Antibacteria Activity of Peganum harmala and Haloxylon salicornicum Leaves Extracts

The use of antibiotics in humans and animals has been marked as a significant step in health due to their effectiveness in controlling and treating bacterial infections. The misuse and overuse of antibiotics have been identified as risk factors for bacterial resistance since microorganisms adapt and develop mechanisms to defend against antibiotics. According to the Centers for Disease Protection and Control (CDC), around 23,000 individuals die every year in the United States due to antibiotic resistance complications. As a result, a demand for alternative treatments has been a goal for scientists as the microbes adapt to selective pressure. The aim of this study is to test the antibacterial activity of leaf extracts of Peganum harmala and Haloxylon salicornicum on both Gram-positive and Gram-negative bacteria on various mediums. The results of the study showed that both P. harmala and H. salicornicum inhibited the bacterial growth in two different media. The results were also compared with different common antibiotics used in both human’s and animal’s fields and showed a promising outcome as alternative antibiotics.

Anticancer Activity of Peganum harmala and Haloxylon salicornicum Leaf Extracts on Lung Cancer A549 and Prostate Cancer PC-3 Cell Lines

Cancer is a worldwide disease that ranks as the second-largest cause of death after cardiovascular disease. In 2019, the estimated number of cancer deaths was around 10 million worldwide and 600,000 in the United States. Due to the high side effects of the available treatments for cancer, such as chemotherapy and radiotherapy, a demand for alternative treatments has been a goal for scientists with less toxicity and side effects. Lung cancer is the most common type of cancer worldwide and the leading cause of death in the United States. In addition, prostate cancer is the second-leading cause of cancer death in American men after lung cancer. Natural sources discovered to have therapeutic medicinal properties against human diseases are the plants Peganum harmala and Haloxylon salicornicum. The aim of this study is to test the anticancer activity of leaf extracts of Peganum harmala and Haloxylon salicornicum on lung cancer (A549) and prostate cancer (PC3) cell lines. The anticancer activity of P. harmala and H. salicornicum was studied using the assays: crystal violet viability, lipid peroxidation, and caspase-3 techniques, which were evaluated in vitro on two human cancer cell lines. The results of the study showed that both plants’ extracts reduced the viability of both cancer cell lines, which depended on the concentration of the extract. Also, P. harmala showed more potent activity against both types of cancer than H. salicornicum. P. harmala and H. salicornicum decreased the lipid peroxidation that induces cancer as well as increased the expression of caspase-3, which causes apoptosis and cell death. This study concluded that P. harmala and H. salicornicum leaf extracts showed significant anticancer properties, which might be due to the presence of phytochemicals, including flavonoids and phenolics.

Triphenylmethanol Conjugates of Triptorelin as Cell-Penetrating Anti-Cancer Prodrugs

Some Triptorelin® (TRP) conjugates of triphenylmethanol derivatives (TPMs) with optimized hydrophobicity were synthesized by reacting 2-substituted methoxy benzenes with 1,3,5-trioxane, followed by the conjugation with TRP and sebacic acid to produce TRP-TPMs derivatives. Comparative antiproliferative assays between TRP-TPMs conjugates and the corresponding non-covalent physical mixtures of the TPMs derivatives and TRP were used to treat human acute lymphoblastic leukemia (CCRF-CEM), human ovarian adenocarcinoma (SK-OV-3) and mouse preadipocytes (3T3-L1) cells. TRP-TPMs conjugates at the 50 μM inhibited cell proliferation in CCRF-CEM, SK-OV-3 and 3T3-L1 cells by 21% - 37%, 24% - 73%, 37% - 56%, respectively following incubation for 72 h. These findings indicate that TRP-TPMs derivatives have the potential to enhance the biological activity of TRP.

Biological Evaluation of New Schiff Bases: Synthesized from 4-Amino-3,5-dimethyl-1,2,4-triazole, Phenathroline and Bipyridine Dicarboxaldehydes

Four new Schiff bases with promising anticancer activity have been synthesized from 4-amino-3,5-dimethyl-1,2,4-triazole and di-pyridyl-aldehydes. Structures have been established by various spectroscopic methods. The compounds were tested in vitro to study their cytotoxicity and anti-oxidative activity in human lung carcinoma (A549), breast carcinoma (BT549), prostate adenocarcinoma (PC3) and mouse preadipocytes (3T3-L1) cells. Compound 1 was found to increase Glutathione (GSH) level slightly in all four cell lines. Compound 4 showed better selectivity and cytotoxicity against both BT549 and A549 cells compared to the anticancer drug tamoxifen. With the exception of compound 4 which reduced GSH levels in A549 and BT549, all other compounds maintained GSH levels in comparison to their respective controls.

Triphenylmethanol Conjugates of Triptorelin as Anti-Lipid Peroxidation Prodrugs

Antioxidants are substances that can prevent or slow damage to cells caused by free radicals, unstable molecules that the body produces as a reaction to environmental and other pressures. Free radicals may play a role in heart disease, cancer and other diseases. If the body cannot process and remove free radicals efficiently, oxidative stress can result. This can harm cells and body function. Free radicals are also known as reactive oxygen species (ROS). In this research, Triptorelin®(TRP) conjugates of triphenylmethanol derivatives (TPMs) were synthesized to evaluate their in vitro lipid peroxidation potency. Comparative lipid peroxidation assays between TRP-TPMs conjugates and the corresponding TPMs derivatives were measured using thiobarbituric reactive substance (TBARS) in a dose- and time-dependent manner following the Fenton’s pathway. Overall, TBARS decreased between 20% - 30% for the treated samples of synthesized conjugates compared to their respective control physical mixtures. These data suggest that TRP-TPMs derivatives can be used to improve the biological activity of TRP.

Synthesis and Antiproliferative Activities of Triphenylmethanol Conjugates of Leuprorelin

Leuprorelin®(LEP) is an FDA drug for breast cancer and prostate cancer treatment. There are several reported adverse effects such as transient hypertension, excessive salivation, and increased dysuria during treatment with LEP. In this study, the efficacy and toxicity of LEP were modified by using a drug delivery system to adjust the physicochemical properties. In this regard, Leuprorelin®conjugates of triphenylmethanol derivatives (TPMs) were synthesized as prodrugs. Comparative antiproliferative assays showed that LEP-TPMs conjugates had significantly higher antiproliferative activities than the corresponding non-covalent physical mixtures of the TPMs and LEP against human invasive ductal carcinoma (BT-549), human prostate carcinoma (PC3), human lung cancer (A549) and mouse pre-adipocytes (3T3-L1) cells.

Triphenylmethanol and Tris(2-(hydroxymethyl)phenol) Derivatives: Synthesis and Application as Indicators for Acid-Base Volumetric Titration

Polyphenols are naturally occurring compounds found largely in fruits, vegetables, cereals and beverages. Currently, there is much interest in the potential health benefits of dietary plant polyphenols as antioxidants. The effect of polyphenols on human cancer cells is most often protective and induces a reduction in the number of tumors or rate of growth. During our course of study on anticancer prodrugs, twelve triphenylmethanol and one tris(2-(hydroxymethyl) phenol derivatives were synthesized as a carrier of several drugs with optimized lipophilicity. Besides application of these compounds as a foundation for anticancer drug delivery systems, these compounds were evaluated as indicators for the acid-base volumetric titration of a standard solution of hydrochloric acid with a standard solution of sodium hydroxide. The experiments indicated a moderate-to-sharp color transition of the solutions near the neutralization point for most indicators. These indicators may have potential applications for acid-base titrations in a narrow range.