Volume 76, Issue 9-10

Lambertianic acid (LA) is a diterpene bioactive compound mainly purified from different species of Pinus . It is an optical isomer of another natural compound daniellic acid and was firstly purified from Pinus lambertiana . LA can be synthesized in laboratory from podocarpic acid. It has been reported to have potential health benefits in attenuating obesity, allergies and different cancers including breast, liver, lung and prostate cancer. It exhibits anticancer properties through inhibiting cancer cell proliferation and survival, and inducing apoptosis, targeting major signalling components including AKT, AMPK, NFkB, COX-2, STAT3, etc. Most of the studies with LA were done using in vitro models, thus warranting future investigations with animal models to evaluate its pharmacological effects such as antidiabetic, anti-inflammatory and neuroprotective effects as well as to explore the underlying molecular mechanisms and toxicological profile. This review describes the chemistry, source, purification and therapeutic potentials of LA and it can therefore be a suitable guideline for any future study with LA.

The methanol extract and its ethyl acetate fraction (EAF) of Actaea acuminata (Wall. ex. Royle) H. Hara roots were reported to exhibit significant antianxiety, anticonvulsant and antidepressant activities, and mild sedative activity. But the constituents responsible for these activities have not been isolated. The present study was undertaken to isolate neuroprotective compounds of A. acuminata following bioactivity-guided-fractionation. The column chromatography of EAF and its sub-fractions led to the isolation of four phenolic compounds (bergenin, gallic acid, acetyl bergenin and racemic mixture of diacetyl bergenin), which were characterized by IR and NMR spectral analysis. All the compounds exhibited significant antianxiety and antidepressant activities with respect to control. The gallic acid and bergenin did not show anticonvulsant activity, whereas acetyl bergenin and racemic mixture of diacetyl bergenin exhibited significant anticonvulsant activity. Neuropharmacological activities of A. acuminata are attributed due to polyphenolic compounds. Scientific validation of traditional claims of A. acuminata has opened up roadmap of research for the development of CNS affecting lead molecules.

This study reports the effects of aqueous extracts obtained from three fern species of Bulgarian origin: Asplenium ceterach L., Asplenium scolopendrium L., and Asplenium trichomanes L. on the contractility and bioelectrogenesis of rat gastric smooth muscle tissues. In the concentration range 0.015–0.150 mg/mL the three extracts contracted smooth muscle tissues in a concentration-dependent manner. The contractions caused by A. ceterach L. and A. scolopendrium L. extracts (0.150 mg/mL) were reduced by ketanserin (5 × 10 −7 and 5 × 10 −6  mol/L), an antagonist of serotonin 5-HT2 receptor. The contraction evoked by A. trichomanes L. (0.150 mg/mL) was significantly reduced by 1 × 10 −6  mol/L atropine, an antagonist of muscarinic receptors, and turned into relaxation against the background of 3 × 10 −7  mol/L galantamine. After combined pretreatment with galantamine and l -arginine (5 × 10 −4  mol/L), this relaxation become more pronounced. The study demonstrates that constituents of A. ceterach L. and A. scolopendrium L. extracts act as agonists of 5-HT2 receptors and cause contraction by activating serotonergic signaling system. A. trichomanes L.-induced reaction is an additive result of two opposite-in-character effects. The dominant contraction is initiated by inhibition of acetylcholinesterase activity. The relaxation develops with pre-inhibited acetylcholinesterase, it is significantly potentiated by l -arginine, and therefore associated with nitrergic signaling pathway.

The aim of the present study is to determine the potent biological activities and carry out isolation studies on Barbarea integrifolia . The antioxidant capacity of the species was evaluated by total phenolic content, FRAP, CUPRAC, and DPPH radical scavenging activity. Anticancer activity studies were performed by MTT assay in MDA-MB-231, MCF-7, Hep3B, PC-3, A549, HCT116, L-929 cell lines. It was observed that the remaining aqueous fraction has higher total phenolic content while higher activity in the CUPRAC and FRAP assays was displayed for the methanolic extract and chloroform fraction. The extracts showed anticancer activity as compared with vincristine. It was observed that chloroform fraction has the highest anticancer activity on MCF-7 cell line, while ethyl acetate fraction has the highest anticancer activity on Hep-3B and A549 cell lines. Methanolic extract has the highest anticancer activity on HCT116 and MDA-MB-23 cell lines. The isolation studies have been performed using several chromatographic methods. The chemical structures of compounds have been identified by means of 1 H NMR, 13 C NMR, 2D-NMR, and MS. Five major compounds, one steroid ( β -Sitosterol), one phenolic acid (Rosmarinic acid), one flavonol heteroside (kaempferol 7- O - α - l -rhamnoside-3- O - β - d -(2- O - β - d -glucosyl)- β - d -glucoside), and two glucosinolates (Gluconasturtiin, Gluconasturtiin choline salt) have been isolated.

Cinnamomum tamala and Cinnamomum verum are known for their folk medicinal usage in treating gastrointestinal ailments. The spasmolytic activity of essential oils was studied using isolated rat ileum. The results indicate that C. tamala , despite having a lower content of eugenol (60%), shows a spasmolytic potential of 68.01 ± 2.63% (EC 50  = 110.12 ± 13.58 μg/mL) while C. verum with rich eugenol (80%) shows lesser spasmolytic potential (38.96 ± 0.63%) and fails to attain an EC 50 value. Upon comparison with standard eugenol’s percentage of spasmolytic (35.68 ± 2.57%), it is evident that the action of these essential oils does not solely rely on the major component but the synergistic role in association with other components of the mixture influences the pharmacological action of the essential oils. In silico docking of phytochemicals of leaf essential oils with M 2 (M 2 AChR) and M 3 muscarinic (M 3 AChR) and nicotinic acetylcholine receptor (nAChR) was carried out to determine the type of receptors through which the essential oils had spasmolytic potential. The binding affinity for eugenol with nAChR shows a better docking score than M 2 AChR and M 3 AChR.

The novel COVID-19 pandemic is a current, major global health threat. Up till now, there is no fully approved pharmacological treatment or a vaccine. Also, its origin is still mysterious. In this study, simple mathematical models were employed to examine the dynamics of transmission and control of COVID-19 taking into consideration social distancing and community awareness. Both situations of homogeneous and nonhomogeneous population were considered. Based on the calculations, a sufficient degree of social distancing based on its reproductive ratio is found to be effective in controlling COVID-19, even in the absence of a vaccine. With a vaccine, social distancing minimizes the sufficient vaccination rate to control the disease. Community awareness also has a great impact in eradicating the virus transmission. The model is simulated on small-world networks and the role of social distancing in controlling the infection is explained.

Ethanolic extract of Nelumbo nucifera petals showed preferential cytotoxic activity against HeLa human cervical cancer cell line with a PC 50 value of 10.4 μg/mL. This active extract was subjected to a phytochemical investigation study which led to the isolation of nine benzylisoquinoline alkaloids ( 1 – 9 ). The isolated compounds exhibited potent antiausterity activities. Moreover, under nutrient-deprived conditions, (−)-lirinidine ( 8 ) induced remarkable alterations in HeLa cell morphology including cell shrinkage and plasma blebbing leading to total cell death within 10 h. Mechanistically, 8 was found to inhibit Akt/mTOR signaling pathway. It also induced apoptosis by promoting caspase-3 activation and inhibiting Bcl-2 expression. Therefore, benzylisoquinoline alkaloids skeleton can be considered as a promising scaffold for the anticancer drug development against cervical cancer.

This experiment proposed to investigate the efficiency of omega 3 fatty acids from fish that improves autoimmune against myocarditis in the rat. Fish oil was extracted from fresh Tuna fish and performed FAME analysis and mice bioassay. The autoimmune myocarditis was induced by subcutaneous injection of porcine cardiac myosin (PCM) into the footpads of rats on the first and seventh day. Rats were dissected on the 21st day to analyze the histopathological, hemodynamic, echocardiographic factors, and immunohistochemistry expressions. In the study, 73.90% of total fatty acids were recorded. Histological analysis revealed that omega 3 fatty acids administrated groups showed tremendous development in the multifocal myocardia hyaline degeneration and necrosis with inflammatory changes. Moreover, omega 3 fatty acids inhabited the expressions of inflammatory cells (CD4, CD8 and CD11b) and suppressed the level of NF-κB. The echocardiographic factors such as heartbeat, SBP, DBP, levels of LVDs, LVDd, LVPW percentage of LVFS, EF, expression levels of inflammatory cytokines (TNF, IL-1β, IFN-ɤ, IL-2, and IL-6) also significantly suppressed by omega 3 fatty acids. Hence, the present study proved that consuming fatty acid-enriched fish might be a successful therapy for improving the inflammatory profile, regenerates the heart tissues, and controlled the production of inflammatory cells.

Although radical treatment of Alzheimer’s and Parkinson’s disease is not possible yet, it is aimed to slow the course of the disease and increase the life quality of individuals with the drugs used in the clinic at the present time. Successful results have been achieved in the use of cholinesterase inhibitors and monoamine oxidase inhibitors together in these neurodegenerative diseases. In this study, indane ring which are in the structure of anticholinesterase effective molecules and 2-hydrazinothiazole structure whose inhibitory activities reported on monoamine oxidase-B (MAO-B) were combined; 4-(substituted phenyl)-2-[2-(3-phenyl-2,3-dihydro-1 H -inden-1-ylidene) hydrazinyl]thiazole derivatives ( 3a–3i ) were synthesized as dual inhibitors. The structures of the compounds were verified by IR, 1 H-NMR, 13 C-NMR, and HRMS spectroscopy. When enzyme inhibition activities were evaluated, it was determined that the compounds 3a (42.33%) and 3d (42.39%) on acetylcholinesterase (AChE) enzyme; compounds 3g (75.42%) and 3h (60.33%) showed inhibition on MAO-B enzyme at most, at 10 −3  M concentration.

The emergence of the pandemic in 2020 is a huge threat to global public health. Severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) was first reported in China in December 2019 and later spread to almost all parts of the world in four months and declared as a pandemic in March 2020. SARS-CoV-2 has infected 15.8 million people worldwide while 641,000 died of it. This study aims to report the seroprevalence of SARS-CoV-2 in Pakistan. Of total of 635 samples of symptomatic individuals processed at Genome Center for Molecular Based Diagnostics and Research Pakistan, 313 (49.3%) were found SARS-CoV-2 seropositive. The study also confirmed more seroprevalence in elderly patients (>80 years) and children less than 13 years.