scholarly journals Machine Learning and In Vitro Chemical Screening of Potential α-Amylase and α-Glucosidase Inhibitors from Thai Indigenous Plants

Nutrients ◽  
2022 ◽  
Vol 14 (2) ◽  
pp. 267
Author(s):  
Tarapong Srisongkram ◽  
Sasisom Waithong ◽  
Thaweesak Thitimetharoch ◽  
Natthida Weerapreeyakul

Diabetes mellitus is a major predisposing factor for cardiovascular disease and mortality. α-Amylase and α-glucosidase enzymes are the rate-limiting steps for carbohydrate digestion. The inhibition of these two enzymes is clinically used for the treatment of diabetes mellitus. Here, in vitro study and machine learning models were employed for the chemical screening of inhibiting the activity of 31 plant samples on α-amylase and α-glucosidase enzymes. The results showed that the ethanolic twig extract of Pinus kesiya had the highest inhibitory activity against the α-amylase enzyme. The respective ethanolic extract of Croton oblongifolius stem, Parinari anamense twig, and Polyalthia evecta leaf showed high inhibitory activity against the α-glucosidase enzyme. The classification analysis revealed that the α-glucosidase inhibitory activity of Thai indigenous plants was more predictive based on phytochemical constituents, compared with the α-amylase inhibitory activity (1.00 versus 0.97 accuracy score). The correlation loading plot revealed that flavonoids and alkaloids contributed to the α-amylase inhibitory activity, while flavonoids, tannins, and reducing sugars contributed to the α-glucosidase inhibitory activity. In conclusion, the ethanolic extracts of P. kesiya, C. oblongifolius, P. anamense, and P. evecta have the potential for further chemical characterization and the development of anti-diabetic recipes.

Pharmacia ◽  
2021 ◽  
Vol 68 (4) ◽  
pp. 755-762
Author(s):  
Dora Trifonova ◽  
Anna Gavrilova ◽  
Galina Dyakova ◽  
Genadi Gavrilov ◽  
Maya Yotova ◽  
...  

The focus of the presented study is the in vitro anti-oxidant activity and anti-diabetic potential of water extracts from the following four herbal substances, not traditionally used for treatment of diabetes mellitus – leaves of Sambucus ebulus L. and Prunus mahaleb L., and flowering stems of Cichorium intybus L. and Satureja kitaibelii Wierzb. ex Heuff. The water extracts are obtained through ultrasonication. The extract of S. kitaibelii stands out due to its highest values in all studied indicators – total phenolic content, scavenging potential (DPPH, ABTS) and α-glucosidase inhibitory activity which was six times higher than acarbose. The extract of C. intybus also showed significant α-glucosidase inhibitory activity compared to acarbose. The flowering stems of both species are promising sources of biologically active substances for blood sugar control in diabetes mellitus.


Author(s):  
Dewi Safitri ◽  
Elin Yulinah Sukandar ◽  
Irda Fidrianny ◽  
Eriwan Susanto

Objective: This study aimed to look for new agents from extracted Indonesia herbs which have antifungal activity with better safety profile against Candida albicans, Microsporum gypseum, and Trichophyton mentagrophytes. Methods: Screening of eleven herbs was perform to determine the highest antifungal activity. Minimum Inhibitory Concentration (MIC) and Minimum Fungicidal Concentration (MFC) of selected extracts, rosemary (Rosmarinus officinalis) leaves, Java turmeric (Curcuma xanthorriza) rhizome, and ginger (Zingiber officinalis) rhizome; were determined by using microdilution and agar diffusion methods. Extracts were then combined to evaluate further activities. Selected extracts were fractionated by using liquid-liquid extraction, analyzed by TLC bioautography.Results: ethanolic extract of rosemary (Rosmarinus officinalis) leaves, Java turmeric (Curcuma xanthorriza) rhizome, and ginger (Zingiber officinalis) rhizome in combination showed the highest activity and synergistic interaction against Trichophyton mentagrophytes. There were several components from fractions were actively inhibiting corresponding fungi according to TLC bioautography method. Conclusion: ethanolic extracts of rosemary, Java turmeric, and ginger had the highest antifungal potency, both as extract and in combination comparable to ketoconazole as reference drug. These selected extracts are potential to be used as new antifungal agents.


Antibiotics ◽  
2021 ◽  
Vol 10 (6) ◽  
pp. 705
Author(s):  
Asmaa M. El-Kady ◽  
Iman A. M. Abdel-Rahman ◽  
Samer S. Fouad ◽  
Khaled S. Allemailem ◽  
Taghrid Istivan ◽  
...  

Giardiasis is a major diarrheal disease affecting approximately 2.5 million children annually in developing countries. Several studies have reported the resistance of Giardia lamblia (G. lamblia) to multiple drugs. Therefore, identifying an effective drug for giardiasis is a necessity. This study examined the antiparasitic effect of Punica granatum (pomegranate) and evaluated its therapeutic efficacy in rats infected with G. lamblia. In vitro study showed high efficacy of pomegranate peel ethanolic extract in killing G. lamblia cysts as demonstrated by eosin vital staining. We showed that treating infected rats with pomegranate extract resulted in a marked reduction in the mean number of G. lamblia cysts and trophozoites in feces and intestine respectively. Interestingly, the number of G. lamblia trophozoites and cysts were significantly lower in the pomegranate extract-treated group compared to the metronidazole-positive control group. Moreover, pomegranate extract treatment significantly induced nitric oxide (NO) and reduced serum IL-6 and TNF-α, compared to infected untreated rats. Histological and scanning electron microscopy (SEM) examination of the jejunum and duodenum of pomegranate extract-treated animals confirmed the antiparasitic effect of the extract, and demonstrated the restoration of villi structure with reduction of villi atrophy, decreased infiltration of lymphocytes, and protection of intestinal cells from apoptotic cell death. In conclusion, our data show that the pomegranate peel extract is effective in controlling G. lamblia infections, which suggests that it could be a viable treatment option for giardiasis.


Antibiotics ◽  
2021 ◽  
Vol 10 (4) ◽  
pp. 416
Author(s):  
Sami I. Alzarea ◽  
Abeer H. Elmaidomy ◽  
Hani Saber ◽  
Arafa Musa ◽  
Mohammad M. Al-Sanea ◽  
...  

LC-MS-assisted metabolomic profiling of the Red Sea-derived brown algae Sargassum cinereum “Sargassaceae” dereplicated eleven compounds 1–11. Further phytochemical investigation afforded two new aryl cresol 12–13, along with eight known compounds 14–21. Both new metabolites, along with 19, showed moderate in vitro antiproliferative activity against HepG2, MCF-7, and Caco-2. Pharmacophore-based virtual screening suggested both 5-LOX and 15-LOX as the most probable target linked to their observed antiproliferative activity. The in vitro enzyme assays revealed 12 and 13 were able to inhibit 5-LOX more preferentially than 15-LOX, while 19 showed a convergent inhibitory activity toward both enzymes. Further in-depth in silico investigation revealed the molecular interactions inside both enzymes’ active sites and explained the varying inhibitory activity for 12 and 13 toward 5-LOX and 15-LOX.


2016 ◽  
Vol 228 ◽  
pp. 96-102 ◽  
Author(s):  
Surapan Jitviriyanon ◽  
Phanida Phanthong ◽  
Pattamapan Lomarat ◽  
Nuntavan Bunyapraphatsara ◽  
Sarthorn Porntrakulpipat ◽  
...  

Author(s):  
Triana Hertiani ◽  
Sylvia Utami Tunjung Pratiwi ◽  
Iramie Duma Kencana Irianto ◽  
Aini Febriana

Dental plaque prevention can be achieved by inhibition of mouth cavity microbes to built biofilm. Kaempferia galanga rhizome has been known as a potential antibacterial agent. This research aimed to reveal the potency of Kaempferia galanga extract and essential oil as anti plaque active agents, based on their in vitro inhibitory activity against the planktonic growth and biofilm of Streptococcus mutans ATCC 21752. Kaempferia galanga extract was obtained by defatting dried-pulverized samples in petroleum ether prior to immersion in 70% ethanol. The fresh rhizome was steam-hydro distilled for 6 h to yield the essential oil. Antibacterial and anti biofilm assays were measured by micro dilution technique on polystyrene 96-wells micro titer plates at 37°C. The percentage of inhibition was calculated by comparing the absorbance of samples to the vehicle (control) measured by micro plate reader at 595 nm. Biofilms formed were first stained by 1% crystal violet. The above assays were performed in triplicates. This study revealed that both K. galanga rhizome essential oil and ethanolic extract showed antibacterial and antibiofilm activity towards S. mutans. The ethanol extract showed MIC90 value at 0.091% w/v and MBC at 2.724% w/v for antibacterial activity; IC50 at 0.048 % w/v for anti biofilm formation activity; and EC50 at 0.052%w/v for biofilm degradation activity. Until the highest concentration tested (0.6%w/v), the MIC90 and MBC values of the essential oil were not revealed, but higher biofilm inhibitory activity i.e. IC50 at 0.025 % w/v; and EC50 at 0.034 %w/v were observed. Key words: biofilm inhibitor, antibacterial, Kaempferia galanga


2020 ◽  
Vol 7 (2) ◽  
pp. 50-55
Author(s):  
Anitha T A ◽  
Pakutharivu T ◽  
Nirubama K ◽  
Akshaya V

The traditional herbal medicines are mainly obtained from plants are used in the management of Diabetes mellitus. The main objective of this work was to assess the presence of phytochemical compounds and to evaluate the in vitro antidiabetic activity of isopropanolic extracts of Pimenta racemosa leaves by studying their α-amylase inhibitory activity and glucose transport across yeast cells. Screening of phytochemicals showed positive results for alkaloids, steroids, cardiac glycosides, terpenoids, reducing sugars, anthraquinones, and results of in vitro α-amylase inhibitory studies demonstrated there was a dose-dependent increase in percentage inhibitory activity by the isopropanolic leaf extracts of Pimenta racemosa. At a concentration of 1 mg/ml, the extract showed a percentage inhibition 33.6 and for 5 mg/ml it was 91.2. The glucose uptake study was also studied through yeast cells by analyzing theamount of glucose remaining in the medium after a specific time intervals. It serves as an indicator for the capability of isopropanolic leaf extracts of Pimenta racemosa to transport the glucose into yeast cells. As a result, we found that the isopropanolic leaf extract of Pimenta racemosa have inhibitory activity against αamylase and also, which is efficient in glucose uptake. This therapeutic potentiality of Pimenta racemosa could be exploited in the treatment of Type 2 Diabetes mellitus. Further studies are also required to elucidate whether the plant have antidiabetic potential by in vivo for corroborating the traditional claim of the plant.


INDIAN DRUGS ◽  
2013 ◽  
Vol 50 (06) ◽  
pp. 24-28
Author(s):  
A.A Rege ◽  
◽  
A. S Chowdhary

Aqueous extracts of Ocimum sanctum Linn., Tinospora cordifolia (Willd.) Miers ex Hook. f. & Thoms, Withania somnifera Dunal, Avicennia officinalis Linn. and Rhizophora mucronata Lam. were included for the present in vitro study. Pepsin was used as a substitute for HIV-protease to evaluate inhibitory activity of these extracts, as pepsin has close resemblance with HIV-protease in proteolytic activity. O. sanctum revealed the highest inhibitory activity followed by R. mucronata. In our earlier study, O. sanctum and R. mucronata exerted anti-HIV activity via multiple mechanisms of action; viz., interference with the gp120 / CD4 interaction and inhibition of HIV-reverse transcriptase. In the present study, they also showed potent inhibitory activity against pepsin enzyme (indirectly against HIV-protease) which may be due their flavonoids content.


Sign in / Sign up

Export Citation Format

Share Document