bluuebunny/crossref_metadata_2025 huggingface dataset:
Targeting Cell Wall Synthesis and Assembly in Microbes: Similarities and Contrasts Between Bacteria and Fungi
Authors: Goldman R. C. , Branstrom A.
Published: January 2023

Microbial cells possess a form of exoskeleton called the cell wall that protects the organism from osmotic pressure and environmental insults. Synthesis of the various building blocks that make up the cell wall occurs in the cytoplasm, and thus microbial cells face specific biochemical and biophysical problems related to the polymerization, transport, and assembly of building blocks into the final wall structure at an extra-cellular site. Cell walls must also be metabolically and
structurally pliable in order to allow for processes such as repair, secretion, DNA exchange, and cell division. In some cases, bacteria and fungi use similar mechanisms, to accomplish synthesis and assembly, while in other cases each used divergent strategies to accomplish specific functions. This review will summarize recent advances in our understanding of fungal and bacterial cell wall synthesis and assembly. We will compare specific pathways used by both fungi and bacteria, paying particular attention to identifying those areas where what is known in one system may point to approaches to solving unanswered questions in the other. The structure, chemical properties, and mechanism of action of select natural and synthetic products which inhibit synthesis or assembly of cells walls will be discussed in terms of similarities in the structures, and/or steps in the synthetic process targeted. In addition, new targets in the pathways will be presented along with recent approaches to the discovery and design of novel inhibitors.
Fish Protein Hydrolysates: Bioactive Properties, Encapsulation and New Technologies
for Enhancing Peptides Bioavailability
Authors: Moya Moreira Thaysa Fernandes , Gonçalves Odinei Hess , Leimann Fernanda Vitória , Ribeiro Ricardo Pereira
Published: January 2023

Fish protein hydrolysates (FPHs) can be obtained from substrates such as fish muscle, skin, and
wastes and assign value to these fish by-products. Proteolytic enzymes catalyze the hydrolysis of these fish substrates'
peptide bonds resulting in smaller peptides that present several bioactive properties. Hydrolysates' bioactive
properties are a function of the fish species used as the substrate, the enzyme selectivity or specificity, pH
and temperature applied in the reaction, etc. Furthermore, many pre-treatment methods are being applied to fish
protein substrates to improve their enzyme susceptibility and increase the number of smaller bioactive peptides.
This review addresses the production of FPHs and the main bioactive properties evaluated recently in the literature
and emphasizes the substrate treatments by high-pressure processing, microwave, ultrasound, and thermal
treatments to achieve better bioactivity making essential amino acids more available in peptides. The bioactive
properties most found in FPHs were antioxidants, antimicrobials, anticancer, and antihypertensive. These bioactivities
may vary depending on the conditions of hydrolysis, fish species, and fractionation and isolation of specific
peptides.New technologies for the treatment of by-products can reduce process losses and achieve better
results by cleavage of proteins. Conversely, encapsulation and film utilization can improve bioactivity, bioavailability,
and controlled release when applied to foods, resulting in improved health.
Liposomal Formulation Improves the Bioactivity of Usnic Acid in RAW
264.7 Macrophage Cells Reducing its Toxicity
Authors: Vasarri Marzia , Ponti Linda , Degl'Innocenti Donatella , Bergonzi Maria Camilla
Published: January 2023

Background:

Reactive oxygen species (ROS) production and oxidative stress may be responsible
for the onset of several chronic diseases. Usnic acid (UA) is a natural secondary metabolite of
lichens with several healthful bioactivities, including antioxidant properties. However, UA is a hydrophobic
compound known for its hepatic toxicity. These aspects limit its therapeutic applications. To
overcome these drawbacks and improve the pharmacological use of hydrophobic compounds, nanotechnology
is widely used. Therefore, the incorporation of UA into appropriate nanocarriers could enhance
the bioactivity of UA by increasing its solubility.

Objective:

The aim of this work was to improve the solubility of UA and its bioactivity in the absence
of cytotoxicity.

Methods:

In this study, UA loaded liposomes (UA-LP) were developed. The formulations were chemically
and physically characterized, and an in vitro release study was performed. Free UA and UA-LP
were tested on RAW 264.7 murine macrophages in terms of cytotoxicity, intracellular ROS production,
and NO release in the absence or presence of pro-oxidant LPS stimulus.

Results:

UA-LP showed excellent physical and chemical stability during storage and improved solubility
of UA. UA-LP showed an antioxidant effect in the absence of cytotoxicity compared with free UA
on LPS-exposed macrophages.

Conclusion:

For the first time, liposomal formulation improved the beneficial action of UA in terms of
solubility and antioxidant activity.
Sequential Developmental Events in the Wax Moth Life Cycle
Authors: Marwaha Lovleen
Published: January 2023

The wax moth (WM) is a holometabolous insect with developmental stages
of egg, larva, pupa, and adult in its life cycle. The development coherence of the wax
moth is influenced by different abiotic and biotic environmental cues, including the
larval diet, temperature, cannibalism, genomic content, insect hormones, and
pheromones. The fecundity and fertility are comparatively high in WM to ensure
species' survival within the honey bee hive. The wax moth adults preferentially infest
the weaker colonies at night, where they live in the concealed space, usually on the top
bar of the wooden chamber. Mating usually takes place on nearby trees; after that, the
gravid female enters the hive to oviposit in the crevices and cracks to hide from the
host honey bees. Afterward, the eggs hatch into the larva that feeds on the bee wax,
honey, pollen, and exuviate of the honey bees. Severe localised concealing sites of WM
in the hive facilitate specific pest protection in the host honey bee colony, eventually
destroying the entire hive and forcing the honey bees to abscond the hive. The present
chapter elucidates the development of a specific devastating pest of honey bee colonies,
including influential abiotic and biotic factors. Furthermore, the differentiation of the
life cycles of the greater wax moth (GWM) and the lesser wax moth (LWM) is also
speculated in detail as per available literature.
The Possible Wax Moth Infestation Regulation
Authors: Marwaha Lovleen
Published: January 2023

The wax moth infestation can be controlled with various physical, chemical,
and biological methods. As the wax moth is a typical lepidopteran insect that is
poikilothermic, exposing multiple developmental stages and imagoes to extremely low
and higher temperatures can provide a solution for the specific pest infestation.
Additionally, divergent pesticides targeting the nervous system, respiratory system,
developmental regulation, and general insect physiology further solve the problem. The
biological control measures include the application of various micro-organisms or their
secreted products that can help regulate the insect population. The present chapter
highlights primary methods for regulating the wax moth infestation with divergent
strategies to reduce economic loss to apiculture.
Axiotherapy of Non-Accountable Perpetrators of Criminal Acts
Authors: Kudlak Grzegorz
Published: January 2023

Axiotherapy is an original project built on value-based therapy carried out in a forensic psychiatry ward. It is addressed to persons who committed a criminal act and were deemed by the court to be non-accountable or of limited accountability at the time of the crime. As a result, they were referred for treatment as part of the imposed preventive measures. Patients treated at the forensic psychiatry ward are most often perpetrators of violent crimes. While suffering from various mental disorders, they also exhibit impulsive behaviour leading to criminal acts. Such behaviour has far-reaching consequences for both the patient and the general public. Mental disorders of forensic psychiatry patients, the course of the disease, the degree of aggression and associated circumstances (such as addiction, sexual preferences disorders, and personality disorders) indicate a crisis in the sphere of values, which could be one of the factors leading to the serious crime. Working with a value system that determines a person’s behaviour means working on a system that motivates and activates them and can change over time. Axiotherapy is intended to help patients to work out their value system and to identify their transcendentals, as appropriate.
The Relation between Environmental Risk Analysis and the Use of Nanomaterials in the Built Environment Sector: A Circular Economy Perspective
Authors: Angrisano Mariarosaria , Fabbrocino Francesco
Published: January 2023

Nowadays, the challenge of climate change and “ecological transition” is substantially an “energy challenge” for every city, which is supposed to become as “energetically self-sufficient” as possible. The construction sector is one of the main contributors to the effects of climate change, starting from the production of materials to the use phase of buildings to their demolition. Recent innovations in sustainable/circular design are related to using “new materials." According to this perspective, nanomaterials are becoming an increasingly widespread practice in various sectors. Nanomaterials are considered very innovative materials able to solve different problems related to buildings' structural and energy efficiency due to their small size. However, the future challenge is to understand whether these materials can be considered “green" from their production stage since risks to human health have been found in both the manufacturing and use and disposal stages. In this regard, an abacus of the most commonly used nanomaterials in the construction industry is defined. Simultaneously, were identified the negative environmental impacts related to the use of these materials, to propose possible solutions to reduce/mitigate them. Therefore, from this analysis, it emerged that a possible solution could be to move to the “industrial biosynthesis process” for producing nanomaterials, according to the circular economy principles. However, this process must always be combined/supported by “Environmental Risk Analysis (ERA)," an evaluation tool capable of identifying and mitigating the adverse negative environmental impacts. The paper concludes with the consideration that new materials for the built environment should be functional and " beautiful," particularly when they are to be used for reuse projects in historic buildings.
Negami: An Augmented Reality App for the Treatment of Spatial Neglect After Stroke
Authors: Stammler Britta , Flammer Kathrin , Schuster Thomas , Lambert Marian , Karnath Hans-Otto
Published: January 2023

Background

A widely applied and effective rehabilitation method for patients experiencing spatial neglect after a stroke is “visual exploration training.” Patients improve their ipsilesional bias of attention and orientation by training exploration movements and search strategies toward the contralesional side of space. In this context, gamification can have a positive influence on motivation for treatment and thus on the success of treatment. In contrast to virtual reality applications, treatment enhancements through augmented reality (AR) have not yet been investigated, although they offer some advantages over virtual reality.

Objective

This study aimed to develop an AR-based app (Negami) for the treatment of spatial neglect that combines visual exploration training with active, contralesionally oriented rotation of the eyes, head, and trunk.

Methods

The app inserts a virtual element (origami bird) into the real space surrounding the patient, which the patient explores with the camera of a tablet. Subjective reports from healthy elderly participants (n=10) and patients with spatial neglect after stroke (n=10) who trained with the new Negami app were analyzed. Usability, side effects, and game experience were assessed by various questionnaires.

Results

Training at the highest defined difficulty level was perceived as differently challenging but not as frustrating by the group of healthy elderly participants. The app was rated with high usability, hardly any side effects, high motivation, and entertainment. The group of patients with spatial neglect after stroke consistently evaluated the app positively on the dimensions of motivation, satisfaction, and fun.

Conclusions

The Negami app represents a promising extension by adding AR to traditional exploration training for spatial neglect. Through participants’ natural interaction with the physical surrounding environment during playful tasks, side effects as symptoms of cybersickness are minimized and patients’ motivation appeared to markedly increase. The use of AR in cognitive rehabilitation programs and the treatment of spatial neglect seems promising and should receive further investigation.
A Family-Based Collaborative Care Model for Treatment of Depressive and Anxiety Symptoms in Perinatal Women: Results From a Pilot Study (Preprint)
Authors: Cluxton-Keller Fallon , Olson Ardis
Published: January 2023

BACKGROUND

Untreated perinatal depression and anxiety can have detrimental consequences on family function. Logistical barriers prevent many perinatal women from accessing treatment, and these barriers are compounded for women residing in rural areas. This paper describes a Family-Based Collaborative Care Model (FBCCM) that is designed to bypass barriers to increase access to care for depressed and anxious perinatal women in rural regions of the United States. The FBCCM includes the following two components: (1) a 10-session video-delivered family therapy treatment for perinatal depression and anxiety and (2) a video-delivered infant care provider training on addressing the parenting needs of depressed and anxious mothers.

OBJECTIVE

This paper describes the feasibility of implementing the FBCCM with families and infant care providers. Findings are presented on the preliminary effectiveness of the video-delivered family therapy treatment in reducing maternal depressive and anxiety symptoms, and family conflict.

METHODS

This pilot study was carried out using an implementation-effectiveness hybrid trial design without a comparison group. Changes in maternal depressive symptoms, maternal anxiety symptoms, and family conflict were measured at posttreatment, 3 months, and 6 months later.

RESULTS

On average, mothers (n=24) attended 9.79 (SD 1.02) sessions. On average, their family members (n=24) attended 9.42 (SD 1.28) sessions. A total of 31 infant care providers attended the training on addressing the parenting needs of depressed and anxious mothers. Mothers reported a significant reduction in depressive symptoms (P<.001) and anxiety symptoms (P<.001) from baseline to the 6-month follow-up. Mothers reported a significant reduction in conflict (P<.001), and their family members also reported a significant reduction in conflict (P=.007) from baseline to the 6-month follow-up.

CONCLUSIONS

The findings from this study provide support for the feasibility and preliminary effectiveness of the FBCCM. The findings will be used to inform a larger study of the FBCCM.
Gejolak di Awal Gerak: Perwari dalam Kemelut Revolusi Indonesia
Authors: Sasi Galuh Ambar
Published: January 2023

The historical narrative of the Indonesian women’s movement is solely about the congressional activities and their results without giving explanation on the meaning and historical context of the movement. This can be seen from the discourse of Indonesian women’s movement during the revolutionary period, which generally centered on four main points, i.e. women’s mobilization in the Red Cross, women paramilitary troops, public kitchen, as well as organizational change and its congress. As an alternative, in this article I examine the first five months of Perwari (the Women Association of Republic Indonesia), its dynamic and historical context. The research finds out that differences of ideologies, perceptions, and expectations about the Indonesian revolution influenced the direction of women’s movement, triggering internal conflict that eventually destroyed them.
STANDARDIZATION OF ORTHOSIPHON ARISTATUS, BLUME MIQ
Authors: FARAMAYUDA FAHRAUK , RIYANTI SORAYA , SURYANI  , SYAM AKHIRUL KAHFI , ELFAHM  , MARIANI TOTIK , SUKRASNO
Published: January 2023

Objective: The main compounds in O. aristatus are rosmarinic acid, sinensetin, and eupatorin. Sinensetin and rosmarinic acid compounds have the potential as antiviral agents. The focus of this research is O. aristatus purple and white-purple varieties. This study aimed to determine the levels of three main secondary metabolites of O. aristatus, one of the specific standardizations. Methods: The standardization parameters to be tested were to determine the main compound levels by using thin-layer chromatography densitometry on two varieties of O. aristatus. Results: The highest value levels of sinensetin and rosmarinic acid in purple variety O. aristatus were 0.53 and 1.32% w/w, respectively. The highest level of eupatorin was 0.88% w/w in the ethanol extract of white-purple varieties of O. aristatus. The main secondary metabolites in the two varieties of O. aristatus were more significant in the leaves than in the stems. Meanwhile, the sinensetin and rosmarinic acid levels in the ethanol extract of leaves and stems of the purple variety O. aristatus were higher and significantly different than in the white-purple ones. However, the levels of eupatorin were higher and significantly (p<0.05) different in the white-purple variety compared to the purple variety. Conclusion: The purple variety is due to greater sinensetin and rosmarinic acid levels in the purple variety than in the white-purple ones.
ALPHA-GLUCOSIDASE INHIBITOR ACTIVITIES AND PHYTOCHEMICALS SCREENING OF THE PEPEROMIA GENUS CULTIVATED IN INDONESIA
Authors: SAEPUDIN SYUMILLAH , SUSILAWATI YASMIWAR
Published: January 2023

Objective: Peperomia is a genus belong to Piperaceae family, which is valuable as ornamental and has several medical uses but not widely explored in their pharmacological activities. Some peperomia plant has been investigated and reported to have various activities, recently as diabetes mellitus. This research was conducted to screening phytochemical profile and to determine alpha-glucosidase inhibitor activities of five species in genus Peperomia that are easy to grow and has been cultivated in Indonesia.

Methods: Dried leaves were macerated with 70% ethanol and vaporized by rotary evaporator. Phytochemical screening was conducted using qualitative chemical analysis and inhibition of alpha-glucosidase was conducted using p-nitrophenyl-α-D-glucopyranoside as substrate, and absorbance was measured with a spectrophotometer UV-Vis.

Results: The phytochemical screening of the leaves extracts demonstrated the presence of various secondary metabolites, such as flavonoids, phenol, tannins, quinone, alkaloids, saponins, steroids, and triterpenoids. The inhibition of alpha-glucosidase showed that the IC50 value of ethanol extract of P. obtusifolia, P. clusiifolia, P. caperata (green), P. caperata (red), and P. argyreia leaves were 2.90; 18.05; 21.46; 23.81; and 48.70 µg/ml respectively.

Conclusion: The highest inhibition of alpha-glucosidase activity was showed by P. obtusifolia with an IC50 value of 2.90 µg/ml. Further research is needed to explore its potential as an antidiabetic.
VALIDATION OF WARFARIN ANALYSIS METHOD IN HUMAN BLOOD PLASMA USING HIGH-PERFORMANCE LIQUID CHROMATOGRAPHY WITH FLUORESCENCE DETECTION
Authors: PUTRIANA NORISCA ALIZA , RUSDIANA TAOFIK , ROSTINAWATI TINA , AKBAR MOHAMMAD RIZKI , NURFUADAH ILMA
Published: January 2023

Objective: Validation of analysis method is important, especially in analyzing narrow-index drugs such as warfarin (WF). This study aimed to obtain a validated method of analyzing warfarin in human plasma according to European Medicine Agency guidelines. Methods: The optimum conditions for the analysis of warfarin in human plasma using fluorescence detector HPLC with Chiralcel OD-RH column (4.6 x 150 mm i.d., 5μm); Chiralcel OD-RH guard column (4.0 x 10 mm, 5μm), column temperature 45 °C. The mobile phase used was acetonitrile: phosphate buffer pH 2 (40:60), with an isocratic flow rate of 1 ml/min and an injection volume of 20 μl. Excitation and emission wavelengths were 310 and 350 nm (warfarin) and 300 and 400 nm (griseofulvin). The retention time of griseofulvin was 6-7.5 min; R-warfarin was 10-11.5 min; S-warfarin was 14-16 min. Results: The result of this validation obtained the optimum condition. This method yielded LOD values of 0.0674 ppm (R-warfarin) and 0.0897 ppm (S-warfarin). LOQ values were 0.225 ppm (R-warfarin) and 0.298 ppm (S-warfarin). Linearity at concentrations of 0.2-3 ppm with the line equation y = 0.0705x+0.0704 with R2 = 0.978 for R-warfarin and y = 0.0513x+0.0297 with R² = 0.9924 for S-warfarin. 75% of the seven concentrations met the reverse concentration requirements, which were below±15%. This method met the requirements of accuracy and precision within and between runs, selectivity and carryover where the %RSD and %diff values were below±15% Conclusion: This analytical method can be declared valid and can be used for sample measurement in warfarin pharmacokinetic studies.
GC-MS PROFILE AND ANTIBACTERIAL ACTIVITY OF ESSENTIAL OIL FROM STROBILANTHES KALIMANTANENSIS LEAVES: A NEW SPECIES FROM EAST KALIMANTAN, INDONESIA
Authors: PRABOWO WISNU CAHYO , NARSA ANGGA CIPTA , ANDARISTA DZAKI BAYU , KUNCORO HADI , KUSUMA SRI AGUNG FITRI , SUSILAWATI YASMIWAR
Published: January 2023

Objective: The aim was to determine the botanical, GC-MS chemical characteristics and antibacterial activity of Strobilanthes. kalimantanensis as a new species.

Methods: Characterization of plants through microscopic and macroscopic analysis, isolation of essential oil (EO) by steam distillation, GC-MS analysis of essential oil content and antibacterial effectiveness tests.

Results: The results of the steam distillation process of essential oil produced yield 0.547%, clear and has fresh scent. GC-MS results from essential oils identified major phytochemicals, including anethole and estragole. Antibacterial activity of EO is 100 mg/ml against Staphylococcus aureus and 150 mg/ml against Bacillus subtilis, Escherichia coli, and Streptococcus epidermidis.

Conclusion: Plant with the first species reported as Strobilanthes kalimantanensis contains essential oils that have antibacterial activity.
ANTICANCER ACTIVITY OF SILVER NANOPARTICLE OF PRODIGIOSIN ON LUNG CANCER
Authors: KARNA SHILPA , R. KAVITHA , N. DAMODHARAN
Published: January 2023

Objective: Nanotechnology is a relatively new branch of science and technology that studies and controls the interactions of synthetic and biological materials. Researchers are becoming more interested in nanoparticles as a result of their vast medicinal potential, particularly against cancer. Methods: The Serratia marcescens culture supernatant containing Prodigiosin was used to synthesize silver nanoparticles in an environmentally benign biogenic manner. The effect of nanoparticles on the growth and proliferation of human lung cancer cell (A549) in vitro was investigated in this work. MTT Assay and DNA fragmentation assay were used to characterize the nanoparticles that had been produced. Results: Cytotoxicity of the Prodigiosin AgNPs was represented as IC50 value of 31.2µg/ml and the viability decrease in the number of nanoparticles-treated cells. DNA fragmentation assay showed the degradation of DNA. Conclusion: The present study conforms as the synthesized Prodigiosin AgNPs can be a promising anticancer agent regarding its mechanism of action.
FOCUS ON NIOSOMAL–BASED DRUG DELIVERY SYSTEMS FOR NASAL ROUTE: APPLICATIONS AND CHALLENGES
Authors: AL-ZUHAIRY SAEED A. S. , S. EL-SAWY HOSSAM`` , EL-NABARAWI MOHAMED A. , TEAIMA MAHMOUD H.
Published: January 2023

For decades, the nasal route of administration is principally used for many therapeutic applications owing to the non-invasive nature of the nasal pathway. Besides, it circumvents blood-brain-barrier (BBB) and hepatic first-pass effect. Consequently, the nasal route is much preferred over other invasive approaches like intravenous, intracerebral, and transcranial for the systemic delivery of drugs and the treatment of central nervous systems (CNS) disorders such as depression, Alzheimer’s disease (AD), multiple sclerosis, and Parkinson’s disease (PD) via the nose-to-brain pathway. Drug applied via the nasal route displays some difficulty to reach the brain, like the dose limitation of the nasal pathway, mucociliary clearance, etc. The efficiency of the nasal route depends on the application delivery system. Lipidic-based drug delivery systems (liposomes, solid lipid nanoparticles …etc.) have been confirmed for their promising impact on the nasal delivery approach. Furthermore, the sensitivity of the nasal route and the touched-complications of clinical trials in CNS disorders assigns the necessity of consideration to the clinical trials and approval process of the niosomal-based nasal drug delivery approach. This review describes different approaches to nasal delivery, lipidic-based delivery systems with a focus on niosomes as a promising nasal delivery system, along with different formulation methodologies, and applications.
INVESTIGATION OF ANTI-SARS COV-2 ACTIVITY OF SOME TETRAHYDRO CURCUMIN DERIVATIVES: AN IN SILICO STUDY
Authors: MURALIKRISHNAN AMRITA , KUBAVAT JASMIN , VASAVA MAHESH , JUPUDI SRIKANTH , BIJU NAMITHA
Published: January 2023

Objective: In the current study, an in silico approach has been utilized to investigate the anti-SARS CoV 2 activity of some derivatives of Tetrahydro curcumin (THC), a curcumin metabolite.
Methods: BioVia Draw 2017 was used to design 168 THC derivatives. All of the derivatives were docked using Maestro Schrodinger programme. Depending on the docking score, the ADME, drug-likeness, and toxicity prediction of a few THC derivatives were conducted.
Results: 168 THC derivatives were designed. 14 derivatives exhibited a better binding score than Remdesivir. All 14 derivatives' pharmacokinetic characteristics were discovered to be within the acceptable range. Lipinski's rule of five was violated by all derivatives, including the reference drug, yet they all stayed within the recommended range. The greatest docking score among the 14 derivatives was displayed by Structure 21. A study on molecular dynamic (MD) stimulation showed that the protein-ligand complex was relatively stable. Toxicity prediction showed that 14 derivatives were non-hepatotoxic, non-cytotoxic, immunotoxic (except S21), non-mutagenic (except S31) and half of the developed structures were carcinogenic, while the other half, including the standard drug, was non-carcinogenic.
Conclusion: Among 168 THC derivatives, 14 derivatives exhibited better binding score than the reference drug. For all 14 derivatives, pharmacokinetic, drug-likeness, and toxicity prediction were found to be satisfactory. It was discovered that the protein-ligand complex was thermodynamically stable. All 14 compounds present exciting prospects for further in vitro and in vivo investigation.
A MODEST UV SPECTROPHOTOMETRIC ASSISTED BY CHEMOMETRIC APPROACH FOR VERIFICATION OF ACETAMINOPHEN LEVEL IN VARIOUS MANUFACTURED TABLETS AND SYRUPS IN INDONESIAN PHARMACIES
Authors: MUNIR MUHAMMAD ABDURRAHMAN , INAYATULLAH AHLAM , IBRAHIM SOFIAN , RIMBA PUTRI IMRAM RADNE , EMELDA EMELDA , FATMAWATI ANNISA , NURHIDAYANTI NURHIDAYANTI
Published: January 2023

Objective: This study aimed to verify the paracetamol level in some fabricated tablets and syrups in Indonesian pharmacies.
Methods: The fabricated tablets and syrups were analyzed using a spectrophotometer UV that was assisted by the chemometric approach. Partial least squares (PLS) and principal component regression (PCR) were the chemometric methods employed to verify the paracetamol level in pharmaceutical products. There were 25 different samples (tablets and syrups) applied in this study. The validation study was employed in this study to verify the approach according to the ICH guidelines. The double-distilled water was applied as a solvent before the samples were analyzed using a spectrophotometer.
Results: This technique was efficient and require double-distilled water only as a solvent. The results of this study reveal that there was a deviation in absorbance of the samples with RSD ranging from (0.15-0.45). The technique was linear, ranging from 1.0–6.0 µg·ml-1, with an R2 (0.9991) obtained at 242 nm. The percentage recovery was applied to study the accuracy of the technique and was acquired at 99.18%. The results have shown that the approach was the potential to be applied in estimating the level of paracetamol in tablets and syrups.
Conclusion: The detection of paracetamol levels in tablets and syrups using UV spectrophotometric showed satisfactory outcomes. The application of the chemometric approach by using PLC and PCR as the statistical assessment indicated that there was no significant distinction among the validated methods. Furthermore, the method can be used by industries particularly small industries to secure medicines that comply with Indonesian rules.
MOLECULAR DYNAMICS SIMULATIONS OF THE STK630921 INTERACTIONS TO INTERLEUKIN-17A
Authors: RIANDONO FRANSISCUS DEDDY , ISTYASTONO ENADE PERDANA
Published: January 2023

Objective: This research aimed to investigate the stability of the STK630921-Interleukin 17A (IL-17A) complex and to predict important residues that interact during molecular dynamics simulations.
Methods: Molecular docking simulations were performed, followed by molecular dynamics (MD) simulations and the free energy of binding calculations using YASARA-Structure. The identification of interacting residues was done using PyPLIF HIPPOS. Molecular docking simulations were performed on the IL-17A binding pocket with the compound 4-[({N-[(4-Oxo-3,4-dihydro-1-phthalazinyl) acetyl] alanyl} amino) methyl] cyclohexane carboxylic acid or known as STK630921. The best-docked pose was selected for the 50 ns MD simulations production run. The MD simulations snapshots were then analyzed to see the stability of IL-17A and for the identification of interacting residues, followed by Molecular Mechanics/Poisson–Boltzmann and surface area (MM/PBSA) analysis for the free energy of binding calculations.
Results: STK630921 is relatively able to stabilize IL-17A. Important interaction residues identified during the MD simulations were: Thr35(A), Pro37(A), Tyr62(A), Pro63(A)(B), Ile66(A)(B), Trp67(A), Ile96(A)(B), Val98(A)(B) and Val117(A)(B).
Conclusion: STK630921 disrupts the interaction of IL-17A to its receptor by binding and stabilizing IL17A.
MECHANISM OF ACTION, SYNTHESIS, PROPERTIES AND ANALYTICAL METHODS OF CABOZANTINIB
Authors: DWIVEDI AKANKSHA , KHABIYA RAKHI , SHRIVASTAVA ALANKAR , TYAGI SIDDHARTH , NAGARAJAN KANDASAMY , DARWHEKAR G. N.
Published: January 2023

Globally, the burden of cancer is substantial and growing. The impact of the burden of such diseases over society is unpredictable in terms of health lost and cost. Unfortunately, the estimates shown the burden may be increasing in the upcoming decades. Cabozantinib (CBZ) is a newly developed tyrosin kinase inhibitor (TKI) for Differentiated thyroid cancer (DTC), Hepatic Cellular Carcinoma (HCC), Medullary thyroid cancer (MTC) and Renal Cell Carcinoma (RCC). The objective of the presented review is to provide updated knowledge of drugs especially covering analytical methodologies. The review covered the introduction, mechanism of action, pharmacokinetics, synthesis and developed analytical methods by various researchers. The review covered one spectrophotometry and about twenty chromatography methods. The review will be helpful for the scientist working in this area and especially helpful for analytical scientists exploring new analytical methodologies for CBZ.
DESIGN AND OPTIMIZATION OF FLUCONAZOLE-LOADED PHARMACOSOME GEL FOR ENHANCING TRANSDERMAL PERMEATION AND TREATING FUNGAL INFECTIONS THROUGH BOX-BEHNKEN DESIGN
Authors: NAVEENTAJ S. , MUZIB Y. INDIRA , RADHA R.
Published: January 2023

Objective: The objective of the selected study was to develop and statistically optimize fluconazole (drug) loaded pharmacosomes (carrier) to enhance transdermal permeation by incorporating into gel base and to treat fungal infections by selecting the Box-Behnken model.
Methods: Fluconazole is an antifungal drug which belongs to BCS class-II with high permeability and choice for topical drug delivery. In the study, the levels of the lecithin (lipid), dichloromethane and DMSO are selected as independent variables were varied to study the influence on particle size, % entrapment efficiency and in vitro drug release as dependent variables. Factorial designs through software Design expert version 13 (Box-Behnken design) is applied for this study and the optimization process was carried out using the desirability plots and point prediction techniques.
Results: Results of the study with the application of a design expert shows that the optimized drug-loaded pharmacosomes with vesicle size of 158.87±0.56 nm as predicted and zeta potential of-30.6mV indicating good stability of the formulation, entrapment efficiency of 90.6±1.12% and in vitro drug release of 97.59±1.84% respectively. The optimized formulation loaded into gel base and compared with the marketed gel formulation. All the evaluation parameters confirmed that the physical mixture of drug and excipients was compatible without any interactions.
Conclusion: Through obtained results, it’s concluded that; the independent variable plays a crucial role in optimizing formulation. Study data provided strong evidence that the optimized vesicular formulation through Box-Behnken factorial design can be potentially useful as a drug carrier for loading drug of selected category for enhancing transdermal delivery.
DEVELOPMENT AND CHARACTERIZATION OF PLANT OIL-BASED POTENT ANTICHOLINESTERASE MICROEMULSION CONTAINING WITHANIA SOMNIFERA EXTRACT WITH ENHANCED TRANSDERMAL DELIVERY OF PHYTOCONSTITUENTS FOR THE TREATMENT OF COGNITIVE DISORDERS
Authors: PRIYA SNEH , JYOTHI DIVYA , LOBO CYNTHIA LIZZIE
Published: January 2023

Objective: This work was carried out to develop Cymbopogan Citratus (lemon grass)oil based microemulsion formulation loaded with the extract of Withania somnifera which possess enhanced transdermal delivery of phytoconstituents with anticholinesterase activity useful in treating Alzheimer’s disease.
Methods: Methanolic extract of Withania somnifera roots were prepared and it was investigated for the inhibition of acetylcholinesterase (AChE) activity by Ellman’s assay. Based on the acetylcholinesterase activity, the specific amount of extract was loaded on to the microemulsion formulation. The Cymbopogan Citratus oil, tween 20, ethanol was used as oil phase, surfactant, and cosurfactant, respectively, for the preparation of microemulsion. Pseudo ternary phase diagram was constructed using a water titration method. The microemulsion formulations were characterized for droplet size, PDI, zeta potential and drug content. The optimized formulation was subjected to in vitro drug release and permeation studies and compared with the extract.
Results: IC50 value of ashwagandha extract for anticholinesterase activity was found to be 68.73 µg/ml. The optimized microemulsion formulation had droplet size of 199.9±0.3 nm with PDI 0.029±0.2, zeta potential of-19.49±0.7mv and drug content was found to be 97.5±1.3%. The optimized microemulsion formulation showed 85±1.02% release of withaferin A after 24 h of in vitro drug release study. The prepared microemulsion loaded with ashwagandha extract showed excellent permeation of withaferin A(1.4µg/cm2/min) than the flux obtained from extract solution (0.7µg/cm2/min).
Conclusion: Optimised microemulsion formulation is suitable for transdermal delivery of anticholinesterase phytoconstituents from ashwagandha extract hence useful in the treatment of Alzheimer’s disease
IN SILICO EVALUATION OF BINDING INTERACTION AND ADME PROPERTIES OF NOVEL 5-(THIOPHEN-2-YL)-1,3,4-OXADIAZOLE-2-AMINE DERIVATIVES AS ANTI-PROLIFERATIVE AGENTS
Authors: ALI YOUSEF SABAH , MAHDI MONTHER FAISAL , RAZIK BASMA M. ABD
Published: January 2023

Objective: The objective of this research was the virtual design of nine novel 1,3,4-oxadiazole derivatives and evaluating their antiproliferative activity as potential cyclin-dependent kinase 2 (CDK-2) inhibitors, which is a major component in cell cycle and proliferation.
Methods: CDK-2 structure, PDB ID, 2R3J, co-crystallized with ligand SCJ from protein data bank was chosen to be docked with a series of nine 5-(thiophen-2-yl)-1,3,4-oxadiazol-2-amine derivatives to evaluate their abilities as potential anti-proliferative agents using Glide software (Maestro 11.4) one of Schrodinger software (Schrodinger, 2018). In addition, the pharmacokinetic properties of these derivatives were evaluated using the Swiss-ADME web tool.
Results: Molecular modeling proposed that these 1,3,4-oxadiazole derivatives have powerful binding interaction with the active binding site of CDK-2 protein. In this article, two molecules have been observed as the most effective as they have docking scores of (-10.654 and-10.169 kcal/mol) respectively, whereas the binding score of the reference ligand was (-9.919 Kcal/mol) and most of the derivatives have fulfilled the Swiss-ADME parameters as potential orally active compounds.
Conclusion: Novel 1,3,4-oxadiazole derivatives had shown promising results to be considered as lead compounds for developing new anti-proliferative agents as two compounds (P-1 and P-5) exhibit better docking score at 2R3J active site than the reference ligand with further biological and pharmacological evaluation required.
A MINI REVIEW ON PROPERTIES, MECHANISM OF ACTION, PHARMACOKINETIC AND PHARMACODYNAMICS AND ANALYTICAL METHODS OF CARIPRAZINE
Authors: SHRIVASTAVA ALANKAR , AGGARWAL RADHIKA , SINGH RISHI PRATAP , KHABIYA RAKHI
Published: January 2023

Cariprazine (CPZ) being a “D2/D3 receptor partial agonist” is used for schizophrenia treatment. CPZ illustrate different functional study at “dopamine receptors depending on the assay system”. This study elaborate review summarizes the structure–activity relationship (SAR), Mechanism of action (MOA), pharmacokinetics, pharmacodynamics and analytical methods published. CPZ was found to be more effective than risperidone. It was analogus with a remarkably longer time to deteriorate than inactive drug in a long-term, phase III,-deteriorate prevention study. This study elaborate the activating and solemn or sedative properties of first-line oral second generation antipsychotics by explore the rates of adverse effect in product labelling for the indications of schizophrenia and ancillary treatment of major depressive disorder (MDD). The common adverse events reported were extrapyramidal disorder, insomnia, dizziness, solemn, anxiety, vomiting and constipation in “fixed dose study of tested 1.5, 3.0, and 4.5 mg/day”. The presented review explains about biological properties, pharmacokinetics, pharmacodynamics, and analytical methods of CPZ.
ENHANCED AQUEOUS SOLUBILITY AND IN VITRO DISSOLUTION OF THE ANTI-HYPERLIPIDEMIC AGENT USING SYNTHESIZED SOLID DISPERSION CARRIER
Authors: TELANGE DARSHAN R. , AGRAWAL SURENDRA S. , PETHE ANIL M. , HADKE ANKITA V.
Published: January 2023

Objective: To improve ATN's solubility, permeability, and dissolution rate of pentaerythritol-eudragit®RS100 co-processed excipients (CE) and their potential as a solid dispersion carrier (ATN-CE-SD).
Methods: The ATN-CE-SD was prepared using the solvent evaporation technique. The pure ATN, physical mixture, CE carrier, and optimized ATN-CE-SD was physicochemically characterized using Scanning electron microscopy, Fourier transforms infrared spectroscopy, differential scanning calorimetry, powder x-ray diffractometry, solubility, and in vitro dissolution was used to evaluate solid dispersions.
Results: Physical and chemical analysis showed that ATN-CE-SD formed via the involvement of weak intermolecular forces of attraction between CE carrier and ATN. The prepared solid dispersion showed the drug content around ~ 96.94 % w/w, indicating that the solvent evaporation method improved the encapsulation of ATN and, thus, enhanced its drug content. Compared to pure ATN (~ 0.11 mg/ml), ATN-CE-SD (1:2) significantly increased the aqueous solubility by around ~ 25-fold (~ 2.78 mg/ml), indicating solid dispersion improves the solubility of ATN. ATN-CE-SD enhanced the rate of dissolution of ATV (~ 65 %) compared to pure ATN (~ 25 %) and PM (~ 34 %). Likewise, ATN-CE-SD (1:2) improved the rate and extent of ATN (~ 60 %) across the biological membrane compared to pure ATN (~ 22 %) and PM (~ 32 %). The ATN-CE-SD (1:2) improved the dissolution efficiency by around ~ (57.31%) compared to pure ATN (~ 7.02%) and PM (~ 20.43%). According to the study, co-processed excipients could serve as a promising solid dispersion carrier and improve ATN's water solubility, permeability, and dissolution rate.
Conclusion: Based on the results, it is possible to use synthetic solid dispersion carriers as alternatives to improve the low water solubility and permeability of ATN.
OPTIMIZATION AND PHYSICAL CHARACTERIZATION OF QUERCETIN NANOEMULGEL FORMULA AS AN ANTIBACTERIAL AGENT
Authors: DWIASTUTI RINI , BAHAR GUMILAR KATARINA NORALITA , YULIANI HARTATI
Published: January 2023

Objective: This research aims to optimize the quercetin nanoemulgel formula to improve quercetin solubility as an antibacterial agent.
Methods: In this research, quercetin was formulated into nanoemulgel with the factorial design of three independent variables, the concentration of oil phase (virgin coconut oil), surfactant (Tween 80), and co-surfactant (Span 80). The nanoemulgel physical properties (viscosity, spreadability, transmittance value, zeta potential, and particle size) were tested. The data were evaluated using Minitab®18 software; if the p-value<0.05, it is stated that there is a statistically significant difference in the formula, and the use of the response optimizer menu in the Minitab® 18 software determines the optimum formula with multiple responses.
Results: The results showed that the concentration of quercetin used to inhibit the growth of Staphylococcus aureus was 2 mg/ml. The size of the particles had a mean of 62.487 nm, the polydispersity index had a mean of 0.365, and the percent transmittance had a mean of 95.533±0.113%. Measurements of the zeta potential had a mean of -26.712±0.154, with the viscosity and spreadability of the preparations made having a mean of 2495±0.250 cps and 4.795±0.028 cm.
Conclusion: This study reported that the VCO amount of 3g, the tween amount of 12g and the span amount of 3.5g were found to be computational recommendations to achieve the optimum conditions only for percent transmittance value response.
ANALYTICAL METHOD VALIDATION AND BIOEQUIVALENCE STUDY OF ERLOTINIB 150 MG TABLETS IN IRANIAN HEALTHY VOLUNTEERS UNDER FASTING CONDITION
Authors: ELHAM GHASEMIAN , SIMA SADRAI , JAVAD SHOKRI , A. ILKA
Published: January 2023

Objective: This study aims to compare a generic formulation of the drug erlotinib 150 mg tablet to the brand-name version to validate the analytical method and bioequivalence studies.
Methods: Erlotinib hydrochloride tablets (test versus reference formulation) were compared in a randomized, two-period crossover study to determine their pharmacokinetic properties and bioequivalence in healthy Iranian volunteers. 14 d passed between each treatment during the washout period. Liquid chromatography-tandem mass spectrometry (LC-MS/MS) was used to analyze erlotinib, and the method validation is presented.
Results: Over the range of 6.25-3200 ng/ml, the analytical method was verified as linear (R2= 0.998). The technique was also accurate and precise at various concentrations. The results showed that the pharmacokinetics of the two products were comparable. Following administration of the test and reference products, the geometric averages for (Area under the curve) AUC0-72, AUCinf, and maximum plasma concentration (Cmax) were 104.71 (90% CI, 93.39-117.40), 104.68 (90% CI, 93.47-117.23), and 104.85 (90% CI, 94.61-116.21), respectively. The outcomes fell within the permitted tolerance of 0.8 to 1.25.
Conclusion: For the determination of erlotinib in plasma, the used analytical approach is accurate, precise, repeatable, and selective. Additionally, the bioequivalence research revealed no appreciable differences in pharmacokinetic characteristics between the reference and test products. Therefore, it is possible to assert that the generic erlotinib product and the reference product are bioequivalent.
BOMBAX CEIBA LINN: A CRITICAL REVIEW ON PHYTOCHEMISTRY, TRADITIONAL USES, PHARMACOLOGY, AND TOXICITY FROM PHYTOPHARMACEUTICAL PERSPECTIVE
Authors: GUPTA NIRAJ , SHARMA DEVENDER , RANI REKHA
Published: January 2023

Traditional medicines are becoming crucial and decisive role in the prevention and cure of diseases and disorders. Traditional medicines have various pharmacological activities which important for human health. Bombax Ceiba widely used from past decades for the treatment of diseases and disorders. Bombax ceiba is usually referred to as kapok tree and moca, which belongs to Bombacaceae. Moca is a crucial medicative, plant widely found in a tropical and subtropical Asian country like India, Pakistan. Various scientific studies or medicative usage has been reported within the traditional systems of drugs like Ayurveda, Siddha and Unani. Owing to this widespread attention about traditional medicines, scientific validations of medicinal plants have become a thrust area of research. In this paper, the scientific validation of Bombax ceiba for various biological activities has been reviewed with its chemical constituents present in the whole plant and with its traditional and contemporary uses. This manuscript also provides deep inside of recent patents associated with Bombax ceiba in the past decade.