- New
- Research Article
- 10.2174/0118715257459303260414165015
- Jun 30, 2026
- Cardiovascular & hematological agents in medicinal chemistry
- Bassil Aljallah + 2 more
Antihypertensive treatments, including diuretics and beta/calcium channel blockers, are associated with a range of adverse effects. Naturally sourced ACE inhibitors may serve as viable alternatives to synthetic medications. Various peptides derived from plants have been assessed for their ACE inhibitory properties through both in vivo and in vitro studies. The objective of this research was to evaluate the ACE inhibitory activity of seed-protein (muskmelon, watermelon, and sunflower) hydrolysates generated using different proteases. ACE was extracted from sheep lung tissue, while protein from the mentioned seeds was isolated and hydrolysed using pepsin, trypsin, and crude enzyme from the stem of Wrightia tinctoria. Tricine-SDS PAGE (16%) was conducted to observe the nature of hydrolysis. The method by Cushman and Cheung was used to examine ACE inhibition. The results were compared across different sources and enzymatic treatments. Muskmelon hydrolysate treated with W. tinctoria enzyme exhibited the highest ACE inhibition at 85.17% ± 0.39 after 3 h of incubation (p <0.001), resembling the inhibitory effects observed in the positive control, Lisinopril, at 86.55% ± 1.15. The enhanced ACE inhibitory activity observed in muskmelon seed hydrolysate suggests the generation of potent bioactive peptides through enzymatic hydrolysis. Differences in inhibitory potential among seed-derived hydrolysates may be attributed to variations in protein composition and peptide profiles resulting from the use of different proteases. Muskmelon seed protein hydrolysate generated using W. tinctoria demonstrated strong in vitro ACE inhibitory activity, which was comparable to that of Lisinopril, a standard drug for ACE inhibition. These findings highlight its potential as a natural source of bioactive peptides for the management of hypertension.
- Research Article
- 10.2174/0118715257459408260428075542
- May 13, 2026
- Cardiovascular & hematological agents in medicinal chemistry
- Rami A Al-Horani
Introduction:Thrombosis remains a major global health burden, necessitating safer and more effective antithrombotic strategies. Current therapies, including vitamin K antagonists, heparin derivatives, and direct oral anticoagulants, are limited by bleeding risks despite the availability of reversal agents. Factor XIa (FXIa), a serine protease in the intrinsic coagulation pathway, has emerged as a promising target due to its central role in thrombosis while having minimal impact on hemostasis. Previous studies identified Sulfated Pentagalloyl Glucopyranose (SPGG) as a potent, selective, but heterogeneous allosteric inhibitor of FXIa. The study aimed to design and synthesize a chemically homogeneous derivative of SPGG (inhibitor 2) and to evaluate its potency, selectivity, and effect on human plasma coagulation, to identify a potentially safer FXIa-targeted anticoagulant candidate.Methods:To address the heterogeneity of SPGG, inhibitor 2, a per-sulfated, chemically homogeneous derivative, was designed and synthesized through a three-step synthetic route. The inhibitory activity of inhibitor 2 against FXIa was evaluated, along with its selectivity against thrombin and FXa. Furthermore, its effect on human plasma coagulation was assessed by measuring the Activated Partial Thromboplastin Time (APTT).Results:Inhibitor 2 demonstrated potent inhibition of FXIa with an IC50 of 1.42 ± 0.10 μM and showed marked selectivity over thrombin and FXa. Treatment with inhibitor 2 significantly prolonged the APTT of human plasma, indicating effective modulation of the intrinsic coagulation pathway.Discussion:Inhibitor 2 overcomes the chemical heterogeneity of SPGG while retaining strong selectivity for FXIa over thrombin and FXa. It effectively prolongs APTT with minimal effect on PT, indicating selective targeting of the intrinsic pathway. These results demonstrate that chemical homogeneity can be achieved without compromising functional selectivity.Conclusion:Inhibitor 2 represents a chemically homogeneous, selective, and potent FXIa inhibitor. These findings support its potential as a lead candidate for the development of FXIa-targeted anticoagulants with a potentially reduced bleeding risk.
- Research Article
- 10.2174/0118715257394272251111130754
- May 6, 2026
- Cardiovascular & hematological agents in medicinal chemistry
- Zahra Tolou-Ghamari
Alterations in the pharmacokinetics or pharmacodynamics of a drug could be the result of interaction with nutritional elements or due to the nutritional status of patients. This review summarizes the findings of previous studies on the interaction between the most prescribed drugs and food variables. From the commencement of databases related to the topic of interest to January 2024, all relevant articles were searched in PubMed, Scopus, and Web of Science. Milk, grapefruit juice, or alcohol could lead to specific food-drug interactions. Patients who require surgery should refrain from using ginseng for at least a week prior to the operation. The interaction of drugs, such as carbamazepine with capsaicin, saquinavir with garlic, and warfarin with ginkgo biloba, needs vigilant attention. Among epileptic patients, in those taking phenobarbital and phenytoin, due to an increase in the metabolism of vitamin D, supplementation of vital minerals might be optional. The curcumin's effect in patients with doxorubicin, due to the modulation of cellular pathways (P-glycoproteins, other ABC transporters), could be complex. Interactions between drug and food variables could cause an alteration in drug efficiency or toxicity due to changes in drug transporters. Attention to the induction or inhibition of cytochrome P450 by food content could help mitigate the risk of unwanted side effects. The population of elderly, patients on drugs with patients on drugs with a narrow therapeutic window, pregnant women, and children needs more attention. To better assess the benefit-risk relationship, a full and comprehensive dietary recall, including simultaneous intake of drugs and food, is recommended.
- Research Article
- 10.2174/0118715257410908251210084136
- May 4, 2026
- Cardiovascular & hematological agents in medicinal chemistry
- Shivam Kumar + 4 more
Elranatamab, an IgG2 bispecific antibody targeting B-cell maturation antigen (BCMA) and CD3 on T cells, is a promising therapeutic option for relapsed or refractory multiple myeloma (RRMM), a hematologic malignancy with limited therapeutic options to date. Elranatamab represents a therapeutic breakthrough in the management of patients with RRMM. Bispecific antibodies targeting cytotoxic immune effector cells (including T cells) and malignant plasma cells have demonstrated a high response rate, especially in patients with penta-refractory disease. Elranatamab activates T cells, which mount a targeted and deadly attack on myeloma cells, leading to a more targeted treatment of the disease. Clinical trials showed encouraging efficacy in heavily pretreated patients, with impressive responses and an acceptable safety profile, including manageable cytokine release syndrome (CRS) and other immune-related adverse effects. Despite these recent advances that have accelerated progress, multiple myeloma remains an incurable disease, and patients often relapse with resistance to available treatments. With the evolving treatment landscape for multiple myeloma, informed by recent clinical trial data and new combination regimens, these drugs may play a crucial role in overcoming drug resistance and improving long-term patient survival.
- Research Article
- 10.2174/0118715257457865260428052651
- Apr 29, 2026
- Cardiovascular & hematological agents in medicinal chemistry
- Ezekiel Etim Ben + 4 more
Leucocytosis, inflammation, and thrombocytosis are major risk factors for diabetes mellitus. This study investigates the effects of administering aspirin, meloxicam, or Terminalia catappa leaf extract on leucocyte count and platelet indices in patients with Diabetes Mellitus (DM). Male Wistar rats were randomly assigned to seven groups of six rats each. The control group received 5 ml/kg of distilled water orally, while the DM was induced with 150 mg/Kg alloxan. The DM+ Terminalia Catappa (TC) group was administered 130 mg/kg, while the DM+Aspirin and DM+Meloxicam groups were administered aspirin (30 mg/kg) and meloxicam (2 mg/kg) orally, respectively. DM+TC+Aspirin and DM+TC+Meloxicam groups received Terminalia catappa in addition to aspirin and meloxicam, respectively, for 14 days. Total WBC, neutrophil and eosinophil counts, tumour necrosis factor-α and interleukin-6 increased significantly (p <0.05), while lymphocytes, monocytes, platelet counts, and platelet indices decreased significantly (p <0.05) in the diabetic group. The raised parameters were significantly (p <0.05) reduced by aspirin, meloxicam, and Terminalia catappa extract compared with the diabetic control group. They were also significantly (p <0.05) reduced in DM-treated with extract and aspirin. Platelet counts and MPV were raised (p < 0.05) in the T. catappa, aspirin, and meloxicam + extract groups compared to the control and diabetic groups. T. catappa extract and aspirin ameliorated inflammation due to their active phytochemicals. Extract of Terminalia catappa, in combination with aspirin, reduced WBC count but increased platelet indices. This indicates the potential of the extract to reduce inflammation in diabetes mellitus, but with the risk of thrombocytosis.
- Research Article
- 10.2174/0118715257414596251206101856
- Apr 7, 2026
- Cardiovascular & hematological agents in medicinal chemistry
- Vikrant Verma
The endothelium forms the inner vital lining of blood vessels and controls vascular tone, hemostasis, and inflammation, maintaining cardiovascular homeostasis. Endothelial dysfunction, characterized by abnormal vasodilation, increased oxidative stress, and decreased nitric oxide bioavailability, is a key pathophysiological mechanism underlying many cardiovascular diseases. The review examines current approaches for addressing endothelial dysfunction in various disease states, with a special emphasis on cardiovascular disease, rheumatoid arthritis, and diabetes mellitus. We performed a thorough review of the literature on studies that investigated interventions for endothelial dysfunction in cardiovascular diseases, rheumatoid arthritis, and diabetes mellitus. Mechanisms of action, clinical effectiveness, and novel strategies were the primary focus of data extraction. Well-established therapies such as statins, ACE inhibitors, and antihypertensive drugs show robust benefits in enhancing endothelial function through antiinflammatory, antioxidant, and vasodilatory actions. Novel therapies targeting molecular pathways such as the NLRP3 inflammasome, YAP/TAZ signaling, and microRNA modulation have shown promising results in preclinical and early-stage clinical trials. Emerging drugs such as resveratrol, astragaloside IV, and SGLT-2 inhibitors also demonstrate favorable effects on endothelial function via various mechanisms. Non-pharmacological lifestyle interventions, including exercise and caloric restriction, provide complementary benefits, especially when used alongside pharmacotherapy. Endothelial dysfunction is a critical modifiable target in many disease states. Although traditional cardiovascular medications remain the cornerstone of treatment, novel targeted therapies and combination strategies are promising approaches to enhance endothelial function and reduce cardiovascular morbidity and mortality. Personalized treatments based on individual patients' specific pathophysiological mechanisms underlying their endothelial dysfunction should be the research focus in the future.
- Research Article
- 10.2174/0118715257437339260225060708
- Apr 1, 2026
- Cardiovascular & hematological agents in medicinal chemistry
- Harshal S Mehta + 6 more
Hyperlipidemia-a metabolic disorder characterized by elevated levels of lipids such as cholesterol and triglycerides in the blood-is a growing global public health concern. It encompasses hypercholesterolemia, hypertriglyceridemia, mixed hyperlipidemia, and altered high-density lipoprotein levels, and is a major risk factor for cardiovascular diseases (CVD), stroke, and metabolic syndrome. Atorvastatin, an FDA-approved HMG-CoA reductase inhibitor, is widely used to manage dyslipidemia and reduce the risk of cardiovascular events. Despite its effectiveness, atorvastatin is occasionally associated with adverse effects, including hepatic dysfunction, muscle-related symptoms, cognitive impairment, and insulin resistance. This has encouraged interest in adjunctive therapies using natural dietary components that may enhance lipid-lowering efficacy and mitigate side effects. This narrative review explores the emerging evidence on plant-based dietary supplements-such as green tea polyphenols, grape seed extract, Fructus schisandrae, isabgol, Phoenix dactylifera, plant sterols, polyphenol extracts, Salvia officinalis, Zingiber officinale (ginger), and legumes like horse gram and groundnut-and their synergistic potential when co-administered with atorvastatin. These natural agents exhibit a range of beneficial properties, including hypolipidemic, antioxidant, antiinflammatory, hepatoprotective, and cardioprotective effects. Studies demonstrate that combining atorvastatin with these dietary agents can enhance lipid profile improvement, reduce oxidative stress, and alleviate drug-induced organ toxicity. Notably, legumes such as horse gram and groundnut show promise in modulating lipid metabolism and inflammatory markers. Clinical trials are necessary to establish standardized doses, treatment durations, and safety profiles for wider human benefit.
- Research Article
- 10.2174/0118715257417253260129223400
- Mar 26, 2026
- Cardiovascular & hematological agents in medicinal chemistry
- Sreevani Mitta + 6 more
Anaemia is the term for low red blood cell numbers or a deficiency of hemoglobin, the protein that carries oxygen in red blood cells. This results in a reduction of oxygen-carrying capacity of blood to various tissues in the body, & lead to symptoms like weakness and exhaustion. There are various forms of anaemia, and they all have unique reasons. The main purpose of the review is to outline the types of anaemia and highlight the potential of artificial intelligence (AI) and machine learning (ML) tools in detection. There is high accuracy in identifying anaemia by using AI and ML tools that include analyzing the laboratory parameters and medical imaging. There are various Machine learning tools to identify anaemia in the past and treat anaemia by using AI tools. Promising approaches for effective anemia identification and treatment are offered by AI-assisted methods. By incorporating these advancements into clinical practice, the burden of undetected or improperly managed anemia could be lessened, and patient outcomes could be improved.
- Research Article
- 10.2174/0118715257423396260126091907
- Mar 25, 2026
- Cardiovascular & hematological agents in medicinal chemistry
- Samman + 7 more
Approximately 422 million individuals worldwide have been diagnosed with Diabetes Mellitus (DM), a severe metabolic disorder, within the last 30 years. The chemical pharmacology of bexagliflozin, the most recent SGLT-2i, has been investigated as a possible treatment for diabetes associated with type 2 (T2DM). Gliflozin Dapagliflozin (DAPA), canagliflozin, and bexgliflozin act by blocking the SGLT-2 protein present in both kidneys and induce the excretion of glucose in the form of urine by decreasing its reabsorption. This potentially effective treatment approach for T2DM has additional benefits, such as weight loss and cardiovascular protection. Similar to canagliflozin or dapagliflozin, explicitly, bexagliflozin is very specific and powerful for SGLT-2 inhibition. In 2023, the FDA granted approval for this medication. The levels of glucose in the blood are significantly lowered as a result of blocking the kidney's proximal tubule from reabsorbing glucose. This study draws attention to the structural advantages of bexagliflozin. Notably, the aryl C-glycoside bond with D-glucopyranose makes this drug exhibit increased metabolic stability and distinguish itself from other gliflozins. It elaborates on advantageous A.D.M.E properties, further efficiency in lowering HbA1c levels, contributing towards weight loss, and improvement of cardiovascular and renal outcomes, mainly among patients suffering from type 2 diabetes and comorbid CKD or cardiovascular risks. It also reviews key clinical trials by focusing on its safety with manageable side effects such as urinary tract infections. Overall, a comprehensive analysis has underlined the potential of bexagliflozin as a preferred treatment in diabetes management.
- Research Article
- 10.2174/0118715257406953251203092804
- Mar 19, 2026
- Cardiovascular & hematological agents in medicinal chemistry
- Pouya Yousefli + 5 more
The objective of this study was to compare the prophylactic efficacy of enoxaparin, dabigatran, and rivaroxaban in ambulatory patients with cancer. In this randomized trial, patients were assigned to three groups: Group 1 received subcutaneous enoxaparin 40 mg daily (n = 35), Group 2 received oral dabigatran 150 mg daily (n = 11), and Group 3 received oral rivaroxaban 10 mg daily (n = 11) for a duration of three months. The primary outcomes were the incidence of Venous Thromboembolism (VTE) and bleeding events. The incidence of VTE was 2 (3.5%) in patients receiving enoxaparin and 1 (1.7%) in those receiving dabigatran (P > 0.05). No thromboembolic events were reported in patients administered rivaroxaban. One patient (1.7%) in the enoxaparin group experienced a major bleeding episode (P > 0.05), while no major bleeding events were observed in patients receiving dabigatran or rivaroxaban. Enoxaparin, dabigatran, and rivaroxaban are widely used for the prevention of VTE in patients with cancer. Although some previous studies have reported differences in bleeding and VTE risk, the present study did not demonstrate significant differences among enoxaparin, dabigatran, and rivaroxaban in VTE prevention. Notably, the risk of VTE is substantially influenced by the type of cancer, the modalities of anticancer treatment, and the patient's clinical status. The efficacy and safety of enoxaparin, dabigatran, and rivaroxaban for the prevention of VTE in patients with cancer appear to be comparable. Iranian Registry of Clinical Trials (IRCT20200407046984N1).