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Sci. Pharm.
Volume 93
Issue 1
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Sci. Pharm., Volume 93, Issue 1 (March 2025) – 5 articles

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13 pages, 3235 KiB  
Article
Safety of Oral Administration of 5-Aminolevulinic Acid Phosphate Combined with Ferrous Iron in Healthy Subjects: An Open-Label Trial
by Fumiko Higashikawa, Hidenori Ito and Tohru Tanaka
Sci. Pharm. 2025, 93(1), 5; https://doi.org/10.3390/scipharm93010005 (registering DOI) - 20 Jan 2025
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Abstract
The combination of 5-aminolevulinic acid (5-ALA) phosphate and sodium ferrous citrate (SFC) has been approved as an ingredient in dietary supplements in several countries, owing to its broad applicability in healthcare. This study aimed to assess the safety of oral administration of 5-ALA [...] Read more.
The combination of 5-aminolevulinic acid (5-ALA) phosphate and sodium ferrous citrate (SFC) has been approved as an ingredient in dietary supplements in several countries, owing to its broad applicability in healthcare. This study aimed to assess the safety of oral administration of 5-ALA and SFC in healthy adults at doses several times higher than those commercially available. This study included 22 healthy subjects (11 males and 11 females) aged 21–59. Doses of 250 mg 5-ALA phosphate and 143.4 mg SFC (15 mg Fe) per day were administered orally for 28 days. Blood tests, urinalysis, and medical interviews were performed to assess safety. No test compound-related adverse events or abnormal changes were observed, except for elevated serum Fe levels, which were mild-to-moderate and transient. In conclusion, the combined oral administration of 5-ALA phosphate and SFC in healthy adults was safe and well-tolerated at the dose and duration investigated in this study. Full article
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20 pages, 6443 KiB  
Article
Anti-Migratory Activity of Brazilin Chemodiversification on Breast Cancer Cells
by Alberto Hernández-Moreno, Dania A. Nava-Tapia, Miriam D. Zuñiga-Eulogio, Jorge Bello-Martínez, Monserrat Olea-Flores, Tadeo Hernández-Moreno, Mario Ordoñez, Ana E. Zacapala-Gómez, Miguel A. Mendoza-Catalán and Napoleón Navarro-Tito
Sci. Pharm. 2025, 93(1), 4; https://doi.org/10.3390/scipharm93010004 - 11 Jan 2025
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Abstract
Breast cancer is the most common and the leading cause of cancer death in women worldwide; treating invasive breast carcinomas is challenging due to the side effects of chemotherapeutics. Compounds isolated from natural sources have been proposed as potential molecules for cancer therapy; [...] Read more.
Breast cancer is the most common and the leading cause of cancer death in women worldwide; treating invasive breast carcinomas is challenging due to the side effects of chemotherapeutics. Compounds isolated from natural sources have been proposed as potential molecules for cancer therapy; for instance, the homoisoflavonoid brazilin has shown pharmacological properties, including anti-tumoral and anti-inflammatory activities. In this study, we isolated brazilin from the heartwood of Haematoxylum brasiletto; then, we performed a semi-synthesis by adding three methyl or acetyl groups to the core structure of brazilin. We confirmed the identity of brazilin and its derivatives by spectroscopic data (1H NMR and 13C NMR) and measured their purity by optical rotation. Then, we analyzed the effects of brazilin and its derivatives in three mammary gland-derived cell lines: the TNBC MDA-MB-231, the ERα(+) MCF7, and the non-tumorigenic MCF10A. We evaluated the cell viability by MTT assays, cell migration by wound-healing assays, and focal adhesion kinase (FAK) activation by Western blot. Regarding biological assays, the MTT assay showed that these compounds showed cytotoxic effects on the MCF7 and MDA-MB-231 breast cancer cells at 20 µM but was not toxic in non-tumorigenic MCF10A mammary epithelial cells. Specifically, the greatest effects found from treatment with the compounds were in the MDA-MB-231 cell line, where the IC50 of brazilin was 49.92 μM, and for MCF7, the brazilin-(OAc)3 was 49.97 μM. These effects were dose- and time-dependent, as well as being associated with a decrease in the levels of cell migration and FAK activation. Full article
(This article belongs to the Topic Antitumor Activity of Natural Products and Related Compounds—2nd Edition)
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20 pages, 3501 KiB  
Article
Development of a Comprehensive Approach to Quality Control of Dermorphin Derivative—Representative of Synthetic Opioid Peptides with Non-Narcotic Type of Analgesia
by Vasilisa A. Sukhanova, Elena V. Uspenskaya, Safdari Ainaz, Hoang Thi Ngoc Quynh and Aleksey A. Timofeev
Sci. Pharm. 2025, 93(1), 3; https://doi.org/10.3390/scipharm93010003 - 31 Dec 2024
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Abstract
Peptides occupy a significant share of the pharmaceutical market and are among the top-200 selling drugs in the group of non-insulin drugs with analgesic, antibacterial and cardiovascular effects. The aim of this work is to develop a comprehensive analytical approach for quality control [...] Read more.
Peptides occupy a significant share of the pharmaceutical market and are among the top-200 selling drugs in the group of non-insulin drugs with analgesic, antibacterial and cardiovascular effects. The aim of this work is to develop a comprehensive analytical approach for quality control of novel synthetic peptides with non-narcotic types of analgesia and to provide docking simulations of dermorphin complex formation at the μ-opioid receptor (MOR) binding site. The materials and methods used include the pharmaceutical substance dermorphin tetrapeptide (DMTP) (tyrosyl-D-arginyl-phenylalanyl-glycinamide); Fourier transform infrared spectroscopy (FT-IR); static and dynamic laser light scattering (DLS, LALLS); scanning optical microscopy (SEM); X-ray fluorescence elements analysis; polarimetry for optical activity determining; and Spirotox method for sample biotesting. FT-IR-Spectra indicated specific amino acid chemical groups in the tetrapeptide sequence at 3300–2700 cm−1, 1670 cm−1. UV-absorption spectra of aqueous solutions of dermorphin tetrapeptide showed an absorption maximum at 275 nm, which is in good agreement with the presented spectrum of the bovine serum albumin (BSA) standard; the Pearson’s r of calibration line “A-C%” in 0.0125% to 0.0500% concentration range is 0.999; and the calculated specific extinction value E1cm 1% = 18.38 ± 0.23. Of the 11 elements detected by X-rays, the elements copper (Cu) and cobalt (Co) have the highest X-ray intensity. Dispersion characteristics of dermorphin solutions were studied in the submicron and micron range. Conglomerates and druzes were detected by SEM, ranging in size from 2 µm to 100 µm. The specific optical activity index was calculated αD20 = +36.18 ± 2.04 [°·mL·g−1·dm−1], according to Biot’s Law. Additionally, the orientation and conformation of the dermorphin molecule in the active binding site of the 8E0G receptor were predicted using molecular modeling, revealing that the contact area affects the key amino acid residue arginine (ARG 182). This comprehensive approach to analytical methods for qualitative and quantitative analysis of dermorphin tetrapeptide can be applied in pharmacies to enhance the understanding of its biological activity and aid in the development of regulatory documentation for a new, non-narcotic analgesic based on the dermorphin tetrapeptide. Full article
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21 pages, 6841 KiB  
Article
Marine Origin vs. Synthesized Compounds: In Silico Screening for a Potential Drug Against SARS-CoV-2
by Amar Osmanović, Mirsada Salihović, Elma Veljović, Lamija Hindija, Mirha Pazalja, Maja Malenica, Aida Selmanagić and Selma Špirtović-Halilović
Sci. Pharm. 2025, 93(1), 2; https://doi.org/10.3390/scipharm93010002 - 26 Dec 2024
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Abstract
Although COVID-19 is not a pandemic anymore, the virus frequently mutates, resulting in new strains and presenting global public health challenges. The lack of oral antiviral drugs makes it difficult to treat him, which makes the creation of broadly acting antivirals necessary to [...] Read more.
Although COVID-19 is not a pandemic anymore, the virus frequently mutates, resulting in new strains and presenting global public health challenges. The lack of oral antiviral drugs makes it difficult to treat him, which makes the creation of broadly acting antivirals necessary to fight current and next epidemics of viruses. Using the molecular docking approach, 118 compounds derived from marine organisms and 92 previously synthesized compounds were screened to assess their binding affinity for the main protease and papain-like protease enzymes of SARS-CoV-2. The best candidates from the xanthene, benzoxazole, and coumarin classes were identified. Marine-derived compounds showed slightly better potential as enzyme inhibitors, though the binding affinities of synthesized compounds were similar, with the best candidates displaying affinity values between 0.2 and 0.4 mM. Xanthenes, among both marine origin and synthesized compounds, emerged as the most promising scaffolds for further research as inhibitors. The papain-like protease was found to be more druggable than the main protease. Additionally, all top candidates met the criteria for various drug-likeness properties, indicating good oral bioavailability and low risk of adverse effects. This research provides valuable insights into the comparative affinities of marine origin and synthesized compounds from the xanthene, coumarin, and benzoxazole classes, highlighting promising candidates for further in vitro and in vivo studies. Full article
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26 pages, 5193 KiB  
Review
Colon Cancer: Overview on Improved Therapeutic Potential of Plant-Based Compounds Using Nanotechnology
by Manuel López-Cabanillas Lomelí, Alexandra Tijerina-Sáenz, David Gilberto García-Hernández, Marcelo Hernández-Salazar, Rogelio Salas García, José Luis González-Llerena, María Julia Verde-Star, Anthonny Cordero-Díaz and Michel Stéphane Heya
Sci. Pharm. 2025, 93(1), 1; https://doi.org/10.3390/scipharm93010001 - 24 Dec 2024
Viewed by 719
Abstract
Colon cancer (CC) is the third most frequent neoplasm, with a considerably high mortality rate. Due to the side effects of conventional forms of CC treatment (surgery, chemotherapy, and radiotherapy), several studies have focused on the use of medicinal plant derivatives to provide [...] Read more.
Colon cancer (CC) is the third most frequent neoplasm, with a considerably high mortality rate. Due to the side effects of conventional forms of CC treatment (surgery, chemotherapy, and radiotherapy), several studies have focused on the use of medicinal plant derivatives to provide a green therapy for CC; although phytochemicals have shown promising results against CC, translating the results obtained in vitro and in vivo to the clinical setting remains a challenge. Indeed, like other orally applied medicines, medicinal plant derivatives have to cross different physiological barriers to reach the CC microenvironment, which considerably limits their dose-dependent therapeutic efficacy. On the other hand, phytocompounds are not free from biopharmaceutical drawbacks, so novel strategies using nanoparticles (NPs) have been proposed to overcome the physiological barriers of the body and provide controlled release of actives of interest. Accordingly, the current review provides an overview and discussion on the predisposing factors to CC and conventional treatment, the use of medicinal plants in CC treatment, and the advantages provided by NPs in the treatment of CC. Full article
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