Vilma Petrikaite

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• Doctor of Pharmacy
• Head of Department at Lithuanian University of Health Sciences

1-Substituted 5-oxopyrrolidine-3-carboxylic acid and its derivatives play an important role as components of many biologically active molecules. This study describes the synthesis of 1-(2,4-difluorophenyl)-5-oxopyrrolidine-3-carboxylic acid derivatives and their anticancer properties. The target compounds were prepared using 2,4-difluoroniline as a...

This study explores the anticancer potential of Cirsium vulgare dry extracts in human colorectal adenocarcinoma (HT-29) and gastric carcinoma (KATO III) cell lines using both traditional 2D monolayer models and advanced 3D spheroid systems. Cell viability was assessed via the MTT assay, while the influence on cell migration was evaluated using a wo...

A series of novel hydrazones bearing diphenylamine and 5-oxopyrrolidine moieties, along with benzene and naphthalene rings substituted with hydroxy, alkoxy, or carboxylic groups, were synthesized. Their anticancer activity was evaluated in vitro using both 2D (MTT and ‘wound healing’ assays) and 3D (cell spheroid) models against human melanoma IGR3...

This study aimed to develop water-in-oil-in-water (W1/O/W2) double emulsion gels (DEGs) with Lactiplantibacillus plantarum subsp. plantarum and Limosilactobacillus reuteri encapsulated within the inner aqueous phase (W1), with a focus on improving probiotic viability under adverse environmental conditions. The system incorporated gelling agents to...

This study investigated the anti-cancer effects of the chemically characterized Tilia species (linden) on MIA PaCa-2 cells by analyzing various cancer-triggering mechanisms, including oxidative stress and inflammation status. Extracts from the flowers, bracts, and inflorescences of T. cordata, T. platyphyllos, T. rubra, and T. tomentosa were evalua...

In this study, we have synthesized novel 4-acetophenone moiety-bearing functionalized imidazole derivatives containing S-, and N-ethyl substituents and evaluated their anticancer activity. Their anticancer activity was studied against human breast carcinoma (MDA-MB-231), human prostate carcinoma (PPC-1), and human glioblastoma (U-87). Compounds 4,...

Rab11 and Rab35 were shown to be responsible for wide-scale intracellular membrane trafficking during the last phases of the cell cycle. Even though data suggests that Rab11 and Rab35 are abscission-related, each gives a different phenotype to dividing cells. Moreover, nobody has ever looked at both and systematically compared the two during the re...

Regenerated fibrous cellulose possesses a unique set of properties, including biocompatibility, biodegradability, and high surface area potential, but its applications in the biomedical sector have not been sufficiently explored. In this study, nanofibrous cellulose matrices were fabricated via a wet‐electrospinning process using a binary system of...

Cytokinetic abscission is a crucial process that guides the separation of daughter cells at the end of each cell division. This process involves the cleavage of the intercellular bridge, which connects the newly formed daughter cells. Over the years, researchers have identified several cellular contributors and intracellular processes that influenc...

Our study focuses on the gelling properties of pea protein (PP), which are comparatively weaker than those of other plant proteins, thereby limiting its application. However, we found that the addition of κ‐carrageenan (κ‐CAR) significantly (P < 0.05) increased PP gels' hardness and water‐holding capacity irrespective of gel formation temperature (...

Triple-negative breast cancer (TNBC) treatment is challenging due to its aggressive nature and heteroge-neity of this type of cancer, characterized by various subtypes and intratumoral diversity. Doxorubicin (DOX) plays a crucial role in TNBC chemotherapy reducing the tumor size and improving patient survival. However, decreased drug uptake and inc...

The phytochemical diversity and potential health benefits of V. oxycoccos and V. macrocarpon fruits call for further scientific inquiry. Our study aimed to determine the phytochemical composition of extracts from these fruits and assess their antioxidant, antibacterial, and anticancer properties in vitro. It was found that the ethanolic extracts of...

A series of hydrazones, azoles, and azines bearing a 4-dimethylaminophenyl-5-oxopyrrolidine scaffold was synthesized. Their cytotoxic effect against human pancreatic carcinoma Panc-1 and triple-negative breast cancer MDA-MB-231 cell lines was established by MTT assay. Pyrrolidinone derivatives 3c and 3d, with incorporated 5-chloro and 5-methylbenzi...

The title compounds were synthesized by the reaction of 5-oxo-1-(4-(phenylamino)phenyl)pyrrolidine-3-carbohydrazide with various aldehydes bearing aromatic and heterocyclic moieties and acetophenones, and their cytotoxicity was tested via MTT assay against human triple-negative breast cancer MDA-MB-231, human melanoma IGR39, human pancreatic carcin...

Aqueous solubility of pharmaceutical substances plays an important role in small molecule drug discovery and development, with ionizable groups often employed to enhance solubility. Drug candidate compounds often contain ionizable groups to increase their solubility. Recognizing that the electro-statically charged form of the compound is much more...

Background: Autologous fat grafting is widely used in plastic and reconstructive surgery. Liposuction methods play a key role in surgeons’ work efficiency, adipocyte viability, graft survival, and outcomes. We investigated the effect of four liposuction methods on adipocyte viability, debris, and surgeons’ work efficiency by measuring the active e...

Breast cancer is a rapidly evolving, multifactorial disease that accumulates numerous genetic and epigenetic alterations. These result in molecular and phenotypic heterogeneity within the tumor, the complexity of which is further amplified through specific interactions between cancer cells. We aimed to analyze cell phenotypic sublines and the influ...

This study aimed to evaluate the anticancer activity of 16 new sunitinib derivatives in brain cancer cells (2D model) and spheroids (3D model). The effect on cell viability was determined by the MTT assay. Single-cell migration assay was performed to examine the effect of selected compounds on individual cell migration. The activity of compounds in...

A series of new derivatives based on sulfamethoxazole were designed and synthesized in this study. The structures of the new compounds were confirmed based on a comprehensive characterization of spectral data by applied IR and ¹H as well as ¹³C NMR spectroscopy. The prepared compounds were tested for their anticancer and antimicrobial properties. H...

Pancreatic cancer remains one of the deadliest cancer types. It is usually characterized by high resistance to chemotherapy. However, cancer-targeted drugs, such as sunitinib, recently have shown beneficial effects in pancreatic in vitro and in vivo models. Therefore, we chose to study a series of sunitinib derivatives developed by us, that were pr...

Multidrug resistance (MDR) is currently a big challenge in cancer therapy and limits its success in several patients. Tumors use the MDR mechanisms to colonize the host and reduce the efficacy of chemotherapeutics that are injected as single agents or combinations. MDR mechanisms are responsible for inactivation of drugs and formbiological barriers...

Fruit and leaf cuticular waxes are valuable source materials for the isolation of triterpenoids that can be applied as natural antioxidants and anticancer agents. The present study aimed at the semi-preparative fractionation of triterpenoids from cuticular wax extracts of Vaccinium vitis-idaea L. (lingonberry) leaves and fruits and the evaluation o...

Cancer cells’ resistance to anticancer drugs represents a major clinical problem and the most important failure of treatment. Combination chemotherapy is more effective than monotherapy due to additive or synergistic effects. The aim of our research was to assess the effects of the combinations of apple extract’s triterpenic compounds, individual t...

The compositions and health-beneficial properties of lingonberry leaves (Vaccinium vitis-idaea L.) are well established; however, their proanthocyanidins are still heavily underutilized. Optimizing their delivery systems is key to enabling their wider applications. The present study investigates the phytochemical and ‘wound-healing’ properties of p...

4-Phenyl-3-[2-(phenylamino)ethyl]-1H-1,2,4-triazole-5(4H)-thione was used as a starting compound for the synthesis of the corresponding 1,2,4-triazol-3-ylthioacetohydrazide, which reacts with isatins and various aldehydes bearing aromatic and heterocyclic moieties provided target hydrazones. Their cytotoxicity was tested by the MTT assay against hu...

One of the most challenging goals of tissue engineering is the search for efficient but simple production methods of 3D cell culture scaffolds. We fabricated novel microfibrous PCL scaffolds using a commercial 3D printer modified with a melt electrospun process. The microfibrous PCL scaffolds featured fibres with width ranging between 10 to 190 µm...

The aim of the research was to evaluate the influence of two P-glycoprotein (P-gp) inhibitors silymarin and quercetin on anticancer drug doxorubicin (DOX) and pegylated liposomal doxorubicin (PLD) delivery into breast cancer cells (2D cultures) and cancer cell spheroids (3D cultures) at different pH. The cytotoxicity of the compounds was assessed u...

Background Klebsiella quasipneumoniae is an opportunistic pathogen causing antibiotic-resistant infections of the gastrointestinal tract in many clinical cases. Orally delivered bioactive Klebsiella-specific antimicrobial proteins, klebicins, could be a promising method to eradicate Klebsiella species infecting the gut. Methods Mouse infection mod...

Beta adrenoblockers are a large class of drugs used to treat cardiovascular diseases, migraines, glaucoma and hyperthyroidism. Over the last couple of decades, the anticancer effects of these compounds have been extensively studied. However, the exact mechanism is still not known, and more detailed studies are required. The aim of our study was to...

The application of the Quality by Design (QbD) concept to extracts obtained from Crocus sativus perianth with potential anticancer activity will ensure the safety, efficiency, and quality control of the entire technological process, as well as determine the critical factors affecting the quality of extracts. Potentially critical points of the produ...

Ethnopharmacological relevance Vaccinium vitis-idaea L. (lingonberry) leaves and fruits have traditionally been used in Asian and European countries as a natural solution for urinary tract infections, gastrointestinal distress, neurodegenerative diseases, and related inflammatory disorders, which are overall associated with free radical damage and...

Three-dimensional (3D) cell culture models have been proposed as alternatives for initial drug screening to increase drug development efficiency. In addition to their ability to reproduce key aspects of the tumor architecture and microenvironment, 3D cell culture models may help decrease the use of laboratory animals in drug testing, in accordance...

Crocus sativus L. (saffron) has been traditionally used as a food coloring or flavoring agent, but recent research has shown its potent pharmacological activity to tackle several health-related conditions. Crocus sp. leaves, and petals are the by-products of saffron production and are not usually used in the medicine or food industries. The present...

The current diagnostic and therapeutic strategies for endometriosis are limited. Although endometriosis is a benign condition, some of its traits, such as increased cell invasion, migration, tissue inflammation, and angiogenesis are similar to cancer. Here we explored the application of homing peptides for precision delivery of diagnostic and thera...

Heterocyclic compounds are one of the main groups of organic compounds possessing wide range of applications in various areas of science and their derivatives are present in many bioactive structures. They display a wide variety of biological activities. Recently, more and more attention has been focused to such heterocyclic compounds as azoles. In...

Background Klebsiella quasipneumoniae is an opportunistic pathogen causing antibiotic-resistant infections of the gastrointestinal tract in many clinical cases. Orally delivered bioactive Klebsiella-specific antimicrobial proteins, klebicins, could be a promising method to eradicate Klebsiella species infecting the gut. Methods Mouse infection mod...

Background: Klebsiella quasipneumoniae is an opportunistic pathogen causing antibiotic-resistant infections of the gastrointestinal tract in many clinical cases. Orally delivered bioactive Klebsiella-specific antimicrobial proteins, klebicins, could be a promising method to eradicate Klebsiella species infecting the gut. Methods: Mouse infection mo...

Protein Carbonic Anhydrase IX (CA IX), which is expressed in various hypoxic solid tumors in order to maintain proper pH, is also related to cancer cell adhesion, invasion, and metastasis processes. Here, we investigated whether CA IX inhibition by a highly CA IX selective agent benzenesulfonamide VD11-4-2 triggers changes in individual cell motili...

Actin is the most abundant protein in almost all the eukaryotic cells. Actin amino acid sequences are highly conserved and have not changed a lot during the progress of evolution, varying by no more than 20% in the completely different species, such as humans and algae. The network of actin filaments plays a crucial role in regulating cells' cytosk...

Despite cancer nanomedicine celebrates already thirty years since its introduction, together with the achievements and progress in cancer treatment area, it still undergoes serious disadvantages that must be addressed. Since the first observation that macromolecules tend to accumulate in tumor tissue due to fenestrated endothelial of vasculature, c...

Synthesis of β-amino acid derivatives containing hydrazone and azole moieties is described. For this purpose, the appropriate hydrazide was treated with aromatic aldehydes, ketones and phenyl iso(thio)cyanates to obtain the desired outcome. The synthesized target compounds were evaluated for their anticancer properties. The assay displayed 3,3'-((2...

A series of novel mono and bishydrazones each bearing a 2-oxindole moiety along with substituted phenylaminopropanamide, pyrrolidin-2-one, benzimidazole, diphenylmethane, or diphenylamine fragments were synthesized, and their anticancer activities were tested by MTT assay against human melanoma A375 and colon adenocarcinoma HT-29 cell lines. In gen...

Background Saffron or stigmas of Crocus sativus L. is one of the most valuable food products with interesting health-promoting properties. C. sativus has been widely used as a coloring and flavoring agent. Stigmas secondary metabolites showed potent cytotoxic effects in previous reports. Methods The present study investigated the chemical composit...

In modern society, cancer is one of the most relevant medical problems. It is important to search for promising plant raw materials whose extracts have strong antioxidant and anticancer effects. The aim of this study was to determine the composition of phenolic compounds in plant extracts, to evaluate their antioxidant and anticancer activity, and...

Cancer initiation and development are closely related to oxidative stress and chronic inflammation. The aim of this study was to evaluate apple extracts and individual tritepenes antioxidant, anti-inflammatory, and cytotoxic activities. Dry extracts of apple were analyzed by HPLC-PDA. A hyaluronidase inhibition assay was selected to determine the a...

The broad studies of cancer have led researchers to the creditable understanding of biological and environmental factors that make benign cells to become malignant, as well as the developmental aspects of the tumour cells, known as the "hallmarks of cancer". However, additional research is needed to uncover the features of cancer biology, which wou...

The anticancer activity of compounds and nanoparticles is most often determined in the cell monolayer. However, three-dimensional (3D) systems, such as tumor spheroids, are more representing the natural tumor microenvironment. They have been shown to have higher invasiveness and resistance to cytotoxic agents and radiotherapy compared to cells grow...

Introduction Statins are a type of drugs that are used to lower cholesterol level in blood. Since the early 1990s, it has been known that statins could be beneficial in cancer therapy. However, data remain controversial, especially regarding estrogen receptors status. Despite many studies in breast cancer models in vitro, the correlations of effect...

Lingonberry leaves and fruits are associated with a range of potential bioactivities related to their phenolic content and composition, but the identification of major biological activity markers remains limited. The present study aimed at the isolation of lingonberry phenolic fractions and biological activity evaluation of them. Crude dry extracts...

Monoclonal and recombinant antibodies are widely used for the diagnostics and therapy of cancer. They are generated to interact with cell surface proteins which are usually involved in the development and progression of cancer. Carbonic anhydrase XII (CA XII) contributes to the survival of tumors under hypoxic conditions thus is considered a candid...

The major groups of antioxidant compounds (isoflavonoids, xanthones, hydroxycinnamic acids) in the rhizome methanol extracts of four Ukrainian Iris sp. (Iris pallida, Iris hungarica, Iris sibirica, and Iris variegata) were qualitatively and quantitatively analyzed using HPLC-DAD and UPLC-MS/MS. Gallic acid, caffeic acid, mangiferin, tectoridin, iri...

Abstract The aim of our study was to evaluate the influence of low-intensity pulsed US on the delivery of doxorubicin (DOX) into MDA-MB-231 triple-negative breast cancer and A549 non-small cell lung cancer cell 2D and 3D cultures. US with pulse repetition frequency of 10 Hz and 1 MHz center frequency was generated with peak negative pressure of 0.5...

The main function of carbonic anhydrases (CAs) in cancer cells is the pH regulation through a conversion of H2 O and CO2 to H+ and HCO3- . However, the data of in vitro and in vivo studies have demonstrated that transmembrane isoforms of CA IX and CA XII are involved in various steps of cancer cell migration, invasion and metastasis. According to l...

Series of novel 3-[(4-methoxyphenyl)amino]propanehydrazide derivatives bearing semicarbazide, thiosemicarbazide, thiadiazole, triazolone, triazolethione, thiophenyltriazole, furan, thiophene, naphthalene, pyrrole, isoindoline-1,3-dione, oxindole, etc. moieties were synthesized and their molecular structures were confirmed by IR, ¹H-, ¹³C-NMR spectr...

The aim of our study was to assess the influence of two carbonic anhydrase (CA) inhibitors (methazolamide (MTZ)) and U-104 on weakly basic anticancer drug doxorubicin (DOX) and pegylated liposomal doxorubicin (PLD) delivery into monolayer-cultured 4T1 murine breast cancer cells (2D cultures) and tumor spheroids (3D cultures) at pH 6.0 and 7.4. The...

The research of how cells sense and adapt the oxygen deficiency has been recognized as worth winning a Nobel Prize in 2019. Understanding hypoxia-driven molecular machinery paved a path for novel strategies in fighting hypoxia-related diseases including cancer. The oxygen depletion inside the tumor provokes HIF-1 dependent gene and proteins express...

Nanomedicine employs nanotechnologies to develop innovative applications, and more specifically nano-objects in the field of human health, through exploitation of the physical, chemical and biological properties of materials at the nanoscale. The use of nanovehicles capable of transporting and releasing the active therapeutic payload into target ce...

Carbonic anhydrase (CA) is a transmembrane enzyme that catalyses the reversible hydration of carbon dioxide to bicarbonate, thus increasing extracellular acidity. CA IX and CA XII are highly overexpressed in tumors. Increased extracellular acidity of tumor causes basic drugs ionization, thus decreasing their penetration into cells and therapeutic e...

Carbonic anhydrase (CA) is a transmembrane enzyme that catalyzes the hydration of carbon dioxide to bicarbonate, thus increasing extracellular acidity. The inhibition of CA IX and XII reduces extracellular acidity, thus preventing weakly basic drugs from ionization and enhancing their delivery into tumor.

Purpose The purpose of our study was to evaluate the influence of two PPIs (omeprazole (OME) and lansoprazole (LANSO)) on weakly basic anticancer drug doxorubicin (DOX) and pegylated liposomal doxorubicin (PLD) delivery to monolayer-cultured 4T1 murine breast cancer cells and tumor spheroids. Methods The effect of PPIs on cell viability was evalua...

Increased extracellular acidity in tumors is one of the factors impairing drug transport into cancer cells. Proton pump inhibitors (PPIs) are a group of medicines used to reduce gastric acid production. According to recent studies, they can reduce extracellular acidity, thus preventing basic drugs from ionization and increasing their delivery to ca...

Heat shock protein 90 (Hsp90) is a widely investigated target for anticancer therapy. The experimental Hsp90 inhibitors ICPD47 and ICPD62 demonstrated anticancer activity against colorectal, osteosarcoma and cervical cancer cell lines. However, their anticancer activity has not been investigated against pancreatic cancer cell lines yet, and there a...

Breast cancer is the most common cancer and the second leading cause of cancer-related death in women worldwide. Despite the early detection of breast cancer and increasing knowledge of its biology and chemo-resistance, metastatic breast cancer is largely incurable disease. We provide a review of the intertumor and intratumor heterogeneity, explai...

Nanotherapeutics gained much of interest of researchers, especially in medicine during last several decades. Nanosystems (nanoparticles, nanoconjugates, nanodevices etc.) are being extensively designed and tested in order to combat wide range of problems, such as cancer, infectious diseases, diabetes, cardiovascular and neurodegenerative disorders....

Background In order to improve the efficacy of chemotherapy an increasing attention is given to the drug transport to tumors. Sonoporation is the application of ultrasound (US) to increase cell membrane permeability. It is thought that US induces expansion, contraction, and explosion of microbubbles (MB) thus creating pores in the cell membrane, en...

In order to improve the efficacy of chemotherapy an increasing attention is given to the drug transport to tumors. Sonoporation is the application of ultrasound (US) to increase cell membrane permeability. It is thought that US induces expansion, contraction, and explosion of microbubbles (MB) thus creating pores in the cell membrane, enhancing dru...

Monoclonal antibodies (MAbs) selectively targeting tumor-associated antigens such as carbonic anhydrase IX (CA IX) can significantly contribute to research, diagnostics, and treatment of CA IX-related cancers. CA IX is overexpressed in numerous hypoxic cancers where it promotes tumor progression. Therefore, it is considered as a promising tumor bio...

Beta adrenoblockers is a large class of drugs mainly used to manage abnormal heart rhythms. Over the last couples of decades, the anticancer effects of these compounds has been extensively studied. There is much evidence about their activity in non-small cell lung, pancreatic, breast, colorectal, prostate and ovarian cancer. However, the mechanism...

Poor drug transport to tumor is one of the major factors limiting the efficacy of chemotherapy. Many techniques, such as tumor pH modulation by proton pump inhibitors (PPIs), can be used to improve drug delivery into cancer cells. PPIs are a group of drugs that are used to reduce gastric acid production. According to recent studies they can reduce...

Triple negative breast cancer (TNBC) is one of the most aggressive and highly heterogeneous tumors with morphologically distinct subtypes. This type of tumor is highly resistant to chemotherapy and it is related to the phenotypic heterogeneity of tumor cell populations. Scientists found that in genetically homogeneous cell populations, the phenotyp...

Triple negative breast cancer (TNBC) includes a heterogeneous subgroup of tumors accounting for approximately 15-20% of all breast cancers. TNBC presents a more aggressive natural history and worse disease-specific outcomes than other breast cancer subtypes. Cellular heterogeneity is observed in TNBC and represents a major hurdle for effective ther...

Carbonic anhydrase IX (CA IX) is a highly overexpressed membrane protein in numerous cancers and is well-recognized hypoxia marker with a promising diagnostic and therapeutic value. CA IX regulates pH in hypoxic tumor cells and contributes to microenviromental acidosis, cell adhesion, migration and invasion. To get better insight of CA IX role in t...

In order to improve the efficacy of chemotherapy an increasing attention is given to the drug transport to tumors. Various methods, such as tumor pH modulation by proton pump inhibitors (PPIs), can be used to improve drug delivery in cancer cell cultures. PPIs are a group of drugs that are used to reduce gastric acid production. Recent studies show...

Triple negative breast cancer (TNBC) is considered as the most aggressive form of breast cancer. In most cases, this type of tumor is highly resistant to chemotherapy. The resistance of TNBC to chemotherapeutic agents is related to the phenotypic heterogeneity of tumor cell populations due to different cell localization in the tumor, their interact...

Increased extracellular acidity of tumor causes basic drugs, such as doxorubicin (DOX) ionization. Positive charge reduces drug ability to permeate cellular membrane and reach the target site, thus limiting drug efficacy. Proton pump inhibitors (PPIs), such as omeprazole and lansoprazole, are a group of drugs that are used to reduce gastric acid pr...