Formulation and evaluation of SGLT2 inhibitory effect of a polyherbal mixture inspired from Ayurvedic system of medicine.

Background and aim: The ingredients viz., Artemisia roxburghiana, Cissampelos pareira, Stephania glabra, Drimia indica, Roylea cinerea, Tinospora sinensis and Curcuma longa of the present formulation are used to treat diabetes in the Indian traditional medical system. Adopting the concept of multiple herbal mixtures for better therapeutic effects from the ancient Ayurvedic text Sarangdhar Samhita, the present study aimed to develop a polyherbal formulation (PHF) of seven herbs and to evaluate its sodium-glucose cotransporter protein-2 (SGLT2) inhibitory effect on type 2 diabetic rats. Experimental procedure: Streptozotocin (STZ) (60 mg/kg) and nicotinamide (NAM) (120 mg/kg) were intraperitoneally administered to induce type 2 diabetes in Wistar rats. The animals were divided into 5 groups viz. normal control, diabetic control, positive control (dapagliflozin at 0.1 mg/kg) and two test groups (PHF at 250 and 500 mg/kg). Various parameters including blood glucose, serum glutamic pyruvic transaminase (SGPT), serum glutamic-oxaloacetic transaminase (SGOT), bilirubin, triglycerides and creatinine were measured. Results and conclusion: The treatment with PHF (250 and 500 mg/kg) showed a significant (p < 0.05) decrease in blood glucose levels by 56.37% and 58.17%, respectively. The levels of SGOT, SGPT and bilirubin were significantly reduced in PHF-fed diabetic rats. Histopathological examination revealed no major changes in the treated groups as compared to the normal control. The molecular docking study showed strong binding of ß-sitosterol, insulanoline, warifteine, dehydrocorydalmine, taraxerol acetate, lupeol, corydalmine and luteolin to SGLT2 protein. The present study concludes that PHF has promising antidiabetic activity via inhibiting SGLT2 protein without showing any adverse effects.

Antidiabetic effect of aqueous-ethanol extract from the aerial parts of Artemisia roxburghiana.

Artemisia roxburghiana is used for the management of diabetes mellitus in the Indian subcontinent. The present work aimed to validate the traditional claim of the plant in diabetes mellitus. In vitro studies were conducted using α-glucosidase and α-amylase assays whereas streptozotocin-nicotinamide-induced diabetic Wistar rats were used for in vivo study. The aqueous-ethanol extract from the aerial parts was found to exhibit α-glucosidase and α-amylase inhibitory activities with the IC50 values of 31.0 and 17.2 mg/mL, respectively when compared with acarbose (IC50 = 8.6 and 16.25 mg/mL, respectively). The extract showed a significant glucose-lowering effect in diabetic rats at the doses of 200 and 400 mg/kg in a dose-dependent manner, while acarbose (10 mg/kg) was used as a standard. The results revealed that A. roxburghiana aerial parts showed antidiabetic activity via inhibiting α-glucosidase and α-amylase enzymes. The present study also validated the ethnomedicinal claim of the plant in diabetes mellitus.

Modulation of gut microbiota with Ayurveda diet and lifestyle: A review on its possible way to treat type 2 diabetes.

Background: The prevalence of type 2 diabetes (T2D) has increased substantially in the past few decades throughout the world. In India, the epidemic of diabetes continues to increase irrespective of area, status, and age. Despite various scientific societies involved in the treatment of diabetes, still, the burden of diabetes keeps growing. Aims: The aim of this work is to explore the Ayurvedic concept of a personalized diet to modulate the gut microbiota for the treatment of T2D. Material and methods: A thorough study of literature from online scientific databases including Web of Science, PubMed, Scopus, and Google Scholar as well as from classical texts of Ayurveda was done. A careful compilation was done to extract the valuable output of the personalized diet to modulate the gut microbiota. Results: There are various diets used to control blood glucose levels, and their effects are also being studied on the transcriptome or epigenome despite 99.9% genomic similarity among human beings. However, microbiomes have only 10% similarity. Ayurvedic diet is given on the basis of Prakriti (body constitution), therefore, it is also called personalized diet. Conclusion: The diets prescribed for T2D in Ayurveda are high in fibers, polyphenols, and complex carbohydrates which enrich butyrate-producing bacteria and decrease lipopolysaccharide-producing bacteria. Hence, there is a need to have a personalized diet to manage the glucose level by enriching beneficial gut microbiota. The approach of a personalized diet associated with gut microbiota can be helpful in maintaining blood sugar in T2D patients.

Emodin - A natural anthraquinone derivative with diverse pharmacological activities.

Emodin (1,3,8-trihydroxy-6-methyl-anthraquinone) is a natural anthraquinone derivative that is present in numerous globally renowned herbal medicines. It is recognised as a protein tyrosine kinase inhibitor and as an anticancer drug, active against various tumour cells, including lung, breast, liver, and ovarian cancer cells. Recently, its role in combination chemotherapy with various allopathic medicines, to minimize their toxicity and to enhance their efficacy, has been studied. The use of emodin in these therapies is gaining popularity, due to fewer associated side effects compared with standard anticancer drugs. Emodin has a broad therapeutic window, and in addition to its antineoplastic activity, it displays anti-ulcer, anti-inflammatory, hepatoprotective, neuroprotective, antimicrobial, muscle relaxant, immunosuppressive and antifibrotic activities, in both in vitro and in vivo models. Although reviews on the anticancer activity of emodin have been published, none coherently unite all the pharmacological properties of emodin, particularly the anti-oxidant, antimicrobial, antidiabetic, immunosuppressive and hepatoprotective activities of the compound. Hence, in this review, all of the available data regarding the pharmacological properties of emodin are explored, with particular emphasis on the modes of action of the molecule. In addition, the manuscript details the occurrence, biosynthesis and chemical synthesis of the compound, as well as its toxic effects on biotic systems.

Protective and therapeutic effects of natural products against diabetes mellitus via regenerating pancreatic ß-cells and restoring their dysfunction.

Diabetes mellitus is a growing public health concern and an increasing interest has been raised to search for new compounds with therapeutic effects on ß-cells. There are chronic insulin resistance and loss of ß-cell mass in the case of type-2 diabetes which covers about 90% of total diabetic patients. This work aims to critically review the protective and regenerative effects of various antidiabetic natural products on pancreatic ß-cells. A thorough literature survey was conducted on the natural molecules and extracts having a protective, regenerative, and repairing effect on ß-cells. The primary source of the literature was online scientific databases such as PubMed, Scopus, and Google Scholar. Besides, selected relevant textbooks were also consulted. Various natural molecules including berberine, curcumin, mangiferin, stevioside and capsaicin, and extracts obtained from the plants like Capsicum annum, Gymnema sylvestre, Stevia rebaudiana and Nymphaea stellate, were found to produce regenerative and anti-apoptosis effects on ß-cells. These natural products were also found to increase insulin secretion by stimulating ß-cells. The present review concluded that a large number of molecules and extracts, abundantly found in nature, possess antidiabetic effect via targeting ß-cells. Further research is warranted to use these agents as a drug against diabetes.

A Molecular Approach on the Protective Effects of Mangiferin Against Diabetes and Diabetes-related Complications.

BACKGROUND: Diabetes and its related complications are now a global health problem without an effective therapeutic approach. There are many herbal medicines which have attracted much attention as potential therapeutic agents in the prevention and treatment of diabetic complications due to their multiple targets. AIM: The aim of this study is to review available knowledge of mangiferin focusing on its mode of action. METHODS: Mangiferin was extensively reviewed for its antidiabetic activity using online database like Scopus, PubMed, and Google Scholar as well as some offline textbooks. A critical discussion based on the mechanism of action and the future perspectives is also given in the present manuscript. RESULTS: Mangiferin is a natural C-glucoside and mainly obtained from its primary source, the leaves of mango tree (Mangifera indica L.). Therapeutic and preventive properties of mangiferin include antimicrobial, anti-inflammatory, antioxidative, antiallergic, neuroprotective, and cognition-enhancing effects. It dissolves well in water, so it can be easily extracted into infusions and decoctions and hence, a number of researches have been made on the therapeutic effect of this molecule. Recently, mangiferin has been proved to be an effective remedy in diabetes and diabetes-related complications. It is a beneficial natural compound for type 2 diabetes mellitus as it improves insulin sensitivity, modulates lipid profile and reverts adipokine levels to normal. CONCLUSION: This study concludes that mangiferin has the potential to treat diabetes and it can be developed as a therapeutic agent for diabetes and the complications caused by diabetes.

Drimia indica: A Plant Used in Traditional Medicine and Its Potential for Clinical Uses.

Drimia indica (Roxb.) Jessop (Asparagaceae) is a reputed Ayurvedic medicine for a number of therapeutic benefits, including for cardiac diseases, indigestion, asthma, dropsy, rheumatism, leprosy, and skin ailments. The present work aimed to critically and extensively review its traditional uses, phytochemistry, pharmacology, toxicology, and taxonomy together with the mechanisms of action of selected extracts of D. indica. A systematic literature survey from scientific databases such as PubMed, Scopus, and Web of Science as well as from some textbooks and classical texts was conducted. The plant, mainly its bulb, contains various bioactive constituents, such as alkylresorcinols, bufadienolides, phytosterols, and flavonoids. Various scientific studies have proven that the plant has anthelmintic, anticancer, antidiabetic, antimicrobial, antioxidant, and wound healing activities. The present work concludes that D. indica has the potential to treat various diseases, mainly microbial infections. This review also suggests that bufadienolides, flavonoids, and steroids might be responsible for its bioactive potential.

Status of Indian medicinal plants in the International Union for Conservation of Nature and the future of Ayurvedic drugs: Shouldn't think about Ayurvedic fundamentals?

The present market for herbal drugs is estimated about ₹40 billion, which is expected to increase by 16% in next 3-4 years. The current production of many Ayurvedic herbs is less than their market demand, which incentivizes adulteration in the Ayurvedic drug supply chain. The present work aims to highlight the most used Ayurvedic plants that have been listed in the International Union for Conservation of Nature's "red list" of endangered or vulnerable plants. The future of Ayurvedic medicines from these listed plants is uncertain, as the collection of herbs from their natural habitat is prohibited and their cultivation does not meet market demands. Many of these plants, such as Taxus baccata and T. wallichiana, are endangered and are only grown in their natural habitats; their cultivation in other areas is impractical. This is the present state, and will worsen as demand continues to grow, with increasing populations and increasing adoption of this system of medicine. It is possible that in coming years most of the Ayurvedic drugs will be adulterated, and will cause only side effects rather than the therapeutic effects. The Ayurvedic fundamentals are under-explored areas where the Ayurvedic practitioners and research scientists can work together. The scientific work on the basic principles will unravel many unknown or little-known facts of this ancient science. Hence, the present review emphasizes the conservation of Ayurvedic herbs, minimization of the use of medicinal plants and the promotion of the research based on Ayurvedic fundamentals.

Ethnomedicinal Investigation of Medicinal Plants of Chakrata Region (Uttarakhand) Used in the Traditional Medicine for Diabetes by Jaunsari Tribe.

The Himalayan region is the treasure house of natural wealth, particularly of medicinal and aromatic plants. These plants are used by the Indian traditional healers for the past many centuries to treat various ailments such as skin disorders, asthma, diabetes, snake bite, fever, pain, eye diseases, diarrhoea, indigestion, jaundice, burn, wound, liver disorder, CNS disorders and urinary tract infection. The indigenous traditional knowledge of medicinal plants and therapies of various local communities has been lost due to changes in traditional culture and the introduction of modern technologies. Therefore, it is essential to explore the traditional knowledge of the indigenous medicinal plants mainly in such areas where there is a severe threat to natural vegetation owing to human inhabitation. The present study aimed to explore the medicinal plants of Chakrata region (Jaunsar-Bawar Hills), Uttarakhand, India used in the folk medicine for the management of diabetes by Jaunsari Tribe. In a comprehensive field survey, the information about the medicinal plants have been mainly collected from the traditional healers and other elderly people belong to the tribal community. All the information about the medicinal plants of the study area was documented in a field book. Various tools have been used to collect the samples for identification purpose and the authentication of the plants was done with the help of taxonomists. The literature on these plants was also searched from online (PubMed and Scopus) as well as from some textbooks and Ayurvedic classical texts. The present survey-based work described a total of 54 plants belonging to 47 genera and 30 families used in the traditional medicine for the management of diabetes in Chakrata region. The information gathered from the local community revealed that the plants are effective in diabetes and one can use most of them without consulting a practitioner or traditional healer. The literature revealed that most of the surveyed plants are already used in the preparation of various antidiabetic formulations such as Chandraprabha vati, Nishamalaki chunra, Amritamehari churna and Nisakathakadi kashayam along with various patent drugs which are frequently prescribed by the Ayurvedic practitioners in India. The present study explored the traditional as well as scientific knowledge on the antidiabetic plants used by the tribal community. The documented information on these plants can be further used by the scientific community to develop new drugs/formulations with the help of modern techniques.

Yoga Practice Improves the Body Mass Index and Blood Pressure: A Randomized Controlled Trial.

BACKGROUND: Yoga, an ancient Indian system of exercise and therapy is an art of good living or an integrated system for the benefit of the body, mind, and inner spirit. Regular practice of yoga can help to increase blood flow to the brain, reduce stress, have a calming effect on the nervous system, and greatly help in reducing hypertension. AIM: Aim of the present study is to evaluate the effect of 1-month yoga practice on body mass index (BMI), and blood pressure (BP). MATERIALS AND METHODS: The present study was conducted to determine the effect of yoga practice on 64 participants (age 53.6 ± 13.1 years) (experimental group) whereas the results were compared with 26 healthy volunteers (control group). We examined the effects of yoga on physiological parameters in a 1-month pilot study. Most of the participants were learner and practiced yoga for 1 h daily in the morning for 1 month. BMI and BP (systolic and diastolic) were studied before and after 1 month of yoga practice. RESULTS: Yoga practice causes decreased BMI (26.4 ± 2.5-25.22 ± 2.4), systolic BP (136.9 ± 22.18 mmHg to 133 ± 21.38 mmHg), and diastolic BP (84.7 ± 6.5 mmHg to 82.34 ± 7.6 mmHg). On the other hand, no significant changes were observed in BMI and BP of control group. CONCLUSION: This study concludes that yoga practice has potential to control BMI and BP without taking any medication.

Ayurvedic concept of Shatkriyakala: a traditional knowledge of cancer pathogenesis and therapy.

The term Kriyakala refers to the recognition of the stage of a disease's progress, which helps to determine appropriate measure to correct the imbalance in Doshas (biological factors). It is a compound expression, comprised of Kriya and Kala, where Kriya means the choice to treatment (medicine, food and daily-routine) used to improve the disturbance in Doshas, and Kala refers to the stage of progress of a disease. Sushruta, an ancient Indian surgeon, has described the concept of Kriyakala in Varnaprashnadhyaya, an ancient Vedic Sanskrit text, which seeks to explain the incidence of Varnas in terms of Doshic disturbances. Varna, in modern parlance, may be described as an inflammatory process that may lead ulceration and chronic inflammation, promoting all stages of carcinogenesis. Abnormal interactions between Prakriti (genotype) and environmental factors vitiate the Doshas and impair immunity, which can lead to aberrant cell growth and cancer. Moreover, the interaction between vitiated Doshas and weak Dhatus (body tissues) manifests as cancers of a specific organ. Shatkriyakala (six stages of progress of a disease), on the other hand, provides a framework to assess the cancer and its pathogenesis in different stages. According to Ayurvedic concepts, all cancer therapies treat the affected tissues indirectly by eliminating vitiated Doshas, rejuvenating Dhatus and restoring immunity in cancer patients. The present review describes the six stages of Shatkriyakala in detail, with an emphasis on research areas to validate the concept of Shatkriyakala. This traditional knowledge can be utilized with modern technologies to detect predisposition for cancer or diagnose cancer in its early stages.

Myricetin: A Dietary Molecule with Diverse Biological Activities.

Myricetin is a common plant-derived flavonoid and is well recognised for its nutraceuticals value. It is one of the key ingredients of various foods and beverages. The compound exhibits a wide range of activities that include strong anti-oxidant, anticancer, antidiabetic and anti-inflammatory activities. It displays several activities that are related to the central nervous system and numerous studies have suggested that the compound may be beneficial to protect against diseases such as Parkinson's and Alzheimer's. The use of myricetin as a preserving agent to extend the shelf life of foods containing oils and fats is attributed to the compound's ability to protect lipids against oxidation. A detailed search of existing literature revealed that there is currently no comprehensive review available on this important molecule. Hence, the present work includes the history, synthesis, pharmaceutical applications and toxicity studies of myricetin. This report also highlights structure-activity relationships and mechanisms of action for various biological activities.

Gingerols and shogaols: Important nutraceutical principles from ginger.

Gingerols are the major pungent compounds present in the rhizomes of ginger (Zingiber officinale Roscoe) and are renowned for their contribution to human health and nutrition. Medicinal properties of ginger, including the alleviation of nausea, arthritis and pain, have been associated with the gingerols. Gingerol analogues are thermally labile and easily undergo dehydration reactions to form the corresponding shogaols, which impart the characteristic pungent taste to dried ginger. Both gingerols and shogaols exhibit a host of biological activities, ranging from anticancer, anti-oxidant, antimicrobial, anti-inflammatory and anti-allergic to various central nervous system activities. Shogaols are important biomarkers used for the quality control of many ginger-containing products, due to their diverse biological activities. In this review, a large body of available knowledge on the biosynthesis, chemical synthesis and pharmacological activities, as well as on the structure-activity relationships of various gingerols and shogaols, have been collated, coherently summarised and discussed. The manuscript highlights convincing evidence indicating that these phenolic compounds could serve as important lead molecules for the development of therapeutic agents to treat various life-threatening human diseases, particularly cancer. Inclusion of ginger or ginger extracts in nutraceutical formulations could provide valuable protection against diabetes, cardiac and hepatic disorders.

Antiplasmodial activity of aqueous extract of Berberis aristata roots against Plasmodium berghei-infected BALB/c mice.

CONTEXT: The rising problem of resistance to present antimalarial drugs stresses the need to look for newer antiplasmodial components with effective modes of action. The roots of Berberis aristata DC. (Berberidaceae) are used in the traditional medicine for malaria in various parts of India. OBJECTIVE: The objective of this study was to evaluate antiplasmodial activity of B. aristata roots extract for the validation of its traditional medicinal use. MATERIAL AND METHODS: Aqueous root extract of Berberis aristata (AREBA) was screened for its in vitro as well as in vivo antiplasmodial activity against lethal rodent malaria parasite Plasmodium berghei NK65. In vitro activity was evaluated against schizont maturation of P. berghei using various concentrations ranging from 1 to 100 µg/mL. For in vivo studies, AREBA at the doses of 150, 250, 350, and 650 mg/kg/d was administered to P. berghei infected BALB/c mice orally for 4 consecutive days (D0-D3). RESULTS: AREBA showed in vitro antiplasmodial activity with an IC50 value of 40 µg/mL. In vivo studies demonstrated a variable dose-dependent chemosuppression with higher efficacy at lower doses. At a dose of 350 mg/kg/d, the suppressive and preventive activities were found to be 67.1% and 53.9%, respectively, followed by enhancing mean survival period up to 12.8 d for the curative assay versus 7.5 d for the untreated mice. DISCUSSION AND CONCLUSION: These results provide relevant scientific evidences for the traditional medicinal use of this plant as malaria remedy and further advocates the isolation and characterization of active antiplasmodial principle from this plant.

A comprehensive scientific overview of Garcinia cambogia.

The fruit rind of Garcinia gummi-gutta, commonly known as Garcinia cambogia (syn.), is extensively used traditionally as a flavourant in fish curries due to its sharp sour taste. Additional ethnobotanical uses include its use as a digestive and a traditional remedy to treat bowel complaints, intestinal parasites and rheumatism. This small fruit, reminiscent of a pumpkin in appearance, is currently most popularly used and widely advertised as a weight-loss supplement. Studies have shown that the extracts as well as (-)-hydroxycitric acid (HCA), a main organic acid component of the fruit rind, exhibited anti-obesity activity including reduced food intake and body fat gain by regulating the serotonin levels related to satiety, increased fat oxidation and decreased de novo lipogenesis. HCA is a potent inhibitor of adenosine triphosphate-citrate lyase, a catalyst for the conversion process of citrate to acetyl-coenzyme A, which plays a key role in fatty acid, cholesterol and triglycerides syntheses. The crude extract or constituents from the plant also exerted hypolipidaemic, antidiabetic, anti-inflammatory, anticancer, anthelmintic, anticholinesterase and hepatoprotective activities in in vitro and in vivo models. Phytochemical studies of various plant parts revealed the presence of mainly xanthones (e.g. carbogiol) and benzophenones (e.g. garcinol) together with organic acids (e.g. HCA) and amino acids (e.g. gamma aminobutyric acid). Currently, a large number of G. cambogia/HCA dietary supplements for weight management are being sold although the possible toxicity associated with the regular use of these supplements has raised concerns. In most cases, complaints have been related to multicomponent formulations and at this stage G. cambogia has not been confirmed as the potentially toxic culprit. This review presents a scientific overview of G. cambogia with reference to relevant botanical aspects, ethnobotanical uses, phytochemistry and biological activity as well as toxicity.

Ayurvedic research and methodology: Present status and future strategies.

Ayurveda is a science of life with a holistic approach to health and personalized medicine. It is one of the oldest medical systems, which comprises thousands of medical concepts and hypothesis. Interestingly, Ayurveda has ability to treat many chronic diseases such as cancer, diabetes, arthritis, and asthma, which are untreatable in modern medicine. Unfortunately, due to lack of scientific validation in various concepts, this precious gift from our ancestors is trailing. Hence, evidence-based research is highly needed for global recognition and acceptance of Ayurveda, which needs further advancements in the research methodology. The present review highlights various fields of research including literary, fundamental, drug, pharmaceutical, and clinical research in Ayurveda. The review further focuses to improve the research methodology for Ayurveda with main emphasis on the fundamental research. This attempt will certainly encourage young researchers to work on various areas of research for the development and promotion of Ayurveda.

Efficacy and safety of Stephania glabra: an alkaloid-rich traditional medicinal plant.

Stephania glabra (Roxb.) Miers (Menispermaceae) has long been used for the treatment of asthma, tuberculosis, dysentery, hyperglycaemia, cancer, fever, intestinal complaints, sleep disturbances and inflammation in many Asian countries. It mainly contains alkaloids and, until now, over 30 alkaloids such as bisbenzylisoquinolines, hasubanalactams, berberines and aporphines have been isolated from its tuber. Most of its traditional medicinal activities are scientifically approved by various in vitro and in vivo studies. It shows remarkable anti-psychotic, anti-diabetic, antipyretic, analgesic, antimicrobial and anti-hypertensive activities. This work includes comprehensive information on the ethnobotany, chemistry and pharmacology of S. glabra. This review also focuses on the future perspectives with main emphasis on the establishment of therapeutic index and safety index of the plant. This review concludes that S. glabra has a great potential to treat various diseases, and could be used as a source for novel healthcare products in the near future, which needs further studies.

From arrow poison to herbal medicine--the ethnobotanical, phytochemical and pharmacological significance of Cissampelos (Menispermaceae).

ETHNOPHARMACOLOGICAL RELEVANCE: Cissampelos species have a rich history of traditional use, being used for both therapeutic and toxic properties. It is traditionally applied therapeutically in a diverse range of conditions and diseases including asthma, cough, fever, arthritis, obesity, dysentery, snakebite, jaundice and heart, blood pressure and skin-related problems. Conversely, it was traditionally included in preparations of curare applied as arrow poison during hunting to cause death of animals by asphyxiation. This review unites the ethnobotanical knowledge on Cissampelos with the phytochemistry and pharmacological activity which has been explored thus far. In addition, it identifies knowledge gaps and suggests further research opportunities. METHODS: The available electronic literature on the genus Cissampelos was collected using database searches including Scopus, Google Scholar, Pubmed, Web of Science, etc. The searches were limited to peer-reviewed English journals with the exception of books and a few articles in foreign languages which were included. RESULTS: The literature revealed that pharmacological activity including analgesic and antipyretic, anti-inflammatory, anti-allergic, bronchodilator, immunomodulatory, memory-enhancing, antidepressant, neuroprotective, antimicrobial, antimalarial, antiparasitic, anti-ulcer, anticancer, anti-oxidant, cardiovascular, muscle-relaxant, hepatoprotective, antidiabetic, antidiarrhoeal, antifertility, and antivenom activity have been confirmed in vitro and/or in vivo for various Cissampelos species. Cissampelos pareira L. and Cissampelos sympodialis Eichl. are the most explored species of this genus and the smallest number of studies have been conducted on Cissampelos laxiflora Moldenke and Cissampelos tenuipes Engl. Many alkaloids isolated from Cissampelos such as warifteine, methylwarifteine, berberine, hayatin and hayatidin showed promising anti-allergic, immunosuppressive, antidepressant, anticancer, vasodilatory and muscle-relaxant activities. CONCLUSION: The plants of this genus are used in traditional medicine for the treatment of various ailments. These plants are a rich source of bioactive bisbenzylisoquinoline and aporphine alkaloids together with other minor constituents. Although these plants are reputable and revered in various traditional medicine systems, many have not yet been screened chemically or pharmacologically and so there is a vast amount of research still to be conducted to validate their traditional use.

A gastroretentive drug delivery system of lisinopril imbibed on isabgol-husk.

The gastroretentive drug delivery system is site-specific and allows the drug to remain in the stomach for a prolonged period of time so that it can be released in a controlled manner in gastrointestinal tract. The present study was carried out to develop a gastroretentive drug delivery system using isabgol as an excipient to prolong the residence time of the model drug lisinopril in the stomach. The gastroretentive ability of isabgol was increased by addition of NaHCO3 as a gas-generating agent while its mucoadhesive property was enhanced by incorporation of HPMC-K4M. The drug, NaHCO3 and HPMC-K3M were imbibed on isabgol-husk as per entrapment efficiency of the isabgol-husk. After drying, the product was filled in a hard gelatin capsule and evaluated for its buoyancy, mucoadhesive properties, swelling index and in vitro drug release. The lisinopril released through isabgol was delayed by 12 hours when compared to a preparation available on the market which released the complete drug in 0.5 hours. The drug release study of lisinopril from the formulation follows first order kinetics using a diffusion controlled mechanism. The results from the present study revealed that isabgol can be used as a potential excipient for the formulation of gastroretentive drug delivery systems in the near future.

Chemical constituents from the stem bark of Symplocos paniculata Thunb. with antimicrobial, analgesic and anti-inflammatory activities.

ETHNOPHARMACOLOGICAL RELEVANCE: The stem bark of Symplocos paniculata Thunb. has been used to check abortion in folk medicine in India. AIM OF THE STUDY: The present study was undertaken to isolate the phytochemicals from the plant together with the evaluation of antimicrobial, analgesic and anti-inflammatory activities of the plant extract and isolated compounds. MATERIALS AND METHODS: The plant extract was subjected to column chromatography for isolation of phytochemicals. The agar diffusion method was adopted for antimicrobial activity to determine MICs. Ethanolic extract and isolated compounds were selected for investigating their analgesic activity on acetic acid-induced writhing response in mice. The anti-inflammatory activity was performed on carrageenan-induced paw edema in rats. RESULTS: The stem bark of the plant afforded seven compounds, 4-(8-hydroxyethyl) cyclohexan-1-oic acid (1); androst-5(6)-ene 17-one 3ß-O-(ß-d-glucopyranoside) (2); 9ß,25-cyclo 3ß-O-(ß-D glucopyranosyl)-echynocystic acid (3); 9ß,19-cyclo 24-methylcholan-5,22-diene 3ß-O-{ß-D-glucopyranosyl (1→6) α-L-rhamnopyranoside} (4); 30-ethyl 2α,16α-dihydroxy 3ß-O-(ß-D-glucopyranosyl) hopan-24-oic acid (5); 32,33,34-trimethyl-bacteriohopan-16-ene 3-O-ß-D-glucopyranoside (6) and flavone 3',4',5',6-tetramethoxy 7-O-ß-D-glucopyranosyl (1→3) ß-D-glucopyranoside (7). The extract and isolated compounds exhibited antimicrobial, analgesic and anti-inflammatory activities. CONCLUSION: The present study concludes that ethanolic extract of the plant and its constituents having significant antimicrobial, analgesic and anti-inflammatory activities.