Background: Boswellic acids are naturally occurring pentacyclic terpenoids that have revealed valuable anti-inflammatory, antiproliferation and anticancerous activities. Instead of these effects boswellic acids also possess antibacterial potential reported in the literature. However, these phytoconstituents associated with low aqueous solubility and bioavailability restrictions. The present study aimed to explore the antibacterial effects of boswellic acids by means of nano formulations. Materials and Methods: Chitosan was utilized as a natural biocompatible material for nanoparticles preparation, employing the ionic gelation technique as an effective approach. Well diffusion method was used to test antibacterial activity against four pathogenic bacteria typhi, and. Escherichia coli. Micro broth dilution technique was used to determine the minimum inhibitory concentration. Results: Boswellic acids-loaded nanoparticles displayed spherical particles with particle size 104.6 nm and 0.081 PDI value, respectively with smooth-surfaced spherical particles. Boswellic acids chitosan nanoparticles have a greater zone of inhibition against Salmonella typhi than Boswellia serrata extract with MIC values of 3.91 and 7.81 mu g/ mL, respectively. Conclusion: Poorly soluble boswellic acids were successfully encapsulated in chitosan nanoparticles and exhibited improved antibacterial activity compared to Boswellia serrata extract.

OBJECTIVES:The study provides a thorough examination of the rhizomes of Curcuma caesia Roxb., which is a medicinal substance sometimes referred to as black turmeric and has not been well studied. METHODS:The study examines the pharmacognostical characteristics, GC-MS profiling, and elemental analysis of the substance to determine its potential for use in medicine. The presence of heavy metal contamination in herbal products is a significant issue, which necessitates the use of Atomic Absorption Spectrophotometry to quantitatively analyze eight elements. RESULTS:The investigation validates the existence of crucial trace elements while guaranteeing that the levels of heavy metals are within the toxicity limits set by the World Health Organization. This indicates that the rhizome is safe for medicinal purposes. The selection of a solvent has a substantial impact on the efficiency of extraction. Acetone has the highest extraction yield, followed by ethanol and ethyl acetate. The GC-MS analysis uncovers a wide range of phytochemicals, such as alkaloids, flavonoids, phenols, tannins, steroids, and proteins. Additionally, particular solvents exclusively detect specific molecules. Epicurzerenone and zederone are chemicals that show promise for use in reducing inflammation and fighting cancer. CONCLUSIONS:On the basis of results it can be concluded that rhizome's quality based on acceptable physicochemical characteristics and provides a strong basis for future pharmacological research. The research has potential for the development of novel organic drugs, utilizing the abundant phytochemical composition of C. caesia Roxb. rhizomes.

Atopic dermatitis is acknowledged as a vital inflammatory disorder associated with the integumentary system of the body and is characterized by the formation of thick reddish-grey scars and erythema formation on skin, prevalent amidst the populace. Numerous synthetic drugs are available for treatment like antihistamines, immunosuppressants, glucocorticoids etc., but contrarily, essential oil therapy is exclusively lime lighted to favour the purpose. The utilization of available engineered drugs, possess the marked adverse effects owing to prolonged duration of therapy and therefore, essential oils are explored well and proved to exhibit the anti-eczematic, anti-inflammatory and antipruritic properties. Ethereal distillates own the assorted and selective therapeutic properties attributable to presence of bioactive compounds liable to treat this torturous and integumentary disorder, likely lavender oil, patchouli oil, frankincense oil etc., have been found to exert their pharmacological actions by impeding the liberation and action of inflammatory mediators and immunological hyperactivities that are engaged in exacerbating this idiopathic illness. The current attempt provided the update with the aim to bring forth the naturally originated treatment that is pertinent to provide the invulnerable therapy by circumventing the noxious symptoms i.e. erythema formation and inflamed lesions.

OBJECTIVES:The purpose of this study was to explore the molecular docking characteristics and antifertility impacts of petroleum ether extract (PEEPO) and chloroform (CHEPO) derived from Pandanus odoratissimus (PO) leaves. METHODS:TriposSybyl-X 2.1 for molecular docking and Swiss ADME for ADME predictions were used. Antifertility activity was determined by using two in vivo animal models, with a focus on estrogenic/antiestrogenic activity and anti-implantation effects. RESULTS:The findings showed that at different doses (100, 200, and 400 mg/kg), PEEPO had more anti-implantation effect than CHEPO. After taking either extract orally for up to 4,000 mg/kg, no acute toxicity was found. Furthermore, both extracts substantially raised blood oestrogen levels while lowering serum cholesterol and LDL levels, improving their antiimplantation and estrogenic activities, whether given alone or in combination with ethinyl estradiol. Molecular docking scores suggested strong interactions between phytochemicals in the extracts and estrogen receptors. ADME studies highlighted four phytochemicals present in PO leaves, showing high gastrointestinal absorption, blood-brain barrier permeability, and negative Log Kp values, indicating their potential as antifertility agents. CONCLUSIONS:The phytochemicals in both PEEPO and CHEPO demonstrated promising antifertility potential and interactions with estrogen receptors. Isolation of these phytochemicals could lead to the development of effective herbal antifertility formulations.

Synthesis, characterisation, and anti-diabetic potential of swertiamarin analogues against DPP-4 enzymatic inhibition was done prior to this study. However, swertiamarin and its analogues inhibited DPP-4 enzyme significantly. Semisynthetic swertiamarin analogues have been studied for antidiabetic potential and mechanism of action utilising molecular docking and in-vitro techniques. The mechanism of action for swertiamarin analogues was determined by in-silico molecular docking studies using glucose-transporters, GLUT-1 (PDB ID: 4PYP), GLUT-3 (PDB ID: 7SPS), and GLUT-4 (PDB ID: 7WSM) along with in-vitro glucose uptake and glucose-induced insulin secretion assays. These studies found that synthesised swertiamarin analogues SNIPERSV3, SNIPERSV4, and SNIPERSV7 shown better docking score against different GLUTs and better anti-diabetic effects on glucose uptake and insulin secretion in NIT-1 cell line than standard glibenclamide and swertiamarin. Thus, swertiamarin analogues might be studied for diabetes therapy in the future.

Diabetes mellitus (DM) is a globally spreading metabolic disorder with a high incidence rate. About 425 million cases took place in 2017 and expected to rise up to 693 million by 2045. In diabetes, the patient elevation of blood glucose level occurs due to the deformation of insulin receptor action/secretion or both. Long term increases in blood glucose level causes chronic effects such as dysfunction and damage of various organs such as eyes, nerves, kidney heart and blood vessels. There are many treatment regimens available in market, but do not able to provide complete relief and cause severe side effects. To overcome these types of problems it becomes important to find different therapeutic targets and use it in combination with conventional medicine for the treatment of diabetes. To surmount the side effect of presently available treatments, now researchers relay on herbal plants. In this review, we discussed the diabetes occurrence, epidemiology, types, different target receptors, and available treatments and describe briefly role of different plant constituents in diabetes management and focused on a main plant, Moringa oleifera.

Swertiamarin is a lead, biologically active compound obtained from Enicostemma littorale Blume and known to be identified for the anti-diabetic activity. Present work comprises the synthesis and structural optimization of seven novel swertiamarin analogues and those were not being reported elsewhere till date. Swertiamarin was isolated, followed by modifications that have been accomplished amidst fluorinating, acetylating and oxidizing agents and also performed chromatographic purity and characterization of analogues. Furthermore, the swertiamarin analogues were screened for dipeptidyl peptidase IV (DPP-IV) enzyme inhibition with in silico studies. Besides, the pharmacokinetics and toxicity of analogues were predicted using ADMET software. In a nutshell, the compounds such as SNIPERSV-4 and SNIPERSV-7 have to pose good initial activity (∼48%) in comparison to standard DPP-IV inhibitor (Sitagliptin). The identified analogues were active against DPP-IV enzyme in preliminary screenings, and these findings would be beneficial for the new age researchers also for the therapy of diabetes.

Cancer a leading cause of human mortality worldwide is characterised by the unseemly growth of cellular mass and signalled through the enlargement of stress. Management of cancer treatment is still buried and has been recently alerting the need to discover a drug molecule with lesser side effects. The objective of the present study is to explore the anticancer activity and docking studies of 1-(5-substituted phenyl) isoxazol-3-yl)-5-phenyl-1H-tetrazole derivatives. The compounds were evaluated for in-vitro anticancer activity under the drug discovery program of National Cancer Institute (NCI), USA. Only seven compounds were selected and screened for anticancer activity at a single high dose (10-5 M) using NCI 60 cancer cell lines. Among all the selected compounds, 4b and 4i exhibited significant anticancer activity against Leukemia cell lines. Molecular docking studies for the 5-phenyl-1-(5-substituted phenylisoxazol-3-yl)-1H-tetrazole analogues was done by Schrodinger software. Docking results stated that the compounds 4b and 4i has good dock score among the other derivatives which shows good binding efficiency towards receptor.

Phytosome is made up of two words and expressed the meaning of “Phyto” means plant and “some” means cell-like. Phytosome, is a developing field which is related to phyto-pharmaceuticals and in which the phytoconstituents of herbal extract bounded with the lipid layer. Water is a universal solvent for most of the bioactive phytoconstituents and lipids are lipophilic. Due to this combination of solubility parameter, Phytosome shows better absorption which leads to better bioavailability than the conventional herbal extracts and increases in the pharmacological and pharmacokinetic properties. This characteristic of Phytosome makes more useful in drug delivery system for the disease treatment. The present review represents the recent advances and applications of herbal extract Phytosome as a tool of drug delivery in the treatment of the diseases. © 2018 iGlobal Research and Publishing Foundation. All rights reserved. Cite this article as: Sanha, A.M.F.; Sharma, P.K.; Kumar, S. Phytosome as a prominent option in drug delivery for the treatment of the diseases: a review. Indo Global J. Pharm. Sci., 2018; 8(3): 119-123. Indo Global Journal of Pharmaceutical Sciences, 2018; 8(3): 119-123 120 phosphotidylcholineproduce a lipid compatible molecular complex with phytoconstituents. Differences between Phytosome and Liposome: Some of the differences between Phytosome and Liposome are mentioned below:  Liposomes are reported for the delivery vehicles only for dietary supplements and not promising clinical efficacy but Phytosome products numerous studies proved better absorbtion and clinical efficacy.  Phytosome represent a unit of bonded hybrid molecules, while the liposome represents a group of many phospholipids molecules which encloses phytoactive molecules without specifically bonding. In liposome the active principle is dissolved in the medium contained in the cavity or in the layers of the membrane, whereas in the phytosome it is an integral part of the membrane, being the molecules anchored through chemical bonds to the polar head of the phospholipids. The complex formation for the liposome (upper segment) versus phytosome (lower segment)as shown below in Figure 1. Phosphotidylcholine-drug complex Water soluble free drug

Genetic modifications or mutations has been a bottleneck for the treatment of cancer; it is widely known to play a vital role in the progression of metastatic level/stage within the nonsmall cell lung cancer (NSCLC). The NSCLC of cancer is responsible for lung cancer lawsuits. In the various genetic mutations related study has been concluded with the various genes findings, which are named as the epidermal growth factor receptor, anaplastic lymphoma kinase, Kristen rat sarcoma virus, ROS proto-oncogene 1, human epidermal growth factor, B-RAF proto-oncogene, rearranged during Transfection, MET, Phosphatidyl 3-kinases CA, IGF-1R, NTRK1, FGFR1, and DDR2. The various research data supported this study. The involvement of the gene in the NSCLC patients made a paradigm shift in the drug discovery. The presence of one mutation in connection with some other could have an impact on NSCLC remedy.Utilizing this genotype-directed therapy for an advanced NSCLC has to turn out to be an appealing and efficacious treatment strategy. Here in the advancement of research, related genetic modulated targets and treatment have been discussed, particular genetic mutations help to find new updated interventions or medicinal drugs for the treatment of NSCLC. In there view, we have comprehensively arranged the mutation type and treatment with the status of NSCLC.

Swertiamarin, a secoiridoid glycoside is one of the major components and an active lead isolated from a perennial herb Enicostemma littorale (EL) Blume. Swertiamarin has been reported for its number of pharmacological activities namely, hepatoprotective, antiedematogenic/anti-inflammatory, free radical scavenging activity, antispastic activity, dyslipidemia, hypolipidemic effect and anti-hyperlipidemic effect. Thus, swertiamarin has the potential to be a successful drug candidate in the future in the treatment of various diseases. Isolation and characterization of the swertiamarin following a published procedure didn’t yield the reported purity. Considering the therapeutic importance of swertiamarin, there is a need for the development of an effective method for the compound in good yield and purity. This method involves column chromatography of a methanolic extract of dried whole plant powder material of Enicostemma littorale Blume for the isolation in pure form. Swertiamarin, as colorless crystals with a yield of 7.3%, 97.5% purity by HPLCPDA analysis was isolated and characterized by MS, IR and H-NMR. Comparison was done with reported literature. The percentage yield and purity of isolated swertiamarin was improved by this method. © 2018 iGlobal Research and Publishing Foundation. All rights reserved. Indo Global Journal of Pharmaceutical Sciences, 2018; 8(1): 1-8 2 Swertiamarin is present in many plants like Anthocleista procera Lept. Ex Bureau, Blackstonia perfoliata L. Hudon, Centaurium erythraea Rafn., Enicostemma littorale, Gentiana macrophylla Pall, Gentiana manshurica Kitag, Gentiana scabra Bunge, Swertia chiraytiya Roxb ex. Flem Kurst., Swertia davidi Franch, Swertia patens Burk, Swertia mileensis, Swertia pseudochinesis H. Hara.. It has very low toxicity and Vishwakarma et al. suggested that swertiamarin was one of the major components of Enicostemma littorale (Fig. 1). Figure 1 Structure of swertiamarin from Enicostemma littorale Swertiamarin is a secoiridoid glycoside and recently it has been reported for its number of pharmacological effects namely, antidiabetic, antiarrithritic activity, hepatoprotective, antiedematogenic/anti-inflammatory, free radical scavenging activity, a CNS depressant effect and anticholinergic activity, anticholinergic, antibacterial activity , neurotrophic activity. The separation, isolation and purification of bioactive compounds with purity, good quality as well as in quantity from a from a crude extract or fractions of an extract is a long and expensive process, because of the target compound(s) presence in a matrix of dozens of other constituents. Natural product chemistry usually begins from the separation and isolation of single pure compound from such many structurally related ingredients. Most separation procedures, however, require diverse chromatographic methods. Column chromatography has found its place in many laboratories for the preparative purpose. The advantage of column chromatography is mainly due to: simple packing procedure, low operating pressure, and inexpensive instrumentation. However, the basic prerequisite for successful separations in column chromatography is the choice of the proper adsorbent and mobile phase. Adsorbent particle size affects how the solvent flows through the column. The previously reported methods of swertiamarin isolation were not efficient at quantitative as well as qualitative levels. Therefore, we have developed a new method for the isolation of pure swertiamarin by column chromatography, which is rapid, economical method for the isolation of swertiamarin in high yields and purity by column chromatography. MATERIALS AND METHODS Plant materials Collection and identification of the plant The whole plant of Enicostemma littorale was collected from Dharampur, Valsad district in November 2012. The material was authenticated by a taxonomist and identity was confirmed by referring Flora of Gujarat. A voucher specimen NIPERA/NP/1112/05 was submitted at NIPERAhmedabad, India. Plant material was shade-dried, powdered and stored in air tight container for further use. Equipment’s/Apparatus/Materials Rotary evaporator (R-210) was used for solvent evaporation and pre-coated TLC plates (silica gel 60 F254 (E. Merck), panisaldehyde reagent (Spectrochem), UV-cabinet (CAMAG), silica gel (230-400#) (Merck, Germany), melting point apparatus (VEEGO-VMP-PM), twin trough TLC chamber (10x10), HPTLC (CAMAG) were used during swertiamarin isolation. Extraction and isolation of swertiamarin Powdered plant material (50 g) was loaded in a 250 ml Erlenmeyer flask and fatty material removed by washing with chloroform (5 x 200 ml) until the extraction solvent became colorless. TLC analysis of the system (chloroform: methanol, 8.5: 1.5 v/v) indicated complete removal of the fats. The material was extracted with methanol (4 x 500 ml) by cold maceration. TLC analysis (chloroform: methanol (8.5: 1.5 v/v) indicated complete extraction of swertiamarin. The methanolic extract was filtered through Whatman filter paper (10 μ) and concentrated to 50 ml. The methanolic extract obtained was treated with cold diethyl ether to obtain 17 g of a precipitate. The precipitate was loaded on a chromatography column with slurry of 230-400 mesh silica gel and eluting solvent chloroform, ensuring that no air bubbles form. Gradient elution, starting with chloroform and then with chloroform /methanol (0–5%), followed by further increment of methanol in the decimal scale (5.1-5.9%). The isolation procedure was monitored by TLC for swertiamarin (chloroform: methanol (8.5: 1.5 v/v). Visualization was done at 254 nm followed by derivatization with p-anisaldehyde for presence of other impurities. Fractions containing swertiamarin were pooled and concentrated to dryness to obtain 3.6 g of the material. The isolated swertiamarin was stored at -20oC until required for further study. The identification of swertiamarin was done by using HPTLC (CAMAG) and purity of standard and isolated swertiamarin at 1 μg/ml and 5 μg/ml was determined by Indo Global Journal of Pharmaceutical Sciences, 2018; 8(1): 1-8 3 HPLC-PDA system (SHIMADZU LC-2010; PDA detector (200-400 nm). The characterization of isolated swertiamarin was done by using different spectral techniques such as: Infrared(IR) spectra were recorded on Fourier-transform Infrared (FTIR) spectrophotometer (Shimadzu), atmospheric pressure ionization with ion spray mass spectra of molecular ions were obtained on a Perkin-Elmer, API 165 mass spectrometer (LC/MS), and 1H-Nuclear magnetic resonance (1H-NMR) spectra was recorded in MeOD using Fouriertransform (FT)-NMR spectrometer (Bruker Advance II (500 MHz), Switzerland). General experimental procedures Preparation of p-Anisaldehyde reagent 85 ml of methanol was taken in 500 ml glass measuring cylinder and 10 ml glacial acetic acid was added and thoroughly mixed with a glass stirring rod. After that 5 ml sulphuric acid (H2SO4) was added in to mixture followed by addition of 0.5 ml p-Anisaldehyde to the mixture and reagent was ready to be prepared fresh before use. Identification and comparison of UV absorption spectrum of isolated swertiamarin with standard swertiamarin HPTLC analysis was performed on pre-coated plates of silica gel 60 F254 (E Merck, 139 Kiesel gel 60 F254, 0.2 mm) and samples were applied on the plates using CAMAG 140 LINOMAT 5 Automatic TLC spotter (Switzerland). The swertiamarin sample along with the standard was developed (chloroform: methanol 8.5: 1.5 v/v), and UV spectra recorded on a CAMAG TLC Scanner 3 with CAMAG 1.3.0 WinCATS software. The melting point of standard and isolated swertiamarin was checked by using a melting point apparatus (VEEGO-VMP-PM) and UV absorption spectrum of the isolated swertiamarin was taken at start, middle, and end positions of the band by HPTLC. Purity profiling of isolated swertiamarin by HPLC Purity of isolated swertiamarin and standard swertiamarin was determined by using HPLC-PDA (High performance thin layer chromatography with photodiode detector) in solvent gradient system Ammonium acetate/Acetonitrile (85: 15) at 1 μg/ml and 5 μg/ml concentration. RESULTS AND DISCUSSION Swertiamarin (Fig. 2) of purity 97.5% was isolated with a yield of 7.3% using the current developed method. The melting point of isolated swertiamarin was observed at 113114 °C. Rf (0.30) of the isolated swertiamarin is same as same as that of standard reference swertiamarin. In addition to swertiamarin, an additional compound was isolated, which had an Rf of 0.28 as shown in (Fig. 5). Overlay UV absorption spectra of isolated swertiamarin with additional compound was recorded (Fig. 9) as well as overlay UV spectrum of standard and isolated unknown compound was recorded and ƛ max of isolated swertiamarin and swertiamarin standard was come at 242 nm as shown in (Fig. 10). The purity of standard and isolated swertiamarin by HPLC was 97.7 and 97.2, respectively at 1 μg/ml and 5 μg/ml concentration as shown in (Fig. 11-14). Figure 2 Structure of Swertiamarin The isolated sample of swertiamarin was identified and characterized from its spectral data (MS, IR, and H-NMR), which matched well with that of the standard swertiamarin. The molecular ion peak of isolated swertiamarin MS m/z was 375.2 (M) (Fig. 6) whereas reference standard swertiamarin MS m/z was 375.1(M).FTIR spectra of isolated swertiamarin and standard swertiamarin showed several intense peaks in the wave number region between 4000-400 cm such as O-H (stretch.) 3347 cm,C-H (stretch.) 2923 cm,C=O (stretch.) 1696 cm,C=C (stretch.) 1617 cm,C-O-C (stretch.) 1408 cm ,C=CH2 (stretch.) 846 cm -1 (Fig. 7). Isolated swertiamarin showed the following H-NMR signals in (MeOD): chemical shift values (δ): 1.28 (ddd, H6-α), 1.28 (ddd, H6-β), 2.83 (dd, H-9), 3.81 (dd, H-7β), 4.26 (dd, H-7α), 5.63 (dd, H-1), 7.54 (s, H-3), Gluocose:3.56 (m, H-2”,3”,4”,5”), 3.81 (dd, H-7α), 4.44 (dd, H-7β), 4.66 (ddd, H-1”) (Fig. 8). Figure 3 Ov

This study was undertaken to assess the antifertility effect of hydroalcoholic leaves extract of Pandanus odoratissimus Linn. which is traditionally used by the woman in Rajasthan state of India to regulate the fertility. The antifertility activity of the extract at dose levels (200 and 400 mg/kg, orally) was evaluated in two experimental animal models. The extract was found to be safe up to a dose of 4000 mg/kg of the extract when administered orally. A good antiimplantation (37.13%) activity in female rats was observed at the tested dose level (400 mg/kg). The extract, when administered alone at 200 mg/kg dose to immature female albino rats, enhanced the estrogen level in the serum whereas significantly decreased the estrogen level at 400 mg/kg dose. The extract along with estradiol at dose level of 400 mg/kg significantly (p < 0.01) decreased the level of estrogen, in comparison to standard group rats indicating the antiestrogenic nature of the extract. The antiestrogenic effect of the extract at higher dose (400 mg/kg) might be due to negative feed-back inhibition on anterior pituitary. Preliminary phytochemical screening has revealed the presence of alkaloids, carbohydrates, flavonoids and saponins in the hydroalcoholic leaf extract of the plant. The antifertility effect of the plant might be due to antiimplantation as well as antiestrogenic effect of the extract which in turn might be due to some of the chemical constituents present in the extract. The results shows that hydroalcoholic extract of P. odoratissimus L. leaves possess significant antifertility activity at 400 mg/kg, thus, justifying the traditional use of this plant in fertility regulation in females.

A series of (3-phenyl-5-(1-phenyl-3-aryl-1H-pyrazol-4-yl)-4,5-dihydro-1H-pyrazol-1-yl)(pyridin-4-yl) methanones was synthesized by condensing suitably substituted chalcones, i.e., 3-(3-aryl-1-phenyl-1H-pyrazol-4-yl)-1-phenylprop-2-en-1-ones, and isoniazid in acetic acid. The structure of newly synthesized compounds has been established on the basis of analytical and spectral data. The new compounds were screened for antimicrobial activity and most of them showed good activity comparable with that of standard drugs ciprofloxacin and fluconazole. Compounds containing methoxy group showed high antimicrobial activity.