from all the formulations (72.13 to 87.06% at the end of 6 hour) with non-fickian diffusion process. Conclusion: Therefore, it was concluded that the herbal macromolecules may be the potential, safe and effective carriers for improving the drug delivery of the metformin like drugs by developing, effective gastroretentive floating drug delivery systems.