bluuebunny/crossref_metadata_2025 huggingface dataset:
HYPOGLYCEMIC ACTIVITY OF A NOVEL POLYHERBAL FORMULATION IN STREPTOZOTOCIN-INDUCED DIABETIC RATS: A THERAPEUTIC STUDY
Authors: MAJUMDER PULAK , M PARIDHAVI
Published: October 2019

Objective: The concept of the synergistic effect of poly-herbalism was as old as medicine history. Present novel polyherbal formulation (PHF) composed of five different herbs. The present investigation aimed to evaluate the synergistic therapeutic hypoglycemic potential of PHF against streptozotocin (STZ) (60 mg/kg b.w, ip)-induced diabetic rats.

Methods: For this therapeutic study, the dose was framed orally once a day to the test objects after STZ dosing at 500 mg/kg/5 ml dosage levels for 21 days. The transformation of body weight and blood glucose level was examined, and the histopathological changes of beta cells of the pancreas, cellular architectures of liver and kidney were also perceived after scarification of the objects.

Results: The outcomes were compared to that of glibenclamide (5 mg/kg) treated group. Declines of body weight and blood glucose levels were perceived in STZ-induced diabetic animals very significantly (p<0.01 or p<0.05). However, these diabetic changes were significantly (p<0.01 or p<0.05) decreased in PHF-dosing groups revealed more encouraging effects compared to that of glibenclamide. In the other hand, various liver function and enzymes test (creatinine, urea, total bilirubin, total albumin, alkaline phosphatase, gamma-glutamyl transferase, aspartate transaminases, and alanine transaminases) and lipid profile (total cholesterol, triglycerides, high-density lipoprotein cholesterol, total protein, low-density lipoprotein [LDL], and very LDL) studies strongly indicate the potential action of this novel formulation.

Conclusions: It is deliberated that PHF has the favorable effect to normalize the blood glucose levels, and also rejuvenation and reproduction of beta cells lead a better futuristic ant diabetic therapy for diabetic management.
EVALUATION OF PRO-APOPTOTIC EFFECTS OF β-MONOLINOLEIN ON METASTATIC BREAST CANCER CELL LINE MDA-MB-231
Authors: SOFI MOHAMMED SHAFI
Published: October 2019

Objectives: The objective of this study was to evaluate the β-monolinolein as a potential therapy for breast cancer treatment.

Methods: The cytotoxic activity of β-monolinolein was evaluated by 3-(4,5-dimetylthiazol-2-yl)-2,5-diphenyltetrazolium bromide and trypan blue exclusion assay. The cellular cytotoxicity and levels of cytosolic enzyme, lactate dehydrogenase (LDH), were measured by assessing μmoles of nicotinamide adenine dinucleotide/well/min. To confirm whether β-monolinolein induces apoptosis in 3,4-methylenedioxyamphetamine (MDA)- MB-231 cells, western blot and semiquantitative reverse transcription-polymerase chain reaction (RT-PCR) analysis were performed.

Results: For the 1st time, it was demonstrated that β-monolinolein strongly inhibits the growth of MDA-MB-231 cells, with an half maximal inhibitory concentration value of 12.5 μg/ml. <90% of cell death was achieved at higher concentrations after 48 h of treatment. Trypan blue assay showed that the cell viability was significantly decreased in a dose-dependent manner in MDA-MB-231 cells after 48 h of treatment. On the other hand, LDH activities in the cultured media were significantly elevated in a dose-dependent manner as compared to the control. Further, the western blot analysis showed that β-monolinolein leads to change in expression levels of important cell cycle regulators such as p21, Bax, Bcl-Xl, and Bcl-2 in MDA-MB-231 cells. The semiquantitative RT-PCR results indicated a significant upregulation of proapoptotic genes such as p53, p21, and Bax and downregulation of antiapoptotic gene Bcl-2.

Conclusion: These results indicate that β-monolinolein leads to change in expression of various cell cycle/apoptotic regulators and hence induces death in MDA-MB-231 cells.
STABILITY INDICATING METHOD DEVELOPMENT AND VALIDATION OF METFORMIN AND ERTUGLIFLOZIN BY HIGH-PERFORMANCE LIQUID CHROMATOGRAPHY WITH PDA DETECTION AND ITS APPLICATION TO TABLET DOSAGE FORM
Authors: JAGADEESH KADALI , N ANNAPURNA
Published: October 2019

Objective: A sensitive, rapid, accurate, and precise stability indicating high-performance liquid chromatography method was developed and validated for the simultaneous estimation of metformin (MET) and ertugliflozin (ERT).

Methods: The planned chromatographic method was developed using Kromasil C18 column using 0.1 M sodium dihydrogen phosphate methanol (50:50, by volume, pH 4.0) as mobile phase system followed by peak area response measurement at 238 nm. The developed method was validated by means of ICH guidelines about system suitability, linearity, sensitivity, selectivity, accuracy, precision, robustness, and specificity.

Results: Calibration curves of MET and ERT are linear from 250 to 750 μg/ml and 3.75 to 11.25 μg/ml, respectively. Relative standard deviation is <2.0% and recovery is ̴ 100%. Successfully, the developed method was applied for the simultaneous determination of MET and ERT in tablets and to study degradation of MET and ERT in acidic, alkaline, oxidation, thermal, and photolytic degradation conditions. No obstructions from additional common excipients of tablets and degradants were observed.

Conclusion: The results recommended method suitability for the analysis of MET and ERT in quality control laboratories.
USING BREWER’S YEAST AND GINGER IN THE MANAGEMENT OF CONSTIPATION-PREDOMINANT IRRITABLE BOWEL SYNDROME: A RANDOMIZED DOUBLE-BLIND PLACEBO-CONTROLLED TRIAL
Authors: AL-JASSIM ZAINAB G
Published: October 2019

Objective: The objective of the present study is to confirm and/or prove the beneficial outcomes from using Brewer’s yeast and Ginger in constipation-predominant irritable bowel syndrome (IBS-C) subjects compared to placebo.

Methods: A total of 45 patients suffering from IBS-C were enrolled in a double-blind placebo-controlled study as defined by Rome III criteria. Parallel groups were randomly assigned in this study: A placebo group, Brewer’s yeast group, and ginger group, taken daily for 20 days. IBS severity scale and visual analog scale for IBS (VAS-IBS) were used to assess the severity of pain, abdominal distention, and constipation (IBS-C) subjects. The data were measured at 3 times: At 0 time (T0), after 10 days of treatment (T10), and after 20 days of treatment (T20) for the three treatment groups.

Results: Intragroup analysis showed a clinically significant reduction in the symptoms of abdominal pain, distention, and constipation, in the Brewer’s yeast group compared to placebo after the 20 days of the study. There was also a significant reduction of abdominal distention and constipation symptoms in the ginger group throughout the study.

Conclusion: This study reveals the beneficial effects of Brewer’s yeast and ginger in reducing troublesome gastrointestinal symptoms in subjects with IBS-C and holds the promise to use them in IBS-C patient.
PROTECTIVE ROLE OF AQUEOUS EXTRACT OF ATRIPLEX HALIMUS L. AGAINST BENZENE-INDUCED DAMAGE ON RENAL FUNCTION AND GLOMERULAR CELLS IN RATS
Authors: ZEGHIB KHAOULA , BOUTLELIS DJAHRA ALI
Published: October 2019

Objective: Benzene (BZ) is an important pollutant compound, present in both occupational and general environment that has been linked to adverse health effect. The aim of the current study was to investigate the curative and preventive effect of Atriplex halimus L. (Ah) extract against BZ-induced nephrotoxicity in rats.

Methods: A total of 30 male albino Wistar rats were divided into five groups (n=6): Control, Ah, BZ, AhP+BZ, and BZ+AhC. BZ (100 mg/kg b.w) was added in their drinking water for 15 weeks. Ah (Aqueous Extract of aerial parts) was given by gavage during the past 30 days of BZ-exposed for curative treatment (AhC) and all the duration of BZ exposure in the animals for preventive treatment (AhP). Some biochemical, oxidative stress parameters, and histopathology of kidney tissue were studied.

Results: Obtained results revealed that BZ exposure to rats caused a significant elevation in urea, creatinine, and malondialdehyde levels. Then, it led to reducing the glutathione level, catalase, and glutathione-S-transferase activities when compared to the control animals. Histopathological studies showed a massive damage in kidneys of the BZ-exposed rat. Our results showed that curative treatment of aqueous extract of Ah has a partial correction of the biochemical, oxidative stress parameters, and kidney morphology, but preventive treatment has a dramatic effect on the previous parameters.

Conclusion: Results demonstrated the beneficial effects of Ah preventive treatment against stress oxidative and kidney damage induced by BZ.
VITEX NEGUNDO EXTRACTS PROTECT HUMAN CORNEAL EPITHELIAL CELLS FROM ULTRAVIOLET C-INDUCED PHOTOTOXICITY
Authors: K DEEKSHA , ARUNACHALAM CYNTHIA
Published: October 2019

Objective: The objective of the study was to investigate the protective effects of Vitex negundo (VN) extracts against ultraviolet (UV) light C-induced oxidative stress in human corneal epithelial cells (HCEC) in vitro.

Methods: The VN extracts were checked for their antioxidant activities by biochemical tests. The preliminary phytochemical analysis was done to check the presence of secondary metabolites. To trigger oxidative stress, the HCEC were exposed to UVC irradiation (200 J/m2). Then, different concentration of VN extracts was administered after 1 h of UVC irradiation. The effects of UVC irradiation and the extracts on the HCEC viability, morphology, cell migration by scratch assay, and reactive oxygen species (ROS) production by dichlorofluorescein diacetate method were measured.

Results: VN ethanol (VNE) extract showed the highest antioxidant activity than the aqueous extract. Phytochemical screening shows the presence of alkaloids, carbohydrates, proteins, phenolics, and tannins. The extracts showed no cytotoxicity on the HCEC and also the VNE extract did not alter the morphology of the cells. Results suggest that the VNE extract enhanced the proliferation and migration of HCEC. The VNE extract significantly decreased UVC-induced oxidative toxicity by inhibiting the intracellular ROS production and maintained cell viability.

Conclusion: VN extracts with its strong antioxidant potential protects HCEC from UVC-induced oxidative stress. The results suggest that these extracts can be used as prophylactic agents or as a therapeutic agent in overcoming UV light-induced damage in various ocular surface diseases such as pterygium and photokeratitis.
EVALUATION OF ANTIBIOTICS USED IN PATIENTS WITH ACUTE RESPIRATORY INFECTIONS IN A HOSPITAL
Authors: GINTING PRICELLA AQWILLA , NASUTION AZIZAH , KHAIRUNNISA KHAIRUNNISA
Published: October 2019

Objective: This study evaluated the use of antibiotics in the treatment of patients with acute respiratory infection (ARI) in the outpatients installation in Bunda Thamrin General Hospital, Medan.

Methods: This prospective descriptive cohort study analyzed the use of antibiotics provided to patients with ARI using Indonesian universal health coverage known as Badan Penyelenggara Jaminan Sosial claims (n=130) in outpatients installations from March to May 2018. The characteristics of the patients were organized and descriptively analyzed in Excel and SPSS programs. The antibiotics provided were grouped according to the Anatomical Therapeutical Chemical code and class; then, the dosage form, defined daily dose (DDD) units, was converted into milligrams. DDD calculation was done by dividing the total DDD usage with the total number of patients.

Results: Mean age of the patients was 32.12±10.579 years. The highest quantity of antibiotic use in DDD/1000 patients-day units was cefixime reaching 1,897.435 mg DDD KPRJ.

Conclusions: Cefixime was the most widely available antibiotic for the treatment of ARI patients.
ERUCA SATIVA LINN.: PHARMACOGNOSTICAL AND PHARMACOLOGICAL PROPERTIES AND PHARMACEUTICAL PREPARATIONS
Authors: S JAAFAR NOOR , S JAAFAR IMAN
Published: October 2019

Eruca sativa (jarjeer) is an annual herb (family Brassicaceae), which contains a wide range of chemicals and minerals with nutraceutical and organoleptic characteristics. Jarjeer was generally used as a food and traditionally mainly consumed due to its aphrodisiac properties. This crop known to contain various phytochemicals such as flavonoids, phenolic acids, terpens, carotenoids, tannins, glycosides, saponins, sterols, alkaloids, and other secondary metabolites. In leaves, kaempferol and its derivatives, glucosativin, are the main flavonoids and glucosinolate, respectively, while erucic acid and glucoerucin are the main fatty acid and glucosinolate, respectively. Medicinally, the plant has antibacterial, antidiabetic, antihypertensive, antiplatelet, and antioxidant activity and stimulates hair growth and other effects. Trails on topical pharmaceutical preparations involve the use of E. sativa which had been done. These preparations include creams and waxs which are intended to be used for potentiating hair growth and skin fungal and bacterial infection.
POMEGRANATE ATTENUATES ACUTE GENTAMICIN-INDUCED NEPHROTOXICITY IN SPRAGUE-DAWLEY RATS: THE POTENTIAL ANTIOXIDANT AND ANTI-INFLAMMATORY EFFECTS
Authors: AL-KURAISHY HAYDER M , AL-GAREEB ALI I , SADEK AL-NAIMI MARWA SALIH
Published: October 2019

Objectives: Nephrotoxicity is a renal-specific situation in which the excretion of toxic metabolites is reduced due to toxic agents and drugs. Gentamicin is an antibiotic belongs to aminoglycoside group which may induce nephrotoxicity due to induction of oxidative stress. Pomegranate is a component of the traditional medicine called Punica granatum with significant nephron-protective effect. Therefore, the objective of the present study was to evaluate the nephronprotective effect of pomegranate in gentamicin-induced nephrotoxicity.

Methods: A total of 30 male Sprague-Dawley rats were used which divided into Group 1 (n=10): Rats treated with distilled water 5 ml/kg plus normal saline 5 ml/kg for 12 days, Group 2 (n=10): Rats treated with distilled water 5 ml/kg plus gentamicin 100 mg/kg for 12 days, and Group 3 (n=10): Rats treated with pomegranate 100 mg/kg plus gentamicin 100 mg/kg for 12 days. Blood urea, serum creatinine, malondialdehyde (MDA), kidney injury molecule (KIM-1), and cystatin-C were measured in both control and experimental groups.

Results: Rats treated with gentamicin showed nephrotoxicity as evident by significant elevation in serum creatinine, blood urea, serum creatinine, KIM-1, MDA, and cystatin-C sera levels. Pomegranate leads to significant reduction of blood urea and serum creatinine compared to gentamicin group, p<0.05. Pomegranate also reduced MDA, KIM-1, and cystatin-C sera levels significantly compared to gentamicin group, p<0.01.

Conclusion: Pomegranate produced significant nephroprotective effect on gentamicin-induced nephrotoxicity through modulation of oxidative stress and inflammatory biomarkers.
CARDIOPROTECTIVE POTENTIAL OF PLANTS AND PLANT-DERIVED PRINCIPLES – A REVIEW
Authors: G NIKITHA , SANDUR V RAJENDRA
Published: October 2019

Cardiovascular diseases (CVDs) are a class of diseases involving heart or blood vessels. Coronary artery diseases include angina, myocardial infarction (MI), stroke, heart failure, hypertensive heart disease, cardiomyopathy, and arrhythmias. CVDs are the leading cause of death globally. Risk factors include high blood pressure, smoking, obesity, poor diet, blood cholesterol, and lack of exercise. It is approximated that 90% of CVDs is preventable. High blood pressure results in 13% of CVD deaths, whereas tobacco outcomes in 9%, diabetes and lack of exercise in around 6%, and obesity in 5%. Due to certain medications such as anticancer drugs like doxorubicin, adverse effects result in MI. Since ancient times, medicinal plants have been widely used in the treatment of diseases. This information may serve as a primer in identifying novel prophylactic as well as therapeutic studies of plant-derived principles. The parts of the plants such as seeds, leaves, flowers, roots, and bark contain these phytoconstituents which are obtained through different extraction processes. Phytoconstituents are broadly classified into alkaloids, saponins, polyphenols, essential oils, carotenoids, glycosides, omega fatty acids, and flavonoids. Each class is responsible for its own pharmacological effects. The underlying mechanism in which they exert the action is different. This review presents an overview of the MI and therapeutic strategies of plant-derived principles that are available to mitigate the effect of MI.
AN UPDATED PHYTOCHEMICAL AND PHARMACOLOGICAL REVIEW ON GYNURA PROCUMBENS
Authors: KAMRAN ASHRAF
Published: October 2019

Nowadays, the use of medicinal plants increased significantly for the aim of producing more effective drugs with fewer side effects. Gynura procumbens (family Asteraceae) is a high value medicinal plant with different properties that are considered less, regardless of having great therapeutic potential in traditional medicine. Many pharmacological studies have established the ability of this plant to exhibit antimicrobial, antioxidant, hepatoprotection, antigenotoxic, antiplasmodial, cytotoxic, cardioactive, antidiabetic, anti-inflammatory, etc. The aim of this study was to review the updated phytochemical, pharmacological investigations as well as the traditional and therapeutic uses of G. procumbens. Important and different experimental data have been addressed along with a review of most of the phytochemicals identified in this plant.
QUANTIFICATION OF ANTICOAGULANTS DABIGATRAN, RIVAROXABAN, AND PRASUGREL BY CHROMATOGRAPHIC AND SPECTROMETRIC TECHNIQUES – REVIEW
Authors: SATYA PRASAD B  , JAYAKUMARI S
Published: October 2019

A review is presented on different analytical techniques used for quantitative analysis of selected anticoagulants dabigatran, rivaroxaban, and prasugrel. Efforts have been made to collate all the relevant references to the extent possible. The review discusses the advantages and disadvantages of the cited analytical techniques, which will help to give insights into the methods used for estimation of selected anticoagulants such as dabigatran, rivaroxaban, and prasugrel, from clinical isolates, and its dosage forms. The review highlights the basic as well as advanced techniques performed for estimating dabigatran, rivaroxaban, and prasugrel. The techniques illustrated here have been demonstrated to be useful for quantitative determination of selected anticoagulants and may find application in analyzing other related properties.
WET CHEMICAL SYNTHESIS, CHARACTERIZATION, AND ANTIBACTERIAL ACTIVITY OF MOLYBDENUM OXIDE NANOPARTICLES AGAINST STAPHYLOCOCCUS EPIDERMIDIS AND ENTEROBACTER AEROGENES
Authors: POONAM SANGWAN  , HARISH KUMAR  , RANI RENU
Published: October 2019

Objective: The objective of this study was to synthesize the molybdenum oxide nanoparticles (NPs) by employing wet chemical method and investigation of their antibacterial properties against pathogenic bacteria.

Methods: Molybdenum trioxide (MoO3) NPs were synthesized using an eco-friendly wet chemical sol–gel technique. The synthesized MoO3 NPs were characterized using X-ray diffraction (XRD), transmission electron microscopy (TEM), Fourier-transform infrared spectroscopy, and ultraviolet-visible spectroscopic techniques to confirm the obtained product, size shape, morphology, functional groups, and absorption spectra, respectively. The size of the MoO3 NPs was found to be 41 nm. The antibacterial activity of these metal NPs was investigated on Staphylococcus epidermidis and Enterobacter aerogenes by measuring the zone of inhibition and colony-forming units on solid medium and by measuring the optical density of the culture solution. Antibacterial activity of MoO3 NPs was also compared with well-known standard antibiotics.

Results: The antibacterial activities of molybdenum oxide NPs possessing size 41 nm were compared with standard antibiotics such as oxacillin, cotrimoxazole, erythromycin, clindamycin, chloramphenicol, and tetracycline. It was found that all of these antibiotics were effective against Staphylococcus epidermidis while Enterobacter aerogenes was resistant to oxacillin, co-trimoxazole and clindamycin, whereas the MoO3 nanoparticles were found to be effective against both of these bacterial pathogens.

Conclusion: Inorganic antimicrobial agents have advantages over organic antimicrobial agents due to their stability, preparation methods, and their ability to prevent bacteria to develop multidrug resistant. It was observed that MoO3 nanoparticles (NPs) possess good antibacterial properties; therefore, these can be used in pharmaceutical industries and provide a path for further research regarding the toxicity study for its use in human being.
FLUORESCENCE ANALYSIS, PHYTOCHEMICAL, AND ANTIOXIDANT ACTIVITIES IN LEAVES AND STEM OF EMBELIA RIBES BURM. F
Authors: VIDYA V. KAMBLE  , NIKHIL B. GAIKWAD
Published: October 2019

Objective: The objective of the present study is to carry out fluorescence analysis, phytochemical, and antioxidant activities using different solvent extract in leaves and stem of Embelia ribes.

Methods: In the present study, fluorescence analysis, phytochemical, and antioxidant activities of leaves and stem of E. ribes are carried out using standard procedures.

Result: The fluorescence analysis under visible and ultraviolet light for leaves and stem powder of E. ribes treated with various chemical reagents shown different fluorescence effect. In the phytochemical analysis, the methanolic extract of leaves has shown the highest total alkaloid content (19.05±0.42 mg CE/g DW), followed by the stem. The methanolic extract of stem exhibited highest total phenolic content (59.82±2.98 mg GAE/g DW), and ethanolic extract showed highest total flavonoid content (10.05±0.36 mg RE/g DW), followed by leaves. The ethanolic extract of stem possesses highest antioxidant activity toward 1,1-diphenyl-2-picrylhydrazyl (DPPH) (84.86±0.11%), whereas methanolic extract of stem reported highest FRAP activity (72.22±0.31 mg Fe+2E/g DW), followed by leaves. Antioxidant activities (DPPH and FRAP) were significantly correlated with TPC.

Conclusion: The results of the present study revealed that the fluorescence analysis of leaves and stem of E. ribes can be helpful for the standardization and quality control of indigenous drug. Both leaves and stem serve as the good source of secondary metabolite and antioxidant agents.
GREEN SYNTHESIS, CHARACTERIZATION, AND ANTIBACTERIAL ACTIVITY OF ZINC OXIDE NANOPARTICLE
Authors: C M NOORJAHAN
Published: October 2019

Objectives: Zinc oxide (ZnO) nanoparticles have received considerable attention due to their antimicrobial, UV blocking, and high catalytic and photochemical activities. Hence, an investigation has been carried out to synthesize the ZnO nanoparticle using aqueous Phyllanthus niruri (Keezhanelli) leaf extract. Aims and objectives of the present study are to synthesize using Keezhanelli (P. niruri) leaf extract, to study its characterization, and to determine its antibacterial activity.

Methods: Green synthesized ZnO nanoparticle was characterized by Fourier transform infrared (FTIR), scanning electron microscope (SEM), and transmission electron microscope (TEM) analysis. Antimicrobial activity of ZnO nanoparticle was carried out using agar well diffusion method.

Results: The result of the synthesized ZnO nanoparticle using Keezhanelli (P. niruri) leaf extract showed the change of color from pale white to brown color. The result of FTIR analysis of green synthesized ZnO nanoparticle revealed the presence of biomolecules such as polyphenols, flavonoids, alkaloids, polysaccharide, amino acid, and proteins. The result of the SEM studies showed that the green synthesized ZnO nanoparticle was spherical and cylindrical in shape. The size of the ZnO nanoparticle was recorded to be 5 μm. The result of TEM studies of ZnO nanoparticle showed that majority of the particles were spherical in shape with the size of 2 μm. The result of antibacterial activity against four bacterial species showed that green synthesized ZnO nanoparticle was found to be efficient in inhibiting the growth of the bacterial isolates. Maximum zone formation was exhibited against Staphylococcus saprophyticus.

Conclusion: Thus, from the results of the present study, it can be concluded that synthesis of ZnO nanoparticle using leaf extract of Keezhanelli (P. niruri) has several advantages such as simple, cost-effective, time consuming, safe, and eco-friendly compared to other methods of nanoparticle synthesis as evidenced in the present study.
REVIEW OF MEDICINAL USES, PHYTOCHEMISTRY, AND PHARMACOLOGICAL PROPERTIES OF DRIMIA ELATA
Authors: ALFRED MAROYI
Published: October 2019

Drimia elata is an important and well-known medicinal plant in tropical Africa. This study critically reviewed the medicinal applications, phytochemistry, and pharmacological activities of D. elata. Literature on medicinal applications, phytochemical, and pharmacological activities of D. elata was collected from multiple internet sources including Elsevier, Google Scholar, SciFinder, Web of Science, PubMed, BMC, ScienceDirect, and Scopus. Complementary information was gathered from pre-electronic sources such as books, book chapters, theses, scientific reports, and journal articles obtained from the university library. This study showed that D. elata is used for treating several medical conditions, particularly general ailments, blood and cardiovascular system, reproductive system and sexual health, urinary system, infections and infestations, digestive system, respiratory system, and muscular-skeletal system disorders. Phytochemical compounds identified from the species include bufadienolides, alkaloids, aromatic acids, flavonoids, phlobatannins, saponins, steroids, tannins, and terpenoids. Ethnopharmacological research revealed that D. elata extracts have acetylcholinesterase enzyme inhibitory, antibacterial, antifungal, antimycobaceterial, anticancer, anti-inflammatory, antioxidant, hemagglutinating, and cytotoxicity activities. D. elata should be subjected to extensive in vivo experiments and also future studies should focus on how potential toxic components of the species can be managed when it is used as herbal medicine.
IN VIVO AMELIORATIVE POTENTIAL OF CAFFEIC ACID AGAINST HEPATOTOXICITY AND NEPHROTOXICITY INDUCED BY MERCURIC CHLORIDE IN ALBINO WISTAR RATS
Authors: MANJU MANOGARAN , GANESAN JAGADEESAN
Published: October 2019

Objective: The current experimental study is designed to scrutinize the possible defensive effect of caffeic acid (CA) against mercury-induced hepatotoxicity in male rats.

Methods: During the treatment periods, a sub-lethal dose of HgCl2 (1.29 mg/kg body weight) was given to rats for 15 days through oral administration and the CA was administrated for 15 days, on mercuric intoxicated rats were observed. After completing the programmed period of experimental work, the blood was drawn through a micro glass tube in the ocular region and separated the serum by centrifuge.

Results: The subsequent serum enzymes were analyzed as the alkaline phosphatase (ALP), alanine transferase (ALT), aspartate transaminase (AST), and lactate dehydrogenase (LDH). Further, the bilirubin, albumin, total cholesterol, urea, and creatinine levels were also noticed in the blood serum of both normal and treated rats. CA is one of the well-known phenolic compounds, and a strong antioxidant helps to prevent oxidative damage and reducing oxidative stress. The biological action of liver biomarker enzymes such as ALT, AST, ALP, and LDH was significantly enhanced and at the same time the drastic increased in the level of albumin was all together decreased. The level of bilirubin, total cholesterol, urea, and creatinine was significantly increased in HgCl2 intoxicated rats. When the treatment of CA on mercury intoxicated rats for 15 days (5 mg/kg body weight), in the serum enzymes (ALT, AST, ALP, and LDH) also declined to near normal level. The level of bilirubin, total cholesterol, urea, and creatinine activities was also significantly declined to near normal level when compared to mercury-treated group. The level of albumin was significantly enhanced. The CA alone treatment showed the enhanced antioxidant levels and not any alteration in the levels of biochemical parameters when compared to control.

Conclusion: These observations of the present experimental work demonstrated the detoxify effects and defensive effect of CA against HgCl2 toxicity in liver tissue.
PHARMACOLOGICAL ACTIVITY OF ULVA LACTUCA POLYPHENOLS FRACTION: HEPATOPROTECTIVE AND ANTIOXIDANT ACTIVITIES AGAINST PARACETAMOL-INDUCED LIVER DAMAGE IN RATS
Authors: RAVINDRAN NT  , MOHAMED SADIQ A
Published: October 2019

Objective: The objective of this study was to assess the activity Ulva lactuca polyphenols fraction in protecting the liver damage induced by high dose of paracetamol.
Methods: This study was performed using Wistar albino rats divided into six groups. Group 1 was the normal group. Groups 2, 3, 4, 5, and 6 received paracetamol (2 g/kg) for 7 days. In addition to paracetamol, Groups 3, 4, 5, and 6 received silymarin (100 mg/kg), U. lactuca polyphenols fraction at the doses of 50, 100, and 200 mg/kg, respectively, for 7 days. On the 8th day, serum and liver samples were collected from the animals and the hepatoprotective and antioxidant activities were assessed by studying the levels of liver marker enzymes, bilirubin, protein, reduced glutathione, and antioxidant enzymes.
Results: U. lactuca polyphenols fraction, at the tested doses, restored the levels of all serum markers and enzymes (aspartate aminotransferase, alanine aminotransferase, alkaline phosphatase, lactate dehydrogenase, γ-glutamyl transferase, total bilirubin, total protein, cholesterol, triglycerides, and reduced glutathione) and liver homogenate markers (reduced glutathione, superoxide dismutase, catalase, and glutathione peroxidase) significantly, in dose-dependent manner.
Conclusion: This study suggests that U. lactuca polyphenols fraction has a hepatoprotective effect against paracetamol-induced liver damage and possesses antioxidant activities.
PHYTOCHEMICALS SCREENING AND ACTIVITIES OF BINAHONG (ANREDERA CORDIFOLIA [TEN.] STEENIS) LEAVES AND BEETROOTS (BETA VULGARIS L.) IN INCREASING SWIMMING ENDURANCE IN MICE
Authors: MASNIAH  , JAMIDIN MANURUNG
Published: October 2019

Objective: The aim of this research was to the identification of bioactive compounds and comparison of binahong (Anredera cordifolia [Ten.] Steenis) leaves and beetroots (Beta vulgaris L.) ethanol extract in swimming endurance activity in mice.

Methods: The type of research that has been carried out is experimental laboratory which includes identification of bioactive content quality and testing of swimming endurance effect by comparing the difference between before and after treatment by binahong leaves and beetroots ethanol extract.

Results: The results of bioactive compounds identification of binahong leaves and beetroots are alkaloids, glycosides, cyanogenic glycosides, flavonoids, and tannins. Steroid compounds are only found in binahong leaves. The results of swimming resistance are significantly different (p<0.05) in all groups. Animals group given 20% binahong leaves extract increased swimming resistance for 36,392 min, followed by caffeine for 33,440 minutes, then 10% binahong leaves extract for 29,142 min.

Conclusion: Binahong leaves and beetroots have almost the same bioactive content except in the steroid content. The binahong leaves swimming endurance activity is higher than the bit bulbs.
DEVELOPMENT OF FROVATRIPTAN SUCCINATE MICROEMULSION FOR NASAL DELIVERY: OPTIMIZATION, IN VITRO AND IN VIVO EVALUATION
Authors: UPENDRA C GALGATTE  , PRAVIN D CHAUDHARI
Published: October 2019

Objective: The main objective of the present research work was to develop, optimize, and characterize microemulsion (ME) of frovatriptan succinate to improve brain transport.

Methods: The pseudoternary phase diagrams were constructed for ME formulations composed of Capmul MCM, Cremophor EL, and propylene glycol. Frovatriptan succinate-loaded ME was optimized by simplex lattice design having the concentration of oil, surfactant, and cosurfactant representing three apex points on the triangle. These were taken as independent variables and percentage drug release as a response variable. All developed batches of ME were characterized for in vitro tests, histopathology study, and pharmacokinetics in Swiss albino rats.

Results: Clear MEs were obtained. F5 having particle size – 142.0 nm, zeta potential – 17.7–−7.8 mv, refractive index – 1.38±0.20, drug content – 98.24±0.20%, and drug diffused through dialysis membrane – 85% was the optimized batch. Drug permeation through the nasal mucosa of F5 in the ex vivo study was found to be 82.32%. Histopathology microscopic study has shown that F5 does not cause any irritation and structural changes in sheep nasal mucosa. The pharmacokinetic parameters were determined after nasal and oral administration of F5. For brain tissue, after nasal administration were Cmax181±1.51 ng/ml, Tmax – 2±1.01, area under curve (AUC)0−6 – 390.0±2.08 ng.h/ml. The AUC0−6 attained by nasal ME was 3.29 times greater than oral solution. Drug targeting index of frovatriptan succinate was 2.06. This was found satisfactory.

Conclusion: Microemulsion of said composition was found to be enhancing delivery of frovatriptan succinate to brain tissues through nasal route.
VALIDATED RP-HPLC METHOD AND UNIQUE MOBILE PHASE FOR THE SIMULTANEOUS ESTIMATION OF AMLODIPINE BESYLATE AND VALSARTAN FROM SOLID DOSAGE FORM AND ROSUVASTATIN AND VALSARTAN FROM BULK
Authors: DYADE GK  , RL SAWANT
Published: October 2019

Objective: A reverse-phase high-performance liquid chromatographic (RP-HPLC) method was developed and validated for the simultaneous estimation of amlodipine besylate (AD) and valsartan (VAL) in pharmaceutical dosage form, and rosuvastatin (RV) and VAL from the bulk mixture.
Method: Chromatographic separation was performed on RP-C18 column. The optimized unique mobile phase (acetonitrile:water and pH adjusted to 4.8 with acetic acid) was pumped at a flow rate of 0.8 ml/min in the ratio of 75:25% v/v, and the eluents were monitored at 245 nm.
Results: The assay was performed with tablet and percentage of assay was found to 101.39 for AD and 100.05 for VAL, respectively, and with bulk mixture, percentage of assay was found to 99.58 for RV and 100.32 for VAL, respectively. Linearity was obtained in the concentration range of 1–12 μg/ml for AD, 5–50 μg/mL for VAL, and 2–20 μg/ml for RV. The method was statistically validated and RSD was found to be <2%, indicating high degree of accuracy and precision of the proposed RP-HPLC method.
Conclusions: The method suggests usefulness of unique mobile phase during the estimation of two or more multicomponent dosage forms. Due to its simplicity, rapidness, high precision, and accuracy, the proposed RP-HPLC method can be applied for simultaneous determination of AD and VAL in pharmaceutical dosage form, and RV and VAL in bulk mixture.
LANNEA SCHIMPERI: REVIEW OF ITS BOTANY, MEDICINAL USES, PHYTOCHEMISTRY, AND BIOLOGICAL ACTIVITIES
Authors: ALFRED MAROYI
Published: October 2019

Lannea schimperi is a well-known fruit tree and medicinal plant in tropical Africa. The current study critically reviewed the botany, medicinal uses, phytochemistry, and pharmacological activities of L. schimperi. Literature on botany, medicinal uses, phytochemical and biological activities of L. schimperi were collected from multiple internet sources including Elsevier, Google Scholar, SciFinder, Web of Science, PubMed, BMC, ScienceDirect, and Scopus. Complementary information was gathered from pre-electronic sources such as books, book chapters, theses, scientific reports, and journal articles obtained from the University Library. This study revealed that the species is used as a source of fiber, edible fruits, and herbal medicine. Phytochemical compounds identified from the species include cyclohexenones, cardanols, alkaloids, anthocyanins, anthracene glycosides, carbohydrates, cardiac glycosides, carotenoids, condensed tannins, coumarins, flavonoids, phenolic glycosides, phenols, polyoses, polyuronoids, reducing sugars, saponins, steroids, tannins, triterpenoids, and volatile compounds. Pharmacological research revealed that extracts and phytochemical constituents isolated from L. schimperi have anesthetic, antibacterial, antifungal, anticoccidial, anti-inflammatory, antinociceptive, antioxidant, anti-trypanosoma, antiulcerogenic, cytotoxicity, and toxicity activities. L. schimperi should be subjected to detailed phytochemical, pharmacological, and toxicological evaluations aimed at correlating its medicinal uses with its phytochemistry and pharmacological activities of the species.
DESIGN AND DEVELOPMENT OF NOVEL DRUG DELIVERY SYSTEM USING HERBAL MEDICINE TO TREAT ALZHEIMER’S DISEASE
Authors: RAMA RAO NADENDLA  , LAKSHMI SWAPNA SAI  , NIHITHA SANKA  , SANTHI PRIYA NAGAM
Published: October 2019

Objective: The present study was focused to design an herbal formulation for the treatment of Alzheimer’s disease (AD) to develop the formulation using various techniques such as spray drying, centrifugation, and lyophilization and to conduct behavioral studies to evaluate the activity of the herbal formulation.

Methods: Formulation contains herbal extracts such as curcumin, guggul, and ashwagandha. To develop this formulation, various techniques such as spray drying, centrifugation, and lyophilization were employed along with a natural polymer chitosan in various combinations of excipient. Preformulation studies such as solubility of herbal extracts and Fourier transmission infrared spectroscopy (FT-IR) studies for compatibility of the natural polymer with herbal extracts were studied. The formulation was characterized by tests such as particle size determination using optical microscopy, surface morphological evaluation using scanning electron microscopy (SEM), and behavioral testing by Morris water maze test using diazepam-induced amnesia method.

Results: The particle size varied from 12.27 μ for normal chitosan to 3.59 μ for spray-dried chitosan. In the same way, the particle of normal formulation (12.9 μ) was about 4–5 times larger than that of spray-dried formulation (2.7 μ). The SEM images showed no proper morphology for chitosan, round surface with wrinkles for spray-dried chitosan, improper structures for normal formulation, and rounded smooth surface for spray-dried formulation. Significant p value was shown when the spray-dried test formulation was tested using diazepam-induced amnesia method. The transfer latency was noted on the 8th day and after 24 h of intraperitoneal administration of diazepam for the test group.

Conclusion: In the present research study, an attempt was made to design and develop a novel drug delivery system using herbal medicine to treat AD. FT-IR compatibility study was carried out using the selected polymer and the herbal extracts using novel spray-drying techniques; behavioral studies were also done.
MAJOR BIOACTIVE TRITERPENOIDS FROM GANODERMA SPECIES AND THEIR THERAPEUTIC ACTIVITY: A REVIEW
Authors: Bhat ZAHOOR AHMAD BHAT , ABDUL HAMID WANI  , MOHD YAQUB BHAT  , ABDUL RASHID MALIK
Published: October 2019

Ganoderma a traditional Chinese medicine popularly used for complementary cancer therapy and longevity for centuries. The vast amount of study has been performed on the medicinal properties of Ganoderma lucidum. G. lucidum contains various compounds with a high grade of biological activity, which increase the immunity. Several of these substances belong to the triterpenoids and polysaccharides. Proteins, sterols, phenols, lipids, etc., are also present. Ganoderma triterpenes are important secondary metabolites of G. lucidum. Ganoderma triterpenes are limestone-tetracyclic terpenes which have been reported to possess antioxidant, antitumor, anti-human immunodeficiency virus, anticancer, anti-inflammation, cytotoxic, hepatoprotective, and neuroprotective activities. This review deals with most important triterpenes isolated from Ganoderma and their therapeutic effects.
MELOXICAM-PECTIN-β-CYCLODEXTRIN TERNARY COMPLEX BY KNEADING FOR ENHANCEMENT OF SOLUBILITY AND DISSOLUTION RATE
Authors: RAJESH JAGTAP  , SHRINIVAS MOHITE
Published: October 2019

Objective: The objective of the present investigation was to improve the solubility and dissolution rate of poorly soluble drug meloxicam by its ternary inclusion complexation with natural polymers and beta-cyclodextrin (β-CD) by kneading.

Methods: Equimolar physical mixture (1:1) was prepared by homogeneously kneading drug and β-CD using a solution of agar and pectin in water to get a paste, then paste was dried overnight to get inclusion complex. Inclusion complex was evaluated for drug content, the yield of the adsorption process, Fourier-transform infrared (FTIR), differential scanning calorimeter (DSC), powder X-ray diffractometry (PXRD), scanning electron microscopy (SEM), dissolution, and stability studies.

Results: The phase solubility diagrams exhibit AL showing a linear increase of drug solubility and indicating the formation of soluble complexes. The FTIR and DSC show compatibility between meloxicam and β-CD, while slight broadening in the peak with a reduction in intensity and early onset indicates the reduction in drug crystallinity which confirms in PXRD pattern. The SEM of binary, as well as ternary, showed no aggregation, and there was a gap between the particles also indicating good redispersibility. The dissolution rate of the drug from the kneaded ternary complex with pectin was significantly rapid compared with the pure drug. The maximum drug release was observed at 85.21±1.84% at the end of 60 min. The ternary complex was found stable after 3 months stability studies.

Conclusion: The results indicated that ternary inclusion complexation with natural polymers and β-CD was most useful for enhancement of solubility and dissolution rate of a poorly soluble drug like meloxicam.
DEVELOPMENT OF ZOLMITRIPTAN MOUTH DISSOLVING FILMS: FORMULATION VARIABLES, MECHANICAL PROPERTIES, AND IN VITRO DRUG RELEASE STUDIES
Authors: SUDHIR MADDELA  , BUCHI N. NALLURI
Published: October 2019

Objective: The objective of the present investigation is to prepare zolmitriptan (ZOL) mouth dissolving films (MDFs) and to investigate the influence of formulation variables on physicomechanical, chemical, and drug release properties of the prepared MDFs.

Methods: The MDFs were prepared by solvent casting technique using wet film applicator. The impact of hydroxypropyl methylcellulose of different viscosity grades (hydroxy propyl methyl cellulose [HPMC] E3, E5, and E15), plasticizers (glycerol and polyethylene glycol [PEG]-400), and solubilizing agents (polyvinyl pyrrolidone [PVP K30] and sodium lauryl sulfate [SLS]) on physicomechanical, chemical, and drug release properties were evaluated. The MDFs were also characterized by Fourier-transform infrared spectroscopy, differential scanning calorimetry, and X-ray diffractometry studies.

Results: The MDFs prepared were transparent and smooth and showed no recrystallization. The tensile strength of the MDFs increased significantly with an increase in polymer viscosities, and about a 2.63-fold increase in tensile strength was observed for HPMC E15 MDFs compared to E3, whereas an increase in film thickness resulted in brittle MDFs with low tensile strength. Similar results were observed with percent elongation and folding endurance of the MDFs. In vitro, drug release studies indicate that higher film thickness and polymer viscosities delayed the MDF disintegration and, in turn, the ZOL release. Addition of PVP K30 and SLS to HPMC E3 formulations resulted in 1.66- and 1.53-fold increase in ZOL release rates.

Conclusion: Overall, F7 formulation showed quicker disintegration (within 11 s) and ZOL release rates (within 180 s) along with good physicomechanical properties. These results indicated that the disintegration and drug release of ZOL can be enhanced to a greater extent by optimizing formulation variables in MDFs.
DEVELOPMENT AND VALIDATION OF A NOVEL METHOD FOR CAUSALITY ASSESSMENT USING SUSPECTED ADVERSE DRUG REACTIONS TO ANGIOTENSIN-CONVERTING ENZYME INHIBITORS
Authors: Sodhi Rupinder Kaur
Published: October 2019

Objectives: The study has been designed to develop, test reliability, and construct validity of a novel versatile causality assessment tool (VCAT) method.

Methods: The study included 427 literature case reports of angiotensin-converting enzyme inhibitors with suspected adverse drug reactions from 1990 to February 25, 2016. The causality of these cases was assessed independently by 3 raters in 3 phases of the study. Kappa (k) and intra-class correlation Intraclass Correlation Coefficient (ICC) were used to test reliability and validity of the VCAT method.

Results: Intra-rater reliability was high between Phase I and Phase III (k=0.84–0.93; % agreement: 92.3–96.3%). Inter-rater agreement was good in Phase I (k=0.87–0.89, % agreement: 93.7–94.1%, ICC: 0.975) and Phase III (k=0.85–0.89, % agreement: 93–94.4%, ICC: 0.973). Validity was proved by the high agreement observed between Phase I and Phase II (k=0.78–0.94; % agreement: 89.7–97.2%; p<0.001); and between Phase II and Phase III (k=0.8–0.9; % agreement: 90.2–94.8%; p<0.001).

Conclusion: VCAT method is a standardized causal assessment tool that gives valid and reproducible results. It has shown good agreement with the expert judgment method. This method may overcome the limitations enthralled with existing methods of causality assessment.
SYNTHESIS AND EVALUATION OF ANTIMICROBIAL ACTIVITY OF PYRIMIDINE DERIVATIVES
Authors: BHAGCHAND JAT  , SWAPNA SANTRA  , PRASANTA KUMAR SANTRA
Published: October 2019

Objectives: Synthesis, characterization, and evaluation of antimicrobial activity of novel pyrimidine derivatives containing O, N, and S in the ring.

Methods: Pyrimidine derivatives were prepared in three steps. In the first step, chalcones containing -NO2 functional group were synthesized using Claisen-Schmidt condensation of aromatic aldehydes with 2-acetyl pyridine/3-acetylpyridine in methanol in the presence of aqueous NaOH. In the second step, -NO2 group was reduced to -NH2 group. Resulting compounds containing NH2 functional group were reacted with different dichlorothienopyrimidines and dichlorofuropyrimidines in the presence of N,N-diisopropylethylamine to obtain pyrimidine derivatives.Antibacterial and antifungal activity of pyrimidine derivatives were studied in vitro.

Results: Pyrimidine derivatives were synthesized and purified using flash column chromatography. Purity of synthesized pyrimidines was determined by high-performance liquid chromatography. Pyrimidines were characterized by elemental analysis, infrared, nuclear magnetic resonance, and mass spectral analysis. Analytical data of synthesized pyrimidines supported the proposed structures. Significant antibacterial and antifungal activity were observed in the synthesized pyrimidine derivatives.

Conclusion: Antibacterial and antifungal activity of the newly synthesized pyrimidine derivatives will definitely inspire future researchers for the preparation of new analogs.