Anti-cancer agents in medicinal chemistry
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Anticancer Agents Med Chem · Jan 2014
ReviewFrom French Paradox to cancer treatment: anti-cancer activities and mechanisms of resveratrol.
Resveratrol (3, 5, 4'-trihydroxy-trans-stilbene, RVT), a stilbenoid, polyphenol phytochemical present in berries, grape, peanuts and wine. It has been suggested as a major contributor to "French Paradox" that reduces the mortality from coronary heart disease (CHD) by consuming RVT in red wine even in some of French population with a high-fat intake. With extensive research, it has been found that RVT is a versatile and pleiotropic agent, it not only possesses cardiovascular-protective benefits by its powerful antioxidant capacity, anti-inflammatory, regulating metabolism and anti-aging effects, but also has strong anti-tumor activities through inhibiting tumor cell proliferation, inducing cell apoptosis, promoting tumor cell differentiation, preventing tumor invasion and metastasis, and further moderating the host immune system to kill tumor cells. This review will focus on RVT's anti-tumor activity and tumor prevention potential including: the anti-tumor spectrum in vitro and in vivo; molecular targets and signal pathways involving RVT anti-tumor mechanisms; evidences from clinical trial for its bioavailability, dosage, toxicity and benefit in humans; and its prospective including its analog, deviations, and combinative chemotherapy.
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Anticancer Agents Med Chem · Oct 2013
Reviewβ-Hydroxy-β-methylbutyrate as a countermeasure for cancer cachexia: a cellular and molecular rationale.
Cancer cachexia is a life-threatening condition characterized by involuntary body weight loss and skeletal muscle wasting. In addition to being associated with poor prognosis and reduced survival, patients with cachexia exhibit a critical loss of physical function that impinges upon their ability to perform basic activities of daily living. Consequently, there is a loss of independence and a drastically reduced quality of life. ⋯ Evidence suggests that HMB treatment promotes regenerative events (i.e. myogenic program), suppresses protein degradation, and activates signaling pathways preceding protein synthesis and skeletal muscle growth. HMB therefore, could conceivably act on key regulatory events driving cancer cachexia, thereby favoring muscle growth/preservation. In this review, we take a mechanistic approach in making a case for the use of HMB provision as a possible therapeutic strategy for cancer cachexia by highlighting the cellular and molecular aspects of HMB function.
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Anticancer Agents Med Chem · Nov 2012
ReviewAnti-cancer effects of curcumin on head and neck cancers.
Head and neck cancer is the sixth large type of cancer in the world. The treatment regimens for head and neck cancer encompass surgery, radiotherapy and chemotherapy. However, all current treatment regimens for head and neck cancer have adverse effects. ⋯ This review summarizes the evidence demonstrating potential use of curcumin as a single chemotherapeutic agent or in combination with other chemotherapeutic agents and radiation to minimize their toxicity in head and neck cancer. Although curcumin has been shown to be safe at doses of 8 g/d in both phase I and phase II clinical trials, its bioavailability is poor. Overcoming the poor bioavailability of curcumin in the near future would facilitate its clinical use.
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Anticancer Agents Med Chem · Jul 2012
ReviewTriple-negative breast cancer and poly(ADP-ribose) polymerase inhibitors.
Recent gene profiling studies have identified at least 5 major subtypes of breast cancer, including normal type, luminal A type, luminal B type, human epidermal growth factor receptor (HER)-2 positive type, and basal-like type. Triple-negative breast cancer (TNBC), showing no or low expressions of estrogen receptor (ER), progesterone receptor (PgR), and HER2, considered important clinical biomarkers, accounts for 10% to 20% of all breast cancers. Hormonal therapy and molecular targeted therapy are not indicated for the management of TNBC, resulting in poor outcomes. ⋯ PARP, a DNA base-excision repair enzyme, is known to play a central role in gene repair, along with BRCA. Because some breast cancers with BRCA1 or BRCA2 mutations are TNBC, the suppression of PARP has attracted attention as a new treatment strategy for TNBC. In this article, we review the clinical characteristics of TNBC, discuss problems in treatment, and briefly summarize the international development status of PARP inhibitors.
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Anticancer Agents Med Chem · Feb 2012
ReviewAnticancer activity of bisphosphonates in breast cancer.
Despite progress in surgical and adjuvant therapy, a subset of patients with early stage breast cancer experience disease recurrence and/or distant metastases. Disseminated tumor cells (DTCs) in the bone marrow are believed to be the source of late relapses in bone and other tissues. Bone is the most common site of breast cancer metastasis, and agents that modify the bone microenvironment could therefore affect the disease course. ⋯ Based on recent data, the role of bisphosphonates in the breast cancer setting is expected to expand in the future. With recent changes to treatment guidelines, routine use of bisphosphonates to prevent bone loss during adjuvant therapy is likely to become standard practice, especially for patients receiving endocrine therapy. Furthermore, the use of zoledronic acid to reduce the risk of recurrence is emerging based on ongoing clinical research.