A Comprehensive Review on Pharmacological Activities of Pachypodol: A Bioactive Compound of an Aromatic Medicinal Plant Pogostemon Cablin Benth.

As is well known, plant products have been increasingly utilized in the pharmaceutical industry in recent years. By combining conventional techniques and modern methodology, the future of phytomedicines appears promising. Pogostemon Cablin (patchouli) is an important herb used frequently in the fragrance industries and has various therapeutic benefits. Traditional medicine has long used the essential oil of patchouli (P. cablin) as a flavoring agent recognized by the FDA. This is a gold mine for battling pathogens in China and India. In recent years, this plant has seen a significant surge in use, and approximately 90% of the world's patchouli oil is produced by Indonesia. In traditional therapies, it is used for the treatment of colds, fever, vomiting, headaches, and stomachaches. Patchouli oil is used in curing many diseases and in aromatherapy to treat depression and stress, soothe nerves, regulate appetite, and enhance sexual attraction. More than 140 substances, including alcohols, terpenoids, flavonoids, organic acids, phytosterols, lignins, aldehydes, alkaloids, and glycosides, have been identified in P. cablin. Pachypodol (C18H16O7) is an important bioactive compound found in P. cablin. Pachypodol (C18H16O7) and many other biologically essential chemicals have been separated from the leaves of P. cablin and many other medicinally significant plants using repeated column chromatography on silica gel. Pachypodol's bioactive potential has been shown by a variety of assays and methodologies. It has been found to have a number of biological activities, including anti-inflammatory, antioxidant, anti-mutagenic, antimicrobial, antidepressant, anticancer, antiemetic, antiviral, and cytotoxic ones. The current study, which is based on the currently available scientific literature, intends to close the knowledge gap regarding the pharmacological effects of patchouli essential oil and pachypodol, a key bioactive molecule found in this plant.

Pinostrobin alleviates testicular and spermatological damage induced by polystyrene microplastics in adult albino rats.

BACKGROUND: Polystyrene microplastics (PS-MPs) have become major environmental pollutants that adversely effects multiple organs specifically testicles. Pinostrobin (PN) is an important flavonoid which, shows several pharmacological potentials. PURPOSE: The current study was designed to elucidate the mitigative effects of PN against PS-MPs induced testicular toxicities in rats. METHODS: 48 male albino rats were randomly distributed into 4 groups, control, PS-MPs group (0.01 mg/kg), PS-MPs + PN group (0.01 mg/kg of PS-MPs; 40 mg/kg of PN) and PN group (40 mg/kg). RESULTS: PS-MPs intoxication substantially lessened the activities of glutathione peroxidase (GPx), glutathione reductase (GSR), superoxide dismutase (SOD) along with catalase (CAT) while, raised the level of malondialdehyde (MDA) as well as reactive oxygen species (ROS). Additionally, PS-MPs reduced luteinizing hormone (LH), plasma testosterone, follicle-stimulating hormone (FSH) concentration, sperm motility, sperm count, expression of steroidogenic enzymes and Bcl-2 (anti-apoptotic protein) along with the count of spermatogenic cells. While, dead sperm count, sperm abnormalities (tail, neck and head), Bax and caspase-3 (apoptotic proteins) expression along with histopathological anomalies were elevated. Moreover, PS-MPs exposure increased the level of inflammatory markers. However, PN treatment considerably decreased oxidative stress (OS) by reducing ROS as well as increased sperm motility and alleviated all the damages induced by the PS-MPs. CONCLUSION: Therefore, it is concluded that PN may prove a potential therapeutic candidate to restore all the PS-MPs-induced testicular toxicities.

Phytochemical-Stabilized Platinum-Decorated Silver Nanocubes INHIBIT Adenocarcinoma Cells and Enhance Antioxidant Effects by Promoting Apoptosis via Cell Cycle Arrest.

(1) Background: The increasing use of silver and platinum bimetallic nanoparticles in the diagnosis and treatment of cancer presents significant advances in biomedical applications due to their extraordinary physicochemical properties. This study investigated the role of aqueous phytochemical extract in stabilizing platinum nanodots-decorated silver nanocubes (w-Pt@AgNPs) for enhancing antioxidant activities and their mechanism. (2) Methods: UV-Vis, Fourier transform infrared (FTIR) spectroscopy, and transmission electron microscopy (TEM) were used to characterize the formed w-Pt@AgNPs. LC-QToF-MS/MS was used to analyze the bioactive compounds, while DPPH, ABTS, and FRAP were used to detect the scavenging potential. Flow cytometric assays were performed to investigate the cytotoxicity and the mechanism of cell death. (3) Results: Morphological studies indicated that w-Pt@AgNPs were cube in shape, decorated by platinum nanodots on the surfaces. Compared to ethanolic extract-synthesized e-Pt@AgNPs, w-Pt@AgNPs exhibited the strongest antioxidant and cytotoxic activity, as data from Annexin V and Dead cell labeling indicated higher induction of apoptosis. Despite the high proportion of early apoptotic cells, the w-Pt@AgNPs triggered a decrease in G1/G0 cell cycle phase distribution, thereby initiating a G2/M arrest. (4) Conclusions: By enhancing the antioxidant properties and promoting apoptosis, w-Pt@AgNPs exhibited remarkable potential for improved cancer therapy outcomes.

Medicinal uses, pharmacological activities, phytochemistry, and the molecular mechanisms of Punica granatum L. (pomegranate) plant extracts: A review.

Punica granatum L (pomegranate) is one of the Mediterranean medicinal plants that has been used for generations in treating ulcers, diarrhea, and male infertility. Increasing evidence has revealed that pomegranate possesses myriads of pharmacological activities such as anti-diabetic, anti-tumor, anti-inflammatory, anti-malaria, anti-fibrotic, anti-fungal, anti-bacterial, and other effects. Consumption of pomegranate could be used to improve gut microbiota, and therefore prevent obesity and diabetes. The mechanisms of actions of pomegranate, mainly involve nuclear factor-erythroid factor 2-related factor 2 (Nrf2), nuclear factor kappa B (NF-kB), and mitogen-activated protein kinase (MAPK) signaling pathways. In recent times, in silico molecular docking studies demonstrated that pomegranate extract and or its phytochemicals are potential inhibitors of severe acute respiratory syndrome coronavirus 2 (SARS-COV-2) spike protein and angiotensin-converting enzyme 2 (ACE2) receptor contact. Also, some clinical trials have indicated that pomegranate can be consumed for alleviation of non-alcoholic fatty liver disease, metabolic syndrome, dental infections, and menopausal symptoms. To date, active compounds, viz. alkaloids, anthocyanidins, tannins, flavonoids, phenolics, proanthocyanidins, sterols, terpenes, terpenoids, xanthonoids, fatty acids, organic acids, lignans, saccharides, and vitamin C have been isolated from pomegranate. Therefore, the current review article aimed to gather and presents an update on the ethnomedicinal uses, pharmacological activities, phytochemistry, and molecular mechanisms of Punica granatum L. This knowledge is of paramount importance in the future in drug discovery for the development of novel natural drugs for the treatment of various ailments.

Ginger from Farmyard to Town: Nutritional and Pharmacological Applications.

Ginger (Zingiber officinale) is one of the most widely used natural products consumed as a spice and medicine for treating diabetes, flatulent intestinal colic, indigestion, infertility, inflammation, insomnia, a memory booster, nausea, rheumatism, stomach ache, and urinary tract infections. To date, over 400 bioactive components, such as diarylheptanoids, gingerol analogues, phenylalkanoids, sulfonates, monoterpenoid glycosides, steroids, and terpene compounds have been derived from ginger. Increasing evidence has revealed that ginger possesses a broad range of biological activities, especially protective effects against male infertility, nausea and vomiting, analgesic, anti-diabetic, anti-inflammatory, anti-obesity, and other effects. The pharmacological activities of ginger were mainly attributed to its active phytoconstituents such as 6-gingerol, gingerdiol, gingerol, gingerdione, paradols, shogaols, sesquiterpenes, zingerone, besides other phenolics and flavonoids. In recent years, in silico molecular docking studies revealed that gingerol (6-gingerol, 8-gingerol, and 10-gingerol) and Shogaol (6-shogaol, 8-shogaol, 10-shogaol) had the best binding affinities to the receptor protein in disease conditions such as diabetes, inflammation, obesity, and SARS-CoV-2. Furthermore, some clinical trials have indicated that ginger can be consumed for alleviation of nausea and vomiting induced by surgery, pain, diabetes, obesity, inflammation, male infertility. This review provides an updated understanding of the scientific evidence on the development of ginger and its active compounds as health beneficial agents in future clinical trials.

Advances in Nanoparticle Delivery System for Erectile Dysfunction: An Updated Review.

INTRODUCTION: The use of current available treatment for male erectile dysfunction (ED) has some limitations that are related to efficacy and adverse effects. Nanotechnology has been used as a new tool in medicine to improve these limitations and new medications potentially to alleviate and cure ED. AIM: To review the currently literature on new nano medications for ED based on scientific and clinical studies, efficacy, safety, mechanisms of action, and to identify gaps for future research. METHODS: A comprehensive literature review was conducted via Google Scholar, Science Direct, and PubMed on English publications using different keywords such as "erectile dysfunction", "emerging treatments", "nanotechnology", and "herbal medicine". The retrieved papers were organized into groups according to the sections covered in this review paper. MAIN OUTCOMES MEASURES: We reviewed novel ED treatments such as nanotechnological phosphodiesterase inhibitors, papaverine hydrochloride, sialorphin, adipose tissue-derived stem cells, sonic hedgehog, and herbal medicine. RESULTS: Numerous preclinical studies have addressed novel phosphodiesterase 5 inhibitors nanoparticle, and their recent delivery systems. Nitric oxide, sialorphin, sonic hedgehog, and herbal medicine loaded nanoparticles and nano adipose tissue-derived stem cells as a potential new treatment for ED. In addition, papaverine-containing nanoparticles have been reported. A limited number of randomized clinical studies have determined the mechanism of these treatments. CONCLUSION: A literature review on the application of nanotechnology in ED therapy was successfully conducted. New nano medications are promising to treat ED. However, further studies are warranted to further assess their efficacy and safety. Masuku NP, Unuofin JO, Lebelo SL. Advances in Nanoparticle Delivery System for Erectile Dysfunction: An Updated Review. Sex Med 2021;9:100420.

Promising role of medicinal plants in the regulation and management of male erectile dysfunction.

Male erectile dysfunction (ED) refers to incompetency to reaching and retaining adequate penile tumescence for sexual intercourse. Over 152 million men globally suffer from ED and by 2025, the number of affected individuals is anticipated to be around 322 million. Pharmacological and nonpharmacological therapies such as phosphodiesterase (PDE) inhibitors, alprostadil, penile prosthesis surgery, and hormonal replacement are available for management and recuperation of ED. Nevertheless, such therapies are reported to have adverse effects as well as life-threatening. Accordingly, diversity of medicinal plant species and bioactive active compounds are preferred as therapeutic options because they are natural, abundant, available, low-cost and cause fewer or no side effects. This current review will emphasise the aetiology, risk factors, mechanisms underlying the pathophysiology of ED, treatments of ED as well as their side effects. It also provides medicinal plants that are proven effective in vivo and in vitro for the mitigation and treatment of male ED. This knowledge could be used in the future in drug discovery for the development of more natural drugs with no side effects.

Antioxidant Effects and Mechanisms of Medicinal Plants and Their Bioactive Compounds for the Prevention and Treatment of Type 2 Diabetes: An Updated Review.

Diabetes mellitus is a metabolic disorder that majorly affects the endocrine gland, and it is symbolized by hyperglycemia and glucose intolerance owing to deficient insulin secretory responses and beta cell dysfunction. This ailment affects as many as 451 million people worldwide, and it is also one of the leading causes of death. In spite of the immense advances made in the development of orthodox antidiabetic drugs, these drugs are often considered not successful for the management and treatment of T2DM due to the myriad side effects associated with them. Thus, the exploration of medicinal herbs and natural products as therapeutic sources for the treatment of T2DM is promoted because they have little or no side effects. Bioactive molecules isolated from natural sources have been proven to lower blood glucose levels via regulating one or more of the following mechanisms: improvement of beta cell function, insulin resistance, glucose (re)absorption, and glucagon-like peptide-1 homeostasis. In recent times, the mechanisms of action of different bioactive molecules with antidiabetic properties and phytochemistry are gaining a lot of attention in the area of drug discovery. This review article presents an update of the findings from clinical research into medicinal plant therapy for T2DM.

In vitro α-amylase, α-glucosidase, lipase inhibitory and cytotoxic activities of tuber extracts of Kedrostis africana (L.) Cogn.

Kedrostis africana, is a tuberous plant commonly used by traditional healers in the Eastern Cape Province of South Africa for the management of obesity. The aim of this study was to investigate the antiobesity and cytotoxic effects of Kedrostis africana extracts in vitro The α-amylase, α-glucosidase and lipase inhibitory activities of aqueous and ethanol extracts of Kedrostis africana tuber were investigated while the cytotoxic effects of these extracts were analyzed using Hoechst 33342 and propidium iodide (PI) dual staining in combination with Molecular Devices ImageXpress Micro XLS Widefield microscope for high content analysis on human cervical (HeLa) cell line. The ethanol extract exhibited the strongest inhibitory effect on pancreatic lipase (IC50 = 381.86 µg/ml) and on α-glucosidase (IC50 = 157.99 µg/mL) while the aqueous extract has strongest α-amylase (IC50 = 439.45 µg/ml). Both tuber extracts were found nontoxic at tested concentrations on HeLa cell lines as confirmed by the Hoechst 33342 and propidium iodide dual staining respectively. This study revealed that both the aqueous and ethanol tuber extract of K. africana exerts a certain degree of inhibitory effect on α-amylase, α-glucosidase and lipase and were also nontoxic to HeLa cell line at tested concentrations.

Evaluation of acute and subacute toxicity of whole-plant aqueous extract of Vernonia mespilifolia Less. in Wistar rats.

OBJECTIVE: This study investigated the acute and subacute toxicity of whole-plant aqueous extract of Vernonia mespilifolia Less. (AEVM) in rats for evaluating its safety profile. METHODS: AEVM for the acute (2000 and 5000 mg/kg) and subacute (200, 400 and 600 mg/kg) toxicity studies was administered orally to rats according the guidelines 425 and 407 of Organization for Economic Cooperation and Development, respectively. Food and water intake as well as body and organ weight of animals were recorded. Signs of toxicity were assessed, and hematological, biochemical and histopathological analyses were performed. RESULTS: In the acute toxicity study, a single dose of the aqueous extract at 2000 or 5000 mg/kg caused no mortality in the animals, suggesting that the median lethal dose is greater than 5000 mg/kg. In the subacute toxicity study, administration of the extract for 28 d, at all doses, caused no significant changes in the body weights or organ weights of rats in the treated groups when compared with the control group. In addition, hematological and biochemical parameters also revealed no toxic effects of the extract on rats. Histological sections of the heart, liver and kidney from test animals showed no signs of degeneration. CONCLUSION: These results showed that AEVM at dosage levels up to 600 mg/kg is nontoxic and could also offer protection on some body tissues. AEVM could, therefore, be considered safe.

Polyphenolic Content, Antioxidant and Antimicrobial Activities of Vernonia mespilifolia Less. Used in Folk Medicine in the Eastern Cape Province, South Africa.

Vernonia mespilifolia Less. is a shrub of the Asteraceae family used in the South African traditional medicine system for the management of weight loss, hypertension, and heartwater disease. There is a need for scientific evaluation to validate its ethnomedicinal usage. In vitro assays were conducted to evaluate the polyphenolic content, antioxidant and antimicrobial properties of different solvent extracts (acetone, aqueous, and ethanol) of the whole plant of Vernonia mespilifolia spectrophotometric and agar dilution techniques, respectively. The result revealed varying amounts of polyphenolics in the different solvent extracts corresponding to the antioxidant activities. Also, only the acetone and ethanol extracts inhibited the growth of the selected bacteria and fungi. These findings reveal that the extracts have strong bioactive compounds and hence support its ethnomedicinal application.

Acute and subacute toxicity of aqueous extract of the tuber of Kedrostis africana (L.) Cogn in Wistar rats.

Kedrostis africana (L.) Cogn (Cucurbitaceae) is used in South African traditional medicine and pharmacopoeia as an emetic, purgative and diuretic, and it is used against dropsy in the management of obesity. Aim of the study In this study, acute and subacute toxicity of aqueous extract of K. africanatuber was evaluated in male and female Wistar rats in order to assess its safety profile. Materials and methods In acute toxicity, the effects of a single oral dose (2,000 and 5,000 mg/kg) of aqueous extract was determined in both sexes. General behavior, adverse effects and mortality were determined for 3 h and then periodically for 14 days. The subchronic toxicity test was performed in rats. The effects of the extract in daily single oral administration at the doses of 200, 400 and 600 mg/kg for 28 days were determined. Food and water intakes were monitored daily while body weight was monitored on a weekly bases. Hematological, biochemical and organ parameters were determined at the end of the 28-day administration. Results In the acute study, a single administration of the aqueous extract at the doses of 2,000 and 5,000 mg/kg did not induce mortality. Thus, the LD50 of the aqueous extract of K. africana (AEKA) has been estimated to be higher than 5,000 mg/kg. In the subchronic study, daily oral administration of the AEKA did not result in death of the rats or significant changes in hematological or biochemical parameters at the highest dose of 600 mg/kg. No alteration was observed in body weight, food and water intake. Liver, kidney and heart histopathology did not reveal morphological alteration. Conclusions The results showed that the aqueous tuber extract of K. africana did not cause any death, nor did it cause abnormalities in necropsy and histopathology findings. There were no acute or subchronic toxicity observed, and this indicates that the plant extract could be considered safe for oral medication.