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Section = Drug Candidates from Natural Sources

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23 pages, 772 KB  
Review
Therapeutic and Adjuvant Effects of Probiotics in the Management of Oral Cancer: A Scoping Review of Preclinical and Clinical Evidence
by Gabriel Tchuente Kamsu and Eugene Jamot Ndebia
Drugs Drug Candidates 2026, 5(2), 30; https://doi.org/10.3390/ddc5020030 - 25 Apr 2026
Viewed by 188
Abstract
Background/Objectives: Oral cancer remains a major global health challenge, with persistent limitations in treatment efficacy and significant therapy-related morbidity. Probiotics, owing to their immunomodulatory, anti-inflammatory, and microbiota-regulating properties, have emerged as potential therapeutic and adjuvant agents. This scoping review aimed to systematically map [...] Read more.
Background/Objectives: Oral cancer remains a major global health challenge, with persistent limitations in treatment efficacy and significant therapy-related morbidity. Probiotics, owing to their immunomodulatory, anti-inflammatory, and microbiota-regulating properties, have emerged as potential therapeutic and adjuvant agents. This scoping review aimed to systematically map and critically appraise preclinical and clinical evidence regarding the therapeutic and supportive effects of probiotics in oral cancer. Methods: A comprehensive literature search was conducted across PubMed, Scopus, Web of Science, and Google Scholar without temporal restrictions, including studies published up to February 2026. Eligible studies comprised in vitro, in vivo, and clinical investigations evaluating the effects of live or non-viable probiotic interventions on oral cancer biology and related clinical outcomes. Results: Twenty-one studies were included: 13 in vitro, 3 in vivo, and 6 clinical studies. Preclinical evidence indicates that strains such as Lactiplantibacillus plantarum, Lactobacillus acidophilus, and Lacticaseibacillus paracasei exert selective antiproliferative effects (up to 85% inhibition) via apoptosis induction, modulation of PTEN/MAPK and NF-κB signaling, and reduction in pro-inflammatory mediators. In vivo models demonstrated tumor growth suppression and improved survival without significant toxicity. Clinically, probiotics reduced treatment-induced oral mucositis, improved salivary function, and enhanced microbiota stability and patient-reported outcomes. However, evidence on direct oncological endpoints remains limited. Conclusions: Probiotics demonstrate biologically plausible, strain-specific antitumor and supportive effects, with the strongest evidence supporting their role as adjunctive agents, particularly in managing treatment-related complications. Further well-designed in vivo and clinical studies are required to define optimal strains, dosing strategies, and integration with standard oncologic treatments. Full article
(This article belongs to the Section Drug Candidates from Natural Sources)
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14 pages, 936 KB  
Article
Cannabidiol Prevents Ovariectomy-Induced Thermoregulatory Dysfunction in Rats: A Preclinical Study on Menopausal Vasomotor Symptoms
by Vitória Leite Lages, Lourdes Fernanda Godinho, Alayanne Santos Guieiro, Thais Trindade, Bruna Oliveira Costa, Joyce Mirlene Moreira Costa, Ramona Ramalho de Souza Pereira, Caíque Olegário Diniz e Magalhães and Kinulpe Honorato-Sampaio
Drugs Drug Candidates 2026, 5(2), 26; https://doi.org/10.3390/ddc5020026 - 18 Apr 2026
Viewed by 321
Abstract
Background/Objectives: Vasomotor symptoms (hot flashes) affect 70–80% of menopausal women, significantly impairing quality of life. Current treatments include hormone therapy, which is contraindicated for many patients, and non-hormonal alternatives with limited efficacy or adverse effects. Cannabidiol (CBD), a non-psychoactive phytocannabinoid, has emerged as [...] Read more.
Background/Objectives: Vasomotor symptoms (hot flashes) affect 70–80% of menopausal women, significantly impairing quality of life. Current treatments include hormone therapy, which is contraindicated for many patients, and non-hormonal alternatives with limited efficacy or adverse effects. Cannabidiol (CBD), a non-psychoactive phytocannabinoid, has emerged as a potential therapeutic candidate due to its interaction with the endocannabinoid system. This study aimed to investigate whether a standardized Cannabis sativa extract containing isolated CBD attenuates heat dissipation in ovariectomized rats, a preclinical model of estrogen deficiency. Methods: Female Wistar rats were randomly assigned to sham-operated vehicle-treated (SHAM-V), ovariectomized vehicle-treated (OVX-V), or ovariectomized CBD-treated (OVX-CBD; 10 mg/kg/day, oral gavage) groups. Treatment began on postoperative day 2 and continued for 21 days. Tail-skin temperature, a surrogate marker of heat dissipation, was assessed by infrared thermography on day 14. Energy metabolism was evaluated by indirect calorimetry on day 21. Uterine weight was measured as a biomarker of estrogen depletion. Results: Ovariectomy significantly increased tail temperature compared to SHAM-V. CBD treatment completely prevented this effect, with OVX-CBD animals exhibiting thermographic profiles similar to SHAM-V. Uterine atrophy was not reversed by CBD. No differences in the calorimetry parameter were observed among groups. Conclusions: This study provides novel preclinical evidence that cannabidiol attenuates ovariectomy-induced heat dissipation in rats, without detectable effects on uterine weight or metabolic parameters. These findings suggest that CBD may represent a potential non-hormonal approach for the management of menopausal vasomotor symptoms; however, further studies are required to elucidate the underlying mechanisms and to determine its translational and clinical relevance. Full article
(This article belongs to the Section Drug Candidates from Natural Sources)
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27 pages, 4221 KB  
Review
Alzheimer’s Disease and Contemporary Therapeutic Approaches: Recent Advances in Natural Products
by Ertugrul Gunday and Fatma Sezer Senol Deniz
Drugs Drug Candidates 2026, 5(1), 21; https://doi.org/10.3390/ddc5010021 - 4 Mar 2026
Cited by 1 | Viewed by 1449
Abstract
Alzheimer’s disease is a progressive neurodegenerative disorder marked by cognitive decline, and its global prevalence is expected to increase substantially in the coming decades. This review examines current therapeutic approaches and explores the potential role of medicinal plants and natural products in the [...] Read more.
Alzheimer’s disease is a progressive neurodegenerative disorder marked by cognitive decline, and its global prevalence is expected to increase substantially in the coming decades. This review examines current therapeutic approaches and explores the potential role of medicinal plants and natural products in the treatment and prevention of Alzheimer’s disease. This review examines the pathophysiology of Alzheimer’s disease, with particular emphasis on the cholinergic, amyloid, and tau hypotheses. It evaluates currently approved therapeutic approaches, including cholinesterase inhibitors and NMDA receptor antagonists, as well as emerging immunotherapies. In addition, this review provides a comprehensive analysis of the pharmacological properties of various medicinal plants and explores innovative drug delivery systems. Research reveals that while conventional drugs like donepezil and memantine provide symptomatic relief, they do not halt disease progression. Recent immunotherapies, including lecanemab and donanemab, show potential to reduce amyloid-beta accumulation and slow cognitive decline; however, they face safety concerns, such as amyloid-related imaging abnormalities, and high costs. By comparison, several natural products—including huperzine A, curcumin, resveratrol, and epigallocatechin-3-gallate—demonstrate multi-target therapeutic potential through anti-inflammatory, antioxidant, and cholinergic-modulating mechanisms. This review offers a comprehensive contrast between natural products and traditional drugs as well as the safety and economic limitations of immunotherapies. Given the multifactorial nature of AD, therapeutic strategies that address multiple pathological pathways appear necessary. In this regard, plant-derived compounds, due to their broad pharmacological activity and generally favorable safety profiles, emerge as promising candidates for long-term management and may contribute meaningfully to the development of future therapeutic approaches for AD. Full article
(This article belongs to the Section Drug Candidates from Natural Sources)
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10 pages, 1470 KB  
Article
Cytotoxic and Antiproliferative Effects of Chlorella vulgaris Lectin on Colon Cancer Cells
by Vivianne Lays Ribeiro Cavalcanti, Maria Carla Santana de Arruda, Thalya Natasha da Silva Santos, Daniela de Araújo Viana Marques, Romero Marcos Pedrosa Brandão Costa, Luiza Rayanna Amorim de Lima, Ana Lúcia Figueiredo Porto and Raquel Pedrosa Bezerra
Drugs Drug Candidates 2025, 4(4), 58; https://doi.org/10.3390/ddc4040058 - 18 Dec 2025
Viewed by 778
Abstract
Background/Objectives: Colon cancer is the third most common type of cancer in the world, characterized by a high risk of metastasis, resistance to various drugs, and late diagnosis. In addition, the drugs used for treatment are associated with serious neurological damage, causing acute [...] Read more.
Background/Objectives: Colon cancer is the third most common type of cancer in the world, characterized by a high risk of metastasis, resistance to various drugs, and late diagnosis. In addition, the drugs used for treatment are associated with serious neurological damage, causing acute and chronic pain and compromising the patient’s quality of life. Meanwhile, lectins are proteins capable of exerting cytotoxic action on cells from various tumors in a selective manner, without exerting significant toxicity on healthy cells. Despite this, studies on the potential of lectins obtained from microalgae are still scarce in the literature. In this sense, the objective of this study was to evaluate the antitumor activity of lectin isolated from the microalgae Chlorella vulgaris (CvL) on colorectal cancer cells, HT-29. Methods: The purified lectin was tested for cytotoxicity using MTT colorimetric methods, in addition to clonogenicity, cell cycle, apoptosis, and necrosis tests, analyzed by flow cytometry. Results: The assays demonstrated that the lectin was able to induce cell death in the HT-29 tumor line by approximately 83.75% with an IC50 value of 21.5 µg/mL−1, reduced colony formation by more than 90%, was able to regulate the cell cycle by apoptosis, and did not present significant necrosis. These results show that microalgae lectins have the potential to be exploited in the control of neoplastic cells. Full article
(This article belongs to the Section Drug Candidates from Natural Sources)
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21 pages, 1046 KB  
Article
Aqueous Leaf Extracts of Bauhinia cheilantha (Bong.) Steud.: Phytochemical Profile, Antioxidant Activity and In Vitro Safety Evaluation
by Palloma Lima de Oliveira, José Rafael da Silva Araújo, Camila Marinho da Silva, Kyria Cilene de Andrade Bortoleti, Silvany de Sousa Araújo, Márcia Vanusa da Silva, Dráulio Costa da Silva, Marcos dos Santos Lima, Ana Paula de Oliveira and Ana Christina Brasileiro-Vidal
Drugs Drug Candidates 2025, 4(4), 54; https://doi.org/10.3390/ddc4040054 - 8 Dec 2025
Cited by 1 | Viewed by 654
Abstract
Background/Objectives: Bauhinia cheilantha Bong. Steud. (Leguminosae; “pata-de-vaca”) is traditionally used in folk medicine for its antidiabetic, anti-inflammatory, and sedative properties. This study aimed to evaluate aqueous leaf extracts of B. cheilantha, non-delipidated and delipidated, regarding their phytochemical composition, phenolic profile, antioxidant potential, [...] Read more.
Background/Objectives: Bauhinia cheilantha Bong. Steud. (Leguminosae; “pata-de-vaca”) is traditionally used in folk medicine for its antidiabetic, anti-inflammatory, and sedative properties. This study aimed to evaluate aqueous leaf extracts of B. cheilantha, non-delipidated and delipidated, regarding their phytochemical composition, phenolic profile, antioxidant potential, and cytotoxic, genotoxic, and antigenotoxic effects. Methods: Phytochemical screening was performed by TLC, and phenolic compounds were determined by HPLC. Antioxidant activity was assessed using DPPH, ABTS, and phosphomolybdenum assays. Cytotoxicity, genotoxicity, and antigenotoxicity were evaluated in L929 murine fibroblast cells using MTT and cytokinesis-block micronucleus (CBMN) assays. Results: Both extracts contained anthocyanins, phenolics, lignans, saponins, and hydrolyzable tannins. The delipidated extract showed higher total phenolic content (17.54 mg/kg) than the non-delipidated (13.76 mg/kg). Major constituents included kaempferol 3-glucoside, quercetin, hesperidin, naringenin, and t-cinnamic acid. Antioxidant assays revealed EC50 values of 25.84, 13.60, and 66.09 µg/mL for the non-delipidated extract, and 26.19, 16.34, and 52.78 µg/mL for the delipidated extract in the DPPH, ABTS, and phosphomolybdenum assays, respectively. No cytotoxicity was observed, except at 1600 µg/mL for the non-delipidated extract and 800–1600 µg/mL for the delipidated extract. Genotoxicity occurred only at 400 µg/mL. Antigenotoxic evaluation showed that the non-delipidated extract (100 µg/mL) reduced methyl methanesulfonate-induced chromosomal damage in simultaneous and post-treatment conditions, while the delipidated extract was only effective for post-treatment. Conclusions: Aqueous extracts of B. cheilantha exhibit antioxidant and antigenotoxic properties. At active concentrations, they were non-cytotoxic and non-genotoxic. The non-delipidated extract, in particular, showed the strongest genome-protective potential, supporting its traditional use and highlighting its relevance in the development of natural therapeutic agents. Full article
(This article belongs to the Section Drug Candidates from Natural Sources)
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29 pages, 3926 KB  
Article
Integration of In Vitro Glucose Utilization, Metabolomics and Network Pharmacology Strategy to Explore Antidiabetic Mechanisms of Gunnera perpensa and Erythrina zeyheri Extracts
by Oyinlola Oluwunmi Olaokun
Drugs Drug Candidates 2025, 4(4), 51; https://doi.org/10.3390/ddc4040051 - 14 Nov 2025
Viewed by 855
Abstract
Background: Type 2 diabetes mellitus (T2DM) is a complex metabolic disease requiring multi-targeted therapeutic strategies. Gunnera perpensa and Erythrina zeyheri are traditionally used in diabetes management, but their mechanisms remain poorly understood. Methods: This study used in vitro, metabolomics, and network [...] Read more.
Background: Type 2 diabetes mellitus (T2DM) is a complex metabolic disease requiring multi-targeted therapeutic strategies. Gunnera perpensa and Erythrina zeyheri are traditionally used in diabetes management, but their mechanisms remain poorly understood. Methods: This study used in vitro, metabolomics, and network pharmacology approaches to elucidate their antidiabetic potential. Leaf extracts were screened for glucose utilization in C2C12 cells, and cytotoxicity in Vero cells. Metabolites profiled via GC×GC-TOF-MS and those retrieved from Phytochemical Interaction Database were evaluated for drug-likeness and target prediction using SwissADME and SwissTargetPrediction. Diabetes-related targets were obtained from databases, and overlapping targets were used to construct interaction networks using Cytoscape and STRING. Functional enrichment analyses were conducted via DAVID for GO and KEGG pathways. Results: G. perpensa acetone and methanol extracts enhanced superior glucose utilization (IC50 = 78.5 and 94.8 µg/mL, respectively), with low cytotoxicity (LC50 > 600 µg/mL). Key compounds including arabinose, identified from both plants, showed multi-target binding potential against STAT3, PIK3RI and JAK2. Enrichment analyses revealed pathways related to insulin signaling, inflammation, and glucose metabolism. Conclusions: This study supports the therapeutic relevance of phytochemical synergy in the traditional use of both plants and demonstrated systems-level approaches for elucidating complex drug–target interactions in T2DM. Full article
(This article belongs to the Section Drug Candidates from Natural Sources)
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12 pages, 706 KB  
Article
Efficient Enrichment of Total Flavonoids and Antibacterial Activity of the Ethyl Acetate Fraction of Croton blanchetianus Baill. (Euphorbiaceae) Leaves
by Pedro Artur Ferreira Marinho, Wêndeo Kennedy Costa, Maria Tereza dos Santos Correia, Wliana Alves Viturino da Silva, Magda Rhayanny Assunção Ferreira, Luiz Alberto Lira Soares, José Jailson Lima Bezerra and Alisson Macário de Oliveira
Drugs Drug Candidates 2025, 4(4), 45; https://doi.org/10.3390/ddc4040045 - 18 Oct 2025
Viewed by 921
Abstract
Background/Objectives: This study investigated the flavonoid enrichment and antimicrobial activity of the ethyl acetate fraction (EAF) obtained from Croton blanchetianus (Euphorbiaceae) leaves against Staphylococcus aureus, including the methicillin-resistant strains (MRSA) that were isolated, as well as its possible mechanism of action. [...] Read more.
Background/Objectives: This study investigated the flavonoid enrichment and antimicrobial activity of the ethyl acetate fraction (EAF) obtained from Croton blanchetianus (Euphorbiaceae) leaves against Staphylococcus aureus, including the methicillin-resistant strains (MRSA) that were isolated, as well as its possible mechanism of action. Methods: Croton blanchetianus leaves were extracted with ethanol:water (50%), then the extract was spray-dried and partitioned (8×) with ethyl acetate. Phytochemical analysis was performed using thin layer chromatography (TLC), while antibacterial activity was conducted using minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) methods. Results: Chemical profiling (TLC) confirmed multiple flavonoid bands and the presence of hyperoside; the total flavonoid content in the EAF reached 25.3% (≈2.28× the spray-dried extract and 6.65× the aqueous fraction). The MIC and MBC assays against S. aureus ATCC 29213 and six clinical isolates showed an MIC of 4–32 μg/mL and an MBC of 16–64 μg/mL for EAF. The combination of EAF with chloramphenicol showed a complete synergistic effect for S. aureus ATCC 29213 and S. aureus UFPEDA 705, a partial effect for S. aureus UFPEDA-659 and S. aureus UFPEDA-671, antagonistic effect for S. aureus UFPEDA 731 and S. aureus UFPEDA 802, and no effect for S. aureus UFPEDA-691. Growth curves indicated time- and concentration-dependent inhibition. Membrane integrity assays revealed K+ efflux and release of DNA/RNA and proteins, suggesting bacterial membrane destabilization as a likely mechanism. Conclusions: The flavonoid-rich fraction of C. blanchetianus exhibits potent anti-S. aureus activity, including MRSA. Furthermore, it was observed that EAF has a synergistic effect with chloramphenicol and acts through membrane damage, making it a candidate for a phytoderived adjuvant in antimicrobial therapies. Full article
(This article belongs to the Section Drug Candidates from Natural Sources)
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69 pages, 1993 KB  
Review
Glycyrrhizin (Glycyrrhizic Acid)—Pharmacological Applications and Associated Molecular Mechanisms
by Deepak Kumar Semwal, Ankit Kumar, Ruchi Badoni Semwal, Nand Kishor Dadhich, Ashutosh Chauhan and Vineet Kumar
Drugs Drug Candidates 2025, 4(4), 44; https://doi.org/10.3390/ddc4040044 - 30 Sep 2025
Cited by 7 | Viewed by 10335
Abstract
Background/Objectives: Natural products, especially plant metabolites, play a crucial role in drug development and are widely used in medicine, cosmetics, and nutrition. The present review aims to provide a comprehensive overview of the pharmacological profile of Glycyrrhizin (GL), with a specific focus on [...] Read more.
Background/Objectives: Natural products, especially plant metabolites, play a crucial role in drug development and are widely used in medicine, cosmetics, and nutrition. The present review aims to provide a comprehensive overview of the pharmacological profile of Glycyrrhizin (GL), with a specific focus on its molecular targets. Methods: Scientific literature was thoroughly retrieved from reputable databases, including Scopus, Web of Science, and PubMed, up to 30 July 2025. The keywords “glycyrrhizin” and “glycyrrhizic acid” were used to identify relevant references, with a focus on pharmacological applications. Studies on synthetic analogs, non-English publications, non-pharmacological applications, and GL containing crude extracts were largely excluded. Results: Glycyrrhizin, the major bioactive constituent of Glycyrrhiza glabra, exhibits diverse pharmacological activities, including anti-inflammatory, antiviral, hepatoprotective, antitumor, neuroprotective, and immunomodulatory effects. These actions are primarily mediated through the inhibition of high-mobility group box 1 (HMGB1) and the modulation of key signaling pathways, including nuclear factor kappa B (NF-κB), mitogen-activated protein kinase (MAPK), phosphoinositide 3-kinase/protein kinase B (PI3K/Akt), and various cytokine networks. As a result of its therapeutic potential, GL-based formulations, including Stronger Neo-Minophagen C, and GL-rich extracts of G. glabra are commercially available as pharmaceutical preparations and food additives. Conclusions: Despite its therapeutic potential, the clinical application of GL is limited by poor oral bioavailability, metabolic variability, and adverse effects such as pseudoaldosteronism. Hence, careful consideration of pharmacokinetics and safety is essential for translating its therapeutic potential into clinical practice. Full article
(This article belongs to the Section Drug Candidates from Natural Sources)
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27 pages, 1379 KB  
Article
A Multifaceted Exploration of Shirakiopsis indica (Willd) Fruit: Insights into the Neuropharmacological, Antipyretic, Thrombolytic, and Anthelmintic Attributes of a Mangrove Species
by Mahathir Mohammad, Md. Jahirul Islam Mamun, Mst. Maya Khatun, Md. Hossain Rasel, M Abdullah Al Masum, Khurshida Jahan Suma, Mohammad Rashedul Haque, Sayed Al Hossain Rabbi, Md. Hemayet Hossain, Hasin Hasnat, Nafisah Mahjabin and Safaet Alam
Drugs Drug Candidates 2025, 4(3), 31; https://doi.org/10.3390/ddc4030031 - 1 Jul 2025
Cited by 16 | Viewed by 2133
Abstract
Background: Shirakiopsis indica (Willd.) (Family: Euphorbiaceae), a mangrove species found in the Asian region, is a popular folkloric plant. Locally, the plant is traditionally used to treat various types of ailments, especially for pain relief. Therefore, the current study investigates the neuropharmacological, [...] Read more.
Background: Shirakiopsis indica (Willd.) (Family: Euphorbiaceae), a mangrove species found in the Asian region, is a popular folkloric plant. Locally, the plant is traditionally used to treat various types of ailments, especially for pain relief. Therefore, the current study investigates the neuropharmacological, antipyretic, thrombolytic, and anthelmintic properties of the S. indica fruit methanolic extract (SIF-ME). Methods: The neuropharmacological activity was evaluated using several bioactive assays, and the antipyretic effect was investigated using the yeast-induced pyrexia method, both in Swiss albino mice models. Human blood clot lysis was employed to assess thrombolytic activity, while in vitro anthelmintic characteristics were tested on Tubifex tubifex. Insights into phytochemicals from SIF-ME have also been reported from a literature review, which were further subjected to molecular docking, pass prediction, and ADME/T analysis and validated the wet-lab outcomes. Results: In the elevated plus maze test, SIF-ME at 400 mg/kg demonstrated significant anxiolytic effects (200.16 ± 1.76 s in the open arms, p < 0.001). SIF-ME-treated mice exhibited increased head dipping behavior and spent a longer time in the light box, confirming strong anxiolytic activity in the hole board and light–dark box tests, respectively. It (400 mg/kg) also significantly reduced depressive behavior during forced swimming and tail suspension tests (98.2 ± 3.83 s and 126.33 ± 1.20 s, respectively). The extract induced strong locomotor activity, causing mice’s mobility to gradually decrease over time in the open field and hole cross tests. The antipyretic effect of SIF-ME (400 mg/kg) was minimal using the yeast-induced pyrexia method, while it (100 μg/mL) killed T. tubifex in 69.33 ± 2.51 min, indicating a substantial anthelmintic action. SIF-ME significantly reduced blood clots by 67.74% (p < 0.001), compared to the control group’s 5.56%. The above findings have also been predicted by in silico molecular docking studies. According to the molecular docking studies, the extract’s constituents have binding affinities ranging from 0 to −10.2 kcal/mol for a variety of human target receptors, indicating possible pharmacological activity. Conclusions: These findings indicate that SIF-ME could serve as a promising natural source of compounds with neuropharmacological, anthelmintic, thrombolytic, and antipyretic properties. Full article
(This article belongs to the Section Drug Candidates from Natural Sources)
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19 pages, 496 KB  
Review
Targeting Oxidative Stress Biomarkers in Breast Cancer Development and the Potential Protective Effect of Phytochemicals
by Anchal Dubey and Bechan Sharma
Drugs Drug Candidates 2025, 4(2), 23; https://doi.org/10.3390/ddc4020023 - 23 May 2025
Cited by 3 | Viewed by 3524
Abstract
Breast cancer continues to represent one of the most widespread and lethal health afflictions on a global scale. The advancement of this malignancy is predominantly influenced by genetic mutations that precipitate unregulated cellular growth and proliferation, with oxidative stress being a crucial factor [...] Read more.
Breast cancer continues to represent one of the most widespread and lethal health afflictions on a global scale. The advancement of this malignancy is predominantly influenced by genetic mutations that precipitate unregulated cellular growth and proliferation, with oxidative stress being a crucial factor in all phases of carcinogenic development. Oxidative stress emerges from a disruption in the equilibrium between reactive oxygen species (ROS) and antioxidants, which inflicts damage on cellular components and facilitates the onset of cancer. Although numerous studies have advocated the notion that augmenting antioxidant levels may confer protection against cancer, other investigations have yielded contradictory results. Nevertheless, the effectiveness of antioxidants in cancer prophylaxis remains contentious, with research exhibiting variable outcomes. Certain studies have indicated that a high consumption of fruits and vegetables abundant in antioxidants may lower cancer risk. However, the irrefutable evidence is currently absent. Furthermore, the chemotherapeutic agents, such as taxanes and cisplatin, utilized in breast cancer management are reported to produce ROS as an integral aspect of their therapeutic mechanisms, thereby highlighting the intricate interplay between redox equilibrium and oncological treatment. This review emphasizes the pro-oxidant hypothesis, which asserts that heightened levels of ROS may selectively annihilate cancer cells, given that normal cells generally sustain low levels of ROS. Some recent reports have indicated that the application of plant-based molecules as a therapeutic supplement may help treat breast cancer effectively. However, a comprehensive understanding of the role of oxidative stress in breast cancer and use of antioxidants could pave the way for more precisely targeted therapeutic strategies aimed at the modulation of redox homeostasis. Full article
(This article belongs to the Section Drug Candidates from Natural Sources)
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18 pages, 2282 KB  
Review
Investigation into the Sleep-Promoting Effects of the Traditional Use of Passionflower (Passiflora spp.), Chamomile (Matricaria chamomilla L.) and Mulungu (Erythrina spp.) in Brazil
by Pedro Carvalho Araújo, Carolina Chaves Ramos and Daniela Barros de Oliveira
Drugs Drug Candidates 2025, 4(1), 11; https://doi.org/10.3390/ddc4010011 - 13 Mar 2025
Cited by 1 | Viewed by 17821
Abstract
Background/Objectives: Sleep is essential to human health, playing a vital role in physical and mental well-being. Sleep disorders can lead to significant health complications, such as cardiovascular problems, diabetes, obesity, and depression. In Brazil, plants such as passionflower (Passiflora spp.), chamomile ( [...] Read more.
Background/Objectives: Sleep is essential to human health, playing a vital role in physical and mental well-being. Sleep disorders can lead to significant health complications, such as cardiovascular problems, diabetes, obesity, and depression. In Brazil, plants such as passionflower (Passiflora spp.), chamomile (Matricaria chamomilla L.) and mulungu (Erythrina spp.) are widely used in folk medicine for their sleep-promoting properties. This article reviews the existing literature on the sleep-promoting effects of these plants, focusing on the Brazilian context and popular knowledge of their use. Methods: An integrative literature review was conducted, including scientific articles in English and Portuguese from PubMed, Scielo and Google Scholar databases. Ethnobotanical studies documenting the traditional use of these plants in Brazil and clinical and preclinical research on their sleep-promoting effects were included. Results: The juice and infusion of the leaves and fruits of passionflower are mainly used to treat anxiety and insomnia, chamomile flower tea is used for its sedative effects, and mulungu bark decoctions are used for their sedative and anxiolytic properties. These popular uses are supported by scientific studies demonstrating the efficacy of these plants in treating insomnia, anxiety, and stress. Conclusions: The recognition of traditional knowledge and the inclusion of these plants in RENISUS highlights their importance for public health in Brazil. However, more rigorous clinical trials are needed to confirm their efficacy and safety and ensure their safe integration into modern medicine. Full article
(This article belongs to the Section Drug Candidates from Natural Sources)
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19 pages, 904 KB  
Review
Tanacetum balsamita L.: Botany, Traditional Uses, Phytochemical Profiling, and Biological Activities
by Sohaib Khatib, Cecilia Faraloni and Latifa Bouissane
Drugs Drug Candidates 2025, 4(1), 10; https://doi.org/10.3390/ddc4010010 - 4 Mar 2025
Cited by 2 | Viewed by 3467
Abstract
Tanacetum balsamita is a perennial medicinal plant belonging to the Asteraceae family. The species bears a long history as a valuable traditional drug in different cultures, while it is an essential component in the traditional cuisine of several countries. In this context, our [...] Read more.
Tanacetum balsamita is a perennial medicinal plant belonging to the Asteraceae family. The species bears a long history as a valuable traditional drug in different cultures, while it is an essential component in the traditional cuisine of several countries. In this context, our literature review aims at providing a comprehensive overview of T. balsamita, covering its traditional uses, phytochemistry, biological activities, and toxicity from 1983 to 2024. Methods: Various databases were used to collect the information, including Scopus, Science Direct, Google Scholar, PubMed, and Web of Science. Results and conclusions: Although many of its traditional uses have gradually faded into obscurity over the centuries, recent decades have rekindled the interest in this species. Recent ethnobotanical surveys have reported the use of this species against various health-related conditions, while current pharmacological studies have corroborated several health benefits of the species, such as antioxidant, antidiabetic, anti-hyperpigmentation, anticancer, and antimicrobial activities. The validated properties are mainly attributed to the presence of multiple phytoconstituents belonging to flavonoids, phenolic acids, terpenes, and fatty acids, which could also indicate potential uses for T. balsamita in the food industry as a natural preservative and flavoring agent of food products. Full article
(This article belongs to the Section Drug Candidates from Natural Sources)
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51 pages, 1567 KB  
Systematic Review
Synergy, Additive Effects, and Antagonism of Drugs with Plant Bioactive Compounds
by Noureddine Chaachouay
Drugs Drug Candidates 2025, 4(1), 4; https://doi.org/10.3390/ddc4010004 - 5 Feb 2025
Cited by 68 | Viewed by 22633 | Correction
Abstract
Background/Objectives: The interaction of bioactive compounds derived from plants with drugs has become a significant area of investigation due to its potential to improve, reduce, or have no effect on therapeutic outcomes. Due to the dual effect of these interactions, elucidating the [...] Read more.
Background/Objectives: The interaction of bioactive compounds derived from plants with drugs has become a significant area of investigation due to its potential to improve, reduce, or have no effect on therapeutic outcomes. Due to the dual effect of these interactions, elucidating the underlying mechanisms is essential for establishing a therapeutic strategy. This study emphasizes the significant findings, mechanisms, and clinical implications of drug–plant bioactive interactions. It calls for more studies to seek safe and effective incorporation into clinical practice. Methods: To identify relevant studies, we performed a systematic literature search based on various scientific databases from 11 August 2024 to 30 December 2024. The search will be based on relevant keywords such as synergy, antagonism, plant bioactive compounds, and drug interactions supplemented with secondary terms such as phytochemicals, herb-drug interactions, pharmacokinetics, and pharmacodynamics. Results: Plant bioactives, including polyphenols, flavonoids, alkaloids, and terpenoids, display valuable biological activities that can interact with medications in three principal ways: synergy, additive effects, and antagonism. Synergy occurs when the combined effects of plant chemicals and pharmaceuticals outweigh the sum of their separate effects, increasing therapeutic effectiveness or allowing dosage decrease to reduce adverse effects. Additive effects occur when the combined impact equals the total individual effects, resulting in better outcomes without increasing risk. Antagonism occurs when a plant ingredient reduces or counteracts the effects of a medicine, thereby jeopardizing treatment. In addition, specific interactions may have no discernible effect. The chemical makeup of bioactive chemicals, medication pharmacokinetics, and individual patient characteristics such as genetics and metabolism all impact the intricacy of these interactions. Conclusions: Pharmacokinetics and pharmacodynamics of drugs can be considerably modulated through their interactions with plant bioactive components, which may cause a significant decrease in efficacy or increase in toxicity of therapeutic agents. More studies are needed to clarify mechanisms of action, prove clinical relevance, and create guidelines for safe co-administration. This integrative approach can mitigate those risks and allow for therapeutic optimization by introducing pharmacogenomics and personalized medicine approaches. Full article
(This article belongs to the Section Drug Candidates from Natural Sources)
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17 pages, 1303 KB  
Article
Extraction and Identification of Flavonoids from the Leaves of Pilocarpus microphyllus: Focus on Antioxidant Activity and Neuroprotective Profile
by Márcia Luana Gomes Perfeito, Fábio de Oliveira Silva Ribeiro, Joilson Ramos de Jesus, Leiz Maria Costa Véras, Alyne Rodrigues de Araújo Nobre, Everton Moraes Lopes, José Carlos Eloi de Queiroz, Andreanne Gomes Vasconcelos, Miguel Gomes Cardoso, João Gonçalves, Fernanda Regina de Castro Almeida, Daniel Dias Rufino Arcanjo and José Roberto de Souza de Almeida Leite
Drugs Drug Candidates 2024, 3(4), 796-812; https://doi.org/10.3390/ddc3040045 - 14 Nov 2024
Cited by 1 | Viewed by 3095
Abstract
This work is based on research aiming to extract and identify flavonoids from jaborandi (Pilocarpus microphyllus) leaves and investigate their antioxidant and acute antinociceptive capacity. Characterization of the constituents of the ethyl acetate fraction (EtOAcF) obtained from the methanolic extract (ME) [...] Read more.
This work is based on research aiming to extract and identify flavonoids from jaborandi (Pilocarpus microphyllus) leaves and investigate their antioxidant and acute antinociceptive capacity. Characterization of the constituents of the ethyl acetate fraction (EtOAcF) obtained from the methanolic extract (ME) was performed by UV-Vis spectrophotometry, infrared spectroscopy, high-performance liquid chromatography (HPLC), mass spectrometry (MS), and cyclic voltammetry, demonstrating the possible majority component of this fraction, the flavone chrysin. Its solubility properties in HPLC are very close to those of the flavonol quercetin, revealing the characteristic presence of this group. An MS spectrum of the fraction revealed a major protonated molecule of m/z 254.9 [M+H]+. The EtOAcF fraction showed three oxidation processes at 0.32 V, 0.54 V, and 0.73 V vs. Ag/AgCl. Three reduction processes at the respective potentials: 0.60 V, −0.03 V, and -0.24 V vs. Ag/AgCl, indicating potential antioxidant activity. At DPPH and ABTS antioxidant radical capture assay, The IC50 obtained was 0.5 mg/mL and 0.81 mg/mL, respectively. In vivo test to determine the mechanical nociceptive threshold in the von Frey test, the dose of 100 mg/kg of the EtOAcF was able to cause inhibition of behavioral changes in neuropathy. The results obtained in this study demonstrate the biological potential of an EtOAcF derived from jaborandi leaves. Full article
(This article belongs to the Section Drug Candidates from Natural Sources)
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Review
Pomolic Acid: Cancer Molecular Targets, Plant Extraction Yields and Availability
by Janaina Fernandes
Drugs Drug Candidates 2024, 3(4), 723-735; https://doi.org/10.3390/ddc3040041 - 29 Oct 2024
Viewed by 2312
Abstract
Pomolic acid (3-beta,19alpha-Dihydroxy-urs-12-en-28-oic acid, PA) is a naturally occurring pentacyclic triterpenoid. Derived from the mevalonate pathway through cyclization of 2,3-oxidosqualene, it has been widely found in several plant species. In the mid-1960s, PA was identified as the genuine aglycone of triterpenoid saponins from [...] Read more.
Pomolic acid (3-beta,19alpha-Dihydroxy-urs-12-en-28-oic acid, PA) is a naturally occurring pentacyclic triterpenoid. Derived from the mevalonate pathway through cyclization of 2,3-oxidosqualene, it has been widely found in several plant species. In the mid-1960s, PA was identified as the genuine aglycone of triterpenoid saponins from Sanguisorba officinalis, and studies on its biological activities began in 1989. Since then, several pharmacological properties have been described for this compound, including antitumoral activity. PA induced cell death in tumors, such as lung, brain, breast, and sensitive and resistant leukemia. Additionally, PA modulates resistant proteins and events involved in metastasis. Even though PA constitutes an important candidate for new treatment against several cancers, its availability hampers the evolution of PA studies toward clinical evaluation. This review discusses the limitations of PA availability, the recent approaches to improve it, and other aspects of the antitumoral studies on PA activity. Full article
(This article belongs to the Section Drug Candidates from Natural Sources)
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