Exploring Chemical Diversity of Phorbas Sponges as a Source of Novel Lead Compounds in Drug Discovery

Porifera, commonly referred to as marine sponges, are acknowledged as major producers of marine natural products (MNPs). Sponges of the genus Phorbas have attracted much attention over the years. They are widespread in all continents, and several structurally unique compounds have been identified from this species. Terpenes, mainly sesterterpenoids, are the major secondary metabolites isolated from Phorbas species, even though several alkaloids and steroids have also been reported. Many of these compounds have presented interesting biological activities. Particularly, Phorbas sponges have been demonstrated to be a source of cytotoxic metabolites. In addition, MNPs exhibiting cytostatic, antimicrobial, and anti-inflammatory activities have been isolated and structurally characterized. This review provides an overview of almost 130 secondary metabolites from Phorbas sponges and their biological activities, and it covers the literature since the first study published in 1993 until November 2021, including approximately 60 records. The synthetic routes to the most interesting compounds are briefly outlined.     

New 3-Acyl Tetramic Acid Derivatives from the Deep-Sea-Derived Fungus Lecanicillium fusisporum

Seven rare C3-C6 reduced 3-acyl tetramic acid derivatives, lecanicilliumins A–G (1–7), along with the known analogue cladosporiumin D (8), were obtained from the extract of the deep-sea-derived fungus Lecanicillium fusisporum GXIMD00542 within the family Clavipitacae. Their structures were elucidated by extensive spectroscopic data analysis, quantum chemistry calculations and chemical reaction. Compounds 1, 2, 5–7 exhibited moderate anti-inflammatory activity against NF-κB production using lipopolysaccharide (LPS) induced RAW264.7 cells with EC₅₀ values range of 18.49–30.19 μM.     

Functional Properties of the Marine Gastropod Molluscs Chicoreus ramosus and Babylonia spirata Collected from the Southern Coast of India

ABSTRACT

This study characterized the functional properties of ethyl acetate-methanol (EA-MeOH) and chloroform extracts of the muricid gastropod Chicoreus ramosus and buccinid Babylonia spirata. The EA-MeOH extract of B. spirata was a potent quencher of radical cation (IC₉₀ < 1 mg/mL), whereas that of C. ramosus held greater anti–inflammatory potential (IC₉₀ 5-lipoxygenase inhibition 1.74 mg/mL) than the buccinid gastropod. The EA-MeOH extract of C. ramosus displayed potent antidiabetic activities as deduced by its attenuation properties against carbolytic enzymes α-amylase and α-glycosidase (IC₉₀ 1.06 and 2.25 mg/mL, respectively) than those exhibited by B. spirata (IC₉₀ 2.32 and 4.50 mg/mL, respectively). The spectroscopic dereplication studies to determine probable chemical groups in the solvent extracts of the studied gastropods revealed the presence of functionalities, which might augment the electronic properties of the bioactive principles present within the extract, thereby enhancing their activity. Thus, the present study recognized that marine gastropods C. ramosus and B. spirata have potential functional implications against oxidative stress-induced diseases, such as diabetes and inflammation. This research supports further investigation of these previously uncharacterized marine gastropod species to isolate potential bioactive leads for use against various biological targets and to develop functional food formulations.     

燕麦抗动脉粥样硬化作用的研究进展

燕麦是全世界种植和食用的古老粮食作物之一,β-葡聚糖是燕麦中的主要活性化合物,燕麦还含有大量其他生物活性化合物,如酚酸、生育酚、燕麦蒽酰胺等。血浆中胆固醇水平升高、炎症反应和脂蛋白的氧化是动脉粥样硬化的特征。燕麦具有降低血浆总胆固醇和低密度脂蛋白胆固醇的作用,并且还具有抗炎、抗氧化以及保护内皮功能的作用;燕麦能够通过改善肠道菌群促进短链脂肪酸产生,加速胆固醇向胆汁酸的转化以降低全身胆固醇水平。研究证明,燕麦具有抗动脉粥样硬化的功效。对燕麦抗动脉粥样硬化作用进行综述,以期对后续研究提供参考。     

Effects of supplements containing turmeric and devil’s claw on equine gastric ulcer scores and gastric juice pH

Supplements containing turmeric (Curcuma longa) and devil’s claw (Harpagophytum species) are commonly fed to horses to decrease inflammation and pain, but because these supplements contain spices and plant irritants, warning labels such as 'these supplements might cause gastric irritation' are required. The purpose of this study was to determine whether supplements containing turmeric and devil’s claw cause or worsen gastric ulcers in stall-confined horses, as suggested in required cautions that appear on the labels of these animal products. Twelve clinically healthy Thoroughbred horses with naturally occurring equine gastric ulcer syndrome (EGUS) scores >0 were included in a noncrossover study design. Horses were stratified by EGUS score and assigned to either the treatment (supplements containing turmeric and devil’s claw) or control (same supplements without active ingredients) group and fed the supplements for 28 days. Gastroscopy was performed on Days 0, 14 and 28. The EGUS score, nonglandular ulcer number (NGN) and severity (NGS) scores, and glandular number (GN) and severity (GS) scores were recorded during each gastroscopy by a masked investigator (F.M.A.). In addition, bodyweight, gastric juice pH, packed cell volume (PCV), total protein (TP) and blood biochemical results were measured on Day 0 and Day 28. Mean EGUS and NGS scores were significantly lower in both treatment and control groups by Days 14 and 28, when compared to Day 0. NGN score was not different among groups. Bodyweight, gastric juice pH and blood parameters did not change during the study. In conclusion, supplements containing turmeric and devil’s claw did not cause or worsen gastric ulcers or alter health parameters after 28 days of feeding.     

香椿提取物对痛风抑制作用的初步研究

研究了香椿老叶提取物对痛风治疗过程中2种关键性酶(黄嘌呤氧化酶和环氧合酶-2)的抑制作用。结果表明,香椿提取物对黄嘌呤氧化酶有显著抑制功效,且呈剂量效应关系,其IC50为151.6μg/mL;香椿提取物对环氧合酶-2有明显的抑制作用(p<0.01),其IC50为2.66μg/mL,效果优于阳性对照。香椿提取物可有效降低尿酸水平,抑制环氧合酶-2的活性;香椿提取物具有较强的抗炎、抗痛风作用。     

Rare Chromone Derivatives from the Marine-Derived Penicillium citrinum with Anti-Cancer and Anti-Inflammatory Activities

Three new and rare chromone derivatives, epiremisporine C (1), epiremisporine D (2), and epiremisporine E (3), were isolated from marine-derived Penicillium citrinum, together with four known compounds, epiremisporine B (4), penicitrinone A (5), 8-hydroxy-1-methoxycarbonyl-6-methylxanthone (6), and isoconiochaetone C (7). Among the isolated compounds, compounds 2–5 significantly decreased fMLP-induced superoxide anion generation by human neutrophils, with IC₅₀ values of 6.39 ± 0.40, 8.28 ± 0.29, 3.62 ± 0.61, and 2.67 ± 0.10 μM, respectively. Compounds 3 and 4 exhibited cytotoxic activities with IC₅₀ values of 43.82 ± 6.33 and 32.29 ± 4.83 μM, respectively, against non-small lung cancer cell (A549), and Western blot assay confirmed that compounds 3 and 4 markedly induced apoptosis of A549 cells, through Bcl-2, Bax, and caspase 3 signaling cascades.     

Unravelling the Dermatological Potential of the Brown Seaweed Carpomitra costata

The ever-increasing interest in keeping a young appearance and healthy skin has leveraged the skincare industry. This, coupled together with the increased concern regarding the safety of synthetic products, has boosted the demand for new and safer natural ingredients. Accordingly, the aim of this study was to evaluate the dermatological potential of the brown seaweed Carpomitra costata. The antioxidant, anti-enzymatic, antimicrobial, photoprotective and anti-inflammatory properties of five C. costata fractions (F1–F5) were evaluated. The ethyl acetate fraction (F3) demonstrated the most promising results, with the best ability to scavenge 2,2-diphenyl-1-picrylhydrazyl (DPPH) radicals (EC₅₀ of 140.1 µg/mL) and the capacity to reduce reactive oxygen species (ROS) production promoted by UVA and UVB radiation in 3T3 cells, revealing its antioxidant and photoprotective potential. This fraction also exhibited the highest anti-enzymatic capacity, inhibiting the activities of collagenase, elastase and tyrosinase (IC₅₀ of 7.2, 4.8 and 85.9 µg/mL, respectively). Moreover, F3 showed anti-inflammatory potential, reducing TNF-α and IL-6 release induced by LPS treatment in RAW 264.7 cells. These bioactivities may be related to the presence of phenolic compounds, such as phlorotannins, as demonstrated by NMR analysis. The results highlight the potential of C. costata as a source of bioactive ingredients for further dermatological applications.     

Screening of In-Vitro Anti-Inflammatory and Antioxidant Activity of Sargassum ilicifolium Crude Lipid Extracts from Different Coastal Areas in Indonesia

Sargassum brown seaweed is reported to exhibit several biological activities which promote human health, such as anticancer, antimicrobial, antidiabetic, anti-inflammatory, and antioxidant activity. This study aimed to investigate the anti-inflammatory and antioxidant activity of crude lipid extracts of Sargassum ilicifolium obtained from four different coastal areas in Indonesia, namely Awur Bay–Jepara (AB), Pari Island–Seribu Islands (PI), Sayang Heulang Beach–Garut (SHB), and Ujung Genteng Beach–Sukabumi (UGB). Results showed that treatment of RAW 264.7 macrophage cells with UGB and AB crude lipid extracts (12.5–50 µg/mL) significantly suppressed the nitric oxide production after lipopolysaccharide stimulation, both in pre-incubated and co-incubated cell culture model. The anti-inflammatory effect was most marked in the pre-incubated cell culture model. Both two crude lipid extracts showed 2,2-diphenyl-1-picrylhydrazyl radical scavenging activity and high ferric reducing antioxidant power, which were amounted to 36.93–37.87 µmol Trolox equivalent/g lipid extract and 681.58–969.81 µmol FeSO₄/g lipid extract, respectively. From this study, we can conclude that crude lipid extract of tropical S. ilicifolium can be further developed as a source of anti-inflammatory and antioxidant agent.