Article
Pharmacology & Pharmacy
Sajid Jalal, Ting Zhang, Jia Deng, Jie Wang, Ting Xu, Tianhua Zhang, Chuanxin Zhai, Ruqiang Yuan, Hongming Teng, Lin Huang
Summary: This study found that LXX-8250 treatment can induce apoptosis in melanoma cells by inhibiting autophagic flux and glycolysis. This effect is mediated by suppression of PFKFB4 expression. The research provides a novel strategy for the treatment of melanoma.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Jae-Han Lee, Eun-Seon Yoo, So-Hee Han, Gi-Hwan Jung, Eun-Ji Han, Eun-Young Choi, Su-Ji Jeon, Soo-Hyun Jung, BumSeok Kim, Sung-Dae Cho, Jeong-Seok Nam, Changsun Choi, Jeong-Hwan Che, Ji-Youn Jung
Summary: This study investigated the anticancer effects of Chrysin in human melanoma cells and found that it can inhibit cell viability by inducing apoptosis and autophagy. The response to autophagy varies in different cell types, and Chrysin also affects the mTOR/S6K pathway.
Article
Cell Biology
Jakub Rok, Justyna Kowalska, Zuzanna Rzepka, Dominika Stencel, Anna Skorek, Klaudia Banach, Dorota Wrzesniok
Summary: Melanoma is the most dangerous form of skin cancer due to its high mortality, aggressiveness, and low effectiveness of therapy. Previous studies have shown the therapeutic potential of minocycline, doxycycline, and chlortetracycline on melanoma cells. This study aimed to evaluate the cytotoxicity of tigecycline, a third-generation tetracycline, on melanotic and amelanotic melanoma cell lines. The results demonstrated that tigecycline efficiently inhibited the proliferation of both types of melanoma cells, accompanied by dysregulation of the cell cycle, depolarization of the mitochondrial membrane, and alterations in various molecular levels. However, the drug induced apoptosis only in melanotic melanoma cells, while amelanotic cells exhibited resistance and showed increased autophagy marker levels.
Review
Chemistry, Medicinal
Amanda S. Hirata, James J. La Clair, Paula C. Jimenez, Leticia Veras Costa-Lotufo, William Fenical
Summary: Seriniquinone is a bioactive compound produced by a marine bacterium, showing significant anti-cancer activity against melanoma cells by targeting dermcidin (DCD). DCD is found to be a peptide associated with cancer cell survival, and seriniquinone exhibits enhanced potency against melanoma cell lines.
Article
Pharmacology & Pharmacy
Zengjin Liu, Hailan Wang, Changzhen Sun, Yuanmin He, Tong Xia, Jianv Wang, Xia Xiong, Qingbi Zhang, Sijin Yang, Li Liu
Summary: A novel fluorescent probe, ZWZ-3, was designed and synthesized for melanoma imaging and treatment. ZWZ-3 selectively targeted melanoma cells viaorganic anion-transporting polypeptide (OATP) and induced apoptosis and autophagy to inhibit tumor growth.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Food Science & Technology
Hsin-Yu Chou, Li-Heng Liu, Chung-Yi Chen, I-Fan Lin, Daoud Ali, Alan Yueh-Luen Lee, Hui-Min David Wang
Summary: NFDE and NWE, isolated from fermented soybeans, showed significant anti-melanoma effects in cell cytotoxicity assays. The extracts increased oxidative stress in melanoma cells, shifting cellular death from autophagy to apoptosis.
FOOD AND CHEMICAL TOXICOLOGY
(2021)
Article
Medicine, Research & Experimental
Su-Ji Jeon, Eun-Young Choi, Eun-Ji Han, Sang-Woo Lee, Jun-Mo Moon, Soo-Hyun Jung, Ji-Youn Jung
Summary: This study demonstrated the anticancer effects of Piperlongumine on human melanoma cells through apoptosis and autophagy pathways mediated by the MAPK/ERK pathway. PL induced apoptosis by affecting the expression of MAPK pathway proteins and triggered an autophagic response.
INTERNATIONAL JOURNAL OF MOLECULAR MEDICINE
(2023)
Article
Integrative & Complementary Medicine
Du Bing-Xin, Lin Pei, Lin Jun
Summary: EGCG and ECG induce apoptosis through the mitochondrial signaling pathway and downregulate autophagy by modulating the AMPK/mTOR and PI3K/AKT/mTOR signaling pathways.
CHINESE JOURNAL OF NATURAL MEDICINES
(2022)
Article
Biochemistry & Molecular Biology
Min-Hee Jo, Yong-Tae Kim, Sun Joo Park
Summary: Dieckol, a natural polyphenol, inhibits the growth of melanoma cells by inducing apoptotic cell death through affecting lysosomal function and mitochondrial membrane. This suggests its potential value as a chemotherapeutic drug candidate for melanoma treatment.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Biochemistry & Molecular Biology
Istvan Szasz, Viktoria Koroknai, Vikas Patel, Tibor Hajdu, Timea Kiss, Roza Adany, Margit Balazs
Summary: HA15 is a new anti-melanoma drug that affects melanoma cell viability through induction of ER stress, and only works under starvation conditions. Melanoma cells may acquire resistance to HA15, and further studies are needed to confirm its efficacy as an anti-cancer agent.
Article
Materials Science, Multidisciplinary
Iuliia Taskaeva, Izabella Gogaeva, Anastasia Shatruk, Nataliya Bgatova
Summary: The study aimed to investigate if lithium salt induces autophagy and apoptosis in skin melanoma cells to enhance cell death. The results showed that lithium treatment suppressed the proliferation of melanoma cells and stimulated autophagy and apoptosis, suggesting its potential as a treatment for melanoma.
MICROSCOPY AND MICROANALYSIS
(2022)
Article
Oncology
Xuan Zheng, Jianyun Zhang, Shuangting Li, Xiaolei Gao, Yixin Zhang, Meng Wang, Liying Dong, Liangjie Sun, Na Zhao, Zeyun Ma, Chong Ding, Yixiang Wang
Summary: We developed a new, safe strategy for treating melanoma by using low doses of niclosamide and quinacrine. We found that the combination of these two drugs activates autophagy-mediated p53-dependent apoptosis, leading to an efficient anti-melanoma effect. This novel strategy also showed a universal anti-cancer role in other types of cancer.
TRANSLATIONAL ONCOLOGY
(2022)
Review
Biochemistry & Molecular Biology
Chunjing Wu, Min You, Dao Nguyen, Medhi Wangpaichitr, Ying-Ying Li, Lynn G. Feun, Macus T. Kuo, Niramol Savaraj
Summary: TRAIL and ADI-PEG20 are two drugs for treating melanoma, and their combination can enhance cytotoxicity to melanoma cells, including resistant ones. Studies show that combination therapy can alter the expression of cell signaling components in melanoma cells to promote cell death.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Biochemistry & Molecular Biology
Adriana Celesia, Antonietta Notaro, Marzia Franzo, Marianna Lauricella, Antonella D'Anneo, Daniela Carlisi, Michela Giuliano, Sonia Emanuele
Summary: This study compared the effects of two HDAC inhibitors, ITF2357 and SAHA, in melanoma cells with the BRAF V600E oncogenic mutation. Results showed that ITF2357 was more effective than SAHA in reducing the viability of BRAF-mutated melanoma cells, and it also decreased the expression of oncogenic BRAF protein and induced a switch from autophagy to classic apoptosis.
Article
Multidisciplinary Sciences
Sujoy Chatterjee, Shivraj M. Yabaji, Oleksii S. Rukhlenko, Bidisha Bhattacharya, Emily Waligurski, Nandini Vallavoju, Somak Ray, Boris N. Kholodenko, Lauren E. Brown, Aaron B. Beeler, Alexander R. Ivanov, Lester Kobzik, John A. Porco, Igor Kramnik
Summary: Macrophages play a crucial role in host immunity and tissue homeostasis, with different activation programs leading to distinct functions. Imbalance of M1 and M2 macrophages can perpetuate chronic inflammation. Rocaglates sensitize macrophages to combat bacterial pathogens more effectively, showing potential for immunomodulation.
Article
Chemistry, Medicinal
Yulin Ren, A. Douglas Kinghorn
JOURNAL OF MEDICINAL CHEMISTRY
(2020)
Review
Plant Sciences
Garima Agarwal, Long-Sheng Chang, Djaja Doel Soejarto, A. Douglas Kinghorn
Summary: Aglaia is a large genus in the family Meliaceae, native to tropical rainforests in the Indo-Australian region. Since the 1960s, researchers have focused on investigating the phytochemical constituents and biological properties of various Aglaia species, particularly the rocaglates. These compounds have shown potential as lead compounds with antineoplastic and antiviral effects, attributed to their unique structures and ability to inhibit eIF4A.
Article
Biochemistry & Molecular Biology
Sanjay Varikuti, Andrew B. Shelton, Sainath R. Kotha, Travis Gurney, Gaurav Gupta, Thomas J. Hund, James R. Fuchs, A. Douglas Kinghorn, Nidhi Srivastava, Abhay R. Satoskar, Narasimham L. Parinandi
Summary: Our study demonstrated that pentalinonsterol activates cPLA(2) in macrophages, which could potentially be used in the development of pharmacological interventions against leishmaniasis.
CELL BIOCHEMISTRY AND BIOPHYSICS
(2022)
Article
Plant Sciences
Ermias Mekuria Addo, Yulin Ren, Gerardo D. Anaya-Eugenio, Ninh Tran Ngoc, Harinantenaina L. Rakotondraibe, Esperanza J. Carcache de Blanco, Djaja D. Soejarto, A. Douglas Kinghorn
Summary: Phytochemical investigation of Homalium cochinchinensis led to the isolation of 11 secondary metabolites, including two rare spermidine alkaloids and six previously undescribed glycosides. The structures of these new isolates were determined primarily by interpreting spectroscopic and spectrometric data.
PHYTOCHEMISTRY LETTERS
(2021)
Review
Oncology
Anusha Amaravathi, Janet L. Oblinger, D. Bradley Welling, A. Douglas Kinghorn, Long-Sheng Chang
Summary: Neurofibromatosis syndromes, characterized by multiple nervous system tumors, are mainly treated by surgery but some are refractory to conventional chemotherapy. Recent advances in genetics and animal models have led to a better understanding of NF tumor biology and potential targeted therapies. Natural compounds may serve as effective treatments in the future for patients with tumor predisposition syndromes.
FRONTIERS IN ONCOLOGY
(2021)
Editorial Material
Plant Sciences
Philip J. Proteau, A. Douglas Kinghorn
JOURNAL OF NATURAL PRODUCTS
(2021)
Article
Cell Biology
Amrita Salvi, Alexandria N. Young, Andrew C. Huntsman, Melissa R. Pergande, Melissa A. Korkmaz, Rathnayake A. Rathnayake, Brittney K. Mize, A. Douglas Kinghorn, Xiaoli Zhang, Kiira Ratia, Markus Schirle, Jason R. Thomas, Scott M. Brittain, Claude Shelton, Leslie N. Aldrich, Stephanie M. Cologna, James R. Fuchs, Joanna E. Burdette
Summary: PHY34 is a synthetic small molecule with potent anticancer activity against ovarian cancer cells. It induces apoptosis in these cells by inhibiting late-stage autophagy. CAS protein is identified as a likely target of PHY34, and its elevated expression in HGSOC is associated with worse clinical outcomes. Additionally, PHY34 interacts with ATP6V0A2 subunit and induces cell death.
CELL DEATH & DISEASE
(2022)
Article
Plant Sciences
Leslie N. Aldrich, Joanna E. Burdette, Esperanza Carcache de Blanco, Christopher C. Coss, Alessandra S. Eustaquio, James R. Fuchs, A. Douglas Kinghorn, Amanda MacFarlane, Brittney K. Mize, Nicholas H. Oberlies, Jimmy Orjala, Cedric J. Pearce, Mitch A. Phelps, Liva Harinantenaina Rakotondraibe, Yulin Ren, Djaja Doel Soejarto, Brent R. Stockwell, Jack C. Yalowich, Xiaoli Zhang
Summary: Research progress in the discovery of potential anticancer agents from various organisms has been summarized. Lead compounds with structural diversity have been obtained, and potential antitumor activities have been demonstrated. Further investigations are warranted for promising lead compounds.
JOURNAL OF NATURAL PRODUCTS
(2022)
Editorial Material
Plant Sciences
Philip J. Proteau, Douglas A. Kinghorn
JOURNAL OF NATURAL PRODUCTS
(2022)
Article
Chemistry, Medicinal
Peter J. Blanco Carcache, Gerardo D. Anaya Eugenio, Tran Ngoc Ninh, Curtis E. Moore, Jose Rivera-Chavez, Yulin Ren, Djaja D. Soejarto, A. Douglas Kinghorn
Summary: Compound kimcuongin (2) isolated from Vietnamese tropical plants showed high cytotoxicity against breast cancer cells in combination with other compounds and enhanced the inhibitory effects of flavonoid 10 on NF -KB and PARP-1. In the zebrafish model, compounds 2, 3, 5, and 6 did not exhibit discernible toxicity effects.
Review
Biochemistry & Molecular Biology
Yulin Ren, Tyler Frank, Gunnar Meyer, Jizhou Lei, Jessica R. Grebenc, Ryan Slaughter, Yu G. Gao, A. Douglas Kinghorn
Summary: Aronia berries have multiple bioactivities beneficial to human health, with phenolic compounds being the major active components. This review focuses on the molecular targets and promising lead compounds of Aronia berry extracts, as well as clinical trial investigations and the potential development of these berries as therapeutic agents.
Article
Plant Sciences
Yulin Ren, Elizabeth N. Kaweesa, Lei Tian, Sijin Wu, Kongmany Sydara, Mouachanh Xayvue, Curtis E. Moore, Djaja D. Soejarto, Xiaolin Cheng, Jianhua Yu, Joanna E. Burdette, A. Douglas Kinghorn
Summary: A cardiac glycoside epoxide, (-)-cryptanoside A (1), was isolated from Cryptolepis dubia and showed potent cytotoxicity against various human cancer cell lines. It also inhibited Na+/K+-ATPase activity and increased the expression of Akt and the p65 subunit of NF-κB. Molecular docking analysis suggested that (-)-cryptanoside A (1) directly targets Na(+)/K+-ATPase to exhibit its cytotoxic effects on cancer cells.
JOURNAL OF NATURAL PRODUCTS
(2023)
Article
Biochemistry & Molecular Biology
Charmaine A. Lindsay, A. Douglas Kinghorn, Harinantenaina L. Rakotondraibe
Summary: Penicillium fungi, represented by various species, can be found worldwide in different environments and have been a source of bioactive compounds with varied bioactivities. This short review focuses on specialized metabolites of the steroid class produced by Penicillium fungi, discussing their cytotoxic, antimicrobial, anti-inflammatory, and phytotoxic activities. The review also highlights the structural diversity of these compounds and their potential for further exploration of their activity.
Review
Biochemistry & Molecular Biology
Esperanza Carcache J. de Blanco, Ermias Mekuria Addo, H. Liva Rakotondraibe, Djaja D. Soejarto, A. Douglas Kinghorn
Summary: This review summarizes the recent accomplishments of a multidisciplinary, multi-institutional anticancer drug discovery project. Plants from Southeast Asia, Central America, and the West Indies were collected and subjected to extraction and biological evaluation. Several bioactive compounds with diverse structures were obtained and characterized. Strategies were developed to optimize the research components, including plant collections and taxonomic identification, in accordance with international treaties and species conservation.
NATURAL PRODUCT REPORTS
(2023)
Article
Chemistry, Medicinal
Gerardo D. Anaya-Eugenio, Peter J. Blanco Carcache, Tran Ngoc Ninh, Yulin Ren, Djaja D. Soejarto, A. Douglas Kinghorn
Summary: PMF isolated from Glycomis ovoidea showed antiproliferative effects against MCF-7 cells by inducing apoptosis through BCL-2 protein family regulation, cell cycle arrest, and inhibition of cell migration. Additionally, PMF did not exhibit toxicity in a zebrafish model, suggesting its potential as an alternative therapy for breast cancer.
PHYTOTHERAPY RESEARCH
(2021)