Synthesis and Antifungal Evaluation of Spirostane Saponins

Methods for the preparation of novel antifungal saponins have been investigated in order to further explore their medicinal utility and provide the opportunity to synthesize their derivatives. Through this work, several partially protected stereoisomers of Cholestane, Androstane and Spirostane have been prepared which could be used for the synthesis of various saponin derivatives in order to discover novel saponin based antifungal agent. Various mono and disaccharide derivatives of these steroids have been synthesized and evaluated for their antifungal activity against four pathogenic fungal strains. Among the various derivatives maltose derivatives were found to have the best antifungal activity. However there is a need for more extensive SAR studies to discover compounds with better potency. Additionally, the branched oligosaccharide synthesis was explored in two parts. First, these results demonstrated that the central 2,3-branched portion can be synthesized efficiently from a partially protected glucopyranosyl acceptor since the C-2 and C-3 alcohols differ in their reactivity in glycosylation reactions. Second, a tagged sugar based strategy for synthesis of branched oliogosaccharides was developed, and found to be effective for general synthesis of branched oligosaccharides. Microwave assisted synthesis of cyclic imides have been explored this was a key precursor for the synthesis of our tag molecules which were required for synthesis of branched oligosachharides. A comparison of microwave versus conventional methods for synthesis of cyclic imides has been studied. The synthesis of tagged sugars and their selective deprotection to remove tag molecules were successfully explored in order to have proof of concept for its applicability towards synthesis of branched oligosaccharides. Benzylic mono and dibromination was achieved in very high yields using microwave conditions using environmentally friendly solvent in order to avoid use of carcinogenic carbon tetrachloride as solvent for this type of reactions. In addition reaction time was reduced to 30 minutes to 3 hours compared to convention methods, which needed more than 15 hours for the benzylic bromination reaction

Estimation of serum lipids in patients with Oral Submucous Fibrosis in India

Objectives: Oral submucous fibrosis (OSMF) is the most prevalent precancerous condition in India. Low levels of lipids serves as a marker and prognostic indicator in the early detection of oral precancerous and cancerous states. In spite of the high prevalence and its potential to undergo malignant transformation, this condition has not widely been investigated with respect to the serum lipid levels. In the present study, an attempt was made to analyze the complete serum lipid profile, total cholesterol (TC), triglycerides (TG), high density lipoprotein (HDL) choleste - rol, low density lipoprotein (LDL) cholesterol and very low density lipoprotein (VLDL) cholesterol in OSMF and controls. Material and Methods: The study was conducted in 45 clinically and histopathologically diagnosed cases of OSMF and 45 age and sex matched controls. The complete lipid profile including TC, TG, HDL cholesterol, LDL choles - terol and VLDL cholesterol was analyzed. Results: The serum lipid levels were significantly lower in the patients with OSMF than in the controls. When the values were compared between different disease stages, the maximum reduction of lipids was evident for stage 3 OSMF. From the present results, it is evident that the level of serum lipids decreases with progression of the disea - se. Conclusions: From these findings, it appears that the decrease in the lipid levels may be considered as a useful marker in the early diagnosis of oral premalignant condition like OSMF

Assessing solutions to overcome Quality 4.0 barriers: a decision-making framework

Purpose The industrial revolution changed the market landscape significantly in all industrial sectors. It has a noteworthy impact on enhancing the quality of goods and services. The quality aspect is of utmost concern and determines the success or failure of any product. Therefore, the presented study analyses the key barriers and solutions of Quality 4.0. Design/methodology/approach Twenty barriers and fifteen solutions were identified using a literature review and investigated using a hybrid approach. Barrier weights were evaluated with the help of the fuzzy AHP method. Furthermore, the computed weights were used to perform computations in the next step using fuzzy-TOPSIS to prioritize the ranking of identified solutions. Findings The research results show that “Lack of applying advanced analytics to uncover Quality 4.0 initiatives” and “Lack of integrating data from various sources across the organization” are the topmost barriers. Furthermore, “Implement a leadership development program focused on Quality 4.0” and “Cross-departmental peer learning environment” are the topmost solutions. Practical implications Managers and industrialists can benefit from Quality 4.0 through improved decision-making, process efficiency, supply chain collaboration, agile quality management, enhanced customer experience and a culture of continuous improvement. This results in better quality, operational effectiveness and a competitive edge. Originality/value The solutions need to be mapped with barriers to adopting Quality 4.0. Furthermore, the research results involve novelty by prioritizing the solutions to overcome the anticipated barriers

Toxicity assessment of the alcoholic leaves extract of Reinwardtia indica

The present study aimed to evaluate the safety of the alcoholic leaves extract of Reinwardtia indica in Charles foster rats through an acute and sub-acute oral administration.For assessment of acute oral toxicity test, ratswere orally treated with single dose of the alcoholic leaves extract of Reinwardtia indica at the doses of 50, 250, 500, 1000 2000 and 5000 mg/kg. In sub-acute toxicity study, using the OECD guidelines no. 407, the extract was administered at the doses of 50, 250, 500, 1000, 2000 mg/kg/day for 28 consecutive days and at the dose of 2000 mg/kg satellite group also used for 6 weeks.In acute toxicity above mentioned doses neither showed mortality nor exterior signs of toxicity. In sub-acute, study no significant changes found in haematological and biochemical level ofthe treated rat after 14 days and 28 days in comparison to control. The histopathology of rat brain, kidney, liver, and heart also showed the no cellular changes after extract treated rat.The alcoholic leaves extract of Reinwardtia indica was found non-toxic in single drug dose administration up to 5000 mg/kg (acute study) and in sub-acute administration up to 2000 mg/kg

The outcome of platelet-rich plasma injection therapy in chronic plantar fasciitis

Background: Plantar Fasciitis is a frequently encountered problem in the everyday practice of orthopaedics. Treatment of Plantar Fasciitis is challenging to treating surgeon. Various conservative non-invasive treatment modalities are available like rest, casting, night splinting, NSAIDs. If conservative management fails then corticosteroid injection over the medial tuberosity of calcaneum is an effective treatment. But in recent years Platelet-rich plasma (PRP) has proved to be a safe alternative approach with less complication. This study aims to find out the effectiveness of PRP injections in Plantar Fasciitis. Material and Method: In this study, 60 patients with Plantar Fasciitis were included. Regular follow up was done at an interval of 4 weeks, 8 weeks and 6 months after PRP injection. Pain intensity was measured before and after injection on every follow up using the Visual Analogue Scale (VAS). Patients who have undergone at least 4 weeks of conservative treatment were included in the study. Results: After analysis of data, the average VAS score before injection was 7.01±1.35. Whereas at the end of the last visit (i.e. 6 months) average VAS score reduced to 2.2±1.25. This difference was statistically significant (ANNOVA test p <0.0001). Conclusion: we concluded that injection of PRP is a safe, convenient and effective approach to treat chronic Plantar Fasciitis

Development and Validation of a Novel LC–MS/MS Method for Simultaneous Determination of Abiraterone and its Seven Steroidal Metabolites in Human Serum: Innovation in Separation of Diastereoisomers Without Use of a Chiral Column

Abiraterone acetate (AA), the prodrug of abiraterone, is FDA-approved for the treatment of castration-resistant prostate cancer. Abiraterone is metabolized in patients to a more potent analogue, D4A. However, we have recently reported that this analogue is further metabolized to additional metabolites in patients treated with AA. Here, we present a liquid chromatography-tandem mass spectrometry method developed to resolve and detect abiraterone and its seven metabolites in human serum using an AB Sciex Qtrap 5500 mass analyzer coupled with a Shimadzu Nexera UPLC station. Analytes and the internal standard (abiraterone-d4) were extracted from human serum using the liquid–liquid extraction procedure. The analytes were separated using a Zorbax Eclipse Plus C18 150 × 2.1 mm, 3.5 μm column at 40 °C and an isocratic mobile phase 35% A (0.1% formic acid in water), 65% B (0.1% formic acid in methanol:acetonitrile; 60:40). Electrospray ionization in positive mode was applied with multiple reaction monitoring in a total run time of 13 min. Abiraterone detection was linear in the range 2–400 ng/mL and all metabolites from 0.1–20 ng/mL. The method was validated following US FDA guidelines for bioanalytical method validation, and all the metabolite results were within the acceptance limits. Despite the similarity in structure and mass transition between the metabolites, the validated method separated all the metabolites, including diastereomers, to allow accurate identification and quantitation of each compound

An overview of the unexplored underutilized fruit crops of Assam, India

Assam is the largest state of North-East India. This state is considered as one of the most extravagant biodiversity hotspots of the world because of its different geography, atmosphere and agro-environmental conditions. Various plant species that incorporate natural products have their starting point in this locale. A considerable number of these are yet to be developed in wild or semi-wild states. Regardless of the huge hereditary decent variety of these natural products, just a couple have been grown as business crops for their monetary, social and strict significance. Some of the explored fruit crops of Assam that have many potentials of being used not only in culinary purpose but also in much Ayurvedic medicine which is still underutilized Some of the underutilized fruit (UUF) crops of Assam are Kordoi/Carambola (Averrhoa Carambola), Leteku/Burmese grape (Baccurea sapida), Amra/Hog plum (Spondius mangifera), Jalphai/Olive (Olea europaea), Bael/Stone apple (Aegle marmelos), Imli/Tamarind (Tamarindus indica), Jamun/Wild Jamun (Sygium cuminii), Thekera/Garcinia spp., Poniol/Govorners plum (Falcourita jangomas), Outenga/Elephant fruit (Delinia indica ) and Amlokhi/ Indian Goose berry (Phyllanthus emblica) etc. Fruits have multipurpose utilisations and consequently assume critical job, particularly, for the prosperity of country individuals by giving sustenance, family pay and business. Huge numbers of these natural fruits have been utilised as customary restorative plants and some have discovered a significant spot in the Indian arrangement of Ayurvedic medicine and Unani since days of yore. Regardless of their latent capacity, these indigenous fruit crops are less known both at scientific and farmers level particularly in our region and some of them like wild jackfruit (Artocarpus hirsutus), Rattan (Calamus rotang) , Naga tenga (Myrica esculenta) etc. which are nearer to extinction