A Review on Ethnobotany, Phytochemistry and Pharmacological activities of Euphorbia antiquorum L.

Euphorbia antiquorum L. is a small plant in the Euphorbiaceae family that is found primarily in tropical and subtropical Asia. It has a long tradition of being utilized in Chinese, Ayurvedic, and other traditional systems for a variety of ailments. To date, More than 116 bioactive constituents were isolated from Euphorbia antiquorum, with diterpenoids being the most abundant. Extracts and isolated chemicals from various portions of the plant have demonstrated significant pharmacological activities such as anti-inflammatory, analgesic, antidiabetic, anticancer etc. It is necessary to conduct an in-depth investigation of the phytochemicals along with the pharmacological properties of E. antiquorum. This review summarised the knowledge of ethnobotany, phytochemistry and pharmacological activities of the plant which will provide a better understanding to clarify the traditional uses of the species and its relation to modern pharmacology which will ultimately pave the way for its clinical application.

Redox-signalling and Redox Biomarkers in Cardiovascular Health and Disease.

Overproduction of reactive nitrogen and oxygen species (RNS and ROS) has been linked to the pathogenesis of diabetes, hypertension, hyperlipidemia, stroke, angina, and other cardiovascular diseases. These species are produced in part by the mitochondrial respiratory chain, NADPH oxidase, and xanthine oxidase. RNS and ROS both contribute to oxidative stress, which is necessary for the development of cardiovascular disorders. In addition to ROS species like hydroxyl ion, hydrogen peroxide, and superoxide anion, RNS species like nitric oxide, peroxynitrous acid, peroxynitrite, and nitrogen dioxide radicals have also been linked to a number of cardiovascular conditions. They promote endothelial dysfunction, vascular inflammation, lipid peroxidation, and oxidative damage, all of which contribute to the development of cardiovascular pathologies. It's crucial to understand the mechanisms that result in the production of RNS and ROS in order to identify potential therapeutic targets. Redox biomarkers serve as indicators of oxidative stress, making them crucial tools for diagnosing and predicting cardiovascular states. The advancements in proteomics, metabolomics, genomics, and transcriptomics have made the identification and detection of these small molecules possible. The following redox biomarkers are notable examples: 3-nitrotyrosine, 4-hydroxy-2-nonenal, 8- iso-prostaglandin F2, 8-hydroxy-2-deoxyguanosine, malondialdehyde, Diacron reactive oxygen metabolites, total thiol, and specific microRNAs (e.g. miRNA199, miRNA21, miRNA1254, miRNA1306-5p, miRNA26b-5p, and miRNA660-5p) are examples. Although redox biomarkers have great potential, their clinical applicability faces challenges. Redox biomarkers frequently have a short half-life and exist in small quantities in the blood, making them challenging to identify and measure. The interpretation of biomarker data may also be influenced by confounding factors and the complex interplay of various oxidative stress pathways. Therefore, in-depth validation studies and the development of sensitive and precise detection methods are needed to address these problems. In the search for redox biomarkers, cutting-edge techniques like mass spectrometry, immunoassays, and molecular diagnostics are applied. New platforms and technologies have made it possible to accurately detect and monitor redox biomarkers, which facilitates their use in clinical settings. Our expanding knowledge of RNS and ROS involvement in cardiovascular disorders has made it possible to develop redox biomarkers as diagnostic and prognostic tools. Overcoming the challenges associated with their utility and utilizing advanced detection techniques, which will improve their clinical applicability, will ultimately benefit the management and treatment of cardiovascular conditions.

Antidiabetic potential of Amomum dealbatum Roxb. flower and isolation of three bioactive compounds with molecular docking and in vivo study.

Amomum dealbatum Roxb. parts have been traditionally used as remedies for joint pain, diabetes, muscular rheumatism, antiseptic, and abscesses in Arunachal Pradesh, Assam, and Tripura. Ethyl acetate sub-fraction E3 had significantly inhibited the α-glucosidase (IC50 5.385 µg/mL). The molecular docking revealed quercetin-3-O-galactoside to be the most potent α-glucosidase inhibitor (binding energy -43.214 kcal/mol). Using the QSAR model, the pIC50 values of myricetin, gallic acid, quercetin-3-O-galactoside, and acarbose were predicted to be 5.65235, 4.39858, 5.65235, and 6.03058, respectively. For the first time, quercetin-3-O-galactoside, myricetin, and gallic acid have been isolated from the flowers of A. dealbatum (ADF). E3 decreased blood glucose level to a near-normal concentration (100.60 ± 2.94 mg/dL) in comparison to diabetic control rats (575.20 ± 24.80 mg/dL). The results have strongly suggested the potential of ADF in treating diabetes. This lesser-known plant has the potential to uncover its full medicinal properties through further in-depth research.

Orchids of Dibru-Saikhowa: A Systematic Review on Their Traditional Use, Pharmacological Activity and Phytochemistry.

BACKGROUND: Dibru-Saikhowa National Park and Biosphere Reserve (DSNPBR), Assam, India, is a part of biodiversity hotspots and a store house of many orchid species. This systematic review was conducted to document the medicinal importante of orchids available in DSNPBR and to analyse their importance in drug discovery. METHODS: This systematic review was conducted using the Preferred Reporting Items for Systematic Review and Meta-Analysis (PRISMA) guidelines. Scientific databases were used to search relevant literature to document ethnomedicinal uses, pharmacological activity and phytochemistry of orchid species available in DSNPBR. RESULTS: We have analysed 84 articles to document relevant information on 52 orchid species available in DSNPBR. Dendrobium (n = 13) is the top genus. Different orchid species available in DSNPBR were used traditionally in India, Nepal, Bangladesh, and China to cure gastrointestinal disorders, disease-associated pain and inflammation, skin diseases, wound, arthritis, menstrual pain, tuberculosis etc. The pre-clinical investigations confirmed that extract/fraction/isolated compounds of orchids possess antirheumatic, anticancer, antitumor, anti-inflammatory, antidiabetic, antimicrobial, nephroprotective and neuroprotective activities through different mechanisms. Biomolecules isolated from orchid species like Dendrobium nobile alkaloids, polysaccharides have shown a potential to be developed as future drug molecules. Many phytochemicals isolated have demonstrated in vitro anticancer activities. The lack of clinical data in support of the therapeutic effectiveness of orchids is a major limitation. CONCLUSION: Orchids found in DSNPBR hold great significance in traditional culture for their medicinal properties and have been effectively studied for their bioactivities. Nevertheless, to confirm their effectiveness as therapeutics, conducting methodical research, examining their molecular mechanisms, and performing toxicity tests are necessary.

Profiling of Polyphenolic Compounds, Antioxidant, Antidyslipidemic and Cardiac Risk Preventive Effect of Keteki Joha and Kola Joha Rice Cultivars Grown in Assam, India: A Comparative Study.

BACKGROUND: Food grains' ability to promote health is widely recognized as a result of their rich nutritional profile and presence of antioxidants. AIM: The present study aimed to investigate the antioxidant, antidyslipidemic, and cardiac risk preventive effects of unpolished whole rice extracts of Keteki and Kola Joha of Assam, India, and to profile the polyphenolic compounds present. METHODS: Whole unpolished rice samples were extracted with ethanol and the efficacy of the extract of both rice cultivars was evaluated against high-fat and high-sugar induced hyperlipidemia in rats. The effects of extracts on lipid profile, hepatic enzyme, endogenous antioxidants, lipid peroxidation, creatine kinase-NAC, lactate dehydrogenase, C-reactive protein and lipoprotein(s) were evaluated. Atherogenic indices were calculated to find the effect of the extract on cardiac risk. HPLC analysis of whole unpolished rice samples was also carried out to profile the polyphenolics present. RESULTS: HPLC analysis revealed the presence of gallic acid, vanillic acid, caffeic acid, sinapic acid, o-coumaric acid, t-coumaric acid, rosamarinic acid, chlorogenic acid, phytic acid in both rice samples. Protocatechuic acid, syringic acid, and p-coumaric acid were detected in keteki joha, and ferulic acid was detected in kola joha only. Ethanol extracts (200 and 400 mg/kg) of both rice varieties for 30 days significantly averted dyslipidemia, preserved the level of endogenous antioxidants, and prevented lipid peroxidation. Levels of creatine kinase-NAC, lactate dehydrogenase, Creactive protein, and lipoprotein (a) were significantly (P < 0.01) less in the extract-treated group compared to the disease-control group. Extract treatment enhanced ApoA1 level while the reduced level of ApoB. ApoB/ApoA1 ratio was found more in the disease control group, which was significantly reduced in the extract-treated group. The atherogenic index, atherogenic coefficient, and cardiac risk ratio were reduced, while the cardioprotective index was enhanced in treatment groups. CONCLUSION: This paper profiled polyphenolic compounds for the first time. Keteki joha exhibited better results than Kola joha. Observations offer novel insights into the hypothesis for the first time that unpolished Keteki and Kola Joha rice can be beneficial in averting hyperlipidemia and its associated coronary events.

Synthesis and characterization of citrate soft rice starch: A new strategy of producing disintegrating agent for design drug and resistant starch.

Assam soft rice starch (ASRS) and Citric acid-esterified Assam soft rice starch (c-ASRS) were studied extensively. FTIR, CHN, DSC, XRD, SEM, TEM and optical microscope studies were performed for native and modified starches. Powder rearrangements, cohesiveness and flowability were studied by the Kawakita plot. Moisture and ash content was around 9 % and 0.5 %. In vitro digestibility of ASRS and c-ASRS produced functional RS. Paracetamol tablets were prepared using ASRS and c-ASRS as granulating-disintegrating agents through wet granulation methods. The prepared tablets' physical properties, disintegrant properties, in vitro dissolution and dissolution efficiency (DE) were performed. The average particle size was obtained at 6.59 ± 0.355 µm and 8.15 ± 0.168 µm for ASRS and c-ASRS, respectively. All the results were statistically significant at p < 0.05, p < 0.01 and p < 0.001. The amylose content was 6.78 %, classifying it as a low amylose type of starch. The disintegration time was reduced with the increasing concentration of ASRS and c-ASRS and facilitated the immediate release of the model drug from the tablet compact to improve its bioavailability. Therefore, the current investigation concludes that ASRS and c-ASRS can be used as novel and functional materials in pharmaceutical industries due to their unique physicochemical attributes. HYPOTHESIS: The central hypothesis of the current work was to develop citrated starch through a one-step reactive extrusion method and investigate its disintegrants property for pharmaceutical tablets. Extrusion is a continuous, simple, high-speed, low-cost, producing very limited wastewater and gas. Characterization was done through different instrumental techniques to confirm successful esterification. The flow properties were evaluated, and tablets were prepared at a different level of ASRS and c-ASRS (disintegrating agent), followed by the evaluation of tablets to confirm the model drug's dissolution and disintegration efficiency. Finally, in vitro digestibility of both ASRS and c-ASRS was analyzed to establish their potential nutritional benefits.

Natural Flavonoids as Potential Therapeutics in the Management of Diabetic Wound: A Review.

Flavonoids are important bioactive phenolic compounds abundant in plants and exhibit different therapeutic potentials. A wound is a significant problem in diabetic individuals. A hyperglycaemic environment alters the normal wound-healing process and increases the risk of microbial infection, leading to hospitalization, morbidity, and amputation. Flavonoids are an important class of phytochemicals with excellent antioxidant, anti-inflammatory, antimicrobial, antidiabetic, antitumor, and wound healing property. Quercetin, hesperidin, curcumin, kaempferol, apigenin, luteolin, morin, etc. have shown their wound healing potential. Flavonoids effectively exhibit antimicrobial activity, scavenge reactive oxygen species, augment endogenous antioxidants, reduce the expression and synthesis of inflammatory cytokines (i.e. IL-1ß, IL-6, TNF-α, NF-κB), inhibit inflammatory enzymes, enhance anti-inflammatory cytokine (IL-10), enhance insulin section, reduce insulin resistance, and control blood glucose level. Several flavonoids like hesperidin, curcumin, quercetin, rutin, naringin, and luteolin have shown their potential in managing diabetic wounds. Natural products that maintain glucose haemostatic, exert anti-inflammatory activity, suppress/inhibit microbial growth, modulate cytokines, inhibit matrix metalloproteinase (MMP), stimulate angiogenesis and extracellular matrix, and modulate growth factor can be considered as a potential therapeutic lead to treat diabetic wound. Flavonoids were found to play a positive role in management of diabetic wounds by regulating MMP-2, MMP-8, MMP-9, MMP-13, Ras/Raf/ MEK/ERK, PI3K/Akt, and nitric oxide pathways. Therefore, it can be assumed that flavonoids could be potential therapeutics to prevent devastating effects of diabetic wounds. This paper focused on the potential role of flavonoids in managing diabetic wounds and discussed their possible mechanism of action.

Implications of metabolic dysfunction associated fatty liver disease in COVID-19.

Metabolic associated fatty liver disorder (MAFLD) characterizes the contributing etiologies (i.e., type 2 diabetes mellitus, metabolic syndrome, overweight) of individuals with fatty liver disease that affects 1/3rd of the world population. In 2020, the coronavirus disease 2019 (COVID-19) crisis was unprecedented, and people with different comorbidities became more susceptible to the infection caused by severe acute respiratory syndrome coronavirus 2. MAFLD patients are frequently obese with added metabolic menace like diabetes, hypertension, and dyslipidemia leading to greater jeopardy of COVID-19. MAFLD patients are 4 to 6-fold more prone towards infections. COVID-19 induces liver injury with elevated levels of aspartate aminotransferase and alanine aminotransferase and insignificantly elevated bilirubin. Hence, MAFLD in COVID-19 patients worsens the condition significantly. The evidence highlighting the interaction between MAFLD and altered liver functioning in COVID-19 suggested that COVID-19 patients with pre-existing MAFLD are at greater risk of morbidity or intensive care unit admission. Direct hepatic injury, enhanced levels of inflammatory cytokines, declined hepatic mitochondrial activity, and compromised immunity are considered as some underlying mechanisms. The main focus of this review is to discuss the implications of metabolic dysfunction associated with fatty liver disease in COVID-19 patients. The review systematically analyzes the effect of striking two worldwide pandemics (MAFLD and COVID-19) together in the present era.

Citric acid esterified Glutinous Assam bora rice starch enhances disintegration and dissolution efficiency of model drug.

The current work was designed to study the starch's physicochemical attributes, tablet disintegration and dissolution efficiency and its derivatives obtained from the glutinous Assam bora rice (G-ABR) variety of Assam, Northeast India. Starch was isolated by a simple protein denaturation method, and a starch derivative was prepared through citric acid modification. G-ABRS and citrated G-ABRS were characterized through FTIR, DSC, XRD and SEM. The rate of consolidation, consolidation index, angle of internal friction, packing rearrangement and cohesive properties were determined to investigate their applications as functional excipients in pharmaceutical industries. G-ABRS and citrated G-ABRS exhibited better packing rearrangement and cohesive properties than standard corn starch. Furthermore, immediate release of API from the tablet compact was observed when the starch concentration increased from 1 to 5 %, indicating facilitation of the tablet compact disintegration. Therefore, G-ABRS and citrated G-ABRS are potentially functional and sustainable materials for pharmaceutical industries.

High-Value Compounds and Bioactivity of Rice Bran, Rice Bran Protein: A review.

BACKGROUND: Rice bran and rice bran protein are important sources of minerals, energy, and vitamins. Other bioactive compounds are abundantly available to exert therapeutical activity. Health-promoting activities of high-value compounds of rice bran were significant, as observed in recent studies. INTRODUCTION: A variety of bioactive components present in rice bran and rice bran extract are responsible to exhibit therapeutical potential like chemopreventive, cardioprotective, hepatoprotective, immunomodulatory, neuroprotective, and lipid-lowering activity. Several bioactivity representative compounds like γ-oryzanol, ferulic acid, caffeic acid, tricin, protocatechuic acid, vanillic acid, coumaric acid, phytic acid, isoferulic acid, gallic acid, γ-amino butyric acid, sinapic acid, saturated and unsaturated fatty acids, vitamin E complexes, ß-sitosterol, stigmasterol, campesterol, cyanidin-3-glucoside, peonidin-3-glucoside, quercetin, rutin, kaemferol, ß-carotene, lutein, vitamin B and lycopene are known to display significant health benefits. The bioactive components produced therapeutical effects by regulation of different mechanisms like increasing faecal excretion, reducing oxidative stress, reducing the level of malondialdehyde (MDA), regulation of NF-kb activation, reduction of proinflammatory cytokines production, suppression of SREBP-1, reduction in the expression of anti-apoptotic protein Bcl-2, elevated the expression of pro-apoptotic protein Bax, up-regulating P53 expression and suppressing COX-2. METHODOLOGY: Several research engines like PubMed, google scholar, science direct, etc. were used to collect the data on the mentioned keywords. Recent scientific works were included in this article. CONCLUSION: In this review paper, we profiled the high-value compounds and focused on their antioxidant, anti-hyperlipidemic, antidiabetic, and anticancer activity with their possible mechanism of action.

Evolving spectrum of diabetic wound: Mechanistic insights and therapeutic targets.

Diabetes mellitus is a chronic metabolic disorder resulting in an increased blood glucose level and prolonged hyperglycemia, causes long term health conse-quences. Chronic wound is frequently occurring in diabetes patients due to compromised wound healing capability. Management of wounds in diabetic patients remains a clinical challenge despite many advancements in the field of science and technology. Increasing evidence indicates that alteration of the biochemical milieu resulting from alteration in inflammatory cytokines and matrix metalloproteinase, decrease in fibroblast and keratinocyte functioning, neuropathy, altered leukocyte functioning, infection, etc., plays a significant role in impaired wound healing in diabetic people. Apart from the current pharmacotherapy, different other approaches like the use of conventional drugs, antidiabetic medication, antibiotics, debridement, offloading, platelet-rich plasma, growth factor, oxygen therapy, negative pressure wound therapy, low-level laser, extracorporeal shock wave bioengineered substitute can be considered in the management of diabetic wounds. Drugs/therapeutic strategy that induce angiogenesis and collagen synthesis, inhibition of MMPs, reduction of oxidative stress, controlling hyperglycemia, increase growth factors, regulate inflammatory cytokines, cause NO induction, induce fibroblast and keratinocyte proliferation, control microbial infections are considered important in controlling diabetic wound. Further, medicinal plants and/or phytoconstituents also offer a viable alternative in the treatment of diabetic wound. The focus of the present review is to highlight the molecular and cellular mechanisms, and discuss the drug targets and treatment strategies involved in the diabetic wound.

Ethnomedicinal Practices and Traditional Medicinal Plants of Barak Valley, Assam: a systematic review.

Objectives: The Barak Valley is well known for its rich diversity of medicinal plants. Ethnomedicinal practices are prominent among Barak Valley's major and minor ethnic groups. This systemic review focuses on traditionally used medicinal plants found in the Barak Valley as reported in different ethnobotanical surveys. Methods: We searched various databases, including PubMed, Web of Science, and Google Scholar, to find ethnomedicinal surveys conducted in the Barak Valley. The search was performed using different terms, including ethnomedicinal survey, folk medicine, indigenous knowledge, and Barak Valley. Potential articles were identified following the exclusion and inclusion criteria. Results: A total of eight ethnobotanical surveys were included in this study. We identified a total of 216 plant species belonging to 167 genera and 87 families, which are widely used by the ethnic communities who live in the rural areas of Barak Valley for the treatment of various diseases and ailments. Conclusion: Folk medicine is the result of decades of accumulated knowledge and practices by people who live in rural communities based on their needs and provides an important source of information to assist the search for new pharmaceuticals. Therefore, available information on traditional medicinal plants needs to be explored scientifically to find effective and alternative treatments for different diseases.

A comprehensive review on polysaccharides with hypolipidemic activity: Occurrence, chemistry and molecular mechanism.

Currently, research on natural products is facing challenging future in various aspects. A large group of natural polysaccharides such as ß-glucan, cellulose, hemicellulose, chitin, pectin, agaropectin, heteroglycans, lignins, hydrocolloids, homopolysaccharides, heteropolysaccharides were studied extensively for their various therapeutical potential. Several research works have already demonstrated those polysaccharides has tremendous health benefits, and found to exhibit anticancer, antiviral, immunomodulatory, antimicrobial, anticoagulant, anti-inflammatory, antidiabetic, antioxidant and antitumor activities. Different mushroom, plant, fungus, algae, vegetables, microalgae etc. are some important source of several polysaccharide macromolecules such as glucans, ulvan A, ulvan B, fucoidan, rhamnan sulfate, laminarin sulfate, agar, alginate, heteroglycans. Earlier research work demonstrated that natural polysaccharides have the highest ability to carry biological properties along with some biopolymers like as proteins and nucleic acids due to their structural variability. The preventive effect of these biomacromolecules was extensively studied, especially their beneficial effect on chronic metabolic conditions like dyslipidemia and related disorders. Dyslipidemia is a serious metabolic disorder associated with coronary heart disease, coronary artery diseases, hypercholesterolemia, atherosclerosis, etc. Dietary natural polysaccharides could play an important role in the management and prevention of dyslipidemia. Polysaccharides from natural sources mainly sulfated polysaccharides exhibited predominant lipid-lowering and cholesterol-lowering activities through different mechanisms. Polysaccharides isolated from different edible plants, vegetables, plant, algae, mushroom with higher biological activities, particularly hypolipidemic activity were highlighted in this paper, in a way for their futuristic therapeutic application. This review aims to comprehensively discuss overall advances in hypolipidemic activity of polysaccharides, including their sources, structural characteristic and chemistry, biological activity and their probable mode of action.

Patient-Specific Implants (PSI) in Maxillary Hypoplasia Secondary to Cleft Lip and Palate Deformity.

Maxillary hypoplasia is often evident in cleft patients due to impaired growth and dense scarring from previous cleft surgeries. For these patients, treatment scenario has taken many turns over ages, evolved from orthognathic correction to distraction osteogenesis, with mixed prognosis and outcome depending on severity of the case and other several factors. We are reporting a case of 24-year-old female with maxillary hypoplasia secondary to bilateral cleft lip and palate with hypoplastic prolabium, who has been treated with two patient-specific implants in bilateral maxillary region for facial profile enhancement.

Diabetes mellitus and COVID-19: Understanding the association in light of current evidence.

Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infections have posed a problematic healthcare situation worldwide since December 2019. Diabetes mellitus is associated with an increased risk and severity of coronavirus disease 2019 (COVID-19). While interacting with various other risk factors, high blood sugar was found to reduce immunity and increase the replication of SARS-CoV-2. Oxidative stress and the release of pro-inflammatory cytokines are greater in diabetic individuals than in healthy people, worsening the outcome of SARS-CoV-2 infection in diabetics. Increased expression of furin and angiotensin converting enzyme 2 (ACE-2) receptor in the hyperglycemic environment may promote the entry of SARS-CoV-2 in the host cell. COVID-19 infection primarily modulates immune and inflammatory responses, and may cause a cytokine storm, resulting in possible lethal outcomes in diabetics. An experimental report suggests that ACE expressed in the pancreas and the SARS-CoV-2 virus invariably destroy ß-cells which contain ACE-2 receptors and results in acute diabetes. Moreover, COVID-19 also causes hyperglycemia in an individual with diabetes which may be related to insulin resistance and destruction of ß-cells during SARS-CoV-2 infection. Early observations also suggest a correlation between oral hypoglycemic agents and the risk of COVID-19. This review focused on the possible cause and mechanism involved in SARS-CoV-2 infection in diabetics and the role of antidiabetic drugs in COVID-19.

Natural Starch in Biomedical and Food Industry: Perception and Overview.

Utilization of native starch is increasing globally because of its wide distribution and natural occurrence. Starch is mainly abundant in tubers and food grains. Scientific research on starch is increasing in recent years due to its unique physiochemical and biomedical properties. Native starch is an emerging biopolymer and copolymer in the biomedical and pharmaceutical areas due to its renewability, biocompatibility, biodegradability, and relative inexpensiveness. Today, there is an increasing interest in natural starches to design and produce diverse products due to their pertinent structural properties and non-toxicity. Due to these attributes, these natural polymers are becoming functional core materials in the biomedical industry, construction materials, medicine industry, food industry, food packaging, and carrier for active drugs. In this paper, we mainly attempt to analyze the physicochemical attributions and the biomedical applications on native or non-conventional starches obtained from the natural botanical sources.

Revival, modernization and integration of Indian traditional herbal medicine in clinical practice: Importance, challenges and future.

In spite of incredible advances in modern science, technology and allopathic medicine a large we are unable to provide quality healthcare to all. Traditional medicine particularly herbal medicine considered as a major healthcare provider around the globe particularly in rural and remote areas. A large section of people depends on such medicine for their primary healthcare mainly in underdeveloped or developing countries. Indian traditional medicinal system like Ayurveda, Siddha and Unani has a very rich history of their effectiveness; modern research also acknowledged the importance of such medicine. Indian traditional medicine or medicinal plants are also considered as a vital source of new drug. Mainstreaming of such medicine is important for the people. Several steps have been taken in India to promote such medicine and to integrate them into clinical practice. Evidence based incorporation of Indian traditional medicine in clinical practice will help to provide quality healthcare to all.

Hepatoprotective and antioxidant activity of Karisalai Karpam, a polyherbal Siddha formulation against acetaminophen-induced hepatic damage in rats.

BACKGROUND: The usage of Siddha medicine in Tamil Nadu and several parts of Southern India has considerably increased over the past two decades and it is steadily crossing the various geographies owing to its inexpensiveness compared to conventional medicines and has fairly high acceptance rates because of its herbal origin and therefore its nontoxic nature. AIM: This study aims to investigate the anti-hepatotoxic and antioxidant potential of the Karisalai Karpam formulation. MATERIALS AND METHODS: Karisalai Karpam tablet at 50, 100, and 200 mg/kg/day, p.o. doses were administered orally to rats for three consecutive days. Single dose of acetaminophen (3 g/kg, p.o.) was administered on the 3(rd) day. Animals were sacrificed 48 h after the administration of acetaminophen, and their serum bilirubin, different hepatic enzymes and in vivo antioxidant activity were estimated. STATISTICAL ANALYSIS: Data were evaluated using analysis of variance, followed by Tukey tests. A level of P < 0.05 was considered statistically significant. RESULTS: Pretreatment with Karisalai Karpam tablet showed dose-dependent hepatoprotective activity. Karisalai Karpam tablet (200 mg/kg) reduces serum glutamic oxaloacetate transaminase, serum glutamic pyruvic transaminase, alkaline phosphatase and total bilirubin, direct bilirubin by 67.8%, 72.3%, 47.6%, 61.3% and 62.9% respectively compared to disease control group. A significant increase (P < 0.001) in antioxidant enzyme level was observed in Karisalai Karpam treated animals. At higher doses, Karisalai Karpam prevented the depletion of glutathione in liver tissue. CONCLUSION: Results confirmed that Karisalai Karpam tablet could protect the liver against acetaminophen-induced oxidative damage possibly by increasing the antioxidant defence mechanism in rats.

An enantioselective formal synthesis of montelukast sodium.

A formal synthesis of the antiasthma drug montelukast sodium is described, wherein the key chiral diol intermediate was accessed with greater convergence of the C-C bond-forming steps as compared to previous routes. Improved synthetic efficiency was achieved by deploying homogeneous metal-based catalysis in two pivotal steps. In the first, a tandem Mizoroki-Heck reaction and double-bond isomerization between a previously known allyl alcohol intermediate and a hindered 2-(2-halophenyl)propan-2-ol secured direct access to the 3-(2-(2-hydroxypropan-2-yl)phenyl)-1-phenylpropan-1-one moiety in the product. In the second step, asymmetric hydrogenation of the ketone functionality in the Mizoroki-Heck reaction product provided a convenient method to introduce the benzylic alcohol chiral center and obtain the desired chiral diol precursor of montelukast sodium. A detailed catalyst screening led to the identification of ((R)-Xyl-BINAP)((R,R)-DPEN)RuCl2 as a catalyst that afforded an enantioselectivity of 99% ee in the hydrogenation step on a multigram lab scale at a molar substrate:catalyst loading of 5000:1.