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11 pages, 2269 KiB

Open AccessArticle

4-(Phenylsulfanyl) Butan-2-One Attenuates the Inflammatory Response Induced by Amyloid-β Oligomers in Retinal Pigment Epithelium Cells

by Peeraporn Varinthra, Shun-Ping Huang, Supin Chompoopong, Zhi-Hong Wen and Ingrid Y. Liu

Mar. Drugs 2021, 19(1), 1; https://doi.org/10.3390/md19010001 - 23 Dec 2020

Cited by 6 | Viewed by 2796

Abstract

Age-related macular degeneration (AMD) is a progressive eye disease that causes irreversible impairment of central vision, and effective treatment is not yet available. Extracellular accumulation of amyloid-beta (Aβ) in drusen that lie under the retinal pigment epithelium (RPE) has been reported as one [...] Read more.

Age-related macular degeneration (AMD) is a progressive eye disease that causes irreversible impairment of central vision, and effective treatment is not yet available. Extracellular accumulation of amyloid-beta (Aβ) in drusen that lie under the retinal pigment epithelium (RPE) has been reported as one of the early signs of AMD and was found in more than 60% of Alzheimer’s disease (AD) patients. Extracellular deposition of Aβ can induce the expression of inflammatory cytokines such as IL-1β, TNF-α, COX-2, and iNOS in RPE cells. Thus, finding a compound that can effectively reduce the inflammatory response may help the treatment of AMD. In this research, we investigated the anti-inflammatory effect of the coral-derived compound 4-(phenylsulfanyl) butan-2-one (4-PSB-2) on Aβ_1-42 oligomer (oAβ_1-42) added to the human adult retinal pigment epithelial cell line (ARPE-19). Our results demonstrated that 4-PSB-2 can decrease the elevated expressions of TNF-α, COX-2, and iNOS via NF-κB signaling in ARPE-19 cells treated with oAβ_1-42 without causing any cytotoxicity or notable side effects. This study suggests that 4-PSB-2 is a promising drug candidate for attenuation of AMD. Full article

(This article belongs to the Special Issue Marine Compounds and Inflammation II)

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13 pages, 2118 KiB

Open AccessArticle

Anti-Neuroinflammatory Agent, Restricticin B, from the Marine-Derived Fungus Penicillium janthinellum and Its Inhibitory Activity on the NO Production in BV-2 Microglia Cells

by Byeoung-Kyu Choi, Song-Hee Jo, Dong-Kug Choi, Phan Thi Hoai Trinh, Hwa-Sun Lee, Van Anh Cao, Tran Thi Thanh Van and Hee Jae Shin

Mar. Drugs 2020, 18(9), 465; https://doi.org/10.3390/md18090465 - 14 Sep 2020

Cited by 8 | Viewed by 2850

Abstract

A new compound containing a triene, a tetrahydropyran ring and glycine ester functionalities, restricticin B (1), together with four known compounds (2–5) were obtained from the EtOAc extract of the marine-derived fungus Penicillium janthinellum. The planar [...] Read more.

A new compound containing a triene, a tetrahydropyran ring and glycine ester functionalities, restricticin B (1), together with four known compounds (2–5) were obtained from the EtOAc extract of the marine-derived fungus Penicillium janthinellum. The planar structure of 1 was determined by detailed analyses of MS, 1D and 2D NMR data. The relative and absolute configurations of 1 were established via the analyses of NOESY spectroscopy data, the comparison of optical rotation values with those of reported restricticin derivatives and electronic circular dichroism (ECD). All the compounds were screened for their anti-neuroinflammatory effects in lipopolysaccharide (LPS)-induced BV-2 microglia cells. Restricticin B (1) and N-acetyl restricticin (2) exhibited anti-neuroinflammatory effects by suppressing the production of pro-inflammatory mediators in activated microglial cells. Full article

(This article belongs to the Special Issue Marine Compounds and Inflammation II)

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12 pages, 4837 KiB

Open AccessArticle

Sponge-Derived 24-Homoscalaranes as Potent Anti-Inflammatory Agents

by Bo-Rong Peng, Kuei-Hung Lai, Yu-Chia Chang, You-Ying Chen, Jui-Hsin Su, Yusheng M. Huang, Po-Jen Chen, Steve Sheng-Fa Yu, Chang-Yih Duh and Ping-Jyun Sung

Mar. Drugs 2020, 18(9), 434; https://doi.org/10.3390/md18090434 - 19 Aug 2020

Cited by 9 | Viewed by 2625

Abstract

Scalarane-type sesterterpenoids are known for their therapeutic potential in cancer treatments. However, the anti-inflammatory properties of this class of metabolites remain elusive. Our current work aimed to investigate the anti-inflammatory scalaranes from marine sponge Lendenfeldia sp., resulting in the isolation of six new [...] Read more.

Scalarane-type sesterterpenoids are known for their therapeutic potential in cancer treatments. However, the anti-inflammatory properties of this class of metabolites remain elusive. Our current work aimed to investigate the anti-inflammatory scalaranes from marine sponge Lendenfeldia sp., resulting in the isolation of six new 24-homoscalaranes, lendenfeldaranes E–J (1–6). The structures of the new metabolites were determined by extensive spectroscopic analyses, and the absolute configuration of 1 was established by electronic circular dichroism (ECD) calculations. Compounds 2 and 3 were discovered to individually reduce the generation of superoxide anions, and compound 1 displayed an inhibitor effect on the release of elastase. These three compounds were proven to be the first anti-neutrophilic scalaranes. Full article

(This article belongs to the Special Issue Marine Compounds and Inflammation II)

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10 pages, 3422 KiB

Open AccessArticle

Briarenols Q–T: Briaranes from A Cultured Octocoral Briareum stechei (Kükenthal, 1908)

by Yi-Lin Zhang, Chih-Chao Chiang, Yi-Ting Lee, Zhi-Hong Wen, Yang-Chang Wu, Yu-Jen Wu, Tsong-Long Hwang, Tung-Ying Wu, Chia-Yuan Chang and Ping-Jyun Sung

Mar. Drugs 2020, 18(8), 383; https://doi.org/10.3390/md18080383 - 24 Jul 2020

Cited by 5 | Viewed by 2097

Abstract

Our continuous chemical study of a cultured octocoral Briareum stechei led to the isolation of four new briarane diterpenoids, briarenols Q–T (1–4). The structures of new metabolites 1–4 were established by spectroscopic methods, and compounds 3 and [...] Read more.

Our continuous chemical study of a cultured octocoral Briareum stechei led to the isolation of four new briarane diterpenoids, briarenols Q–T (1–4). The structures of new metabolites 1–4 were established by spectroscopic methods, and compounds 3 and 4 were found to inhibit the generation of inducible nitric oxide synthase (iNOS) from RAW 264.7 stimulated by lipopolysaccharides (LPS). Full article

(This article belongs to the Special Issue Marine Compounds and Inflammation II)

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22 pages, 6708 KiB

Open AccessArticle

Modulation of Glial Responses by Furanocembranolides: Leptolide Diminishes Microglial Inflammation in Vitro and Ameliorates Gliosis In Vivo in a Mouse Model of Obesity and Insulin Resistance

by Miriam Corraliza-Gómez, Amalia B. Gallardo, Ana R. Díaz-Marrero, José M. de la Rosa, Luis D’Croz, José Darias, Eduardo Arranz, Irene Cózar-Castellano, María D. Ganfornina and Mercedes Cueto

Mar. Drugs 2020, 18(8), 378; https://doi.org/10.3390/md18080378 - 22 Jul 2020

Cited by 2 | Viewed by 2989

Abstract

Neurodegenerative diseases are age-related disorders caused by progressive neuronal death in different regions of the nervous system. Neuroinflammation, modulated by glial cells, is a crucial event during the neurodegenerative process; consequently, there is an urgency to find new therapeutic products with anti-glioinflammatory properties. [...] Read more.

Neurodegenerative diseases are age-related disorders caused by progressive neuronal death in different regions of the nervous system. Neuroinflammation, modulated by glial cells, is a crucial event during the neurodegenerative process; consequently, there is an urgency to find new therapeutic products with anti-glioinflammatory properties. Five new furanocembranolides (1−5), along with leptolide, were isolated from two different extracts of Leptogorgia sp., and compound 6 was obtained from chemical transformation of leptolide. Their structures were determined based on spectroscopic evidence. These seven furanocembranolides were screened in vitro by measuring their ability to modulate interleukin-1β (IL-1β) production by microglial BV2 cells after LPS (lipopolysaccharide) stimulation. Leptolide and compounds 3, 4 and 6 exhibited clear anti-inflammatory effects on microglial cells, while compound 2 presented a pro-inflammatory outcome. The in vitro results prompted us to assess anti-glioinflammatory effects of leptolide in vivo in a high-fat diet-induced obese mouse model. Interestingly, leptolide treatment ameliorated both microgliosis and astrogliosis in this animal model. Taken together, our results reveal a promising direct biological effect of furanocembranolides on microglial cells as bioactive anti-inflammatory molecules. Among them, leptolide provides us a feasible therapeutic approach to treat neuroinflammation concomitant with metabolic impairment. Full article

(This article belongs to the Special Issue Marine Compounds and Inflammation II)

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12 pages, 18880 KiB

Open AccessArticle

Topical Application of Phlorotannins from Brown Seaweed Mitigates Radiation Dermatitis in a Mouse Model

by Kyungmi Yang, Shin-Yeong Kim, Ji-Hye Park, Won-Gyun Ahn, Sang Hoon Jung, Dongruyl Oh, Hee Chul Park and Changhoon Choi

Mar. Drugs 2020, 18(8), 377; https://doi.org/10.3390/md18080377 - 22 Jul 2020

Cited by 12 | Viewed by 3964

Abstract

Radiation dermatitis (RD) is one of the most common side effects of radiotherapy; its symptoms progress from erythema to dry and moist desquamation, leading to the deterioration of the patients’ quality of life. Active metabolites in brown seaweed, including phlorotannins (PTNs), show anti-inflammatory [...] Read more.

Radiation dermatitis (RD) is one of the most common side effects of radiotherapy; its symptoms progress from erythema to dry and moist desquamation, leading to the deterioration of the patients’ quality of life. Active metabolites in brown seaweed, including phlorotannins (PTNs), show anti-inflammatory activities; however, their medical use is limited. Here, we investigated the effects of PTNs in a mouse model of RD in vivo. X-rays (36 Gy) were delivered in three fractions to the hind legs of BALB/c mice. Macroscopic RD scoring revealed that PTNs significantly mitigated RD compared with the vehicle control. Histopathological analyses of skin tissues revealed that PTNs decreased epidermal and dermal thickness compared with the vehicle control. Western blotting indicated that PTNs augmented nuclear factor erythroid 2-related factor 2 (NRF2)/heme oxygenase-1 (HO-1) pathway activation but attenuated radiation-induced NF-κB (nuclear factor kappa-light-chain-enhancer of activated B cells) and inflammasome activation, suggesting the mitigation of acute inflammation in irradiated mouse skin. PTNs also facilitated fast recovery, as indicated by increased aquaporin 3 expression and decreased γH2AX (histone family member X) expression. Our results indicate that topical PTN application may alleviate RD symptoms by suppressing oxidative stress and inflammatory signaling and by promoting the healing process. Therefore, PTNs may show great potential as cosmeceuticals for patients with cancer suffering from radiation-induced inflammatory side effects such as RD. Full article

(This article belongs to the Special Issue Marine Compounds and Inflammation II)

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15 pages, 2075 KiB

Open AccessArticle

Meroterpenoids from the Brown Alga Cystoseira usneoides as Potential Anti-Inflammatory and Lung Anticancer Agents

by Hanaa Zbakh, Eva Zubía, Carolina de los Reyes, José M. Calderón-Montaño, Miguel López-Lázaro and Virginia Motilva

Mar. Drugs 2020, 18(4), 207; https://doi.org/10.3390/md18040207 - 11 Apr 2020

Cited by 16 | Viewed by 4101

Abstract

The anti-inflammatory and anticancer properties of eight meroterpenoids isolated from the brown seaweed Cystoseira usneoides have been evaluated. The algal meroterpenoids (AMTs) 1–8 were tested for their inhibitory effects on the production of the pro-inflammatory cytokines tumor necrosis factor (TNF-α), interleukin-6 (IL-6), and [...] Read more.

The anti-inflammatory and anticancer properties of eight meroterpenoids isolated from the brown seaweed Cystoseira usneoides have been evaluated. The algal meroterpenoids (AMTs) 1–8 were tested for their inhibitory effects on the production of the pro-inflammatory cytokines tumor necrosis factor (TNF-α), interleukin-6 (IL-6), and interleukin-1β (IL-1β), and the expression of cyclooxygenase-2 (COX-2), and inducible nitric oxide synthase (iNOS) in LPS-stimulated THP-1 human macrophages. The anticancer effects were assessed by cytotoxicity assays against human lung adenocarcinoma A549 cells and normal lung fibroblastic MRC-5 cells, together with flow cytometry analysis of the effects of these AMTs on different phases of the cell cycle. The AMTs 1–8 significantly reduced the production of TNF-α, IL-6, and IL-1β, and suppressed the COX-2 and iNOS expression, in LPS-stimulated cells (p < 0.05). The AMTs 1–8 displayed higher cytotoxic activities against A549 cancer cells than against MRC-5 normal lung cells. Cell cycle analyses indicated that most of the AMTs caused the arrest of A549 cells at the G2/M and S phases. The AMTs 2 and 5 stand out by combining significant anti-inflammatory and anticancer activities, while 3 and 4 showed interesting selective anticancer effects. These findings suggest that the AMTs produced by C. usneoides may have therapeutic potential in inflammatory diseases and lung cancer. Full article

(This article belongs to the Special Issue Marine Compounds and Inflammation II)

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Review

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14 pages, 3950 KiB

Open AccessReview

Biological Activities of Rhamnan Sulfate Extract from the Green Algae Monostroma nitidum (Hitoegusa)

by Koji Suzuki and Masahiro Terasawa

Mar. Drugs 2020, 18(4), 228; https://doi.org/10.3390/md18040228 - 24 Apr 2020

Cited by 21 | Viewed by 7456

Abstract

Monostroma nitidum is a green single-cell layered algae that grows on the southwest coast of Japan. It is often used for salad ingredients, boiled tsukudani, soups, etc., due to its health benefits. M. nitidum is composed of many cell aggregates, and the various [...] Read more.

Monostroma nitidum is a green single-cell layered algae that grows on the southwest coast of Japan. It is often used for salad ingredients, boiled tsukudani, soups, etc., due to its health benefits. M. nitidum is composed of many cell aggregates, and the various substances that fill the intercellular space are dietary fibers, vitamins, and minerals. Rhamnan sulfate (RS), a sulfated polysaccharide, is main the component of the fiber extracted from M. nitidum. Recently, some biological properties of RS have been demonstrated by in vitro and in vivo studies that probably protect human subjects from viruses and ameliorate vascular dysfunction caused by metabolic disorders, especially lifestyle-related diseases. In this review, we focus on the antithrombotic effects of RS and introduce its antiviral and other biological activities. Full article

(This article belongs to the Special Issue Marine Compounds and Inflammation II)

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