Colorectal cancer (CRC) represents a formidable global health challenge, with over 1.14 million new cases and 538,000 deaths estimated in 2022. The multifactorial nature of CRC carcinogenesis limits conventional therapies, thus demanding innovative treatment approaches. Metallodrugs have emerged as promising anticancer agents due to their unique physicochemical properties and unique mechanisms of action. However, their clinical translation is hindered by poor aqueous solubility, limited stability, and significant systemic toxicity.This comprehensive review examines the integration of organic nanoparticles and biomimetic smart nanocarriers to overcome metallodrug limitations in CRC therapy. We systematically analyse three major nanocarrier classes: lipid-based systems, protein-based platforms, and polymeric carriers. Critical evaluation criteria encompass synthesis complexity, scalability, biocompatibility, and translational feasibility. Each nanocarrier offers exclusive advantages: liposomes provide clinical maturity, protein nanoparticles present exceptional biocompatibility, and polymeric systems enable superior customization. Current preclinical successes demonstrate remarkable therapeutic improvements, with several candidates advancing to clinical evaluation. Although widespread impact is expected to happen gradually, ongoing developments continue to show promise. Advances in manufacturing scalability and long-term safety will be some critical points for the progress of these nanotherapeutic strategies for CRC management.

Melanoma is the most aggressive skin cancer and, despite therapeutic advances in recent years, it continues to be associated with the highest mortality rates. Thus, the development of more effective and safer treatment options remain imperative. In this context, and driven by the discovery of the antineoplastic properties and consequent clinical approval of cisplatin, metal-based complexes have gained increasing attention. In this work, previously synthesized vanadium and nickel-based complexes which exhibited cytotoxic activity towards melanoma cell lines in their free form, were incorporated into liposomes to improve solubility and enhance tumor cell selectivity. Nickel-based nanoformulations showed higher loading capacity than the vanadium complex and were therefore selected for further studies. The optimized nickel lipid nanoformulation was tested in vitro regarding antiproliferative properties and cellular mechanism of action in B16F10 and A375 melanoma cells. Lastly, the therapeutic potential and the biodistribution profile were also evaluated in an in vivo syngeneic murine melanoma model. In vitro studies demonstrated that 24 and 48 h after incubation in melanoma cell lines, the nickel-based complex retained its antiproliferative activity following association with liposomes. Furthermore, the liposomal formulation promoted cell cycle arrest in G2/M phase in both cell lines, while hemolytic assays demonstrated its safety for intravenous administration. Finally, in vivo proof of concept studies confirmed that both the free and liposomal forms of the nickel-based complex significantly impaired tumor progression achieving effects comparable to the positive control 5-Fluorouracil, despite the latter being administered at a four-fold higher dose. Moreover, biodistribution studies revealed that labelled liposomes accumulated and persisted at tumor sites, thus correlating with the observed therapeutic effects. Overall, the safety and efficacy of this strategy highlight its strong potential for melanoma management.

We report the synthesis and characterization of five novel metal complexes. Three of them are vanadium complexes with the general formula [VO(Ln)2], where Ln are Schiff bases derived from the condensation of 2-carbaldehyde-8-hydroxyquinoline with either 4-(2-aminoethyl)morpholine (L1), 3-morpholinopropylamine (L2) or 1-(2-aminoethyl)piperidine (L3). The two other metal complexes are [Ni(L1)2] and [Fe(L1)2]Cl. They were characterized by analytical, spectroscopic (Fourier transform infrared, UV-visible absorption), and mass spectrometric techniques as well as by single-crystal X-ray diffraction (for all [VO(Ln)2] complexes and [Ni(L1)2]). While, in the crystal structure, the V(IV)O complexes show distorted square–pyramidal geometry with the ligands bound as bidentate through quinolate NO donors, the Ni(II) complex shows octahedral geometry with two ligand molecules coordinated through NNO donors. Stability studies in aqueous media revealed that the vanadium complexes are not stable, undergoing oxidation to VO2(L), which was corroborated by 51V NMR and MS. This behavior is also observed in organic media, though at a significantly slower rate. The Ni complex exhibited small spectral changes over time in aqueous media. Nonetheless, all compounds show enhanced stability in the presence of bovine serum albumin (BSA). Fluorescence studies carried out for the Ni(II) and Fe(III) complexes indicate reversible binding to albumin. The cytotoxicity of the L1 metal complexes was assessed on melanoma (B16F10 and A375) and colon cancer (CT-26 and HCT-116) cell lines, with 5-fluorouracil (5-FU) as a reference drug. The V- and Ni complexes showed the lowest IC50 values (<10 μM) in either A375 or HCT-116 cells after 48 h of incubation, while the Fe(III) complex presented minimal antiproliferative effects. The complexes were generally more cytotoxic to human than murine cancer cells. Synergistic in vitro studies with 5-FU revealed antagonism in most cases, except in A375 cells, where an additive effect was observed for the combination with the V-complex. Overall, these compounds show promising potential for cancer treatment, mostly for melanoma.

Background/Objectives: Head and neck cancer (HNC) is the sixth most common cancer worldwide, with a high mortality, particularly from head and neck squamous cell carcinoma (HNSCC). Although some therapeutic strategies are available, they might cause severe side effects. For example, surgery may result in disfigurement and functional loss, severely impacting the patient’s quality of life. Thus, minimally invasive and more effective alternatives are needed. Gold nanoparticle (AuNP)-mediated photothermal therapy (PTT) is a promising approach for HNC, which relies on AuNP photothermal efficiency and tumor localization. This study aimed to synthesize and characterize AuNPs, evaluate their safety without laser activation, and assess their efficacy with laser activation. Methods and Results: Their physicochemical and photostability over three months and sterility were confirmed. In vitro safety was tested using human non-cancerous and HNC cell lines, while in vivo biocompatibility was evaluated in the hen’s egg chorioallantoic membrane (CAM) model, with no adverse effects observed. Upon laser activation, AuNPs reduced HNC cell viability by 50–70%, including HNSCC lines. In vivo biodistribution studies showed that AuNPs remained at the injection site for up to one month without toxicity. Conclusions: Overall, the developed AuNP formulation demonstrates stability, biocompatibility, and prolonged local retention, key attributes for effective and targeted PTT. These findings support the potential of AuNP-mediated photothermal therapy as a promising treatment modality for HNC, although further preclinical and clinical studies are needed to optimize treatment parameters.

Colorectal cancer (CRC) is the third most prevalent malignancy worldwide and in both sexes. Numerous animal models for CRC have been established to study its biology, namely carcinogen-induced models (CIMs) and genetically engineered mouse models (GEMMs). CIMs are valuable for assessing colitis-related carcinogenesis and studying chemoprevention. On the other hand, CRC GEMMs have proven to be useful for evaluating the tumor microenvironment and systemic immune responses, which have contributed to the discovery of novel therapeutic approaches. Although metastatic disease can be induced by orthotopic injection of CRC cell lines, the resulting models are not representative of the full genetic diversity of the disease due to the limited number of cell lines suitable for this purpose. On the other hand, patient-derived xenografts (PDX) are the most reliable for preclinical drug development due to their ability to retain pathological and molecular characteristics. In this review, the authors discuss the various murine CRC models with a focus on their clinical relevance, benefits, and drawbacks. From all models discussed, murine CRC models will continue to be an important tool in advancing our understanding and treatment of this disease, but additional research is required to find a model that can correctly reflect the pathophysiology of CRC.

The antimicrobial activity of dehydroabietic acid (DHA) for its use as an antibiofilm agent was tested in this work. DHA was assayed against a collection of Gram-positive, Gram-negative sensitive and resistant bacteria and yeasts through the minimum inhibitory concentration (MIC), MIC with Bioburden challenge, minimum bactericidal concentration (MBC), minimum biofilm inhibitory concentration (MBIC), MBIC with Bioburden challenge and growth curve studies. Toxicological studies (Artemia salina, sulforhodamine B (SRB) assay) were done to assess if the compound had antimicrobial and not cytotoxic properties. Furthermore, microencapsulation and stability studies were carried out to evaluate the chemical behavior and stability of DHA. On MIC results, Gram-positive bacteria Staphylococcus aureus ATCC 1228 and Mycobacterium smegmatis ATCC 607 presented a high efficiency (7.81 µg/mL), while on Gram-negative bacteria the highest MIC value of 125 µg/mL was obtained by all Klebsiella pneumoniae strains and Escherichia coli isolate strain HSM 303. Bioburden challenge showed that MIC, MBIC and percentage biofilm inhibition (BI) values suffered alterations, therefore, having higher concentrations. MBIC values demonstrated that DHA has a higher efficiency against S. aureus ATCC 43866 with a percentage of BI of 75.13 ± 0.82% at 0.49 µg/mL. Growth curve kinetic profiles of DHA against S. aureus ATCC 25923 were observed to be bacteriostatic. DHA-alginate beads had a average size of 2.37 ± 0.20 and 2.31 ± 0.17 × 103 µm2 with an encapsulation efficiency (EE%) around 99.49 ± 0.05%, a protection percentage (PP%) of 60.00 ± 0.05% in the gastric environment and a protection efficiency (PE%) around 88.12 ± 0.05% against UV light. In toxicological studies DHA has shown IC50 of 19.59 ± 7.40 µg/mL and a LC50 of 21.71 ± 2.18%. The obtained results indicate that DHA is a promising antimicrobial candidate against a wide range of bacteria and biofilm formation that must be further explored.

Cancer is a major cause of morbidity and mortality worldwide. Chemotherapeutic agents currently used in cancer treatment are associated with severe side effects and development of resistance. Thus, there is a pressing need for novel and more potent anticancer drugs with high selectivity for tumor cells and reduced toxicity to normal tissue. Natural products remain an important source of bioactive compounds and drug prototypes that can lead to new and more effective antitumor agents. Coniferous plants are rich in abietane diterpenoids with a wide range of biological activities that provide useful templates for synthetic modification. Abietic acid and dehydroabietic acid (DHA), the major diterpenic resin acids from Pinus rosin, and dehydroabietylamine found in commercial disproportionated rosin amine, display antibacterial and antitumor properties. These compounds and their synthetic derivatives have been reported as promising anticancer agents with potent growth inhibitory activity against several types of human cancer cell lines, including breast, ovarian, prostate, colon, liver, lung and cervical carcinoma cells. Their mechanisms of action are diverse and include DNA binding, induction of apoptosis or oncosis, tubulin polymerization inhibition and disruption of intracellular cholesterol transport. This review covers the main aspects of natural rosin abietane diterpenoids (abietic acid, DHA and DHAA) and synthetic derivatives concerning their anti-proliferative, cytotoxic and antitumor activities, mechanisms of action and structure-activity relationships relevant for the development of novel anticancer agents for cancer chemotherapy.

The convenient synthesis of dihydroberberine by the reduction of berberine is described as an experiment for an upper-division undergraduate organic chemistry laboratory course. Students obtained up to 74% yield of the desired pure product without the use of chromatographic techniques. The antimicrobial activities of both compounds against Staphylococcus aureus and Candida albicans were then assessed and compared in an upper-division undergraduate microbiology laboratory course. The students verified that berberine shows higher antimicrobial activity than its derivative dihydroberberine, demonstrating that small changes in a chemical structure can result in great biological differences.

This work focused on the screening of biological activities of several Plectranthus spp.(P.madagascariensis, P. neochilus, P. grandidentatus, P. ecklonii, P. porcatus, P. prostratus, P. ornatus and P. saccatus).The biological activity screening aimed at unraveling novel ethnopharmacological roles regarding antioxidant, anti-skin ageing, anti-inflammatory and anti-mycobacterial activities, of several extracts (aqueous, methanol, acetone and ethyl acetate) and isolated compounds (rosmarinic acid; chlorogenic acid; a mixture of β-sitosterol : stigmasterol (1:1); a mixture of α-amyrin : β-amyrin (3:1); a mixture of oleanolic acid : ursolic acid (1:4); a mixture of 1,6-di-O-acetylforskolin : 1,6-di-O-acetyl-9-deoxyforskolin (1:1); (11R*,13E)-11-acetoxyhalima-5,13-dien-15-oic acid; (11R*,13E)-15-butyryloxyhalima-5,13-dien-11-ol; (11R*,13E)-halima-5,13-diene-11,15-diol; (11R*,13E)-11-acetoxyhalima-5,13-dien-15-oic methyl ester; (13S,15S)-6β,7α,12α,19-tetrahydroxy-13β,16-cyclo-8-abietene-11,14-dione; 1α,6β-diacetoxy-8α,13R*-epoxy-14-labden-11-one; Parvifloron D; 6,7-dehydroroyleanone; 7α-acetoxy-6β-hydroxyroyleanone; and 6β,7α-dihydroxyroyleanone

Antibiotic resistance is a global public health concern. The choline-based ionic liquids (ILs) have raised particular attention in the design of "greener" ILs and can exert a broad-spectrum of antimicrobial activity. To improve antimicrobial chemotherapy, we herein tested the antimicrobial activity and toxicity of a wide range of choline-based ILs. Two series of compounds were synthesized -dimethylethanolamine monoquaternary ammonium salts (Series A) and -methyl diethanolamine, diethanolamine and triethanolamine monoquaternary ammonium salts (Series B). The antimicrobial screening revealed that compounds N-(2-hydroxyethyl)-N,N-dimethyl-1-tetradecanaminium bromide ([N-1,N-1,N-14,N-2(OH)]Br), N-(2-hydroxyethyl)-N,N-dimethyl-1-hexadecanaminium bromide ([N-1,N-1,N-16,N-2(OH)]Br) and N-(2-hydroxyethyl)-N,N-dimethyl-1-octadecanaminium bromide ([N-1,N-1,N-18,N-2(OH)]Br) are potent antimicrobial agents. The presence of a hydroxyethyl group and as mention previously in the literature, the C-14 to C-16 linker in a choline compound improves the antimicrobial activity and lowers the cytotoxic properties of this class of compounds.

In this work we report the antibacterial activity of alkylaminophenols. A series of such compounds was prepared by a multicomponent Petasis-borono Mannich reaction starting from salicylaldehyde and its derivatives. The obtained compounds were tested against a large panel of microorganisms, Gram-positive and Gram-negative bacteria, and a yeast. Among the several tertiary amine derivatives tested, indoline-derived aminophenols containing a nitro group at the para-phenol position showed considerable activity against bacteria tested with minimal inhibitory concentrations as low as 1.36m against Staphyloccocus aureus and Mycobacterium smegmatis. Cytotoxicity of the new para-nitrophenol derivatives was observed only at concentrations much higher than those required for antibacterial activity.